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Sample records for lidocaine

  1. Lidocaine Viscous

    MedlinePlus

    Lidocaine viscous, a local anesthetic, is used to treat the pain of a sore or irritated mouth ... associated with cancer chemotherapy and certain medical procedures. Lidocaine viscous is not normally used for sore throats ...

  2. Lidocaine toxicity.

    PubMed

    Mehra, P; Caiazzo, A; Maloney, P

    1998-01-01

    Local anesthetics are the most commonly used drugs in dentistry. The number of adverse reactions reported, particularly toxic reactions, are extraordinarily negligible. This article reports a case of lidocaine toxicity with its typical manifestation in a 37-yr-old healthy male. The toxic reaction followed transoral/transpharyngeal topical spraying of lidocaine preoperatively during preparation for general anesthesia. A review of dosages of the most commonly used local anesthetic drugs in dentistry and the management of a toxic reaction is presented. Clinicians need to be in a position to recognize and successfully manage this potential adverse reaction.

  3. Lidocaine Transdermal Patch

    MedlinePlus

    Lidocaine patches are used to relieve the pain of post-herpetic neuralgia (PHN; the burning, stabbing pains, ... for months or years after a shingles infection). Lidocaine is in a class of medications called local ...

  4. Estimated Maximal Safe Dosages of Tumescent Lidocaine

    PubMed Central

    Jeske, Daniel R.

    2016-01-01

    BACKGROUND: Tumescent lidocaine anesthesia consists of subcutaneous injection of relatively large volumes (up to 4 L or more) of dilute lidocaine (≤1 g/L) and epinephrine (≤1 mg/L). Although tumescent lidocaine anesthesia is used for an increasing variety of surgical procedures, the maximum safe dosage is unknown. Our primary aim in this study was to measure serum lidocaine concentrations after subcutaneous administration of tumescent lidocaine with and without liposuction. Our hypotheses were that even with large doses (i.e., >30 mg/kg), serum lidocaine concentrations would be below levels associated with mild toxicity and that the concentration-time profile would be lower after liposuction than without liposuction. METHODS: Volunteers participated in 1 to 2 infiltration studies without liposuction and then one study with tumescent liposuction totally by local anesthesia. Serum lidocaine concentrations were measured at 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, and 24 hours after each tumescent lidocaine infiltration. Area under the curve (AUC∞) of the serum lidocaine concentration-time profiles and peak serum lidocaine concentrations (Cmax) were determined with and without liposuction. For any given milligram per kilogram dosage, the probability that Cmax >6 μg/mL, the threshold for mild lidocaine toxicity was estimated using tolerance interval analysis. RESULTS: In 41 tumescent infiltration procedures among 14 volunteer subjects, tumescent lidocaine dosages ranged from 19.2 to 52 mg/kg. Measured serum lidocaine concentrations were all <6 μg/mL over the 24-hour study period. AUC∞s with liposuction were significantly less than those without liposuction (P = 0.001). The estimated risk of lidocaine toxicity without liposuction at a dose of 28 mg/kg and with liposuction at a dose of 45 mg/kg was ≤1 per 2000. CONCLUSIONS: Preliminary estimates for maximum safe dosages of tumescent lidocaine are 28 mg/kg without liposuction and 45 mg/kg with liposuction. As a

  5. 21 CFR 862.3555 - Lidocaine test system.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Lidocaine test system. 862.3555 Section 862.3555....3555 Lidocaine test system. (a) Identification. A lidocaine test system is a device intended to measure lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by...

  6. 21 CFR 862.3555 - Lidocaine test system.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 8 2011-04-01 2011-04-01 false Lidocaine test system. 862.3555 Section 862.3555....3555 Lidocaine test system. (a) Identification. A lidocaine test system is a device intended to measure lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by...

  7. 21 CFR 862.3555 - Lidocaine test system.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 8 2013-04-01 2013-04-01 false Lidocaine test system. 862.3555 Section 862.3555....3555 Lidocaine test system. (a) Identification. A lidocaine test system is a device intended to measure lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by...

  8. 21 CFR 862.3555 - Lidocaine test system.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 8 2012-04-01 2012-04-01 false Lidocaine test system. 862.3555 Section 862.3555....3555 Lidocaine test system. (a) Identification. A lidocaine test system is a device intended to measure lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by...

  9. 21 CFR 862.3555 - Lidocaine test system.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 8 2014-04-01 2014-04-01 false Lidocaine test system. 862.3555 Section 862.3555....3555 Lidocaine test system. (a) Identification. A lidocaine test system is a device intended to measure lidocaine, an antiarrythmic and anticonvulsant drug, in serum and plasma. Measurements obtained by...

  10. Lidocaine block of cardiac sodium channels.

    PubMed

    Bean, B P; Cohen, C J; Tsien, R W

    1983-05-01

    Lidocaine block of cardiac sodium channels was studied in voltage-clamped rabbit purkinje fibers at drug concentrations ranging from 1 mM down to effective antiarrhythmic doses (5-20 muM). Dose-response curves indicated that lidocaine blocks the channel by binding one-to-one, with a voltage-dependent K(d). The half-blocking concentration varied from more than 300 muM, at a negative holding potential where inactivation was completely removed, to approximately 10 muM, at a depolarized holding potential where inactivation was nearly complete. Lidocaine block showed prominent use dependence with trains of depolarizing pulses from a negative holding potential. During the interval between pulses, repriming of I (Na) displayed two exponential components, a normally recovering component (tauless than 0.2 s), and a lidocaine-induced, slowly recovering fraction (tau approximately 1-2 s at pH 7.0). Raising the lidocaine concentration magnified the slowly recovering fraction without changing its time course; after a long depolarization, this fraction was one-half at approximately 10 muM lidocaine, just as expected if it corresponded to drug-bound, inactivated channels. At less than or equal to 20 muM lidocaine, the slowly recovering fraction grew exponentially to a steady level as the preceding depolarization was prolonged; the time course was the same for strong or weak depolarizations, that is, with or without significant activation of I(Na). This argues that use dependence at therapeutic levels reflects block of inactivated channels, rather than block of open channels. Overall, these results provide direct evidence for the "modulated-receptor hypothesis" of Hille (1977) and Hondeghem and Katzung (1977). Unlike tetrodotoxin, lidocaine shows similar interactions with Na channels of heart, nerve, and skeletal muscle.

  11. Pharmacokinetics of Lidocaine and Its Metabolites Following Vaginal Administration of Lidocaine Gel to Healthy Female Subjects

    PubMed Central

    Kushner, Harvey; Richardson, Elaine; Mize, Amy; Mayer, Philip

    2016-01-01

    Abstract Lidocaine vaginal bioadhesive gel is being developed as a local anesthetic for use in minimally invasive outpatient gynecological procedures and was investigated in single‐dose and multiple‐dose studies in healthy young adult women. Lidocaine doses of 2.5%, 5%, and 10% (w/w) were administered, and parent drug and metabolites monoethylglycinexylidide and glycinexylidide were measured in plasma. Lidocaine was absorbed through vaginal tissue and into the systemic circulation in a dose‐proportional manner, and there was little systemic accumulation. Plasma concentrations were 10‐ to 20‐fold lower than concentrations obtained after administration of intravenous lidocaine used to treat arrhythmic activity, thus demonstrating a wide safety margin for a vaginal lidocaine product. PMID:27297519

  12. [Lidocaine elimination and MEGX formation after oral lidocaine administration--a practicable test for assessment of quantitative liver function].

    PubMed

    Klinker, H; Joeres, R; Bomhard, M; Keller, F; Dorer, J; Zilly, W; Richter, E

    1993-02-01

    Oral load with 200 mg Lidocain was performed in 370 patients with chronic liver disease. The 120- and 240-minute Lidocain plasma concentrations as well as the 30- and 60-minute MEGX plasma concentrations, main metabolite of Lidocain, were measured by means of gas chromatography and with the commercial TDX test from the firm Abbott. No side effects caused by the load were observed and all of the patients resorbed Lidocain. Peak concentrations were found both for Lidocain and for MEGX in the 60-minute tests. Patients with liver cirrhosis of different aetiology showed significantly higher Lidocain plasma concentrations and lower MEGX values than patients with chronic non-cirrhotic liver disease. The differentiation of these two groups of patients was most successful via the determination of the 240-minute Lidocain plasma concentration. Oral load with 200 mg Lidocain has turned out to be a practicable and meaningful test for the estimation of the Cytochrom P450-dependent liver function.

  13. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Embutramide, chloroquine, and lidocaine solution... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications. Each....; and 1.9 mg lidocaine, U.S.P. (b) Sponsor. See No. 059130 in § 510.600(c) of this chapter....

  14. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Embutramide, chloroquine, and lidocaine solution... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications. Each....; and 1.9 mg lidocaine, U.S.P. (b) Sponsor. See No. 000859 in § 510.600(c) of this chapter....

  15. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Embutramide, chloroquine, and lidocaine solution... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications. Each....; and 1.9 mg lidocaine, U.S.P. (b) Sponsor. See No. 000859 in § 510.600(c) of this chapter....

  16. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Embutramide, chloroquine, and lidocaine solution... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications. Each....; and 1.9 mg lidocaine, U.S.P. (b) Sponsor. See No. 059130 in § 510.600(c) of this chapter....

  17. 21 CFR 522.810 - Embutramide, chloroquine, and lidocaine solution.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Embutramide, chloroquine, and lidocaine solution... ANIMAL DRUGS § 522.810 Embutramide, chloroquine, and lidocaine solution. (a) Specifications. Each....; and 1.9 mg lidocaine, U.S.P. (b) Sponsor. See No. 059130 in § 510.600(c) of this chapter....

  18. Investigation of bioequivalence and tolerability of intramuscular ceftriaxone injections by using 1% lidocaine, buffered lidocaine, and sterile water diluents.

    PubMed Central

    Hayward, C J; Nafziger, A N; Kohlhepp, S J; Bertino, J S

    1996-01-01

    The pharmacokinetics and tolerability of 1-g doses of ceftriaxone diluted in sterile water, 1% lidocaine, or buffered lidocaine were investigated. No difference in bioequivalence was noted between the three treatments. No difference in peak creatine kinase values was seen. By use of a quantitative pain scale, injection of ceftriaxone with the water diluent was significantly more painful than that with either of the other two diluents. No difference in injection pain was noted for lidocaine or buffered lidocaine. PMID:8834905

  19. [Lidocaine: local anaesthetic with systemic toxicity].

    PubMed

    van Donselaar-van der Pant, K A M I; Buwalda, M; van Leeuwen, H J

    2008-01-12

    In 4 patients, 3 women aged 63, 17 and 43 years, and a man aged 67 years, lidocain was used as a local anaesthetic for a transthoracic esophageal fundoplication (first patient), severe painful gonarthrosis (fourth patient) and legal abortion (second and third patients). All patients suffered from systemic toxicity as a result, a rare complication. They all had an uneventful recovery, except for the second patient who died from adult respiratory distress syndrome after two weeks in the intensive care unit. The second and third patients had inadvertently been given a solution of lidocain that was too strong (10% instead of 1%). The presenting symptoms of systemic toxicity include numbness of the tongue, dizziness, tinnitus, visual disturbances, muscle spasms, convulsions, reduced consciousness, coma, and respiratory arrest. Physicians who use lidocain as a local anaesthetic should be aware of its systemic toxicity.

  20. Identification of the epidural space: loss of resistance with air, lidocaine, or the combination of air and lidocaine.

    PubMed

    Evron, Samuel; Sessler, Daniel; Sadan, Oscar; Boaz, Mona; Glezerman, Marek; Ezri, Tiberiu

    2004-07-01

    The ideal technique for identifying the epidural space remains unclear. Five-hundred-forty-seven women in labor who requested epidural analgesia were randomly allocated to three groups according to the technique by which the epidural space was identified: 1) loss-of-resistance with air (air; n = 180), 2) loss-of-resistance with lidocaine (lidocaine; n = 185), and 3) loss-of-resistance with both air and lidocaine (air-plus-lidocaine; n = 182). We assessed ease of epidural catheter insertion, characteristics of the blockade, quality of analgesia, and complications. The inability to thread the epidural catheter occurred in 16% of the air, 4% of the lidocaine, and 3% of the air-plus-lidocaine patients (P < 0.001). More patients from the air group had unblocked segments (6.6% versus 3.2% and 2.2%, respectively; P < 0.02). The incidence of accidental dural puncture was greater in the air group (1.7% versus 0% in the other two groups; P < 0.02). Pain scores, time to onset of analgesia, upper sensory level, motor blockade, and the incidence of hypotension, transient neurological deficits, postpartum urinary retention, and postdural puncture headache were comparable. Identification of the epidural space with air was more difficult and caused more dural punctures than with lidocaine or air plus lidocaine. Additionally, sequential use of air and lidocaine had no advantage over lidocaine alone.

  1. Chromatographic Determination of Aminoacridine Hydrochloride, Lidocaine Hydrochloride and Lidocaine Toxic Impurity in Oral Gel.

    PubMed

    Bebawy, Lories I; Elghobashy, Mohamed R; Abbas, Samah S; Shokry, Rafeek F

    2016-04-01

    Two sensitive and selective analytical methods were developed for simultaneous determination of aminoacridine hydrochloride and lidocaine hydrochloride in bulk powder and pharmaceutical formulation. Method A was based on HPLC separation of the cited drugs with determination of the toxic lidocaine-related impurity 2,6-dimethylaniline. The separation was achieved using reversed-phase column C18, 250 × 4.6 mm, 5 µm particle size and mobile phase consisting of 0.05 M disodium hydrogen phosphate dihydrate (pH 6.0 ± 0.2 adjusted with phosphoric acid) and acetonitrile (55 : 45, v/v). Quantitation was achieved with UV detection at 240 nm. Linear calibration curve was in the range of 1.00-10.00, 13.20-132.00 and 1.32-13.20 µg mL(-1) for aminoacridine hydrochloride, lidocaine hydrochloride and 2,6-dimethylaniline, respectively. Method B was based on TLC separation of the cited drugs followed by densitometric measurement at 365 nm on the fluorescent mode for aminoacridine hydrochloride and 220 nm on the absorption mode for lidocaine hydrochloride. The separation was carried out using ethyl acetate-methanol-acetic acid (65 : 30 : 5 by volume) as a developing system. The calibration curve was in the range of 25.00-250.00 ng spot(-1) and 0.99-9.90 µg spot(-1) for aminoacridine hydrochloride and lidocaine hydrochloride, respectively. The results obtained were statistically analyzed and compared with those obtained by applying the manufacturer's method.

  2. Studies on the interaction of lidocaine with plasma proteins

    SciTech Connect

    Adotey, J.

    1985-01-01

    This study sought to quantitate lidocaine's interaction with alpha-1-acid glycoprotein (AAG), human serum albumin (HSA), and AAG in the presence of HSA, and to determine the extent of displacement of lidocaine from its binding site(s) by selected cardiovascular drugs (dipyridamole, disopyramide and quinidine). Since the limited experimental work reported in this area has involved the use of a single lidocaine concentration, this study involved the evaluation of a range of lidocaine concentrations. Lidocaine interaction with plasma proteins (AAG and HSA) was studied at 37/sup 0/C using an isothermal equilibrium dialysis system and /sup 14/C-lidocaine HCl. A dialysis membrane (M.W. cutoff 12,000 to 14,000) separated the two chambers of each dialysis cell. The extent of /sup 14/C-lidocaine dialysis was studied with respect to both drug and protein concentrations. Aliquots of each chamber of each of the cells were subjected to liquid scintillation counting (LSC) analyses for /sup 14/C-lidocaine. The ratio of bound to free (R/F) lidocaine was evaluated as a function of AAG concentration from the LSC data. Scatchard and/or Rosenthal analyses were employed to evaluate n and k values where appropriate. Linear and multiple linear regression analyses of the data were appropriately performed.

  3. Nanoethosomes for Dermal Delivery of Lidocaine

    PubMed Central

    Babaie, Soraya; Ghanbarzadeh, Saeed; Davaran, Soodabeh; Kouhsoltani, Maryam; Hamishehkar, Hamed

    2015-01-01

    Purpose: It is necessary for local anesthetics to pass through the stratum corneum to provide rapid pain relief. Many techniques have been reported to enhance intradermal penetration of local anesthetics such as vesicular lipid carriers. Ethosomes are lipid vesicles containing phospholipids, ethanol at relatively high concentration. We hypothesized that synergistic effects of phospholipids and high concentration of ethanol in formulation could accelerate penetration of nanoethosomes in deep layers of skin. Methods: Lidocaine-loaded nanoethosomes were prepared and characterized by size and zeta analyzer, scanning electron microscopy (SEM) and X-ray diffractometer (XRD). Furthermore, encapsulation efficiency (EE), loading capacity (LC), and skin penetration capability were evaluated by in vitro and in vivo experiments. Results: results showed that the particle size, zeta potential, EE and LC of optimum formulation were 105.4 ± 7.9 nm, -33.6 ± 2.4 mV, 40.14 ± 2.5 %, and 8.02 ± 0.71 respectively. SEM results confirmed the non-aggregated nano-scale size of prepared nanoethosomes. Particle size of ethosomes and EE of Lidocaine were depended on the phospholipid and ethanol concentrations. XRD results demonstrated the drug encapsulation in amorphous status interpreting the achieved high drug EE and LC values. In vitro and in vivo assays confirmed the appropriate skin penetration of Lidocaine with the aid of nanoethosomes and existence of deposition of nanoethosomes in deep skin layers, respectively. Conclusion: The developed nanoethosomes are proposed as a suitable carrier for topical delivery of anesthetics such as Lidocaine. PMID:26819928

  4. Lidocaine Inhibits HCN Currents in Rat Spinal Substantia Gelatinosa Neurons

    PubMed Central

    Hu, Tao; Liu, Nana; Lv, Minhua; Ma, Longxian; Peng, Huizhen; Peng, Sicong

    2016-01-01

    BACKGROUND: Lidocaine, which blocks voltage-gated sodium channels, is widely used in surgical anesthesia and pain management. Recently, it has been proposed that the hyperpolarization-activated cyclic nucleotide (HCN) channel is one of the other novel targets of lidocaine. Substantia gelatinosa in the spinal dorsal horn, which plays key roles in modulating nociceptive information from primary afferents, comprises heterogeneous interneurons that can be electrophysiologically categorized by firing pattern. Our previous study demonstrated that a substantial proportion of substantia gelatinosa neurons reveal the presence of HCN current (Ih); however, the roles of lidocaine and HCN channel expression in different types of substantia gelatinosa neurons remain unclear. METHODS: By using the whole-cell patch-clamp technique, we investigated the effect of lidocaine on Ih in rat substantia gelatinosa neurons of acute dissociated spinal cord slices. RESULTS: We found that lidocaine rapidly decreased the peak Ih amplitude with an IC50 of 80 μM. The inhibition rate on Ih was not significantly different with a second application of lidocaine in the same neuron. Tetrodotoxin, a sodium channel blocker, did not affect lidocaine’s effect on Ih. In addition, lidocaine shifted the half-activation potential of Ih from −109.7 to −114.9 mV and slowed activation. Moreover, the reversal potential of Ih was shifted by −7.5 mV by lidocaine. In the current clamp, lidocaine decreased the resting membrane potential, increased membrane resistance, delayed rebound depolarization latency, and reduced the rebound spike frequency. We further found that approximately 58% of substantia gelatinosa neurons examined expressed Ih, in which most of them were tonically firing. CONCLUSIONS: Our studies demonstrate that lidocaine strongly inhibits Ih in a reversible and concentration-dependent manner in substantia gelatinosa neurons, independent of tetrodotoxin-sensitive sodium channels. Thus, our

  5. Pharmacokinetics of lidocaine delivered from a transmucosal patch in children.

    PubMed Central

    Leopold, Andrea; Wilson, Stephen; Weaver, Joel S.; Moursi, Amr M.

    2002-01-01

    The DentiPatch lidocaine transoral delivery system (Noven Pharmaceuticals) is indicated for mild topical anesthesia of mucosal membranes in the mouth. The DentiPatch is a mucoadhesive patch containing 46.1 mg of lidocaine (20% concentration). Current studies in adults report that DentiPatch application produces very low plasma concentrations of lidocaine. However, it is not known what plasma levels are obtained when the same dosage is used in children. The purpose of this study was to determine whether the plasma lidocaine concentrations generated by the DentiPatch are within a safe range for children. The sample in this study was 11 children aged 2-7 years requiring general anesthesia for comprehensive dental care. A lidocaine DentiPatch was placed on the buccal mucosa above the maxillary incisors for 5 minutes. Blood samples were drawn before placing the DentiPatch and at various time intervals after removing it. Blood samples were analyzed by fluorescence polarization immunoassay to determine the plasma concentrations of lidocaine and its major metabolite, monoethylglycinexylidide. The lidocaine and monoethylglycinexylidide absorbed from the DentiPatch did not reach toxic plasma levels in children. However, plasma concentrations were much higher than in adults and were high enough to require inclusion in the calculation of total lidocaine administered to a pediatric patient. Images Figure 1 PMID:15384296

  6. Preparation and characterization of lidocaine rice gel for oral application.

    PubMed

    Okonogi, Siriporn; Kaewpinta, Adchareeya; Yotsawimonwat, Songwut; Khongkhunthian, Sakornrat

    2015-12-01

    The objective of the present study was to prepare buccal anesthetic gels using rice as gelling agent. Rice grains of four rice varieties, Jasmine (JM), Saohai (SH), Homnil (HN), and Doisket (DS) were chemically modified. Buccal rice gels, containing lidocaine hydrochloride as local anesthetic drug were formulated using the respective modified rice varieties. The gels were evaluated for outer appearance, pH, color, gel strength, foaming property, adhesion, in vitro drug release and in vivo efficacy. It was found that the developed rice gels possessed good texture. Rice varieties showed influence on gel strength, color, turbidity, adhesive property, release property, and anesthetic efficacy. JM gel showed the lowest turbidity with light transmission of 86.76 ± 1.18% whereas SH gel showed the highest gel strength of 208.78 ± 10.42 g/cm(2). Lidocaine hydrochloride can cause a decrease in pH and adhesive property but an increase in turbidity of the gels. In vitro drug release profile within 60 min of lidocaine SH gel and lidocaine HN gel showed that lidocaine could be better released from SH gel. Evaluation of in vivo anesthetic efficacy in 100 normal volunteers indicates that both lidocaine rice gels have high efficacy but different levels. Lidocaine SH gel possesses faster onset of duration and longer duration of action than lidocaine HN gel.

  7. Lidocaine Metabolism and Toxicity: A Laboratory Experiment for Dental Students.

    ERIC Educational Resources Information Center

    Kusek, J. C.

    1980-01-01

    A laboratory exercise for dental students is presented using a toxic dose of lidocaine in place of an anesthetic dose of pentobarbital. The use of lidocaine demonstrates its toxic and lethal actions and increases the relevance of the experience for dental students. (Author/MLW)

  8. Topical lidocaine adrenaline tetracaine (LAT gel) versus injectable buffered lidocaine for local anesthesia in laceration repair.

    PubMed Central

    Ernst, A A; Marvez-Valls, E; Nick, T G; Mills, T; Minvielle, L; Houry, D

    1997-01-01

    The objective of the study was to compare topical lidocaine adrenaline tetracaine (LAT gel) with injectable buffered lidocaine with epinephrine regarding pain of application or injection and anesthesia effectiveness. The study was a randomized prospective comparison trial in an urban emergency department. Physicians and patients ranked the pain of application, injection, and suturing according to a 10-cm visual analog scale. Sixty-six patients were entered, 33 in the LAT gel group and 33 in the injectable buffered lidocaine group. Injection was found to be significantly more painful than application of gel (P < 0.001). For anesthesia effectiveness, there was no difference according to patients (P = 0.48) or physicians (P = 0.83) for topical vs injectable forms. The number of sutures causing pain was not statistically different in the two groups (P = 0.28). In conclusion, LAT gel compared favorably with injectable buffered lidocaine for local anesthesia effectiveness and was significantly less painful to apply. It may be the preferred local anesthetic for this reason. PMID:9291744

  9. Spreading of a Lidocaine Formulation on Microneedle-Treated Skin.

    PubMed

    Nayak, Atul; Das, Diganta B; Chao, Tzu C; Starov, Victor M

    2015-12-01

    The spreadability of a liquid drug formulation on skin is an indication of it either remaining stationary or distributing (spreading) as a droplet. Factors determining droplet spreadability of the formulation are spreading area, diameter of the droplet base, viscosity of the liquid, contact angle, volume of droplet on skin and any others. The creation of microcavities from the application of microneedle (MN) has the potential to control droplet spreading, and hence, target specific areas of skin for drug delivery. However, there is little work that demonstrates spreading of liquid drug formulation on MN-treated skin. Below, spreading of a lidocaine hydrogel formulation and lidocaine solution (reference liquid) on porcine skin is investigated over MN-treated skin. Controlled spreadability was achieved with the lidocaine hydrogel on MN-treated skin as compared with lidocaine solution. It was observed that the droplet spreading parameters such as spreading radius, droplet height and dynamic contact angle were slightly lower for the lidocaine hydrogel than the lidocaine solution on skin. Also, the lidocaine hydrogel on MN-treated skin resulted in slower dynamic reduction of droplet height, contact angle and reduced time taken in attaining static advancing droplets because of the MN microcavities.

  10. Investigations into distribution of lidocaine in human autopsy material.

    PubMed

    Oertel, Reinhard; Arenz, Norman; Zeitz, Sten Gunnar; Pietsch, Jörg

    2015-08-01

    With screening methods in the legal medicine drugs were often detected in autopsy material. In this study the antiarrhythmic and the local anesthetic drug lidocaine could be proved in fifty-one cases and determined in different autopsy materials. For the first time the comparison of so many distribution patterns of lidocaine in human compartments was possible. A liquid-liquid extraction procedure, a standard addition method and LC/MS/MS were used for analytics. The measured concentrations in blood were in the therapeutic range or lower. The time between lidocaine application and death was given in twenty-nine cases. These data were very helpful to estimate and interpret the distribution process of lidocaine between application and death. This time exerted a crucial influence on the distribution of lidocaine in the compartments. Most of the intravenous applicated lidocaine was found in heart blood after a very short time of distribution. Afterwards the highest concentrations were measured in brain. Later the highest concentration was found in the kidney samples or in urine. If the time between lidocaine application and death is known, the results of this study can be used to deepen the knowledge of its pharmacokinetics. If this time is unknown, the circumstances and the causes of death can be better explained.

  11. Transdermal delivery of lidocaine in vitro by alternating current.

    PubMed

    Kinoshita, Tatsuki; Shibaji, Takao; Umino, Masahiro

    2003-03-01

    The purpose of this study was to investigate whether lidocaine could be transported through excised rat skin in vitro using alternating current (AC). In addition, the relationships between factors such as voltage and frequency, and transported lidocaine concentration were studied using the in vitro model. A pair of platinum plate electrodes was installed at opposite ends of two cylindrical glass cells in parallel to the full-thickness rat skin. The donor compartment was filled with 10 % lidocaine hydrochloride, and the receptor compartment with Ringer solution. A sinusoidal wave was applied between the electrodes at 5 kinds of constant voltages at 1 kHz and at 4 kinds of frequencies at 20 volts. Our experimental system was successfully used to quantify the concentration of transported lidocaine induced by AC application. The applied sinusoidal waves evoked the transport of lidocaine through the rat skin at every voltage and frequency protocol. Our results suggest that the applied electric voltage and frequency affect the movement of the lidocaine ions. We conclude that the transdermal delivery of lidocaine by AC iontophoresis has a possibility to use for local anesthesia and the pain management of the skin.

  12. Local anesthetic cream prepared from lidocaine-tetracaine eutectic mixture.

    PubMed

    Ohzeki, Keiichi; Kitahara, Masaki; Suzuki, Noriko; Taguchi, Kyoji; Yamazaki, Yuki; Akiyama, Shinji; Takahashi, Kentaro; Kanzaki, Yasushi

    2008-04-01

    Local anesthetic creams for the clinical treatment of conditions such as postherpetic neuralgia were prepared as an in-house formulation from the eutectic mixture of lidocaine-tetracaine (LT cream) using two eutectic mixtures of local anesthetic (EMLA) type bases. The LT formulation was compared with a lidocaine-prilocaine (LP cream) eutectic mixture formulated using the same base as EMLA. The chemical stability of lidocaine was examined in advance and was found to be stable for more than 3 months either in LT cream or in LP cream. The release rate of lidocaine from the formulated creams was examined using a cellulose ester membrane. The release rate of lidocaine from LT cream was similar to that from LP cream. The release rate of tetracaine was slightly slower than that of lidocaine in LT cream reflecting the larger molecular size of tetracaine. The penetration rate was examined in vitro using a Yucatan micropig skin. The penetration rate of lidocaine was similar between LT and LP creams. Infiltration anesthesia action examined in guinea pigs indicated that the difference between the two creams was statistically insignificant. The present study suggests the equivalence of the LT and LP creams as a local anesthetic and the potential of LT cream for clinical use either in the easy formulation or in the low-cost formulation.

  13. Neutralized lidocaine with epinephrine for local anesthesia--II.

    PubMed

    Stewart, J H; Chinn, S E; Cole, G W; Klein, J A

    1990-09-01

    The pain usually associated with intradermal injection of lidocaine and epinephrine is significantly attenuated by the addition of either sodium bicarbonate or sodium hydroxide to 1% lidocaine with epinephrine. This suggests that sodium bicarbonate attenuates pain by increasing the pH of the anesthetic solution. The clinical effects of a solution of lidocaine (1%) with epinephrine (1:100,000) and sodium bicarbonate (80 meq/L) were assessed after infiltration in skin. Anesthetic stored for 1 week caused nearly equal areas of anesthesia and vasoconstriction as an identical solution prepared on the day of use.

  14. [Effect of lidocaine and lidocaine with adrenaline on development of cerebral seizures].

    PubMed

    Tsilosani, N A; Nanobashvili, Z I; Azikuri, G Sh; Bekaia, G L

    2006-05-01

    Experiments were carried out on male albino rats of 200-250 g weight with bipolar electrodes implanted in neocortex, as well as in the right and the left dorsal hippocampus for the study of the effect of lidocaine and its combination with adrenaline on the electric activity of brain. On the fifth day from the implantation in the first group of animals 0,3 ml 2% lidocaine was injected intra-peritoneally and the electric activity from the above mentioned structures was registered. In the second group 0,3 ml 2% lidocaine with adrenaline was injected intra-peritoneally (1:100000). In 8-12 sec after injection in the first group of animals the encephalogram showed sharply defined clone type seizure activity, which soon obtained tonus character. Simultaneously clone-tonus type behavioural manifestation was revealed, which lasted for 20-25 minutes. In the second group of animals in 30-40 sec after injection the encephalogram revealed convulsion activity with high amplitude synchronous oscillations, which lasted for 20-25 minutes, although in this group, in distinct from the first group, no clone-tonus behavioural manifestation was detected.

  15. Clinical effectiveness of lidocaine and benzocaine for topical anesthesia.

    PubMed Central

    Rosa, A. L.; Sverzut, C. E.; Xavier, S. P.; Lavrador, M. A.

    1999-01-01

    The effectiveness of lidocaine and benzocaine in reducing pain produced by needle insertion into the palate was evaluated in a double-blind and placebo-controlled study using a more suitable method. Twenty subjects, 10 men and 10 women, submitted to 4 sessions in which they were randomly treated with 5% lidocaine, a placebo that tasted like lidocaine, 20% benzocaine, and a placebo that tasted like benzocaine. At each session, a 27-gauge needle was inserted into the palate twice, once before (baseline) and once after drug application for 1 minute. Immediately after each insertion, subjects indicated on a visual analog scale the pain intensity perceived. Lidocaine and benzocaine were equally efficient, and both were better than placebo in reducing pain caused by insertion of needles into the palate. PMID:11692349

  16. Lidocaine decreases the xylazine-evoked contractility in pregnant cows.

    PubMed

    Piccinno, M; Rizzo, A; Mutinati, M; D'Onghia, G; Sciorsci, R L

    2016-08-01

    The objective of this in vitro study was to evaluate and compare the effects of xylazine on basal uterine contractility of bovine pregnant uterine strips and that of lidocaine on xylazine-sensitized bovine pregnant uterine strips, at different stages of pregnancy. Basal contractility was evaluated in an isolated organ bath and the functionality of the strips throughout the experiment was evaluated using a dose of carbachol (10(-5)M). Uterine motility, expressed with amplitude, frequency of contractions as well as the area under the curve, was recorded in different stages of pregnancy and data were collected at 15-min intervals (5-min before and 5-min after xylazine administration and 5-min after lidocaine addition on the plateau contraction induced by xylazine). Uterine motility increased in all the stages of pregnancy after xylazine addition and gradually decreased after treatment with lidocaine. These data suggest that lidocaine might decrease the tonic effect induced by xylazine on bovine pregnant uteri.

  17. Lidocaine Infusion: A Promising Therapeutic Approach for Chronic Pain

    PubMed Central

    Kandil, Enas; Melikman, Emily; Adinoff, Bryon

    2017-01-01

    Opioid abuse is a national epidemic in the United States, where it is estimated that a prescription drug overdose death occurs every 19 minutes. While opioids are highly effective in acute and subacute pain control, their use for treatment of chronic pain is controversial. Chronic opioids use is associated with tolerance, dependency, hyperalgesia. Although there are new strategies and practice guidelines to reduce opioid dependence and opioid prescription drug overdose, there has been little focus on development of opioid-sparing therapeutic approaches. Lidocaine infusion has been shown to be successful in controlling pain where other agents have failed. The opioid sparing properties of lidocaine infusion added to its analgesic and antihyperalgesic properties make lidocaine infusion a viable option for pain control in opioid dependent patients. In this review, we provide an overview of the opioid abuse epidemic, and we outline current evidence supporting the potential use of lidocaine infusion as an adjuvant therapeutic approach for management of chronic pain. PMID:28239510

  18. Acute intoxication of lidocaine and chlorpheniramine: report of one case.

    PubMed

    Hua, Yi-Ming; Hung, Chih-Hsing; Yuh, Yeong-Seng

    2005-01-01

    A case of acute intoxication involving lidocaine and chlorpheniramine (an antihistamine) in a 13-month-old child after ingestion of a commercial topical agent is presented. The major toxic reaction consisted of convulsion, coma, tachycardia, fever, and fatigue. This report shows that parents and physicians should be made aware of the hazards of lidocaine and overdose of other topical agents in infants and children.

  19. A comparative study of centbucridine and lidocaine in dental extraction.

    PubMed

    Vacharajani, G N; Parikh, N; Paul, T; Satoskar, R S

    1983-01-01

    A randomized double-blind study comparing the efficacy and tolerability of centbucridine (0.5%) with those of lidocaine (2%) as an anaesthetic agent was conducted in the dental outpatient department on patients attending for dental extraction. One hundred and twenty patients were studied. The degree of analgesia attained with centbucridine compared well with that obtained with lidocaine. The compound was well tolerated with no significant changes in the cardiovascular parameters and no serious side-effects.

  20. Rifampicin induction of lidocaine metabolism in cultured human hepatocytes.

    PubMed

    Li, A P; Rasmussen, A; Xu, L; Kaminski, D L

    1995-08-01

    In our laboratory, cultured human hepatocytes are being evaluated as an experimental system to study drug interactions. We report the effect of a known cytochrome P450 (CYP) inducer, rifampicin, on the metabolism of lidocaine by primary human hepatocytes. Rifampicin has been shown to induce CYP3A4, a major human hepatic CYP isozyme that is known to metabolize lidocaine to its primary metabolite, monoethylglycinexylidide. Human hepatocytes were cultured on collagen-coated plates in serum-free, hormone-supplemented Waymouth medium for a 3-day period before they were treated with rifampicin at 50 microM for 1 to 3 days. Hepatocytes isolated from five individuals were studied, and, in all cases, lidocaine metabolism was found to be induced by rifampicin, as demonstrated by a higher rate of monoethylglycinexylidide formation than concurrent controls. For three of the hepatocyte cultures, lidocaine metabolism was evaluated at various times after treatment. Induction was observed at 1 day after treatment, and reached higher levels at day 2 or 3. The level of induction was found to be approximately 100% for two hepatocyte isolations and approximately 600% for one isolation. In a separate experiment, hepatocytes were treated with rifampicin for a 2-day period. Rate of lidocaine metabolism at multiple substrate concentrations (10-120 microM) were then studied. Rifampicin induction of lidocaine metabolism (approximately 100%) was observed at all the lidocaine concentrations studied. Lineweaver-Burk plot of the data showed an increase in Vmax and a less significant change in Km. Induction of lidocaine metabolism by rifampicin (concentrations of 0.1-50 microM) was found to be dose-dependent, with significant induction observed at 1 microM and higher concentrations. (ABSTRACT TRUNCATED AT 250 WORDS)

  1. [Comparative study between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on endotracheal tube cuff as regards postoperative sore throat].

    PubMed

    Mekhemar, Nashwa Abdallah; El-Agwany, Ahmed Samy; Radi, Wafaa Kamel; El-Hady, Sherif Mohammed

    2016-01-01

    Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups. Benzydamine hydrochloride gel, 5% lidocaine hydrochloride gel, 10% lidocaine hydrochloride spray, or normal saline were applied on endotracheal tube cuffs before endotracheal intubation. The patients were examined for sore throat (none, mild, moderate, or severe) at 0, 1, 6, 12, and 24h after extubation. The results were collected, analyzed and presented in table and figure. The highest incidence of postoperative sore throat occurred at 6h after extubation in all groups. There was a significantly lower incidence of postoperative sore throat in the benzydamine group than 5% lidocaine gel, 10% lidocaine spray, and normal saline groups. The benzydamine group had significantly decreased severity of postoperative sore throat compared with the 10% lidocaine, 5% lidocaine, and normal saline groups at observation time point. Compared with the 5% lidocaine the 10% lidocaine group had significantly increased incidence and severity of postoperative sore throat after extubation. Compared with normal saline the 10% lidocaine group had increased incidence of postoperative sore throat. There were no significant differences among groups in local or systemic side effects. So in conclusion, benzydamine hydrochloride gel on the endotracheal tube cuff is a simple and effective method to reduce the incidence and severity of postoperative sore throat. Application of 10% lidocaine spray should be avoided because of worsening of postoperative sore

  2. Comparative study between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on endotracheal tube cuff as regards postoperative sore throat.

    PubMed

    Mekhemar, Nashwa Abdallah; El-Agwany, Ahmed Samy; Radi, Wafaa Kamel; El-Hady, Sherif Mohammed

    2016-01-01

    Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups. Benzydamine hydrochloride gel, 5% lidocaine hydrochloride gel, 10% lidocaine hydrochloride spray, or normal saline were applied on endotracheal tube cuffs before endotracheal intubation. The patients were examined for sore throat (none, mild, moderate, or severe) at 0, 1, 6, 12, and 24h after extubation. The results were collected, analyzed and presented in table and figure. The highest incidence of postoperative sore throat occurred at 6h after extubation in all groups. There was a significantly lower incidence of postoperative sore throat in the benzydamine group than 5% lidocaine gel, 10% lidocaine spray, and normal saline groups. The benzydamine group had significantly decreased severity of postoperative sore throat compared with the 10% lidocaine, 5% lidocaine, and normal saline groups at observation time point. Compared with the 5% lidocaine the 10% lidocaine group had significantly increased incidence and severity of postoperative sore throat after extubation. Compared with normal saline the 10% lidocaine group had increased incidence of postoperative sore throat. There were no significant differences among groups in local or systemic side effects. So in conclusion, benzydamine hydrochloride gel on the endotracheal tube cuff is a simple and effective method to reduce the incidence and severity of postoperative sore throat. Application of 10% lidocaine spray should be avoided because of worsening of postoperative sore

  3. Lidocaine Concentration in Oral Tissue by the Addition of Epinephrine.

    PubMed

    Tanaka, Eri; Yoshida, Kenji; Kawaai, Hiroyoshi; Yamazaki, Shinya

    2016-01-01

    The vasoconstrictive effect due to the addition of epinephrine to local anesthetic has been clearly shown by measuring blood-flow volume or blood anesthetic concentration in oral mucosal tissue. However, there are no reports on the measurement of anesthetic concentration using samples directly taken from the jawbone and oral mucosal tissue. Consequently, in this study, the effect of lidocaine concentration in the jawbone and oral mucosal tissue by the addition of epinephrine to the local anesthetic lidocaine was considered by quantitatively measuring lidocaine concentration within the tissue. Japanese white male rabbits (n = 96) were used as test animals. General anesthesia was induced by sevoflurane and oxygen, and then cannulation to the femoral artery was performed while arterial pressure was constantly recorded. Infiltration anesthesia was achieved by 0.5 mL of 2% lidocaine containing 1 : 80,000 epinephrine in the upper jawbone (E(+)) and 0.5 mL of 2% of epinephrine additive-free lidocaine (E(0)) under the periosteum. At specified time increments (10, 20, 30, 40, 50, and 60 minutes), samples from the jawbone, oral mucosa, and blood were collected, and lidocaine concentration was directly measured by high-performance liquid chromatography. No significant differences in the change in blood pressure were observed either in E(+) or E(0). In both E(+) and E(0) groups, the serum lidocaine concentration peaked 10 minutes after local anesthesia and decreased thereafter. At all time increments, serum lidocaine concentration in E(+) was significantly lower than that in E(0). There were no significant differences in measured lidocaine concentration between jawbone and mucosa within either the E(+) or the E(0) groups at all time points, although the E(0) group had significantly lower jawbone and mucosa concentrations than the E(+) group at all time points when comparing the 2 groups to each other. Addition of epinephrine to the local anesthetic inhibited systemic

  4. Lidocaine Concentration in Oral Tissue by the Addition of Epinephrine

    PubMed Central

    Tanaka, Eri; Yoshida, Kenji; Kawaai, Hiroyoshi; Yamazaki, Shinya

    2016-01-01

    The vasoconstrictive effect due to the addition of epinephrine to local anesthetic has been clearly shown by measuring blood-flow volume or blood anesthetic concentration in oral mucosal tissue. However, there are no reports on the measurement of anesthetic concentration using samples directly taken from the jawbone and oral mucosal tissue. Consequently, in this study, the effect of lidocaine concentration in the jawbone and oral mucosal tissue by the addition of epinephrine to the local anesthetic lidocaine was considered by quantitatively measuring lidocaine concentration within the tissue. Japanese white male rabbits (n = 96) were used as test animals. General anesthesia was induced by sevoflurane and oxygen, and then cannulation to the femoral artery was performed while arterial pressure was constantly recorded. Infiltration anesthesia was achieved by 0.5 mL of 2% lidocaine containing 1 : 80,000 epinephrine in the upper jawbone (E+) and 0.5 mL of 2% of epinephrine additive–free lidocaine (E0) under the periosteum. At specified time increments (10, 20, 30, 40, 50, and 60 minutes), samples from the jawbone, oral mucosa, and blood were collected, and lidocaine concentration was directly measured by high-performance liquid chromatography. No significant differences in the change in blood pressure were observed either in E+ or E0. In both E+ and E0 groups, the serum lidocaine concentration peaked 10 minutes after local anesthesia and decreased thereafter. At all time increments, serum lidocaine concentration in E+ was significantly lower than that in E0. There were no significant differences in measured lidocaine concentration between jawbone and mucosa within either the E+ or the E0 groups at all time points, although the E0 group had significantly lower jawbone and mucosa concentrations than the E+ group at all time points when comparing the 2 groups to each other. Addition of epinephrine to the local anesthetic inhibited systemic absorption of local

  5. Effect of dexmedetomidine priming on convulsion reaction induced by lidocaine.

    PubMed

    Wang, Xi-Feng; Luo, Xiao-Ling; Liu, Wei-Cheng; Hou, Ben-Chao; Huang, Jian; Zhan, Yan-Ping; Chen, Shi-Biao

    2016-10-01

    To study the effect of dexmedetomidine priming on convulsion reaction induced by lidocaine.The New Zealand white rabbits were applied for the mechanism study of dexmedetomidine priming for preventing convulsion reaction induced by lidocaine. The influence of dexmedetomidine priming with different doses on the time for convulsion occurrence and the duration time of convulsion induced by lidocaine, as well as contents of excitatory amino acids (aspartate [Asp], glutamate [Glu]) and inhibitory amino acids (glycine [Gly], γ-aminobutyric acid [GABA]) in the brain tissue were investigated.With 3 and 5 μg/kg dexmedetomidine priming, the occurrence times of convulsion were prolonged from 196 seconds to 349 and 414 seconds, respectively. With dexmedetomidine priming, the contents of excitatory amino acids (Asp, Glu) were much reduced at occurrence time of convulsion comparing with that without dexmedetomidine priming, while content of inhibitory amino acids Gly was much enhanced.The application of dexmedetomidine before local anesthetics can improve intoxication dose threshold of the lidocaine, delay occurrence of the convulsion, and helped for the recovery of convulsion induced by lidocaine. The positive effect of dexmedetomidine on preventing convulsion would owe to not only the inhibition of excitatory amino acids (Asp, Glu), but also the promotion of inhibitory amino acids Gly secretion.

  6. Distinct pharmacologic substrate in lidocaine-sensitive, repetitive atrial tachycardia.

    PubMed

    Chiale, Pablo A; Faivelis, Luciano; Garro, Hugo A; Fernández, Pablo A; Herrera Paz, Juan J; Elizari, Marcelo V

    2012-06-01

    Lidocaine-sensitive, repetitive atrial tachycardia is an uncommon arrhythmia. The electrophysiologic substrate is still unknown, and the pharmacologic responses have not been fully explored. The aim of this study was to investigate the effects of intravenous adenosine and verapamil in patients with lidocaine-sensitive atrial tachycardia. In 9 patients with repetitive uniform atrial tachycardia, the response to intravenous adenosine (12 mg), lidocaine (1 mg/kg body weight), and verapamil (10 mg) were sequentially investigated. Simultaneous 12-lead electrocardiogram (ECG) was recorded at baseline and continuously monitored thereafter. Tracings were obtained at regularly timed intervals right after the administration of each drug to evaluate changes in the arrhythmia characteristics. Repetitive atrial tachycardia was abolished by intravenous lidocaine in the 9 patients within the first 2 minutes after the end of injection. Adenosine suppressed the arrhythmia in 2 patients and shortened the runs of atrial ectopic activity in 1 patient, while verapamil was effective in 2 patients, 1 of them insensitive to adenosine and the other 1 sensitive to this agent. In 5 patients, the arrhythmia was abolished by radiofrequency ablation at different sites of the right atrium. Lidocaine-sensitive atrial tachycardia may eventually be also suppressed by adenosine and/or verapamil. This suggests that this enigmatic arrhythmia may be caused by different underlying electrophysiologic substrates and that at least in some cases, delayed afterdepolarizations seem to play a determining role.

  7. Effect of dexmedetomidine priming on convulsion reaction induced by lidocaine

    PubMed Central

    Wang, Xi-Feng; Luo, Xiao-Ling; Liu, Wei-Cheng; Hou, Ben-Chao; Huang, Jian; Zhan, Yan-Ping; Chen, Shi-Biao

    2016-01-01

    Abstract To study the effect of dexmedetomidine priming on convulsion reaction induced by lidocaine. The New Zealand white rabbits were applied for the mechanism study of dexmedetomidine priming for preventing convulsion reaction induced by lidocaine. The influence of dexmedetomidine priming with different doses on the time for convulsion occurrence and the duration time of convulsion induced by lidocaine, as well as contents of excitatory amino acids (aspartate [Asp], glutamate [Glu]) and inhibitory amino acids (glycine [Gly], γ-aminobutyric acid [GABA]) in the brain tissue were investigated. With 3 and 5 μg/kg dexmedetomidine priming, the occurrence times of convulsion were prolonged from 196 seconds to 349 and 414 seconds, respectively. With dexmedetomidine priming, the contents of excitatory amino acids (Asp, Glu) were much reduced at occurrence time of convulsion comparing with that without dexmedetomidine priming, while content of inhibitory amino acids Gly was much enhanced. The application of dexmedetomidine before local anesthetics can improve intoxication dose threshold of the lidocaine, delay occurrence of the convulsion, and helped for the recovery of convulsion induced by lidocaine. The positive effect of dexmedetomidine on preventing convulsion would owe to not only the inhibition of excitatory amino acids (Asp, Glu), but also the promotion of inhibitory amino acids Gly secretion. PMID:27787355

  8. Characterization and comparison of lidocaine-tetracaine and lidocaine-camphor eutectic mixtures based on their crystallization and hydrogen-bonding abilities.

    PubMed

    Gala, Urvi; Chuong, Monica C; Varanasi, Ravi; Chauhan, Harsh

    2015-06-01

    Eutectic mixtures formed between active pharmaceutical ingredients and/or excipients provide vast scope for pharmaceutical applications. This study aimed at the exploration of the crystallization abilities of two eutectic mixtures (EM) i.e., lidocaine-tetracaine and lidocaine-camphor (1:1 w/w). Thermogravimetric analysis (TGA) for degradation behavior whereas modulated temperature differential scanning calorimetry (MTDSC) set in first heating, cooling, and second heating cycles, was used to qualitatively analyze the complex exothermic and endothermic thermal transitions. Raman microspectroscopy characterized vibrational information specific to chemical bonds. Prepared EMs were left at room temperature for 24 h to visually examine their crystallization potentials. The degradation of lidocaine, tetracaine, camphor, lidocaine-tetracaine EM, and lidocaine-camphor EM began at 196.56, 163.82, 76.86, 146.01, and 42.72°C, respectively, which indicated that eutectic mixtures are less thermostable compared to their individual components. The MTDSC showed crystallization peaks for lidocaine, tetracaine, and camphor at 31.86, 29.36, and 174.02°C, respectively (n = 3). When studying the eutectic mixture, no crystallization peak was observed in the lidocaine-tetracaine EM, but a lidocaine-camphor EM crystallization peak was present at 18.81°C. Crystallization occurred in lidocaine-camphor EM after being kept at room temperature for 24 h, but not in lidocaine-tetracaine EM. Certain peak shifts were observed in Raman spectra which indicated possible interactions of eutectic mixture components, when a eutectic mixture was formed. We found that if the components forming a eutectic mixture have crystallization peaks close to each other and have sufficient hydrogen-bonding capability, then their eutectic mixture is least likely to crystallize out (as seen in lidocaine-tetracaine EM) or vice versa (lidocaine-camphor EM).

  9. Caudal epidural analgesia using lidocaine alone or in combination with ketamine in dromedary camels Camelus dromedarius.

    PubMed

    Azari, Omid; Molaei, Mohammad M; Ehsani, Amir H

    2014-02-27

    This study was performed to investigate the analgesic effect of lidocaine and a combination of lidocaine and ketamine following epidural administration in dromedary camels. Ten 12-18-month-old camels were randomly divided into two equal groups. In group L, the animals received 2% lidocaine (0.22 mg/kg) and in group LK the animals received a mixture of 10% ketamine (1 mg/kg) and 2% lidocaine (0.22 mg/kg) administered into the first intercoccygeal (Co1-Co2) epidural space while standing. Onset time and duration of caudal analgesia, sedation level and ataxia were recorded after drug administration. Data were analysed by U Mann-Whitney tests and significance was taken as p < 0.05. The results showed that epidural lidocaine and co-administration of lidocaine and ketamine produced complete analgesia in the tail, anus and perineum. Epidural administration of the lidocaine-ketamine mixture resulted in mild to moderate sedation, whilst the animals that received epidural lidocaine alone were alert and nervous during the study. Ataxia was observed in all test subjects and was slightly more severe in camels that received the lidocaine-ketamine mixture. It was concluded that epidural administration of lidocaine plus ketamine resulted in longer caudal analgesia in standing conscious dromedary camels compared with the effect of administering lidocaine alone.

  10. The effects of lidocaine or a lidocaine-bupivacaine mixture administered into the infraorbital canal in dogs.

    PubMed

    Pascoe, Peter J

    2016-07-01

    OBJECTIVE To determine the onset, duration, and extent of regional nerve blocks performed by administration of lidocaine or lidocaine-bupivacaine into the infraorbital canal in dogs. ANIMALS 6 healthy hound-type dogs. PROCEDURES Under general anesthesia, stimulating needles were inserted into the gingiva dorsolateral to both maxillary canine (MC) teeth and the maxillary fourth premolar (MPM4) and second molar (MM2) teeth on the treatment side. A reflex-evoked muscle potential (REMP) was recorded from the digastricus muscle after noxious electrical stimulation at each site. After baseline measurements, 1 mL of 2% lidocaine solution or a 2% lidocaine-0.5% bupivacaine mixture (0.5 mL each) was injected into the infraorbital canal (at approx two-thirds of the canal length measured rostrocaudally). The REMPs were recorded for up to 7 hours. The REMP data for the contralateral (untreated control) canine tooth were used to normalize results for all stimulation sites. RESULTS With both treatments, nerve block for MC teeth on the treated side was achieved by 5 (n = 5 dogs) or 10 (1) minutes after injection, but nerve block for ipsilateral MPM4 and MM2 teeth was successful for only 3 dogs and 1 dog, respectively. Mean duration of nerve blocks for MC teeth was 120 and 277 minutes following injection of lidocaine and lidocaine-bupivacaine, respectively. CONCLUSIONS AND CLINICAL RELEVANCE Local anesthesia, as performed in this study, successfully blocked innervation of MC teeth, but results for MPM4 and MM2 teeth were inconsistent. This specific technique should not be used during tooth extractions caudal to the MC teeth.

  11. Dissecting lidocaine action: diethylamide and phenol mimic separate modes of lidocaine block of sodium channels from heart and skeletal muscle.

    PubMed Central

    Zamponi, G W; French, R J

    1993-01-01

    We have investigated block of sodium channels by diethylamide and phenol, which resemble the hydrophilic tertiary amine head and the hydrophobic aromatic tail of the lidocaine molecule, respectively. Diethylamide and phenol separately mimicked the fast and slow modes of block caused by lidocaine. Experiments were performed using single batrachotoxin-activated bovine cardiac and rat skeletal muscle sodium channels incorporated into neutral planar lipid bilayers. Diethylamide, only from the intracellular side, caused a voltage-dependent reduction in apparent single channel amplitude ('fast' block). Block was similar for cardiac and skeletal muscle channels, and increased in potency when extracellular sodium was replaced by N-methylglucamine, consistent with an intrapore blocking site. Thus, although occurring at 15-fold higher concentrations, block by diethylamide closely resembles the fast mode of block by lidocaine (Zamponi, G. W., D. D. Doyle, and R. J. French. 1993. Biophys. J. 65:80-90). For cardiac sodium channels, phenol bound to a closed state causing the appearance of long blocked events whose duration increased with phenol concentration. This slow block depended neither on voltage nor on the side of application, and disappeared upon treatment of the channel with trypsin. For skeletal muscle channels, slow phenol block occurred with only very low probability. Thus, phenol block resembles the slow mode of block observed for lidocaine (Zamponi, G. W., D. D. Doyle, and R. J. French. 1993. Biophys. J. 65:91-100). Our data suggest that there are separate sites for fast lidocaine block of the open channel and slow block of the "inactivated" channel. Fast block by diethylamide inhibited the long, spontaneous, trypsin-sensitive (inactivation-like) closures of cardiac channels, and hence secondarily antagonized slow block by phenol or lidocaine. This antagonism would potentiate shifts in the balance between the two modes of action of a tertiary amine drug caused by

  12. [Treatment of persistent postmastectomy pain with 5% Lidocaine medicated plaster].

    PubMed

    Cruto, M E; Baricocchi, E; Battistella, M; Bona, F; Giacoletto, G; Iacobellis, A; Moselli, N; Palomba, G; Sardo, E; Savojardo, M; Suita, L; Zocca, E; Debernardi, F

    2015-04-01

    Persistent postmastectomy pain (PPMP) syndrome is characterized by neuropathic pain that develops following surgery in breast cancer patients. The reported incidence of PPMP ranges between 30% and 50% and is estimated to increase as the number of women surviving cancer continues to rise. Though effective, today's drug treatments are poorly tolerated, limiting their use and reducing adherence to therapy. Since neuropathic pain is localized, international guidelines suggest that topical treatment with 5% Lidocaine medicated plaster either alone or combined with systemic drugs can be considered for pain management. In this retrospective study we reviewed the medical records of 11 patients treated with 5% lidocaine medicated plaster for moderate-to-severe PPMP at our institute between November 2013 and October 2014. Analysis showed that treatment with 5% Lidocaine medicated plaster, either alone or in combination with systemic drugs, achieved significant pain control already after the first week of therapy. The effectiveness and tolerability of 5% Lidocaine medicated plaster we observed suggests that it is a viable option in the management of PPMP.

  13. Evaluation of chemical enhancers in the transdermal delivery of lidocaine.

    PubMed

    Lee, Philip J; Ahmad, Naina; Langer, Robert; Mitragotri, Samir; Prasad Shastri, V

    2006-02-03

    The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl myristate (IPM) showed no significant flux enhancement. However, the binary system of IPM/n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6 +/- 8.4 microg cm(-2) h(-1) through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (p < 0.001). NMP was also found to co-transport through human skin with lidocaine free base and improve enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs.

  14. Immediate reaction to lidocaine with periorbital edema during upper blepharoplasty

    PubMed Central

    Presman, Benjamin; Vindigni, Vincenzo; Tocco-Tussardi, Ilaria

    2016-01-01

    Introduction Blepharoplasty is the fourth most commonly performed cosmetic surgery in the US, with 207,000 operations in 2014. Lidocaine is the preferred anesthetic agent for blepharoplasty. Presentation of case We describe the unusual case of acute periorbital edema following local anesthesia with lidocaine for upper blepharoplasty. At present, only two other reports of periorbital reactions to lidocaine are present in the literature. The reactions observed are significant palpebral swelling and erythema with scaling of the cheek. Fortunately the swelling, although marked, is transient in nature and resolves almost spontaneously without affecting the visual acuity. Discussion Patients reporting adverse reactions should be screened for allergy according to the standard protocols, but skin testing has only been reported to be positive in less than 10% of all cases and allergy confirmation with IgE is even more rare. Conclusion In clinical practice, we recommend that patient should be informed about the possibility of recurrence of an adverse reaction in case of re-exposure to lidocaine, even in the vast majority of cases where true allergy could not be proven. In case of further need for local anesthesia with history of an adverse event, a different agent may be chosen even from the same class (another amide) as cross-reactions in the amide group are rare. Otherwise, an anesthetic from the ester group can also be safely used. PMID:26785079

  15. Lidocaine attenuates cognitive impairment after isoflurane anesthesia in old rats.

    PubMed

    Lin, Daowei; Cao, Lin; Wang, Zhi; Li, Jiejie; Washington, Jacqueline M; Zuo, Zhiyi

    2012-03-17

    Post-operative cognitive dysfunction (POCD) is a clinical phenomenon that has drawn significant attention from the public and scientific community. Age is a risk factor for POCD. However, the contribution of general anesthesia/anesthetics to POCD and the underlying neuropathology are not clear. Here, we showed that 18-month-old male Fisher 344 rats exposed to 1.2% isoflurane, a general anesthetic, for 2h had significant learning and memory impairments assessed at 2-4 weeks after isoflurane exposure. These isoflurane effects were attenuated by intravenous lidocaine (1.5mg/kg as a bolus and then 2mg/kg/h during isoflurane exposure), a local anesthetic that has neuroprotective effect. Exposure to isoflurane or isoflurane plus lidocaine did not change the neuronal and synaptic density as well as the expression of NeuN (a neuronal protein), drebrin (a dendritic spine protein), synaptophysin (a synaptic protein), activated caspase 3 and caspase-activated DNase in the hippocampus at 29 days after isoflurane exposure when cognitive impairment was present. Isoflurane and lidocaine did not affect the amount of β-amyloid peptide, total tau and phospho-tau in the cerebral cortex as well as interleukin-1β and tumor necrosis factor-α in the hippocampus at 29 days after isoflurane exposure. Thus, isoflurane induces learning and memory impairment in old rats. Lidocaine attenuates these isoflurane effects. Isoflurane may not cause long-lasting neuropathological changes.

  16. [Capsaicin and lidocaine usage in functional disorders of urinary bladder].

    PubMed

    Juszczak, Kajetan; Thor, Piotr J

    2011-01-01

    Most of the drugs in the treatment of functional disorders of the urinary bladder has a peripheral effect. Their work consists mainly in reducing detrusor contractility of the bladder, or effects on the afferent innervation. Anticholinergics are the first drugs of choice. An alternative pharmacological treatment is to eliminate the overactivity by acting on the bladder afferent innervation, while not inhibiting its contractility. One option is to modulate the pharmacological activity of sensory mechanisms governing the functioning of the bladder via the vanilloid receptor (TRPV1) and ancyrin (TRPA1). Intravesical treatment with capsaicin or lidocaine only partially reduces bladder sensation. Furthermore, clinical use of lidocaine in the treatment of overactive bladder (OAB) is reduced to intravesical supply before capsaicin instillation to reduce the symptoms associated with initial phase of C-fibres sensitization. This paper presents the current state of knowledge regarding the use of capsaicin and lidocaine in functional disorders of the urinary bladder, as well as discusses the impact of these substances on afferent C-fibres and the activity of the urinary bladder. Based on previous studies intravesical capsaicin and lidocaine therapy is one of the alternative treatment options in selected patients with functional disorders of the urinary bladder (in particular OAB) in addition to standard anticholinergics therapy or the newer generation of therapies using botulinum toxin.

  17. Lidocaine: an inhibitor in the free-radical-induced hemolysis of erythrocytes.

    PubMed

    Tang, You-Zhi; Liu, Zai-Qun; Wu, Di

    2009-01-01

    Lidocaine was reported to protect erythrocytes from hemolysis induced by 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). Since AAPH-induced hemolysis was a convenient in vitro experimental system to mimic erythrocytes undergoing peroxyl radicals attack, the aim of this work was to investigate the antioxidant effect of lidocaine on AAPH-induced hemolysis by chemical kinetics. As a result, one molecule of lidocaine can only trap 0.37 radical, much lower than melatonin. Meanwhile, lidocaine cannot protect erythrocytes from hemolysis induced by hemin, which the mechanism of hemolysis was due to the erythrocyte membrane destroyed by hemin. Accordingly, lidocaine protected erythrocytes by scavenging radicals preferentially rather than by stabilizing membrane. Moreover, the interactions of lidocaine with two radical species, including 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) radical cation (ABTS(+*)) and 2,2'-diphenyl-1-picrylhydrazyl (DPPH), indicated that lidocaine can reduce ABTS(+*) with 260 microM as the 50% inhibition concentration (IC(50)) and cannot react with DPPH. Thus, lidocaine served as a reductant rather than a hydrogen donor to interact with radicals. Finally, the quantum calculation proved that, compared with the melatonin radical, the stabilization of N-centered radical of lidocaine was higher than the amide-type N-centered radical but lower than the indole-type N-centered radical in melatonin. These results provided basic information for lidocaine to be an antiradical drug.

  18. Intravenous Lidocaine as an Adjuvant for Pain Associated with Sickle Cell Disease.

    PubMed

    Nguyen, Natalie L; Kome, Anne M; Lowe, Denise K; Coyne, Patrick; Hawks, Kelly G

    2015-01-01

    The objectives of this study were to evaluate the efficacy and safety of adjuvant intravenous (IV) lidocaine in adults with sickle cell disease (SCD). This was a retrospective review. Adults with SCD receiving at least one IV lidocaine infusion from 2004 to 2014 were included. Patient demographics, lidocaine treatment parameters, pain scores, pain medications, and adverse effects were recorded. Eleven patients were identified, yielding 15 IV lidocaine trials. Clinical improvement in pain scores from pre-lidocaine challenge to 24 hours post-lidocaine challenge, defined by ≥ 20% reduction in pain scores, was achieved in 53.3% (8 of 15) of IV lidocaine challenges. Of the 8 clinically successful trials, the mean reduction in morphine dose equivalents (MDE) from 24 hours pre-lidocaine challenge to 24 hours post-lidocaine challenge was 32.2%. Additionally, clinically successful trials had a mean initial and a maximum dose of 1 mg/kg/h (range: 0.5-2.7 mg/kg/h) and 1.3 mg/kg/h (range: 0.5-1.9 mg/kg/h), respectively. On average, these patients underwent 3 dose titrations (range: 1-8) and received lidocaine infusions for 4.4 days (range: 2-8 days). Two patients experienced disorientation and dizziness. The authors conclude that adjuvant IV lidocaine provided pain relief and a mean reduction in MDE during sickle cell pain crisis. These results provide preliminary insight into the use of IV lidocaine for treating pain in patients with SCD, although prospective studies are needed to determine efficacy, dosing, and tolerability of IV lidocaine in this patient population.

  19. The disposition of lidocaine during a 12-hour intravenous infusion to postoperative horses.

    PubMed

    Milligan, M; Kukanich, B; Beard, W; Waxman, S

    2006-12-01

    Lidocaine is administered as an intravenous infusion to horses for a variety of reasons, but no study has assessed plasma lidocaine concentrations during a 12-h infusion to horses. The purpose of this study was to evaluate the plasma concentrations and pharmacokinetics of lidocaine during a 12-h infusion to postoperative horses. A second purpose of the study was to evaluate the in vitro plasma protein binding of lidocaine in equine plasma. Lidocaine hydrochloride was administered as a loading dose, 1.3 mg/kg over 15 min, then by a constant rate IV infusion, 50 microg/kg/min to six postoperative horses. Lidocaine plasma concentrations were measured by a validated high-pressure liquid chromatography method. One horse experienced tremors and collapsed 5.5 h into the study. The range of plasma concentrations during the infusion was 1.21-3.13 microg/mL. Lidocaine plasma concentrations were significantly increased at 0.5, 4, 6, 8, 10 and 12 h compared with 1, 2 and 3 h. The in vitro protein binding of lidocaine in equine plasma at 2 microg/mL was 53.06+/-10.28% and decreased to 27.33+/-9.72% and 29.52+/-6.44% when in combination with ceftiofur or the combination of ceftiofur and flunixin, respectively. In conclusion, a lower lidocaine infusion rate may need to be administered to horses on long-term lidocaine infusions. The in vitro protein binding of lidocaine is moderate in equine plasma, but highly protein bound drugs may displace lidocaine increasing unbound concentrations and the risk of lidocaine toxicity.

  20. Plasma concentrations of lidocaine in dogs following lidocaine patch application over an incision compared to intact skin.

    PubMed

    Joudrey, S D; Robinson, D A; Kearney, M T; Papich, M G; da Cunha, A F

    2015-12-01

    The objective was to compare plasma lidocaine concentrations when a commercially available 5% lidocaine patch was placed on intact skin vs. an incision. Our hypothesis was that greater absorption of lidocaine would occur from the incision site compared to intact skin. Ten dogs were used in a crossover design. A patch was placed over an incision, and then after a washout period, a patch was placed over intact skin. Plasma lidocaine concentrations were measured at patch placement; 20, 40 and 60 min; and 2, 4, 6, 12, 24, 36, 48, 72 and 96 h after patch placement. After patch removal, the skin was graded using a subjective skin reaction system. No dogs required rescue analgesia, and no toxicity or skin reaction was noted. Mean ± SD AUC and CMAX were 3054.29 ± 1095.93 ng·h/mL and 54.1 ± 15.84 ng/mL in the Incision Group, and 2269.9 ± 1037.08 ng·h/mL and 44.5 ± 16.34 ng/mL in the No-Incision Group, respectively. The AUC was significantly higher in the Incision Group. The results of the study demonstrate that the actual body exposure to lidocaine was significantly higher when an incision was present compared to intact skin. No adverse effects were observed from either treatment. Efficacy was not evaluated.

  1. The immediate effects of lidocaine iontophoresis using interferential current on pressure sense threshold and tactile sensation.

    PubMed

    Yoosefinejad, Amin Kordi; Motealleh, Alireza; Abbasnia, Keramatollah

    2016-01-01

    Iontophoresis is the noninvasive delivery of ions using direct current. The direct current has some disadvantages such as skin burning. Interferential current is a kind of alternating current without limitations of direct current; so the purpose of this study is to investigate and compare the effects of lidocaine, interferential current and lidocaine iontophoresis using interferential current. 30 healthy women aged 20-24 years participated in this randomized clinical trial study. Pressure, tactile and pain thresholds were evaluated before and after the application of treatment methods. Pressure, tactile and pain sensitivity increased significantly after the application of lidocaine alone (p < 0.005) and lidocaine iontophoresis using interferential current (p < 0.0001). Lidocaine iontophoresis using interferential current can increase perception threshold of pain, tactile stimulus and pressure sense more significantly than lidocaine and interferential current alone.

  2. Stability of lidocaine hydrochloride in 5% dextrose injection in plastic bags

    SciTech Connect

    Smith, F.M.; Nuessle, N.O.

    1981-11-01

    The stability of lidocaine injection mixed with 5% dextrose injection and refrigerated or stored at room temperature was studied. Lidocaine injection was added to 5% dextrose injection to provide a lidocaine hydrochloride concentration of 4 mg/ml. Samples were assayed for lidocaine and its degradation product, 2,6-dimethylaniline, after 30, 60, and 120 days of storage at room temperature (30 degrees C) and refrigerated temperature (4 degrees C). The analysis was by a stability-indicating HPLC method. Degradation product 2,6-dimethylaniline was not detected at any assay time at either temperature. No statistically significant loss of lidocaine occurred at either temperature. Lidocaine hydrochloride injection is chemically stable for up to 120 days at either 30 degrees C or 4 degrees C when mixed with 5% dextrose injection in plastic infusion bags.

  3. Kinetics of Uptake and Washout of Lidocaine in Rat Sciatic Nerve In Vitro

    PubMed Central

    Leeson, Stanley; Strichartz, Gary

    2012-01-01

    Background The potency and efficacy of local anesthetics injected clinically for peripheral nerve block depends strongly on the rate of neural drug uptake. However, since diffusion into surrounding tissues and removal by the vascular system are major factors in the overall distribution of lidocaine in vivo, true kinetics of drug/neural tissue interactions must be studied in the absence of those confounding factors. Methods Uptake: Ensheathed or desheathed isolated rat sciatic nerves were exposed to [14C]-lidocaine for 0-180min and then removed and the lidocaine content of nerve and sheath analyzed. Washout: Isolated nerves were soaked in [14C]-lidocaine for 60min and then placed in lidocaine-free solution for 0-30min, with samples removed at different times to assess the drug content. Experimental variables included the effects of the ensheathing epineurium, lidocaine concentration, pH, presence of CO2-bicarbonate, and incubation duration. Results The equilibrium uptake of lidocaine increased with incubation time, concentration and the fraction of molecules in the non-ionized form. The uptake rate was unaffected by drug concentration, but was about halved by the presence of the epineurial sheath, with the washout rate slowed less. Slight alkalinization, from pH 6.8 to pH 7.4, by bicarbonate-CO2 buffer or a non-bicarbonate buffer, enhanced the neural uptake, and to the same degree. The washout of lidocaine was faster after shorter incubations at high concentrations than when equal amounts of lidocaine were taken up after long incubations at low lidocaine concentrations. Conclusion Lidocaine enters a nerve by a process other than free diffusion, through an epineurial sheath that is a slight obstacle. Given the rapid entry in vitro compared to the much smaller and transient content measured in vivo, it seems highly unlikely that lidocaine equilibrates with the nerve during a peripheral blockade. PMID:23400993

  4. Attenuation of Cardiovascular Response with Lidocaine 1.5 mg/kg and Labetalol 10 mg

    DTIC Science & Technology

    1990-07-01

    5 ug/ml). Low dose 7 IV Lidocaine has been demonstrated to decrease opioid requirements for post operative pain , and also has been shown to reduce...means of alleviating acute and chronic pain . As adjuncts to general anesthesia, infusions of lidocaine have been used to supplement thiopental and...REPORIV DOC~UMENTAT;O(.)N PAGE - - Ir . . . .. .. . . . . . . - 1990 THESISiEGGEREMM Attenuation of Cardiovascular Response with Lidocaine N 1.5 mg

  5. Comparison of Iontophoretic Lidocaine to EMLA Cream for Pain Reduction Prior to Intravenous Fannulation in Adults

    DTIC Science & Technology

    2000-10-01

    i COMPARISON OF IONTOPHORETIC LIDOCAINE TO EMLA CREAM FOR PAIN REDUCTIONPRIOR TO INTRAVENOUS CANNULATION IN ADULTS Kenneth Lee Spence LT, NC, USN...COMPARISON OF IONTOPHORETIC LIDOCAINE TO EMLA CREAM FOR PAIN REDUCTION PRIOR TO INTRAVENOUS CANNULATION IN ADULTS 5a. CONTRACT NUMBER 5b. GRANT...most operative anesthesia, can be a source of pain and anxiety. Lidocaine , a local anesthetic, is frequently injected intradermally to decrease pain

  6. [Proven and expected benefits of intravenous lidocaine administered during the perioperative period].

    PubMed

    Giudice, V; Lauwick, S; Kaba, A; Joris, J

    2012-02-01

    Local anesthetics which inhibit sodium channels are used for neural blockade during infiltration and locoregional anesthesia. Furthermore lidocaine given intravenously acts on other cellular systems and produces multiple properties, some of which are beneficial during the perioperative period. Indeed, intravenous lidocaine is analgesic, antihyperalgesic, antiinflammatory, and improves the recovery of bowel function after abdominal surgery. As a consequence, lidocaine has been added to postoperative analgesic strategies. This article reviews clinically relevant properties of intravenous lidocaine. Its future perspectives for the prevention of chronicisation of postoperative pain, facilitation of postoperative fast track programs, and prevention of tumoral recurrence are also discussed.

  7. Effect of fentanyl and lidocaine on the end-tidal sevoflurane concentration preventing motor movement in dogs.

    PubMed

    Suarez, Martin A; Seddighi, Reza; Egger, Christine M; Rohrbach, Barton W; Cox, Sherry K; KuKanich, Butch K; Doherty, Thomas J

    2017-01-01

    OBJECTIVE To determine effects of fentanyl, lidocaine, and a fentanyl-lidocaine combination on the minimum alveolar concentration of sevoflurane preventing motor movement (MACNM) in dogs. ANIMALS 6 adult Beagles. PROCEDURES Dogs were anesthetized with sevoflurane in oxygen 3 times (1-week intervals). Baseline MACNM (MACNM-B) was determined starting 45 minutes after induction of anesthesia. Dogs then received 1 of 3 treatments IV: fentanyl (loading dose, 15 μg/kg; constant rate infusion [CRI], 6 μg/kg/h), lidocaine (loading dose, 2 mg/kg; CRI, 6 mg/kg/h), and the fentanyl-lidocaine combination at the same doses. Determination of treatment MACNM (MACNM-T) was initiated 90 minutes after start of the CRI. Venous blood samples were collected at the time of each treatment MACNM measurement for determination of plasma concentrations of fentanyl and lidocaine. RESULTS Mean ± SEM overall MACNM-B for the 3 treatments was 2.70 ± 0.27 vol%. The MACNM decreased from MACNM-B to MACNM-T by 39%, 21%, and 55% for fentanyl, lidocaine, and the fentanyl-lidocaine combination, respectively. This decrease differed significantly among treatments. Plasma fentanyl concentration was 3.25 and 2.94 ng/mL for fentanyl and the fentanyl-lidocaine combination, respectively. Plasma lidocaine concentration was 2,570 and 2,417 ng/mL for lidocaine and the fentanyl-lidocaine combination, respectively. Plasma fentanyl and lidocaine concentrations did not differ significantly between fentanyl and the fentanyl-lidocaine combination or between lidocaine and the fentanyl-lidocaine combination. CONCLUSIONS AND CLINICAL RELEVANCE CRIs of fentanyl, lidocaine, and the fentanyl-lidocaine combination at the doses used were associated with clinically important and significant decreases in the MACNM of sevoflurane in dogs.

  8. Intravenous Lidocaine Infusion to Treat Chemotherapy-Induced Peripheral Neuropathy.

    PubMed

    Papapetrou, Peter; Kumar, Aashish J; Muppuri, Rudram; Chakrabortty, Shushovan

    2015-11-01

    Chemotherapy-induced peripheral neuropathy is a debilitating side effect of chemotherapy, which manifests as paresthesias, dysesthesias, and numbness in the hands and feet. Numerous chemoprotective agents and treatments have been used with limited success to treat chemotherapy-induced peripheral neuropathy. We report a case in which a patient presenting with chemotherapy-induced peripheral neuropathy received an IV lidocaine infusion over the course of 60 minutes with complete symptomatic pain relief for a prolonged period of 2 weeks.

  9. Dexamethasone added to lidocaine prolongs axillary brachial plexus blockade.

    PubMed

    Movafegh, Ali; Razazian, Mehran; Hajimaohamadi, Fatemeh; Meysamie, Alipasha

    2006-01-01

    Different additives have been used to prolong regional blockade. We designed a prospective, randomized, double-blind study to evaluate the effect of dexamethasone added to lidocaine on the onset and duration of axillary brachial plexus block. Sixty patients scheduled for elective hand and forearm surgery under axillary brachial plexus block were randomly allocated to receive either 34 mL lidocaine 1.5% with 2 mL of isotonic saline chloride (control group, n = 30) or 34 mL lidocaine 1.5% with 2 mL of dexamethasone (8 mg) (dexamethasone group, n = 30). Neither epinephrine nor bicarbonate was added to the treatment mixture. We used a nerve stimulator and multiple stimulations technique in all of the patients. After performance of the block, sensory and motor blockade of radial, median, musculocutaneous, and ulnar nerves were recorded at 5, 15, and 30 min. The onset time of the sensory and motor blockade was defined as the time between last injection and the total abolition of the pinprick response and complete paralysis. The duration of sensory and motor blocks were considered as the time interval between the administration of the local anesthetic and the first postoperative pain and complete recovery of motor functions. Sixteen patients were excluded because of unsuccessful blockade. The duration of surgery and the onset times of sensory and motor block were similar in the two groups. The duration of sensory (242 +/- 76 versus 98 +/- 33 min) and motor (310 +/- 81 versus 130 +/- 31 min) blockade were significantly longer in the dexamethasone than in the control group (P < 0.01). We conclude that the addition of dexamethasone to lidocaine 1.5% solution in axillary brachial plexus block prolongs the duration of sensory and motor blockade.

  10. Infiltrated lidocaine 2% with epinephrine 1:80,000 causes more postoperative pain than lidocaine 2% after oral soft tissue surgery.

    PubMed Central

    Jorkjend, L.; Skoglund, L. A.

    1999-01-01

    A controlled, randomized, double-blind, within-patient, crossover study was made with 50 patients (28 women and 22 men) of mean age 47 years (range, 32-69 years) who were subjected to identical bilateral gingivectomies. On one occasion, lidocaine 2% was infiltrated as the local anesthetic. On the other occasion, lidocaine 2% with epinephrine 1:80,000 was given. Postoperative pain intensity was recorded by the patients on a 100-mm visual analogue scale every hour during an 11-hour observation period. The mean pain intensity was numerically higher after lidocaine 2% at 0 hours and 1 hour postoperatively. Then the mean pain intensity after lidocaine 2% was lower than that after lidocaine 2% with epinephrine 1:80,000 throughout the remaining observation period. The difference in pain intensity was statistically significant (P < .05) at 2, 4, 5, 6, and 7 hours after surgery. Mean sum (SEM) pain intensity over the 11-hour observation period was lower (P = .03) after lidocaine 2%, 66.5 (13.4) mm than after lidocaine 2% with epinephrine 1:80,000, 92.6 (15.4) mm. The study shows that high epinephrine concentration (1:80,000) increases the postoperative pain after dental soft tissue surgery with mild pain. PMID:10853568

  11. A Comparative Study of Lidocaine and Lidocaine­ Mannitol in Anesthetizing Human Teeth with Inflamed Pulps

    PubMed Central

    Talati, Ali; Bidar, Maryam; Sadeghi, Ghazal; Nezami, Hossein

    2006-01-01

    INTRODUCTION: Failure to achieve adequate and profound anesthesia in teeth with acute pulp inflammation is a common condition during emergency visits in root canal therapy. Many different anesthetic solutions such as morphine and capsaicin have accordingly been examined. Mannitol­ an alcoholic sugar with high osmotic pressure level- is applicated for reducing intracranial and post retinal pressure in medicine. It has also been used for its diuretic effect. In combination with local anesthetic solution, it increases permeability of the nerve fiber sheath and leads to influx of the local anesthetic through cytoplasmic membrane .The purpose of the present study was to compare the efficacy of routine local anesthesia with or without using mannitol in teeth with inflamed pulps. MATERIALS AND METHODS: one hundred patients with acute dental pain in posterior teeth were selected. Vials with 3 ml anesthetic solution containing 2.5% lidocaine with 1/80000 epinephrine or 2.5% lidocaine with 1/80000 epinephrine and 0.5 mol mannitol were used for anesthesia. For each patient, the routine injection technique was applied, during the removal of decay and dentine. Depth of anesthesia was evaluated and the supplementary injection was done in case of pain feeling and then pulpotomy was done. The analysis of data was done using chi-square statistical test. RESULTS: The results showed that complete anesthesia after the first injection was obtained with lidocaine mannitol in 46% and with lidocaine alone in 38% of cases. However, the difference was not significant. CONCLUSION: These finding suggest that the addition of mannitol to the standard anesthetic solution could insignificantly increase the level of anesthesia in teeth with inflamed pulps. PMID:24494021

  12. Effects of glucose administered with lidocaine solution on spinal neurotoxicity in rats

    PubMed Central

    Ma, Hanxiang; Xu, Tingting; Xiong, Xiangsheng; Mao, Jingjing; Yang, Fan; Zhang, Yonghai; Bai, Zhixia; Chen, Xuexin

    2015-01-01

    To investigate whether intrathecal administration of 10% glucose increases functional impairment and histologic damage in rats when mixed with 5% lidocaine. After implanted intrathecal catheter, 32 male Sprague-Dawley rats were randomly assigned to one of four groups: lidocaine group (Group L, n=8) received 5% lidocaine 20 µL, lidocaine with glucose group (Group LG, n=8) received 5% lidocaine with 10% glucose 20 µL, glucose group (Group G, n=8) received 10% glucose 20 µL and normal saline group received normal saline 20 µL (Group NS, n=8). Four days after intrathecal injection, sensory impairments of rats in the four groups were evaluated by using the tail-flick test. The histologic changes of spinal cord and nerve roots were observed by electron microscopy and light microscopy. There was no significant difference in baseline tail-flick latencies between the four groups (P=0.284). On the 4th day after intrathecal injection, the assessment result of sensory function was similar to baseline (P=0.217) in saline-treated animals. Sensory impairment occurred after intrathecal administration of 5% lidocaine, and 10% glucose with 5% lidocaine worsen this satiation (P=0.0001); histologic changes in 10% glucose with 5% lidocaine-treated group has differ significantly from lidocaine-treated group (P=0.001). Sensory function after intrathecal administration of 10% glucose was similar to baseline and did not differ from the saline group (P=0.995); histologic changes in 10% glucose-treated rats did not differ significantly from saline controls (P=0.535). These results suggest that 5% lidocaine can induce spinal neurotoxicity and 10% glucose with 5% lidocaine could worsen spinal neurotoxicity. PMID:26884984

  13. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  14. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  15. The molecular structure and vibrational, (1)H and (13)C NMR spectra of lidocaine hydrochloride monohydrate.

    PubMed

    Badawi, Hassan M; Förner, Wolfgang; Ali, Shaikh A

    2016-01-05

    The structure, vibrational and NMR spectra of the local anesthetic drug lidocaine hydrochloride monohydrate salt were investigated by B3LYP/6-311G(∗∗) calculations. The lidocaine·HCl·H2O salt is predicted to have the gauche structure as the predominant form at ambient temperature with NCCN and CNCC torsional angles of 110° and -123° as compared to 10° and -64°, respectively in the base lidocaine. The repulsive interaction between the two N-H bonds destabilized the gauche structure of lidocaine·HCl·H2O salt. The analysis of the observed vibrational spectra is consistent with the presence of the lidocaine salt in only one gauche conformation at room temperature. The (1)H and (13)C NMR spectra of lidocaine·HCl·H2O were interpreted by experimental and DFT calculated chemical shifts of the lidocaine salt. The RMSD between experimental and theoretical (1)H and (13)C chemical shifts for lidocaine·HCl·H2O is 2.32 and 8.21ppm, respectively.

  16. Cardiopulmonary Effects of Constant-Rate Infusion of Lidocaine for Anesthesia during Abdominal Surgery in Goats.

    PubMed

    Malavasi, Lais M; Greene, Stephen A; Gay, John M; Grubb, Tammy L

    2016-01-01

    Lidocaine is commonly used in ruminants but has an anecdotal history of being toxic to goats. To evaluate lidocaine's effects on selected cardiopulmonary parameters. Isoflurane-anesthetized adult goats (n = 24) undergoing abdominal surgery received a loading dose of lidocaine (2.5 mg/kg) over 20 min followed by constant-rate infusion of lidocaine (100 μg/kg/min); control animals received saline instead of lidocaine. Data collected at predetermined time points during the 60-min surgery included heart rate, mean arterial blood pressure, pO2, and pCO2. According to Welch 2-sample t tests, cardiopulmonary variables did not differ between groups. For example, after administration of the loading dose, goats in the lidocaine group had a mean heart rate of 88 ± 28 bpm, mean arterial blood pressure of 70 ± 19 mm Hg, pCO2 of 65 ± 13 mm Hg, and pO2 of 212 ± 99 mm Hg; in the saline group, these values were 90 ± 16 bpm, 76 ± 12 mm Hg, 61 ± 9 mm Hg, and 209 ± 83 mm Hg, respectively. One goat in the saline group required an additional dose of butorphanol. Overall our findings indicate that, at the dose provided, intravenous lidocaine did not cause adverse cardiopulmonary effects in adult goats undergoing abdominal surgery. Adding lidocaine infusion during general anesthesia is an option for enhancing transoperative analgesia in goats.

  17. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  18. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  19. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  20. Hepatic Chemoembolization: Effect of Intraarterial Lidocaine on Pain and Postprocedure Recovery

    SciTech Connect

    Hartnell, George G.; Gates, Julia; Stuart, Keith; Underhill, Jonathan; Brophy, David P.

    1999-07-15

    Purpose: To determine if intraarterial lidocaine reduces pain during and after chemoembolization, and whether it influences postprocedure recovery. Methods: Two patient cohorts undergoing selective hepatic chemoembolization were compared. Chemoembolization was performed without lidocaine (control group) in 27 patients and intraarterial lidocaine was used (lidocaine group) in 29 similar patients. Objective changes in patient management were assessed. Pain reduction in 31 more procedures with lidocaine (total 60) was assessed and related to tumor type. Results: During chemoembolization, intraarterial lidocaine reduced the need for additional intravenous analgesics from 69% to 19%. After chemoembolization the mean Dilaudid dose in the first 24 hr was reduced from 9.5 mg to 4.15 mg; accordingly, the mean length of hospital stay was reduced from 67.5 to 53.5 hr. During the day of chemoembolization, the mean oral fluid intake increased from 420 ml (control group) to 487 ml (lidocaine group); the percentage of patients taking solid food on the day of chemoembolization increased from 3% to 43%. Conclusion: Intraarterial lidocaine during chemoembolization reduces the severity and duration of pain after chemoembolization resulting in faster recovery thus reducing the length of hospitalization.

  1. Synergistic effect of lidocaine with pingyangmycin for treatment of venous malformation using a mouse spleen model

    PubMed Central

    Bai, Nan; Chen, Yuan-Zheng; Mao, Kai-Ping; Fu, Yanjie; Lin, Qiang; Xue, Yan

    2014-01-01

    Aims: To explore whether lidocaine has the synergistic effect with pingyangmycin (PYM) in the venous malformations (VMs) treatment. Methods: The mouse spleen was chosen as a VM model and injected with different concentration of lidocaine or PYM or jointly treated with lidocaine and PYM. After 2, 5, 8 or 14 days, the mouse spleen tissues were acquired for hematoxylin-eosin (HE) staining, transmission electron microscopy (TEM) analysis, TUNEL assay and quantitative RT-PCR analysis to examine the toxicological effects of lidocaine and PYM on splenic vascular endothelial cells. Results: 0.4% of lidocaine mildly promoted the apoptosis of endothelial cells, while 2 mg/ml PYM significantly elevated the apoptotic ratios. However, the combination of 0.2% lidocaine and 0.5 mg/ml PYM notably elevated the apoptotic ratios of splenic cells and severely destroyed the configuration of spleen, compared to those of treatment with 0.5 mg/ml PYM alone. Conclusion: Lidocaine exerts synergistic effects with PYM in promoting the apoptosis of mouse splenic endothelial cells, indicating that lidocaine possibly promotes the therapeutic effects of PYM in VMs treatment via synergistically enhancing the apoptosis of endothelial cells of malformed venous lesions. PMID:24966943

  2. Anesthetic efficacy of lidocaine/meperidine for inferior alveolar nerve blocks in patients with irreversible pulpitis.

    PubMed

    Bigby, Jason; Reader, Al; Nusstein, John; Beck, Mike

    2007-01-01

    The purpose of this prospective, randomized, single-blind study was to compare the anesthetic efficacy of lidocaine with epinephrine to lidocaine plus meperidine with epinephrine for inferior alveolar nerve blocks (IAN) in patients with mandibular posterior teeth experiencing irreversible pulpitis. Forty-eight emergency patients diagnosed with irreversible pulpitis of a mandibular posterior tooth randomly received, in a single-blind manner, 36 mg of lidocaine with 18 mug epinephrine or 36 mg of lidocaine with 18 mug of epinephrine plus 36 mg meperidine with 18 mug epinephrine, using a conventional inferior alveolar nerve block. Endodontic access was begun 15 minutes after solution deposition, and all patients were required to have profound lip numbness. Success was defined as no or mild pain (visual analog scale recordings) upon endodontic access or initial instrumentation. The success rate for the inferior alveolar nerve block using the lidocaine solution was 26%, and for the lidocaine/meperidine solution, the success rate was 12%. There was no significant difference (p = 0.28) between the two solutions. In conclusion, for mandibular posterior teeth with irreversible pulpitis, the addition of 36 mg of meperidine to a lidocaine solution administered in a conventional IAN block did not improve the success rate over a standard lidocaine solution.

  3. Cardiopulmonary Effects of Constant-Rate Infusion of Lidocaine for Anesthesia during Abdominal Surgery in Goats

    PubMed Central

    Malavasi, Lais M; Greene, Stephen A; Gay, John M; Grubb, Tammy L

    2016-01-01

    Lidocaine is commonly used in ruminants but has an anecdotal history of being toxic to goats. To evaluate lidocaine's effects on selected cardiopulmonary parameters. Isoflurane-anesthetized adult goats (n = 24) undergoing abdominal surgery received a loading dose of lidocaine (2.5 mg/kg) over 20 min followed by constant-rate infusion of lidocaine (100 μg/kg/min); control animals received saline instead of lidocaine. Data collected at predetermined time points during the 60-min surgery included heart rate, mean arterial blood pressure, pO2, and pCO2. According to Welch 2-sample t tests, cardiopulmonary variables did not differ between groups. For example, after administration of the loading dose, goats in the lidocaine group had a mean heart rate of 88 ± 28 bpm, mean arterial blood pressure of 70 ± 19 mm Hg, pCO2 of 65 ± 13 mm Hg, and pO2 of 212 ± 99 mm Hg; in the saline group, these values were 90 ± 16 bpm, 76 ± 12 mm Hg, 61 ± 9 mm Hg, and 209 ± 83 mm Hg, respectively. One goat in the saline group required an additional dose of butorphanol. Overall our findings indicate that, at the dose provided, intravenous lidocaine did not cause adverse cardiopulmonary effects in adult goats undergoing abdominal surgery. Adding lidocaine infusion during general anesthesia is an option for enhancing transoperative analgesia in goats. PMID:27423150

  4. Lidocaine reduces neutrophil recruitment by abolishing chemokine-induced arrest and transendothelial migration in septic patients.

    PubMed

    Berger, Christian; Rossaint, Jan; Van Aken, Hugo; Westphal, Martin; Hahnenkamp, Klaus; Zarbock, Alexander

    2014-01-01

    The inappropriate activation, positioning, and recruitment of leukocytes are implicated in the pathogenesis of multiple organ failure in sepsis. Although the local anesthetic lidocaine modulates inflammatory processes, the effects of lidocaine in sepsis are still unknown. This double-blinded, prospective, randomized clinical trial was conducted to investigate the effect of lidocaine on leukocyte recruitment in septic patients. Fourteen septic patients were randomized to receive either a placebo (n = 7) or a lidocaine (n = 7) bolus (1.5 mg/kg), followed by continuous infusion (100 mg/h for patients >70 kg or 70 mg/h for patients <70 kg) over a period of 48 h. Selectin-mediated slow rolling, chemokine-induced arrest, and transmigration were investigated by using flow chamber and transmigration assays. Lidocaine treatment abrogated chemokine-induced neutrophil arrest and significantly impaired neutrophil transmigration through endothelial cells by inhibition of the protein kinase C-θ while not affecting the selectin-mediated slow leukocyte rolling. The observed results were not attributable to changes in surface expression of adhesion molecules or selectin-mediated capturing capacity, indicating a direct effect of lidocaine on signal transduction in neutrophils. These data suggest that lidocaine selectively inhibits chemokine-induced arrest and transmigration of neutrophils by inhibition of protein kinase C-θ while not affecting selectin-mediated slow rolling. These findings may implicate a possible therapeutic role for lidocaine in decreasing the inappropriate activation, positioning, and recruitment of leukocytes during sepsis.

  5. TRPA1 activation by lidocaine in nerve terminals results in glutamate release increase

    SciTech Connect

    Piao, L.-H.; Fujita, Tsugumi; Jiang, C.-Y.; Liu Tao; Yue, H.-Y.; Nakatsuka, Terumasa; Kumamoto, Eiichi

    2009-02-20

    We examined the effects of local anesthetics lidocaine and procaine on glutamatergic spontaneous excitatory transmission in substantia gelatinosa (SG) neurons in adult rat spinal cord slices with whole-cell patch-clamp techniques. Bath-applied lidocaine (1-5 mM) dose-dependently and reversibly increased the frequency but not the amplitude of spontaneous excitatory postsynaptic current (sEPSC) in SG neurons. Lidocaine activity was unaffected by the Na{sup +}-channel blocker, tetrodotoxin, and the TRPV1 antagonist, capsazepine, but was inhibited by the TRP antagonist, ruthenium red. In the same neuron, the TRPA1 agonist, allyl isothiocyanate, and lidocaine both increased sEPSC frequency. In contrast, procaine did not produce presynaptic enhancement. These results indicate that lidocaine activates TRPA1 in nerve terminals presynaptic to SG neurons to increase the spontaneous release of L-glutamate.

  6. TRPA1 activation by lidocaine in nerve terminals results in glutamate release increase.

    PubMed

    Piao, Lian-Hua; Fujita, Tsugumi; Jiang, Chang-Yu; Liu, Tao; Yue, Hai-Yuan; Nakatsuka, Terumasa; Kumamoto, Eiichi

    2009-02-20

    We examined the effects of local anesthetics lidocaine and procaine on glutamatergic spontaneous excitatory transmission in substantia gelatinosa (SG) neurons in adult rat spinal cord slices with whole-cell patch-clamp techniques. Bath-applied lidocaine (1-5 mM) dose-dependently and reversibly increased the frequency but not the amplitude of spontaneous excitatory postsynaptic current (sEPSC) in SG neurons. Lidocaine activity was unaffected by the Na(+)-channel blocker, tetrodotoxin, and the TRPV1 antagonist, capsazepine, but was inhibited by the TRP antagonist, ruthenium red. In the same neuron, the TRPA1 agonist, allyl isothiocyanate, and lidocaine both increased sEPSC frequency. In contrast, procaine did not produce presynaptic enhancement. These results indicate that lidocaine activates TRPA1 in nerve terminals presynaptic to SG neurons to increase the spontaneous release of L-glutamate.

  7. Neuroprotective and anti-inflammatory effects of lidocaine in kainic acid-injected rats.

    PubMed

    Chiu, Kuan Ming; Lu, Cheng Wei; Lee, Ming Yi; Wang, Ming Jiuh; Lin, Tzu Yu; Wang, Su Jane

    2016-05-04

    Lidocaine, the most commonly used local anesthetic, inhibits glutamate release from nerve terminals. Given the involvement of glutamate neurotoxicity in the pathogenesis of various neurological disorders, this study investigated the role of lidocaine in hippocampal neuronal death and inflammatory events induced by an i.p. injection of kainic acid (KA) (15 mg/kg), a glutamate analog. The results showed that KA significantly led to neuronal death in the CA3 pyramidal layers of the hippocampus and this effect was attenuated by the systemic administration of lidocaine (0.8 or 4 mg/kg, i.p.) 30 min before KA injection. Moreover, KA-induced microglia activation and gene expression of proinflammatory cytokines, namely, interleukin-1β, interleukin-6, and tumor necrosis factor-α, in the hippocampus were reduced by the lidocaine pretreatment. Altogether, the results suggest that lidocaine can effectively treat glutamate excitotoxicity-related brain disorders.

  8. Prospective randomized study of viscous lidocaine versus benzocaine in a GI cocktail for dyspepsia.

    PubMed

    Vilke, Gary M; Jin, Albert; Davis, Daniel P; Chan, Theodore C

    2004-07-01

    We hypothesized that Benzocaine (Hurricaine) would work as quickly and effectively as viscous Lidocaine in this preparation. This was a prospective randomized, single-blinded comparison between Benzocaine and Lidocaine as the topical anesthetic in a gastrointestinal (GI) cocktail. Patients 18 years or older were approached for participation when a GI cocktail was ordered by the Emergency Physician. Patients were randomized to equivalent doses of either Benzocaine or viscous Lidocaine in addition to 30 cc of Maalox and 10 cc of Donnatal. Assessment using a visual analog pain scale occurred at time intervals of 0, 5, 15, and 30 min. Eighty-two patients were enrolled (44 to Benzocaine, 38 to viscous Lidocaine), with each group having a statistically significant improvement in pain (p < 0.001). There were no statistical differences between the Benzocaine and viscous Lidocaine groups in terms of the relief of symptoms at each of the assessment times. There were no adverse outcomes in either group.

  9. Nebulized lidocaine blunts airway hyper-responsiveness in experimental feline asthma.

    PubMed

    Nafe, Laura A; Guntur, Vamsi P; Dodam, John R; Lee-Fowler, Tekla M; Cohn, Leah A; Reinero, Carol R

    2013-08-01

    Nebulized lidocaine may be a corticosteroid-sparing drug in human asthmatics, reducing airway resistance and peripheral blood eosinophilia. We hypothesized that inhaled lidocaine would be safe in healthy and experimentally asthmatic cats, diminishing airflow limitation and eosinophilic airway inflammation in the latter population. Healthy (n = 5) and experimentally asthmatic (n = 9) research cats were administered 2 weeks of nebulized lidocaine (2 mg/kg q8h) or placebo (saline) followed by a 2-week washout and crossover to the alternate treatment. Cats were anesthetized to measure the response to inhaled methacholine (MCh) after each treatment. Placebo and doubling doses of methacholine (0.0625-32.0000 mg/ml) were delivered and results were expressed as the concentration of MCh increasing baseline airway resistance by 200% (EC200Raw). Bronchoalveolar lavage was performed after each treatment and eosinophil numbers quantified. Bronchoalveolar lavage fluid (BALF) % eosinophils and EC200Raw within groups after each treatment were compared using a paired t-test (P <0.05 significant). No adverse effects were noted. In healthy cats, lidocaine did not significantly alter BALF eosinophilia or the EC200Raw. There was no difference in %BALF eosinophils in asthmatic cats treated with lidocaine (36±10%) or placebo (33 ± 6%). However, lidocaine increased the EC200Raw compared with placebo 10 ± 2 versus 5 ± 1 mg/ml; P = 0.043). Chronic nebulized lidocaine was well-tolerated in all cats, and lidocaine did not induce airway inflammation or airway hyper-responsiveness in healthy cats. Lidocaine decreased airway response to MCh in asthmatic cats without reducing airway eosinophilia, making it unsuitable for monotherapy. However, lidocaine may serve as a novel adjunctive therapy in feline asthmatics with beneficial effects on airflow obstruction.

  10. Quantitative and fiber-selective evaluation of dose-dependent nerve blockade by intrathecal lidocaine in rats.

    PubMed

    Oda, Mayuko; Kitagawa, Norihito; Yang, Bang-Xiang; Totoki, Tadahide; Morimoto, Masatoshi

    2005-03-01

    We investigated whether cutaneous stimulus threshold (CST), as determined using a Neurometer, could be used for quantitative and differential nerve evaluation of reversible and irreversible nerve block following intrathecal lidocaine administration in rats. Rats with intrathecal catheters were randomly assigned to one of five groups (saline or 2, 5, 10, or 20% lidocaine). Prior to and 4 days after drug administration, CST was determined at 5, 250, and 2000 Hz. In the 2% lidocaine group, CST from end of lidocaine infusion to recovery from anesthesia was also monitored. Skin-clamp testing and gait observation were performed for comparison with CST findings. Behavioral examinations revealed persistent sensory or motor impairment lasting 4 days in groups receiving >/=5% lidocaine but not in the saline and 2% lidocaine groups. With 2% lidocaine, return to baseline CSTs at 5 and 250 Hz was delayed compared with thresholds at 2000 Hz. Although CSTs in the 5% group at 5 and 250 Hz increased significantly, thresholds at 2000 Hz did not differ from those in rats administered saline. CSTs with >/=10% lidocaine displayed no differences between frequencies. At each frequency, CSTs for rats with >/=5% lidocaine increased in a clearly concentration-dependent manner. These results suggest that CST testing enables evaluation of the different nerve functions for Abeta, Adelta, and C fibers in rats for lidocaine concentrations lidocaine in rats.

  11. Intraarticular lidocaine versus intravenous analgesic for reduction of acute anterior shoulder dislocations. A prospective randomized study.

    PubMed

    Matthews, D E; Roberts, T

    1995-01-01

    We performed a prospective, randomized study to evaluate the use of injected lidocaine as an anesthetic for closed reduction of acute anterior shoulder dislocations. Thirty consecutive patients who presented at the emergency department with acute anterior shoulder dislocations were randomly placed in one of two groups. One group received an intraarticular injection of 20 ml of 1% lidocaine and the other group, intravenous injections of morphine sulfate and midazolam. The groups were compared regarding time of reduction maneuver, difficulty of reduction, subjective pain, complications, and total time spent in the emergency department. The lidocaine provided adequate anesthesia and secondary relief of muscle spasm in 15 of 15 (100%) patients. When compared with the intravenous sedation group, the lidocaine group showed no statistically significant difference in time for reduction maneuver, difficulty of reduction, or subjective pain. The lidocaine group had no complications and had a statistically significant shorter emergency department visit when compared with the intravenous sedation group (mean, 78 minutes versus 186 minutes; P = 0.004). Lidocaine provides excellent anesthesia for patients with uncomplicated anterior shoulder dislocations and can be very beneficial when sedation is contraindicated. Lidocaine injections also proved to be cost effective in our institution, reducing total costs by as much as 62%.

  12. Radioprotective Effect of Lidocaine on Function and Ultrastructure of Salivary Glands Receiving Fractionated Radiation

    SciTech Connect

    Hakim, Samer George; Benedek, Geza Attila; Su Yuxiong; Jacobsen, Hans Christian; Klinger, Matthias; Dendorfer, Andreas; Hemmelmann, Claudia; Meller, Birgit; Nadrowitz, Roger; Rades, Dirk; Sieg, Peter

    2012-03-15

    Purpose: Radiation-induced xerostomia still represents a common side effect after radiotherapy for head-and-neck malignancies. The aim of the present study was to examine the radioprotective effect of lidocaine hydrochloride during fractionated radiation in an experimental animal model. Methods and Materials: To evaluate the influence of different radiation doses on salivary gland function and the radioprotective effect of lidocaine, rabbits were irradiated with 15, 25, 30, and 35 Gy (equivalent doses in 2-Gy fractions equivalent to 24, 40, 48, and 56 Gy, respectively). Lidocaine hydrochloride (10 and 12 mg/kg) was administered before every radiation fraction in the treatment groups. Salivary gland function was assessed by flow sialometry and sialoscintigraphy, and the morphologic changes were evaluated using transmission electron microscopy. Results: Functional impairment was first observed after 35 Gy and pretreatment with lidocaine improved radiation tolerance of both parotid and submandibular glands. The use of 12 mg/kg lidocaine was superior and displayed significant radioprotection with regard to flow sialometry and sialoscintigraphy. The ultrastructure was largely preserved after pretreatment with both lidocaine doses. Conclusions: Lidocaine represents an effective radioprotective agent and a promising approach for clinical application to avoid radiation-induced functional impairment of salivary glands.

  13. Intravenous lipid emulsion given to volunteers does not affect symptoms of lidocaine brain toxicity.

    PubMed

    Heinonen, Juho A; Litonius, Erik; Salmi, Tapani; Haasio, Juhani; Tarkkila, Pekka; Backman, Janne T; Rosenberg, Per H

    2015-04-01

    Intravenous lipid emulsion has been suggested as treatment for local anaesthetic toxicity, but the exact mechanism of action is still uncertain. Controlled studies on the effect of lipid emulsion on toxic doses of local anaesthetics have not been performed in man. In randomized, subject-blinded and two-phase cross-over fashion, eight healthy volunteers were given a 1.5 ml/kg bolus of 20% Intralipid(®) (200 mg/ml) or Ringer's acetate solution intravenously, followed by a rapid injection of lidocaine 1.0 mg/kg. Then, the same solution as in the bolus was infused at a rate of 0.25 ml/kg/min. for 30 min. Electroencephalography (EEG) was recorded, and 5 min. after lidocaine injection, the volunteers were asked to report subjective symptoms. Total and un-entrapped lidocaine plasma concentrations were measured from venous blood samples. EEG band power changes (delta, alpha and beta) after the lidocaine bolus were similar during lipid and during Ringer infusion. There were no differences between infusions in the subjective symptoms of central nervous system toxicity. Lidocaine was only minimally entrapped in the plasma by lipid emulsion, but the mean un-entrapped lidocaine area under concentration-time curve from 0 to 30 min. was clearly smaller during lipid than Ringer infusion (16.4 versus 21.3 mg × min/l, p = 0.044). Intravenous lipid emulsion did not influence subjective toxicity symptoms nor affect the EEG changes caused by lidocaine.

  14. The topical 5% lidocaine medicated plaster in localized neuropathic pain: a reappraisal of the clinical evidence

    PubMed Central

    de León-Casasola, Oscar A; Mayoral, Victor

    2016-01-01

    Topical 5% lidocaine medicated plasters represent a well-established first-line option for the treatment of peripheral localized neuropathic pain (LNP). This review provides an updated overview of the clinical evidence (randomized, controlled, and open-label clinical studies, real-life daily clinical practice, and case series). The 5% lidocaine medicated plaster effectively provides pain relief in postherpetic neuralgia, and data from a large open-label controlled study indicate that the 5% lidocaine medicated plaster is as effective as systemic pregabalin in postherpetic neuralgia and painful diabetic polyneuropathy but with an improved tolerability profile. Additionally, improved analgesia and fewer side effects were experienced by patients treated synchronously with the 5% lidocaine medicated plaster, further demonstrating the value of multimodal analgesia in LNP. The 5% lidocaine medicated plaster provides continued benefit after long-term (≤7 years) use and is also effective in various other LNP conditions. Minor application-site reactions are the most common adverse events associated with the 5% lidocaine medicated plaster; there is minimal risk of systemic adverse events and drug–drug interactions. Although further well-controlled studies are warranted, the 5% lidocaine medicated plaster is efficacious and safe in LNP and may have particular clinical benefit in elderly and/or medically compromised patients because of the low incidence of adverse events. PMID:26929664

  15. Effect of pH modification by bicarbonate on pain after subcutaneous lidocaine injection

    PubMed Central

    Parham, Shelley M.; Pasieka, Janice L.

    1996-01-01

    Objective To quantify the pain experienced on subcutaneous injection of lidocaine, lidocaine with sodium bicarbonate (NaHCO3) and saline. Design A double-blind randomized prospective study. Setting A clinical research unit in a university-affiliated hospital. Participants Forty-two healthy adult volunteers who did not have a history of adverse reaction to lidocaine or peripheral neuropathy and were not pregnant. The study was performed in two phases. In Phase 1, 1 mL each of thee solutions (2 mL of 8.4% NaHCO3 in 20 mL 1% lidocaine, 2 mL saline in 20 mL lidocaine and saline alone) were injected by an investigator, blinded as to the identity of the solutions, in random order to five volunteers to measure onset and duration of anesthesia and the perceived pain on injection. In Phase 2, 37 volunteers were injected with the three solutions in random order, by an investigator blinded as to the identity of the solutions. Main Outcome Measure Pain on injection measured with the visual analogue scale. Results There were no clinically significant differences between onset and duration of action of lidocaine with and without NaHCO3, as determined by Kruskal–Wallis one-way analysis of variance and the Wilcoxon signed-ranks test. Injection of lidocaine with NaHCO3 was significantly less painful than injection of plain lidocaine (p = 0.041). Injection of saline was the most painful. Conclusion The addition of NaHCO3 to lidocaine produces significant reduction in pain experienced on injection without significantly affecting the onset or duration of action. PMID:8599788

  16. Lidocaine carboxymethylcellulose with gelatine co-polymer hydrogel delivery by combined microneedle and ultrasound.

    PubMed

    Nayak, Atul; Babla, Hiten; Han, Tao; Das, Diganta Bhusan

    2016-01-01

    A study that combines microneedles (MNs) and sonophoresis pre-treatment was explored to determine their combined effects on percutaneous delivery of lidocaine from a polymeric hydrogel formulation. Varying ratios of carboxymethylcellulose and gelatine (NaCMC/gel ranges 1:1.60-1:2.66) loaded with lidocaine were prepared and characterized for zeta potential and particle size. Additionally, variations in the formulation drying techniques were explored during the formulation stage. Ex vivo permeation studies using Franz diffusion cells measured lidocaine permeation through porcine skin after pre-treatment with stainless steel MNs and 20 kHz sonophoresis for 5-and 10-min durations. A stable formulation was related to a lower gelatine mass ratio because of smaller mean particle sizes and high zeta potential. Lidocaine permeability in skin revealed some increases in permeability from combined MN and ultrasound pre-treatment studies. Furthermore, up to 4.8-fold increase in the combined application was observed compared with separate pre-treatments after 30 min. Sonophoresis pre-treatment alone showed insignificant enhancement in lidocaine permeation during the initial 2 h period. MN application increased permeability at a time of 0.5 h for up to ∼17 fold with an average up to 4 fold. The time required to reach therapeutic levels of lidocaine was decreased to less than 7 min. Overall, the attempted approach promises to be a viable alternative to conventional lidocaine delivery methods involving painful injections by hypodermic needles. The mass transfer effects were fairly enhanced and the lowest amount of lidocaine in skin was 99.7% of the delivered amount at a time of 3 h for lidocaine NaCMC/GEL 1:2.66 after low-frequency sonophoresis and MN treatment.

  17. Effect of skin surface lipid on the skin permeation of lidocaine from pressure sensitive adhesives.

    PubMed

    Cheng, Y H; Hosoya, O; Sugibayashi, K; Morimoto, Y

    1994-12-01

    Pressure sensitive adhesives (PSA) tapes containing different concentrations of lidocaine were prepared by a general casting method using styrene-isoprene-styrene block copolymer, and the in vitro skin permeation of lidocaine from each tape was evaluated using diffusion cell and excised hairless rat skin. The skin permeation was proportionally increased by up to 40% lidocaine in the PSA tape and did not change after this concentration. Although the bending point of the steady-state flux via skin concentration curve was found at 40%, saturated concentration or solubility of lidocaine in the tape was estimated to be about 20% by differential scanning calorimetry (DSC) measurement. In addition, the steady-state flux of lidocaine through skin from water or silicone fluid suspension (92 or 120 micrograms/cm2.h, respectively) was very similar to those of 40, 50 and 60% tapes (105, 101 and 112 micrograms/cm2.h, respectively). Decrease in the concentration in tapes during the permeation experiment explained only part of these phenomena. To analyze them further, the drug free PSA tape with or without (control) skin surface lipid was affixed to 50% lidocaine PSA tape for 48 h, and the amount of lidocaine crystal in the layered tapes was measured by DSC. The amount was found to be lower in the lipid-containing tape than in the lipid-free tape, suggesting that skin surface lipid can dissolve lidocaine crystal or solid in PSA tape to decrease its thermodynamic activity. Thus it is important to follow the concentration and thermodynamic activity of lidocaine in PSA tape, skin and the interface between the two layers to exactly assess its skin permeation flux.

  18. How acidic is the lidocaine we are injecting, and how much bicarbonate should we add?

    PubMed Central

    Frank, Simon G; Lalonde, Donald H

    2012-01-01

    BACKGROUND: The infiltration of local anesthetics can be painful, which is likely due, in part, to their acidity. In spite of a Cochrane study that recommended neutralizing lidocaine with bicarbonate to decrease the pain of injection, not many surgeons have adopted the practice, and there are many ‘recipes’ for how much bicarbonate one should add. OBJECTIVE: To determine the acidity of lidocaine and the correct ratio of bicarbonate that should be added to neutralize lidocaine to achieve body pH. METHODS: Fifty samples each of commonly used anesthetics (lidocaine 1% and 2%, with and without epinephrine 1:100,000) were obtained and tested for pH. Data were also analyzed according to whether the vials had been previously opened. Ten additional samples of lidocaine 1% with 1:100,000 epinephrine were titrated against sodium bicarbonate 8.4% and tested for pH and the presence of precipitate. RESULTS: A solution of 1% lidocaine with 1:100,000 epinephrine had a mean (± SD) pH of 4.24±0.42, and 2% lidocaine with 1:100,000 epinephrine had a mean pH of 3.93±0.43. Plain 1% lidocaine had a pH of 6.09±0.16, and plain 2% lidocaine had a pH of 6.00±0.27. Epinephrine-containing solutions were more acidic when they had been previously opened. One per cent lidocaine with epinephrine required 8.4% sodium bicarbonate at a ratio of 1.1 mL:10 mL to 1.8 mL:10 mL to achieve the target tissue pH of 7.38 to 7.62. CONCLUSION: Lidocaine with epinephrine was approximately 1000 times more acidic than subcutaneous tissue. The addition of bicarbonate to the local anesthetic solution is simple to perform and is inexpensive. The proper volume ratio of 8.4% sodium bicarbonate to 1% lidocaine with 1:100,000 epinephrine is approximately 1 mL:10 mL. Surgeons should be more aware of the simplicity and value of buffering with bicarbonate to decrease the pain of injection. PMID:23730153

  19. Efficacy of Intravenous Lidocaine During Endoscopic Submucosal Dissection for Gastric Neoplasm

    PubMed Central

    Kim, Ji Eun; Choi, Jong Bum; Koo, Bon-Nyeo; Jeong, Hae Won; Lee, Byung Ho; Kim, So Yeon

    2016-01-01

    Abstract Endoscopic submucosal dissection (ESD) is an advanced therapy for early gastric neoplasm and requires sedation with adequate analgesia. Lidocaine is a short-acting local anesthetic, and intravenous lidocaine has been shown to have analgesic efficacy in surgical settings. The aim of this study was to assess the effects of intravenous lidocaine on analgesic and sedative requirements for ESD and pain after ESD. Sixty-six patients scheduled for ESD randomly received either intravenous lidocaine as a bolus of 1.5 mg/kg before sedation, followed by continuous infusion at a rate of 2 mg/kg/h during sedation (lidocaine group; n = 33) or the same bolus and infusion volumes of normal saline (control group; n = 33). Sedation was achieved with propofol and fentanyl. The primary outcome was fentanyl requirement during ESD. We recorded hemodynamics and any events during ESD and evaluated post-ESD epigastric and throat pain. Fentanyl requirement during ESD reduced by 24% in the lidocaine group compared with the control group (105 ± 28 vs. 138 ± 37 μg, mean ± SD; P < 0.001). The lidocaine group reached sedation faster [40 (20–100) vs. 55 (30–120) s, median (range); P = 0.001], and incidence of patient movement during ESD decreased in the lidocaine group (3% vs. 26%, P = 0.026). Numerical rating scale for epigastric pain was significantly lower at 6 hours after ESD [2 (0–6) vs. 3 (0–8), median (range); P = 0.023] and incidence of throat pain was significantly lower in the lidocaine group (27% vs. 65%, P = 0.003). No adverse events associated with lidocaine were discovered. Administration of intravenous lidocaine reduced fentanyl requirement and decreased patient movement during ESD. Moreover, it alleviated epigastric and throat pain after ESD. Thus, we conclude that the use of intravenous adjuvant lidocaine is a new and safe sedative method during ESD. PMID:27149489

  20. Lidocaine transport through a cellophane membrane by alternating current iontophoresis with a duty cycle.

    PubMed

    Hayashi, Shizuka; Ogami, Saori; Shibaji, Takao; Umino, Masahiro

    2009-02-01

    The purpose of this study was to determine whether lidocaine can be efficiently transported across a cellophane membrane using a square-wave alternating current (AC) with an adjusted duty cycle. Three voltages at 1 kHz with 6 duty cycles were applied for 60 min to the diffusion cells on both sides of the cellophane membrane. The donor chamber was filled with 1% lidocaine hydrochloride solution. The transport of lidocaine was enhanced in a voltage-, and duty cycle-dependent manner. These findings indicate that voltage and the direct current (DC) component of the square-wave AC play important roles in generating the driving force necessary for lidocaine delivery. Additionally, the periodic polarity alteration could reduce the electrode polarization. The higher voltages and duty cycles induced a pH change. The practical electrical conditions which are preferable for clinical application were 10 V with a 70% duty cycle or 20 V with a 60% duty cycle.

  1. Severe methemoglobinemia caused by continuous lidocaine infusion in a term neonate.

    PubMed

    Bohnhorst, Bettina; Hartmann, Hans; Lange, Matthias

    2016-12-28

    Neonates and young infants are especially prone to develop drug-induced methemoglobinemia. Therefore, lidocaine is not licensed as local anesthetic in children below the age of 3 months. However, its systemic use is advocated for neonatal seizures. Cardiac arrhythmia has been reported as sole major side effect. Here we report a case of severe methemoglobinemia caused by continuous infusion of lidocaine in a term neonate with neonatal seizures. The increase of methemoglobin up to 13.8% was accompanied by hypoxemia and cyanosis, necessitating additional inspired oxygen and CPAP ventilation. After stopping lidocaine infusion methemoglobin levels fell and the neonate could be weaned from ventilation. Neonates treated with lidocaine for seizures must be monitored for the occurrence of methemoglobinemia.

  2. Submucous infiltration of betamethasone and lidocaine in the treatment of vulvar vestibulitis.

    PubMed

    Segal, David; Tifheret, Hemda; Lazer, Simcha

    2003-03-26

    We present a case of persistent vulvar vestibulitis treated for several years unsuccessfully that has come to an end using a six week course of submucous infiltration of betamethasone and lidocaine in the vestibular area.

  3. [Patient's experience of topical anesthesia by lidocaine vaginal gel for oocyte retrieval].

    PubMed

    Guillaume, A; Schuller-Dufour, E; Faitot, V; Pirrello, O; Rongières, C; Ohl, J; Nisand, I; Bettahar, K

    2016-10-01

    A recent adverse effect of a paracervical block (cardiac arrest) occurred during an oocyte retrieval (OR), forcing us to reconsider our pain management during OR. Since then, we decided to use intravaginal lidocaine gel as analgesia during OR.

  4. Pharmacokinetics of lidocaine with epinephrine following local anesthesia reversal with phentolamine mesylate.

    PubMed

    Moore, Paul A; Hersh, Elliot V; Papas, Athena S; Goodson, J Max; Yagiela, John A; Rutherford, Bruce; Rogy, Seigried; Navalta, Laura

    2008-01-01

    Phentolamine mesylate accelerates recovery from oral soft tissue anesthesia in patients who have received local anesthetic injections containing a vasoconstrictor. The proposed mechanism is that phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. Assessments of the pharmacokinetics of lidocaine and phentolamine, and the impact of phentolamine on the pharmacokinetics of lidocaine with epinephrine were performed to characterize this potentially valuable strategy. The blood levels of phentolamine were determined following its administration intraorally and intravenously. Additionally, the effects of phentolamine mesylate on the pharmacokinetics of intraoral injections of lidocaine with epinephrine were evaluated. Sixteen subjects were enrolled in this phase 1 trial, each receiving 4 drug treatments: 1 cartridge lidocaine/epinephrine followed after 30 minutes by 1 cartridge phentolamine (1L1P), 1 cartridge phentolamine administered intravenously (1Piv), 4 cartridges lidocaine/epinephrine followed after 30 minutes by 2 cartridges phentolamine (4L2P), and 4 cartridges lidocaine/epinephrine followed by no phentolamine (4L). Pharmacokinetic parameters estimated for phentolamine, lidocaine, and epinephrine included peak plasma concentration (Cmax), time to peak plasma concentration (Tmax), area under the plasma concentration-time curve from 0 to the last time point (AUClast) or from time 0 to infinity (AUCinf), elimination half-life (t1/2), clearance (CL), and volume of distribution (Vd). The phentolamine Tmax occurred earlier following the intravenous administration of 1Piv (7 minutes than following its submucosal administration in treatment 1L1P (15 minutes) or 4L2P (11 minutes). The phentolamine t1/2, CL, and Vd values were similar for 1L1P, 1Piv, and 4L2P. The Tmax for lidocaine occurred

  5. Pharmacokinetics of Lidocaine With Epinephrine Following Local Anesthesia Reversal With Phentolamine Mesylate

    PubMed Central

    Moore, Paul A; Hersh, Elliot V; Papas, Athena S; Goodson, J. Max; Yagiela, John A; Rutherford, Bruce; Rogy, Seigried; Navalta, Laura

    2008-01-01

    Phentolamine mesylate accelerates recovery from oral soft tissue anesthesia in patients who have received local anesthetic injections containing a vasoconstrictor. The proposed mechanism is that phentolamine, an alpha-adrenergic antagonist, blocks the vasoconstriction associated with the epinephrine used in dental anesthetic formulations, thus enhancing the systemic absorption of the local anesthetic from the injection site. Assessments of the pharmacokinetics of lidocaine and phentolamine, and the impact of phentolamine on the pharmacokinetics of lidocaine with epinephrine were performed to characterize this potentially valuable strategy. The blood levels of phentolamine were determined following its administration intraorally and intravenously. Additionally, the effects of phentolamine mesylate on the pharmacokinetics of intraoral injections of lidocaine with epinephrine were evaluated. Sixteen subjects were enrolled in this phase 1 trial, each receiving 4 drug treatments: 1 cartridge lidocaine/epinephrine followed after 30 minutes by 1 cartridge phentolamine (1L1P), 1 cartridge phentolamine administered intravenously (1Piv), 4 cartridges lidocaine/epinephrine followed after 30 minutes by 2 cartridges phentolamine (4L2P), and 4 cartridges lidocaine/epinephrine followed by no phentolamine (4L). Pharmacokinetic parameters estimated for phentolamine, lidocaine, and epinephrine included peak plasma concentration (Cmax), time to peak plasma concentration (Tmax), area under the plasma concentration-time curve from 0 to the last time point (AUClast) or from time 0 to infinity (AUCinf), elimination half-life (t1/2), clearance (CL), and volume of distribution (Vd). The phentolamine Tmax occurred earlier following the intravenous administration of 1Piv (7 minutes than following its submucosal administration in treatment 1L1P (15 minutes) or 4L2P (11 minutes). The phentolamine t1/2, CL, and Vd values were similar for 1L1P, 1Piv, and 4L2P. The Tmax for lidocaine occurred

  6. Injectable microparticle-gel system for prolonged and localized lidocaine release. I. In vitro characterization.

    PubMed

    Chen, Pen-Chung; Park, Yoon Jeong; Chang, Li-Chien; Kohane, Daniel S; Bartlett, Robert H; Langer, Robert; Yang, Victor C

    2004-09-01

    Current treatment protocol for postoperative pain is to infuse anesthetic solution around nerves or into the epidural space. This clinical practice is beset by the short duration of the anesthetic effect unless the infusion is continuous. Continuous infusion, however, requires hospitalization of the patients, thereby increasing medical costs. In addition, it also causes systemic accumulation of the drug. We reported herein a novel treatment for the postoperative pain by applying to the surgical site a biodegradable microsphere-gel system for prolonged and localized release of encapsulated anesthetic drugs. This lidocaine-containing biodegradable poly(D,L-lactic acid) (PLA) microsphere system, although being established previously by other investigators, was hindered by a burst release and a followed rapid release of the drug within several hours in vitro. In this article, we demonstrated that by a step-by-step modification of the formulation, prolonged release of lidocaine, up to several days in vitro, could be achieved. Differential scanning calorimetry revealed a lower glass transition temperature for these lidocaine-loaded microspheres comparing to that of lidocaine-free microspheres. This decreased Tg explained for the tendency of the lidocaine-loaded microspheres to physically fuse at higher temperatures. In vitro studies showed that microspheres, when loaded with 35% lidocaine, yielded a threefold increase in the degradation rate. The molecular weight of PLA of the drug-loaded microspheres was reduced by 50% within a period of 1 month. Based on the results (of prolonged lidocaine release and rapid PLA microsphere degradation), this lidocaine-loaded PLA microsphere system could offer a simple solution to the treatment of postoperative pain.

  7. Lidocaine for systemic sclerosis: a double-blind randomized clinical trial

    PubMed Central

    2011-01-01

    Background Systemic sclerosis (scleroderma; SSc) is an orphan disease with the highest case-specific mortality of any connective-tissue disease. Excessive collagen deposit in affected tissues is a key for the disease's pathogenesis and comprises most of the clinical manifestations. Lidocaine seems to be an alternative treatment for scleroderma considering that: a) the patient's having excessive collagen deposits in tissues affected by scleroderma; b) the patient's demonstrating increased activity of the enzyme prolyl hydroxylase, an essential enzyme for the biosynthesis of collagen; and c) lidocaine's reducing the activity of prolyl hydroxylase. The aim of this study was to evaluate the efficacy and safety of lidocaine in treating scleroderma. Methods A randomized double-blind clinical trial included 24 patients with scleroderma randomized to receive lidocaine or placebo intravenously in three cycles of ten days each, with a one-month interval between them. Outcomes: cutaneous (modified Rodnan skin score), oesophageal (manometry) and microvascular improvement (nailfold capillaroscopy); improvement in subjective self-assessment and in quality of life (HAQ). Results There was no statistically significant difference between the groups for any outcome after the treatment and after 6-months follow-up. Improvement in modified Rodnan skin score occurred in 66.7% and 50% of placebo and lidocaine group, respectively (p = 0.408). Both groups showed an improvement in subjective self-assessment, with no difference between them. Conclusions Despite the findings of a previous cohort study favouring the use of lidocaine, this study demonstrated that lidocaine at this dosage and means of administration showed a lack of efficacy for treating scleroderma despite the absence of significant adverse effects. However, further similar clinical trials are needed to evaluate the efficacy of lidocaine when administered in different dosages and by other means. PMID:21299861

  8. Buffered lidocaine and bupivacaine mixture - the ideal local anesthetic solution?

    PubMed

    Best, Corliss A; Best, Alyssa A; Best, Timothy J; Hamilton, Danielle A

    2015-01-01

    The use of injectable local anesthetic solutions to facilitate pain-free surgery is an integral component of many procedures performed by the plastic surgeon. In many instances, a solution that has both rapid onset and prolonged duration of analgesia is optimal. A combination of lidocaine and bupivacaine, plain or with epinephrine, is readily available in most Canadian health care settings where such procedures are performed, and fulfills these criteria. However, commercially available solutions of both medications are acidic and cause a burning sensation on injection. Buffering to neutral pH with sodium bicarbonate is a practical method to mitigate the burning sensation, and has the added benefit of increasing the fraction of nonionized lipid soluble drug available. The authors report on the proportions of the three drugs to yield a neutral pH, and the results of an initial survey regarding the use of the combined solution with epinephrine in hand surgery.

  9. Understanding the large solubility of lidocaine in 1-n-butyl-3-methylimidazolium based ionic liquids using molecular simulation.

    PubMed

    Ley, Ryan T; Paluch, Andrew S

    2016-02-28

    Room temperature ionic liquids have been proposed as replacement solvents in a wide range of industrial separation processes. Here, we focus on the use of ionic liquids as solvents for the pharmaceutical compound lidocaine. We show that the solubility of lidocaine in seven common 1-n-butyl-3-methylimidazolium based ionic liquids is greatly enhanced relative to water. The predicted solubility is greatest in [BMIM](+)[CH3CO2](-), which we find results from favorable hydrogen bonding between the lidocaine amine hydrogen and the [CH3CO2](-) oxygen, favorable electrostatic interactions between the lidocaine amide oxygen with the [BMIM](+) aromatic ring hydrogens, while lidocaine does not interfere with the association of [BMIM](+) with [CH3CO2](-). Additionally, by removing functional groups from the lidocaine scaffold while maintaining the important amide group, we found that as the van der Waals volume increases, solubility in [BMIM](+)[CH3CO2](-) relative to water increases.

  10. Understanding the large solubility of lidocaine in 1-n-butyl-3-methylimidazolium based ionic liquids using molecular simulation

    NASA Astrophysics Data System (ADS)

    Ley, Ryan T.; Paluch, Andrew S.

    2016-02-01

    Room temperature ionic liquids have been proposed as replacement solvents in a wide range of industrial separation processes. Here, we focus on the use of ionic liquids as solvents for the pharmaceutical compound lidocaine. We show that the solubility of lidocaine in seven common 1-n-butyl-3-methylimidazolium based ionic liquids is greatly enhanced relative to water. The predicted solubility is greatest in [BMIM]+[CH3CO2]-, which we find results from favorable hydrogen bonding between the lidocaine amine hydrogen and the [CH3CO2]- oxygen, favorable electrostatic interactions between the lidocaine amide oxygen with the [BMIM]+ aromatic ring hydrogens, while lidocaine does not interfere with the association of [BMIM]+ with [CH3CO2]-. Additionally, by removing functional groups from the lidocaine scaffold while maintaining the important amide group, we found that as the van der Waals volume increases, solubility in [BMIM]+[CH3CO2]- relative to water increases.

  11. The Impact of Intravenous Lidocaine on ICP in Neurological Illness: A Systematic Review

    PubMed Central

    Zeiler, F. A.; Sader, N.; Kazina, C. J.

    2015-01-01

    Background. The goal of our study was to perform a systematic review of the literature to determine the effect that intravenous (IV) lidocaine had on ICP in patients with neurological illness. Methods. All articles are from MEDLINE, BIOSIS, EMBASE, Global Health, Scopus, Cochrane Library, the International Clinical Trials Registry Platform (inception to March 2015). The strength of evidence was adjudicated using both the Oxford and GRADE methodology. Results. Ten original articles were considered for the final review. There were 189 patients studied. Seven studies focused on prophylactic pretreatment with IV lidocaine to determine if there would be an attenuation of ICP spikes during stimulation, with 4 displaying an attenuation of ICP. Three studies focused on a therapeutic administration of IV lidocaine in order to determine ICP reduction effects. All therapeutic studies displayed a reduction in ICP. Conclusions. We cannot make a strong definitive recommendation on the effectiveness of IV lidocaine on the attenuation of ICP spikes during stimulation. There currently exists both Oxford 2b and GRADE B literature to support and refute the attenuation of ICP spikes with IV lidocaine during stimulation. There currently exists Oxford 2b, GRADE B evidence to support ICP reduction with lidocaine when used as a therapeutic agent. PMID:26448873

  12. Effects of ketamine and lidocaine in combination on the sevoflurane minimum alveolar concentration in alpacas.

    PubMed

    Queiroz-Williams, Patricia; Doherty, Thomas J; da Cunha, Anderson F; Leonardi, Claudia

    2016-04-01

    This study investigated the effects of ketamine and lidocaine in combination on the minimum alveolar concentration of sevoflurane (MACSEVO) in alpacas. Eight healthy, intact male, adult alpacas were studied on 2 separate occasions. Anesthesia was induced with SEVO, and baseline MAC (MACB) determination began 45 min after induction. After MACB determination, alpacas were randomly given either an intravenous (IV) loading dose (LD) and infusion of saline or a loading dose [ketamine = 0.5 mg/kg body weight (BW); lidocaine = 2 mg/kg BW] and an infusion of ketamine (25 μg/kg BW per minute) in combination with lidocaine (50 μg/kg BW per minute), and MACSEVO was re-determined (MACT). Quality of recovery, time-to-extubation, and time-to-standing, were also evaluated. Mean MACB was 1.88% ± 0.13% and 1.89% ± 0.14% for the saline and ketamine + lidocaine groups, respectively. Ketamine and lidocaine administration decreased (P < 0.05) MACB by 57% and mean MACT was 0.83% ± 0.10%. Saline administration did not change MACB. Time to determine MACB and MACT was not significantly different between the treatments. The quality of recovery, time-to-extubation, and time-to-standing, were not different between groups. The infusion of ketamine combined with lidocaine significantly decreased MACSEVO by 57% and did not adversely affect time-to-standing or quality of recovery.

  13. Evaluation of a constant rate infusion of lidocaine for balanced anesthesia in dogs undergoing surgery.

    PubMed

    Ortega, Maria; Cruz, Ignacio

    2011-08-01

    This study assessed the intraoperative analgesic effects of intravenous lidocaine administered by a constant rate infusion (CRI) in surgical canine patients. A prospective, blinded, randomized study was designed with 2 treatment groups: A (lidocaine) and B (placebo), involving 41 dogs. All patients were premedicated with acepromazine and buprenorphine, induced with propofol and midazolam; anesthesia was maintained with isoflurane in oxygen. Group A received 2 mg/kg IV lidocaine immediately after induction, followed within 5 min by a CRI at 50 μg/kg/min. Group B received an equivalent volume of saline instead of lidocaine. Changes in heart rate and blood pressure during maintenance were treated by increasing CRI. Fentanyl was used as a supplemental analgesic when intraoperative nociceptive response was not controlled with the maximum dose of lidocaine infusion. There was a significantly lower use of supplemental intraoperative analgesia in the lidocaine than in the placebo group. Group B dogs had almost twice as high a risk of intraoperative nociceptive response as group A dogs.

  14. The Impact of Intravenous Lidocaine on ICP in Neurological Illness: A Systematic Review.

    PubMed

    Zeiler, F A; Sader, N; Kazina, C J

    2015-01-01

    Background. The goal of our study was to perform a systematic review of the literature to determine the effect that intravenous (IV) lidocaine had on ICP in patients with neurological illness. Methods. All articles are from MEDLINE, BIOSIS, EMBASE, Global Health, Scopus, Cochrane Library, the International Clinical Trials Registry Platform (inception to March 2015). The strength of evidence was adjudicated using both the Oxford and GRADE methodology. Results. Ten original articles were considered for the final review. There were 189 patients studied. Seven studies focused on prophylactic pretreatment with IV lidocaine to determine if there would be an attenuation of ICP spikes during stimulation, with 4 displaying an attenuation of ICP. Three studies focused on a therapeutic administration of IV lidocaine in order to determine ICP reduction effects. All therapeutic studies displayed a reduction in ICP. Conclusions. We cannot make a strong definitive recommendation on the effectiveness of IV lidocaine on the attenuation of ICP spikes during stimulation. There currently exists both Oxford 2b and GRADE B literature to support and refute the attenuation of ICP spikes with IV lidocaine during stimulation. There currently exists Oxford 2b, GRADE B evidence to support ICP reduction with lidocaine when used as a therapeutic agent.

  15. Skin biopsy and quantitative sensory testing do not predict response to lidocaine patch in painful neuropathies.

    PubMed

    Herrmann, David N; Pannoni, Valerie; Barbano, Richard L; Pennella-Vaughan, Janet; Dworkin, Robert H

    2006-01-01

    Predictors of response to neuropathic pain treatment in patients with painful distal sensory neuropathies are lacking. The 5% lidocaine patch is believed to exert its effects on neuropathic pain via a local stabilizing effect on cutaneous sensory afferents. As such, it provides a model to assess whether the status of epidermal innervation as determined by skin biopsy or quantitative sensory testing (QST) of small- and large-diameter sensory afferents might serve as predictors of response to topical, locally active treatment. In this study we assessed associations between epidermal nerve fiber (ENF) densities, sensory nerve conduction studies (NCS), QST, and response to a 5% lidocaine patch in patients with painful distal sensory neuropathies. We observed no association between distal leg epidermal and subepidermal innervation and response to the lidocaine patch. Several patients with complete loss of distal leg ENF showed a response to the lidocaine patch. Similarly we observed no consistent association between treatment response and QST for vibration, cooling, warm, heat-pain, and cold-pain thresholds, or distal sensory NCS. Thus, distal-leg skin biopsy, QST, and sensory NCS cannot be used to identify patients with painful polyneuropathy likely to respond to a lidocaine patch in clinical practice. Further studies are required to clarify precisely the mechanism and site of action of the lidocaine patch in patients with peripheral neuropathic pain.

  16. Lidocaine Enhances Contractile Function of Ischemic Myocardial Regions in Mouse Model of Sustained Myocardial Ischemia

    PubMed Central

    Kania, Gabriela; Osto, Elena; Jakob, Philipp; Krasniqi, Nazmi; Beck-Schimmer, Beatrice; Blyszczuk, Przemyslaw; Eriksson, Urs

    2016-01-01

    Rationale Perioperative myocardial ischemia is common in high-risk patients. The use of interventional revascularisation or even thrombolysis is limited in this patient subset due to exceedingly high bleeding risks. Blockade of voltage-gated sodium channels (VGSC) with lidocaine had been suggested to reduce infarct size and cardiomyocyte cell death in ischemia/reperfusion models. However, the impact of lidocaine on cardiac function during sustained ischemia still remains unclear. Methods Sustained myocardial ischemia was induced by ligation of the left anterior descending artery in 12–16 weeks old male BALB/c mice. Subcutaneous lidocaine (30 mg/kg) was used to block VGSC. Cardiac function was quantified at baseline and at 72h by conventional and speckle-tracking based echocardiography to allow high-sensitivity in vivo phenotyping. Infarct size and cardiomyocyte cell death were assessed post mortem histologically and indirectly using troponin measurements. Results Ischemia strongly impaired both, global systolic and diastolic function, which were partially rescued in lidocaine treated in mice. No differences regarding infarct size and cardiomyocyte cell death were observed. Mechanistically, and as shown with speckle-tracking analysis, lidocaine specifically improves residual contractility in the ischemic but not in the remote, non-ischemic myocardium. Conclusion VGSC blockade with lidocaine rescues function of ischemic myocardium as a potential bridging to revascularisation in the setting of perioperative myocardial ischemia. PMID:27140425

  17. Lidocaine stability in cardioplegic solution stored in glass bottles and polyvinyl chloride bags.

    PubMed

    Lackner, T E; Baldus, D; Butler, C D; Amyx, C; Kessler, G

    1983-01-01

    The stability of lidocaine hydrochloride in buffered cardioplegic solutions stored in glass and polyvinyl chloride bags was studied. Concentrations of lidocaine (incorporated as the hydrochloride salt) were measured in buffered cardioplegic solutions containing potassium chloride, sodium bicarbonate, dextrose, and sodium chloride. Solutions were stored at 22 +/- 2 degrees C and 4 degrees C in glass bottles and 500-ml and 250-ml polyvinyl chloride (PVC) containers; some 250-ml PVC bags were underfilled to study the effects of varying surface area-volume ratios. Lidocaine concentrations were measured using a homogeneous enzyme immunoassay (EMIT, Syva Corporation) on days 0, 1, 2, 7, and 21. Lidocaine concentrations decreased significantly in all PVC bags stored at 22 degrees C and in underfilled PVC bags stored at 4 degrees C. Lidocaine loss in PVC bags appeared to result from sorption. It is concluded that lidocaine is stable in cardioplegic solutions when these are refrigerated and stored in glass containers or filled large-volume PVC bags for 21 days.

  18. Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride

    PubMed Central

    Banga, Ajay K.

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2 h was 1069.87 ± 120.03 μg/sq·cm compared to 744.81 ± 125.41 μg/sq·cm after modulated alternating current iontophoresis for 2 h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71 μg/sq·cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2 h at frequency of 1 kHz was found to be comparable to the continuous direct current iontophoresis for 1 h. PMID:24959580

  19. Stability indicating HPLC method for the estimation of oxycodone and lidocaine in rectal gel.

    PubMed

    Gebauer, M G; McClure, A F; Vlahakis, T L

    2001-07-31

    An HPLC method for the quantification of oxycodone and lidocaine in a gel matrix is described. The mobile phase consisted of methanol--water--acetic acid (35:15:1 v/v/v) and was delivered at 1.5 ml/min through a 4.6 x 250 mm Zorbax SB-C8 column. Oxycodone was detected at 285 nm and lidocaine at 264 nm. Linear calibration curves were obtained for oxycodone in the range of 0.05--1.5% (w/w) and for lidocaine in the range of 0.1--5.0% (w/w). Oxycodone and lidocaine were treated with hydrogen peroxide and the oxidation products were readily separated on the column. The method was applied to assess the stability of a gel containing oxycodone hydrochloride (0.3% w/w) and lidocaine (1.5% w/w). The gel was stored under refrigeration in ready-to-use syringes and under these conditions oxycodone and lidocaine were stable for at least 1 year. The gel is useful in the management of tenesmus in rectal cancer.

  20. Lidocaine permeation from a lidocaine NaCMC/gel microgel formulation in microneedle-pierced skin: vertical (depth averaged) and horizontal permeation profiles.

    PubMed

    Nayak, Atul; Short, Liam; Das, Diganta B

    2015-08-01

    Common local anaesthetics such as lidocaine are administered by the hypodermic parenteral route but it causes pain or anxiety to patients. Alternatively, an ointment formulation may be applied which involves a slow drug diffusion process. In addressing these two issues, this paper aims to understand the significance of the 'poke and patch' microneedle (MN) treatment on skin in conjunction to the lidocaine permeation, and in particular, the vertical (depth averaged) and horizontal (e.g. lateral) permeation profiles of the drug in the skin. The instantaneous pharmacokinetics of lidocaine in skin was determined by a skin denaturation technique coupled with Franz diffusion cell measurements of the drug pharmacokinetics. All pharmacokinetic profiles were performed periodically on porcine skin. Three MN insertion forces of 3.9, 7.9 and 15.7 N were applied on the MN to pierce the skin. For the smaller force (3.9 N), post MN-treated skin seems to provide an 'optimum' percutaneous delivery rate. A 10.2-fold increase in lidocaine permeation was observed for a MN insertion force of 3.9 N at 0.25 h and similarly, a 5.4-fold increase in permeation occurred at 0.5 h compared to passive diffusional delivery. It is shown that lidocaine permeates horizontally beyond the area of the MN-treated skin for the smaller MN insertion forces, namely, 3.9 and 7.9 N from 0.25 to 0.75 h, respectively. The lateral diffusion/permeation of lidocaine for larger MN-treated force (namely, 15.7 N in this work) seems to be insignificant at all recorded timings. The MN insertion force of 15.7 N resulted in lidocaine concentrations slightly greater than control (passive diffusion) but significantly less than 3.9 and 7.9 N impact force treatments on skin. We believe this likelihood is due to the skin compression effect that inhibits diffusion until the skin had time to relax at which point lidocaine levels increase.

  1. The analgesic efficacy of intravenous lidocaine infusion after laparoscopic fundoplication: a prospective, randomized, double-blind, placebo-controlled trial.

    PubMed

    Dale, Gregory J; Phillips, Stephanie; Falk, Gregory L

    2016-01-01

    This study aimed to determine if intravenous lidocaine infusion reduces postoperative pain intensity following laparoscopic fundoplication surgery and to also validate the safety of intravenous lidocaine at the dose tested. This was an equally randomized, double-blind, placebo-controlled, parallel-group, single center trial. Adult patients undergoing laparoscopic fundoplication were recruited. The intervention group received 1 mg/kg intravenous lidocaine bolus prior to induction of anesthesia, then an intravenous infusion at 2 mg/kg/h for 24 hours. The primary outcome was pain, measured using a numeric rating scale for 30 hours postoperatively. Secondary outcomes were nausea and vomiting, opioid requirements, adverse events, serum lidocaine concentration, and length of hospital stay. The study was terminated after an interim analysis of 24 patients showed evidence of futility. There was no difference in postoperative pain scores (lidocaine versus control, mean ± standard deviation) at rest (2.0 ± 2.7 vs 2.1 ± 2.4, P=0.286) or with movement (2.0 ± 2.6 vs 2.6 ± 2.7, P=0.487). Three adverse events occurred in the lidocaine group (25% of patients). Intravenous lidocaine did not provide clinically significant analgesia to patients undergoing laparoscopic fundoplication. The serum lidocaine concentration of patients who experienced adverse events were within the therapeutic range. This trial cannot confirm the safety of intravenous lidocaine at the dose tested.

  2. Comparative trial of succinylcholine vs low dose atracurium-lidocaine combination for intubation in short outpatient procedures.

    PubMed Central

    Luyk, N. H.; Weaver, J. M.; Quinn, C.; Wilson, S.; Beck, F. M.

    1990-01-01

    Despite its many disadvantages, succinylcholine is the most commonly used drug for intubation of patients for short out-patient procedure. This double blind trial compared a low dose atracurium/lidocaine combination to succinylcholine for intubation in 40 ASA1 adult patients. Low dose atracurium/lidocaine provided clinical intubating conditions at two minutes and cardiovascular stability equivalent to succinylcholine with significantly less myalgia. Spontaneous respiration was slower after low dose atracurium/lidocaine relative to succinylcholine. Low dose atracurium/lidocaine may provide an acceptable alternative to succinylcholine for intubation in short outpatient procedures. PMID:2096747

  3. The analgesic efficacy of intravenous lidocaine infusion after laparoscopic fundoplication: a prospective, randomized, double-blind, placebo-controlled trial

    PubMed Central

    Dale, Gregory J; Phillips, Stephanie; Falk, Gregory L

    2016-01-01

    This study aimed to determine if intravenous lidocaine infusion reduces postoperative pain intensity following laparoscopic fundoplication surgery and to also validate the safety of intravenous lidocaine at the dose tested. This was an equally randomized, double-blind, placebo-controlled, parallel-group, single center trial. Adult patients undergoing laparoscopic fundoplication were recruited. The intervention group received 1 mg/kg intravenous lidocaine bolus prior to induction of anesthesia, then an intravenous infusion at 2 mg/kg/h for 24 hours. The primary outcome was pain, measured using a numeric rating scale for 30 hours postoperatively. Secondary outcomes were nausea and vomiting, opioid requirements, adverse events, serum lidocaine concentration, and length of hospital stay. The study was terminated after an interim analysis of 24 patients showed evidence of futility. There was no difference in postoperative pain scores (lidocaine versus control, mean ± standard deviation) at rest (2.0 ± 2.7 vs 2.1 ± 2.4, P=0.286) or with movement (2.0 ± 2.6 vs 2.6 ± 2.7, P=0.487). Three adverse events occurred in the lidocaine group (25% of patients). Intravenous lidocaine did not provide clinically significant analgesia to patients undergoing laparoscopic fundoplication. The serum lidocaine concentration of patients who experienced adverse events were within the therapeutic range. This trial cannot confirm the safety of intravenous lidocaine at the dose tested. PMID:27980437

  4. Fast lidocaine block of cardiac and skeletal muscle sodium channels: one site with two routes of access.

    PubMed Central

    Zamponi, G W; Doyle, D D; French, R J

    1993-01-01

    We have studied the block by lidocaine and its quaternary derivative, QX-314, of single, batrachotoxin (BTX)-activated cardiac and skeletal muscle sodium channels incorporated into planar lipid bilayers. Lidocaine and QX-314, applied to the intracellular side, appear to induce incompletely resolved, rapid transitions between the open and the blocked state of BTX-activated sodium channels from both heart and skeletal muscle. We used amplitude distribution analysis (Yellen, G. 1984. J. Gen. Physiol. 84:157-186.) to estimate the rate constants for block and unblock. Block by lidocaine and QX-314 from the cytoplasmic side exhibits rate constants with similar voltage dependence. The blocking rate increases with depolarization, and the unblocking rate increases with hyperpolarization. Fast lidocaine block was virtually identical for sodium channels from skeletal (rat, sheep) and cardiac (beef, sheep) muscle. Lidocaine block from the extracellular side occurred at similar concentrations. However, for externally applied lidocaine, the blocking rate was voltage-independent, and was proportional to concentration of the uncharged, rather than the charged, form of the drug. In contrast, unblocking rates for internally and externally applied lidocaine were identical in magnitude and voltage dependence. Our kinetic data suggest that lidocaine, coming from the acqueous phase on the cytoplasmic side in the charged form, associates and dissociates freely with the fast block effector site, whereas external lidocaine, in the uncharged form, approaches the same site via a direct, hydrophobic path. PMID:8396459

  5. Buffered Lidocaine Hydrochloride Solution With and Without Epinephrine: Stability in Polypropylene Syringes

    PubMed Central

    Pascuet, Elena; Donnelly, Ronald F; Garceau, Danielle; Vaillancourt, Régis

    2009-01-01

    Background: Pain associated with infiltrating the skin with lidocaine can be reduced by buffering the solution with sodium bicarbonate. Objectives: To determine the physical compatibility and chemical stability of lidocaine hydrochloride solution buffered with 8.4% sodium bicarbonate, with and without epinephrine, packaged in polypropylene syringes and stored at 5°C with protection from light. Methods: Lidocaine solutions (1% and 2%), with and without epinephrine 1:100 000, were diluted 10:1 with 8.4% sodium bicarbonate, packaged in 3-mL polypropylene syringes, and stored at 5°C (range 3°C to 8°C). On each of days 0, 3, 7, 10, 14, 17, 21, 24, and 28, the contents of 3 syringes for each solution of lidocaine combined with epinephrine were collected separately in glass vials and frozen at −70°C for subsequent analysis. In addition, on days 0, 7, 14, 21, and 28, the contents of 3 syringes for each lidocaine solution without epinephrine were collected separately in glass vials and frozen at −70°C for subsequent analysis. Chemical stability was determined with a validated, stability-indicating high-performance liquid chromatography method. Changes in colour, clarity, and pH were used to determine physical compatibility of the solutions. Results: All buffered lidocaine solutions containing epinephrine (1:100 000) retained at least 93.3% of the original concentration of epinephrine and 97.5% of the lidocaine concentration for 7 days when stored at 5°C with protection from light. In contrast, the epinephrine-free solutions retained at least 94.7% of the initial concentration of lidocaine for the duration of the study (28 days). All samples remained clear, colourless, and free of precipitate throughout the study, and there were no significant changes in pH. Conclusion: Extemporaneously prepared buffered lidocaine (1% and 2%) packaged in polypropylene syringes remained stable for up to 28 days when properly refrigerated with protection from light. A 7-day expiry

  6. Peribulbar anesthesia. Effect of bicarbonate on mixtures of lidocaine, bupivacaine, and hyaluronidase with or without epinephrine.

    PubMed

    Zahl, K; Jordan, A; McGroarty, J; Sorensen, B; Gotta, A W

    1991-02-01

    The pH-adjustment of local anesthetic solutions with sodium bicarbonate may shorten onset time and improve spread of neural blockade. The authors undertook a prospective, double-masked, randomized study to see if a pH-adjusted mixture of lidocaine, bupivacaine, and hyaluronidase had faster and more complete onset of neural blockade, when used for peribulbar anesthesia. Eighty patients were randomly assigned to four groups and received a peribulbar block with one of four mixtures: group 1 (L) = 2% lidocaine, group 2 (LPH) = 2% lidocaine with 0.06 meq/ml sodium bicarbonate, group 3 (LE) = 2% lidocaine with 1:100,000 epinephrine (commercially prepared), or group 4 (LEPH) = 2% lidocaine with 1:100,000 epinephrine with 0.06 meq/ml sodium bicarbonate. To 5 ml of each of the preceding groups, 5 ml of 0.75% bupivacaine and 150 units of hyaluronidase was added. After each block, extraocular muscle movement was followed in each quadrant until akinesia developed. In the event of incomplete akinesia, blocks were supplemented at 20 minutes. The LPH group had the fastest onset to complete akinesia (7.0 +/- 2.0 minutes, mean +/- SEM) when compared with the onset time of all other groups (group 1 = 11.5 +/- 1.9 minutes, group 4 = 13.1 +/- 1.4 minutes, and group 3 = 16.0 +/- 1.8 minutes, significance greater than 95% by analysis of variance). Furthermore, when compared with group 3 by analysis of variance, group 4 had a faster onset time. The authors conclude that pH-adjustment of solutions with bicarbonate of either lidocaine/bupivacaine/hyaluronidase or commercially prepared lidocaine with epinephrine/bupivacaine/hyaluronidase decreases the onset time of peribulbar anesthesia.

  7. Onset and duration of intradermal mixtures of bupivacaine and lidocaine with epinephrine

    PubMed Central

    Collins, James B; Song, Juhee; Mahabir, Raman C

    2013-01-01

    BACKGROUND/OBJECTIVE: Bupivacaine and lidocaine are often used concurrently, in theory, to combine the more rapid onset of lidocaine and the longer duration of bupivacaine. The purpose of this study was to evaluate this concept. METHODS: Twenty-five subjects were enrolled in a double-blinded, randomized block design study to evaluate the onset and duration of four different mixtures of lidocaine and bupivacaine with epinephrine. The study was designed to achieve 80% power to detect an effect size of 0.37 at 5% overall significance. The four mixtures tested were: 0.25% bupivacaine with epinephrine (1:200,000); 1% lidocaine with epinephrine (1:100,000); 0.125% bupivacaine and 0.5% lidocaine with epinephrine (1:150,000); and 0.25% bupivacaine and 1% lidocaine with epinephrine (1:150,000). Four intradermal injections were made in the volar forearms of each participant. Time to effect and duration were measured by sensation of a sharp skin prick. RESULTS: Mean time to onset ranged from 12 s to 29 s without statistical significance across all tested solutions (P=0.891). Mean duration of effect ranged from 6 h 38 min to 7 h 25 min with a statistically significant difference across the tested solutions (P=0.036). CONCLUSIONS: No statistical benefit was measured when comparing lidocaine with epinephrine, bupivacaine with epinephrine, and mixtures of these local anesthetics with regard to onset of action. While a statistical difference was observed in duration of effect, the clinical benefit measured was narrow. PMID:24431939

  8. Regional myocardial lidocaine concentration following continuous intravenous infusion early and later after myocardial infarction

    SciTech Connect

    Zito, R.A.; Caride, V.J.; Holford, T.; Zaret, B.L.

    1982-09-01

    The regional concentration of lidocaine using a double constant infusion technique (250 micrograms/kg/min x 15 minutes followed by 35 micrograms/kg/mg/min x 120 minutes) was studied immediately (2 hours) in seven dogs and 24 hours (six dogs) after myocardial infarction. Tissue levels were determined by gas chromatography and related to regional myocardial blood flow as determined by the radioactive microsphere technique in multiple samples. At 2 hours after infarction a significantly higher lidocaine concentration (4.1 +/- 0.42 micrograms/g) was found in zones with greatly reduced blood flow (regional myocardial blood flow less than 0.2 ml/min per g) when compared with that (2.6 +/- 0.19 micrograms/g) in zones with normal blood flow (regional myocardial blood flow greater than 0.8 ml/min per g) (p less than 0.01). In contrast, in the 24 hour model the opposite situation was observed. Although the concentration of lidocaine in the infarct zone was substantial, a significant decline in lidocaine tissue concentration was found in the zones of lowest blood flow (regional myocardial blood flow less than 0.2 ml/min per g) when compared with that in normal zones (1.76 +/- 0.21 versus 3.38 +/- 0.21 micrograms/g, p less than 0.001). In addition, no significant differences in lidocaine concentrations were found between endocardium and epicardium in any of the groups other than those related to regional myocardial blood flow. Thus, with the double constant infusion technique, lidocaine reached normal and ischemic myocardium in concentrations equivalent to therapeutic plasma concentrations, even in lower infarct blood flow zones, with no significant differences between endocardium and epicardium. Of perhaps greater significance, the age of the ischemic insult is an important determinant of lidocaine tissue distribution in infarcted myocardium.

  9. Perioperative intravenous lidocaine infusion on postoperative pain relief in patients undergoing upper abdominal surgery.

    PubMed

    Baral, B K; Bhattarai, B K; Rahman, T R; Singh, S N; Regmi, R

    2010-12-01

    Due to unpleasant nature and physiological consequences of postoperative pain, search of safe and effective modalities for its management has remained a subject of interest to clinical researchers. Analgesic action of lidocaine infusion in patients with chronic neuropathic pain is well known but its place in relieving postoperative pain is yet to be established. The study aimed to assess the effectiveness of perioperative intravenous lidocaine infusion on postoperative pain intensity and analgesic requirement. Sixty patients undergoing major upper abdominal surgery were recruited in this randomized double blinded study. Thirty patients received lidocaine 2.0% (intravenous bolus 1.5 mg/kg followed by an infusion of 1.5 mg/kg/h), and 30 patients received normal saline according to randomization. The infusion started 30 min before skin incision and stopped 1 h after the end of surgery. Postoperative pain intensity and analgesic (diclofenac) requirement were assessed at the interval 15 minutes for 1 hour then 4 hourly up to 24 hours. The pain intensity at rest and movement as well as the total postoperative analgesic (diclofenac) requirement were significantly lower (142.50 +/- 37.80 mg vs.185.00 +/- 41.31 mg, P<0.001) in lidocaine group. The extubation time was significantly longer in lidocaine group (14.43 +/- 3.50 minutes vs. 6.73 +/- 1.76 minutes, P<0.001). The time for the first dose of analgesic requirement was longer in lidocaine group (60.97 +/- 18.05 minutes vs.15.73 +/- 7.46 minutes, P<0.001). It can be concluded that perioperative infusion of low dose of lidocaine decreases the intensity of postoperative pain, reduces the postoperative analgesic consumption, without causing significant adverse effects in patients undergoing upper abdominal surgery.

  10. Injectable microparticle-gel system for prolonged and localized lidocaine release. II. In vivo anesthetic effects.

    PubMed

    Chen, Pen-Chung; Kohane, Daniel S; Park, Yoon Jeong; Bartlett, Robert H; Langer, Robert; Yang, Victor C

    2004-09-01

    Current treatment protocols for postoperative pain are beset by either the short duration of the anesthetic effect or requirement of hospitalization of the patients. We reported herein a novel treatment by applying to the surgical site a biodegradable microparticle-gel system for prolonged and localized release of encapsulated anesthetic drugs. In a previous publication, lidocaine-loaded poly(D,L-lactic acid) microspheres were fabricated and their formulations were optimized. In vitro characterization of these lidocaine-loaded microspheres, however, revealed a shortcoming of this system; that is, microspheres tend to fuse physically. Fusion of the microspheres could hinder their clinical applications, as it would clog the needle. In this article, we demonstrated that fabricating microspheres with high molecular weight (approximately 60 KDa) poly(lactic-co-glycolic acid) would increase the glass transition temperature of the microspheres after lidocaine loading, thereby increasing their mechanical stability and eliminating their fusion during storage. Such microspheres containing 31% (w/w) lidocaine in the presence or absence of 25% (w/v) poloxamer 407 gel were then evaluated in vivo by monitoring the sensory and motor functions of the rats after sciatic nerve block, using the previously established hot-plate and weight-bearing testing methods. Results showed that microspheres formulated with poloxamer 407 gel yielded the longest duration of sensory and motor block for a period of approximately 8.5 h, compared to 5 h by microspheres in saline, 5 h by lidocaine in poloxamer 407 gel, and 2 h by lidocaine in saline. This study suggests that the microsphere-gel system containing lidocaine could potentially be applied clinically to the treatment of postoperative pain.

  11. Reduction of ischemic myocardial damage in the dog by lidocaine infusion.

    PubMed Central

    Schaub, R. G.; Stewart, G.; Strong, M.; Ruotolo, R.; Lemoie, G.

    1977-01-01

    The effects of lidocaine infusion on the ultrastructural damage induced in cardiac muscle by normothermic cardiopulmonary bypass were assessed in 15 dogs. Six dogs received no medication other than sodium pentobarbital (25 mg/kg, intravenously) while 9 dogs were treated with lidocaine after anesthesia. Lidocaine was given as a 2-mg/kg loading dose 10 minutes prior to ischemic arrest and a 2-mg/min continuous infusion during the entire experimental period. Biopsy samples of the left ventricular apex were taken 15 and 45 minutes after the start of ischemic arrest and 5 minutes after resumption of coronary blood flow. Biopsy samples were also obtained from 4 animals after thoracotomy to serve as controls for experimental procedures. Myocardial ultrastructure in the 4 control animals was comparable to that reported by other investigators. Five of 6 of the nontreated dogs and 8 of 9 lidocaine-treated dogs survived the entire period of ischemia and 5 minutes of coronary reperfusion. However, the extent of ultrastructural damage varied considerably between the two groups. In the experimental dogs receiving no lidocaine, mitochondria were swollen, cristae were absent, the mitochondrial matrix was cleared, and sarcomeres were disrupted. Myelin figures and contraction bands were also observed. None of the surviving lidocaine-treated animals had ultrastructural changes comparable to the worst ones in nontreated dogs. Damage was limited to some swelling of mitochondria with focal clearing of matrix. Most cristae remained intact. There were no myelin figures and few contraction bands. The results suggest that lidocaine protects the integrity of ischemic myocardium. It is suggested that this protection resulted from stabilization of plasma and/or mitochondrial membranes. (Am J Pathol 87:399-414, 1977). Images Figure 3 Figure 4 Figure 5 Figure 6 Figure 7 Figure 8 Figure 1 Figure 2 PMID:851172

  12. Reversal of visceral and somatic hypersensitivity in a subset of hypersensitive rats by intracolonic lidocaine

    PubMed Central

    Zhou, QiQi; Price, Donald D.; Verne, G. Nicholas

    2010-01-01

    Chronic abdominal pain is a common gastrointestinal symptom experienced by patients. We have previously shown that IBS patients with visceral hypersensitivity also have evidence of thermal hypersensitivity of the hand and foot that is reversed by rectal lidocaine jelly. We have also recently developed an animal model of chronic visceral and somatic hypersensitivity in rats treated with intracolonic trinitrobenzene sulfonic acid (TNBS). The objective of the current study was to determine the effects of intracolonic lidocaine on visceral/somatic hypersensitivity in TNBS-treated rats. A total of 20 hypersensitive rats received either 20 mg intracolonic lidocaine (n = 10) or saline jelly (n = 10). In comparison to saline jelly, intracolonic lidocaine jelly reduced responses to nociceptive visceral/somatic stimuli in hypersensitive rats. The effects were present within 5–30 min after administration of lidocaine and lasted for 6 h. Lidocaine had no effects on recovered rats or control rats that had originally been treated with intracolonic saline instead of TNBS. Local anesthetic blockade of peripheral impulse input from the colon reduces both visceral and somatic hypersensitivity in TNBS-treated rats, similar to results in IBS patients. The results provide further evidence that visceral and secondary somatic hypersensitivity in a subset of TNBS-treated rats reflect central sensitization mechanisms maintained by tonic impulse input from the colon. This study evaluates the reversal of visceral/somatic hypersensitivity in a subset of TNBS-treated rats with intracolonic lidocaine. This animal model may be used in the future to study the mechanisms of local anesthetic agents applied to the gut to reduce visceral pain. PMID:18486344

  13. [Effects of lidocaine on arterial and venous circulation of limbs in man].

    PubMed

    Edouard, A; Probst, D; Duranteau, J; Tarot, J P; Pussard, E

    1991-01-01

    The effects of intravenous lidocaine on limb arteries and veins were investigated in a placebo-controlled study. Seven young healthy volunteers, 23 to 28-years-old, were included. Electrocardiogram, arterial pressure and arm and leg blood flows were recorded continuously. Systolic and diastolic blood pressures were measured in the left arm by finger photoplethysmography. Limb blood flow and the limb venous system were studied by venous occlusive plethysmography. The venous parameters studied were venous tone, lowest closing pressure, venous volume at 30 mmHg, and venous distensibility. After an initial bolus of 1.5 mg.kg-1 lidocaine had been given, 30, and then 60, micrograms.kg-1.min-1 were given for one hour each. Plasma noradrenaline and serum lidocaine titres were measured before giving the lidocaine, and at the end of each one hour period. Placebo consisted in a two hour infusion of 0.25 ml.min-1 normal saline. Lidocaine titres were 1.64 +/- 0.40 microgram.ml-1 after one hour, and 2.55 +/- 0.69 microgram.ml-1 after two hours. Lidocaine increased vascular resistances in both the forearm (+81% to +93%) and the calf (+38% to +57%). There was a concomitant increase in mean arterial blood pressure (+21% to +28%) without any change in heart rate. There was a significant dose-dependent increase in plasma noradrenaline levels during the second period of the lidocaine infusion with respect to the preinfusion period and the same period during the placebo infusion. Venous capacitance measured before any infusion had been started was greater in the leg than in the arm.(ABSTRACT TRUNCATED AT 250 WORDS)

  14. Comparison of the Effects of Lidocaine Prilocaine Cream (EMLA) and Lidocaine Injection on Reduction of Perineal Pain During Perineum Repair in Normal Vaginal Delivery

    PubMed Central

    Kargar, Roxana; Aghazadeh-Nainie, Afsaneh; Khoddami-Vishteh, Hamid Reza

    2016-01-01

    Objective: To compare the efficacy of EMLA cream and lidocaine injection to reduce pain during episiotomy repair. Materials and methods: A total of 46 primiparous women with normal pregnancy who referred for normal vaginal delivery and needed episiotomy repair were selected and randomly divided into two groups. For EMLA group, one hour before the estimated time of delivery, 5g of EMLA cream was applied to perinealmediolateral incision, and after the delivery of the fetus and placenta, again 5g of EMLA cream was applied to healthy skin around the episiotomy for repair. In the other group, lidocaine 2% was used before episiotomy and for its repair, too. Results: Only 8 people (19%) were in need of further analgesia. The mean ± SD of pain during repair of episiotomy on the VAS scale in all cases was 4.2 ± 2.3 cm. Most people (97%) were satisfied with their episiotomy repair. Comparing the two groups of EMLA and lidocaine, there was no difference between the two groups in terms of the duration of episiotomy repair, need for further analgesia, pain on the VAS scale, and satisfaction with the repair method. Conclusion: The findings of this study showed that the use of EMLA cream in the site of episiotomy incision in primiparous women can induce a level of analgesia equal to that of lidocaine, and cause a similar level of satisfaction. PMID:27385970

  15. Impact of intravenous lidocaine infusion on postoperative analgesia and recovery from surgery: a systematic review of randomized controlled trials.

    PubMed

    McCarthy, Grace C; Megalla, Sohair A; Habib, Ashraf S

    2010-06-18

    Postoperative pain continues to be inadequately managed. While opioids remain the mainstay for postoperative analgesia, their use can be associated with adverse effects, including ileus, which can prolong hospital stay. A number of studies have investigated the use of perioperative intravenous lidocaine infusion for improving postoperative analgesia and enhancing recovery of bowel function. This systematic review was performed to determine the overall efficacy of intravenous lidocaine infusion on postoperative analgesia and recovery from surgery in patients undergoing various surgical procedures. We searched the databases of MEDLINE, CINAHL and the Cochrane Library from 1966 to December 2009. We searched for randomized controlled comparisons of lidocaine infusion with placebo in the surgical setting and reporting on postoperative analgesia and other aspects of patient recovery from surgery. The quality of all included studies was assessed using the Modified Oxford Scale. Information on postoperative pain intensity and analgesic requirements was extracted from the trials and compared qualitatively. Other relevant data such as return of bowel function, length of hospital stay, intraoperative anaesthetic requirement and adverse effects were also compared. Sixteen trials were included. A total of 395 patients received intravenous lidocaine with 369 controls. In open and laparoscopic abdominal surgery, as well as in ambulatory surgery patients, intravenous perioperative infusion of lidocaine resulted in significant reductions in postoperative pain intensity and opioid consumption. Pain scores were reduced at rest and with cough or movement for up to 48 hours postoperatively. Opioid consumption was reduced by up to 85% in lidocaine-treated patients when compared with controls. Infusion of lidocaine also resulted in earlier return of bowel function, allowing for earlier rehabilitation and shorter duration of hospital stay. First flatus occurred up to 23 hours earlier

  16. Microdialysis and Delivery of Iontophoresis-Driven Lidocaine Into the Human Gastrocnemius Muscle

    PubMed Central

    Coglianese, Mark; Draper, David O.; Shurtz, Joseph; Mark, Gary

    2011-01-01

    Context: Iontophoresis is used frequently in physical medicine and rehabilitation, but many research techniques do not adequately measure it for depth of medicine delivery. Objective: To determine if iontophoresis delivers lidocaine 5 mm under the surface of human skin. Design: Descriptive laboratory study. Setting: Therapeutic modalities research laboratory. Patients or Other Participants: Eight men and 5 women volunteers (age range = 21 ± 2.3 years) who had less than 5 mm of adipose tissue in the area we measured participated in the study. Intervention(s): We inserted a microdialysis probe 5 mm under the skin of both legs and into the triceps surae muscle groups of 10 participants. Microdialysis was performed for 60 minutes to allow a recovery period for local skin blood flow to return to baseline. We then delivered 2 mL of 1% lidocaine to the treatment leg via iontophoresis at 40 mA/min. Next, microdialysis was performed continuously in both legs during the treatment and for 30 minutes posttreatment to collect the lidocaine samples. After we had gathered the samples, several saline solutions with various amounts of lidocaine (0.005%, 0.025%, 0.05%, and 0.1%) were prepared in vitro and analyzed. Although we did not intend to do so as a part of the original study, we also performed an identical follow-up study at 3 mm in 3 participants. Main Outcome Measure(s): Both in vitro and in vivo samples were analyzed via reverse-phase high-performance liquid chromatography (RP-HPLC). A protocol for detection and quantification of lidocaine using RP-HPLC was followed. Results: We did not detect any measurable levels or concentrations of lidocaine in the 10 control samples. According to the RP-HPLC analysis, the 10 treatment samples also were negative for the presence of lidocaine. However, when we performed the study at 3 mm, microdialysis detected lidocaine in the 3 participants at this depth in the treatment leg only. Conclusions: Measurable levels of lidocaine were not

  17. Effect of epinephrine and lidocaine therapy on outcome after cardiac arrest due to ventricular fibrillation.

    PubMed

    Weaver, W D; Fahrenbruch, C E; Johnson, D D; Hallstrom, A P; Cobb, L A; Copass, M K

    1990-12-01

    One hundred ninety-nine patients with out-of-hospital cardiac arrest persisted in ventricular fibrillation after the first defibrillation attempt and were then randomly assigned to receive either epinephrine or lidocaine before the next two shocks. The resulting electrocardiographic rhythms and outcomes for each group of patients were compared for each group and also compared with results during the prior 2 years, a period when similar patients primarily received sodium bicarbonate as initial adjunctive therapy. Asystole occurred after defibrillation with threefold frequency after repeated injection of lidocaine (15 of 59, 25%) compared with patients treated with epinephrine (four of 55, 7%) (p less than 0.02). There was no difference in the proportion of patients resuscitated after treatment with either lidocaine or epinephrine (51 of 106, 48% vs. 50 of 93, 54%) and in the proportion surviving (18, 19% vs. 21, 20%), respectively. Resuscitation (64% vs. 50%, p less than 0.005) but not survival rates (24% vs. 20%) were higher during the prior 2-year period in which initial adjunctive drug treatment for persistent ventricular fibrillation primarily consisted of a continuous infusion of sodium bicarbonate. The negative effect of lidocaine or epinephrine treatment was explained in part by their influence on delaying subsequent defibrillation attempts. Survival rates were highest (30%) in a subset of patients who received no drug therapy between shocks. We conclude that currently recommended doses of epinephrine and lidocaine are not useful for improving outcome in patients who persist in ventricular fibrillation.(ABSTRACT TRUNCATED AT 250 WORDS)

  18. Paced mating behavior is affected by clitoral-vaginocervical lidocaine application in combination with sexual experience.

    PubMed

    Meerts, Sarah H; Strnad, Helen K; Schairer, Rosemary S

    2015-03-01

    The present study tested the effects of lidocaine anesthetic ointment applied to the vaginocervical (Experiment 1) or clitoral-vaginocervical (Experiment 2) areas on the display of paced mating behavior over the course of five weekly tests in ovariectomized, hormone-primed, Long-Evans rats. Experiment 3 tested whether rats that acquired sexual experience without ointment application would exhibit altered paced mating behavior on a fifth test under clitoral-vaginocervical lidocaine or vehicle application. Although rats in Experiment 1 and Experiment 2 exhibited shorter contact-return latencies after intromission and reduced likelihood of leaving the male compartment following mounts and intromissions after gaining sexual experience, only rats that received clitoral-vaginocervical lidocaine exhibited altered paced mating behavior relative to vehicle. Specifically, clitoral-vaginocervical lidocaine resulted in shorter contact-return latency to ejaculation and greater percentage of time with the male. Paced mating behavior of sexually experienced rats in Experiment 3 was not disrupted when tested after clitoral-vaginocervical lidocaine treatment. Together, these studies suggest that the sensory input during repeated mating encounters affects the pattern of paced mating behavior that develops with sexual experience.

  19. [Topical pharmacologic approach with 5% lidocaine medicated plaster in the treatment of localized neuropathic pain].

    PubMed

    Provinciali, L; Lattanzi, S; Chiarlone, R; Fogliardi, A; Intelligente, F; Irace, C; Lanzilotta, M; Palomba, R; Storelli, E; Zampi, M

    2014-12-01

    The treatment of neuropathic pain is a medical challenge. The responsiveness to the different classes of drugs is often unsatisfactory and frequently associated to a wide range of side effects. International guidelines suggest for the "localized" neuropathic pain the topical treatment with 5% lidocaine medicated plaster, alone or associated to systemic drugs, as the first choice since its favorable efficacy and tolerability profile. Many clinical experiences support the rationale for using 5% lidocaine medicated plaster in different kinds of localized neuropathic pain, such as postherpetic and trigeminal neuralgia, compressive syndromes, painful diabetic polyneuropathy and pain secondary to trauma or surgical interventions. This paper reports a series of clinical cases whose heterogeneity suggests the wide burden of applicability of the topical 5% lidocaine, either alone and associated to systemic drugs. All the described conditions were characterized by a highly intense pain, not adequately controlled by actual medications, which improved after the use of topical lidocaine. The good response to lidocaine allowed the reduction, of even the withdrawal, of concurrent drugs and improved the patients' quality of life.

  20. A comparison of the anesthetic efficacy of articaine and lidocaine in patients with irreversible pulpitis.

    PubMed

    Tortamano, Isabel Peixoto; Siviero, Marcelo; Costa, Carina Gisele; Buscariolo, Inês Aparecida; Armonia, Paschoal Laércio

    2009-02-01

    The purpose of the present study was to compare the anesthetic efficacy of 4% articaine with 1:100,000 epinephrine with that of 2% lidocaine with 1:100,000 epinephrine during pulpectomy in patients with irreversible pulpitis in mandibular posterior teeth. Forty volunteers, patients with irreversible pulpitis admitted to the Emergency Center of the School of Dentistry at the University of São Paulo, randomly received a conventional inferior alveolar nerve block containing 3.6 mL of either 4% articaine with 1:100,000 epinephrine or 2% lidocaine with 1:100,000 epinephrine. During the subsequent pulpectomy, we recorded the patients' subjective assessments of lip anesthesia, the absence/presence of pulpal anesthesia through electric pulp stimulation, and the absence/presence of pain through a verbal analogue scale. All tested patients reported lip anesthesia after the application of either inferior alveolar nerve block. Regarding pulpal anesthesia success as measured with the pulp tester, the lidocaine solution had a higher success rate (70%) than the articaine solution (65%). For patients reporting none or mild pain during pulpectomy, the success rate of the articaine solution (65%) was higher than that of the lidocaine solution (45%). Yet, none of the observed differences between articaine and lidocaine were statistically significant. Apparently, therefore, both local anesthetic solutions had similar effects on the patients with irreversible pulpitis in mandibular posterior teeth. Neither of the solutions, however, resulted in an effective pain control during irreversible pulpitis treatments.

  1. E. coli endotoxin shock in the dog; treatment with lidocaine or indomethacin.

    PubMed Central

    Fletcher, J R; Ramwell, P W

    1978-01-01

    1 Dogs treated with lidocaine (1 mg kg-1 h-1) or indomethacin (1.5 mg/kg) before and after an LD60 dose (1 mg/kg) of E. coli endotoxin survived for at least 72 h. 2 Although all dogs in both treated groups survived, only those treated with indomethacin were significantly protected against the fall in the arterial blood pressure 1 to 2 min following endotoxin administration. 3 Endotoxin increased the plasma prostaglandin F2alpha (PGF2alpha) concentration in the control and lidocaine-treated groups, however, no increase was observed with indomethacin treatment. 4 Neither lidocaine nor indomethacin alone had any significant effect on the parameters measured in this model. 5 Following the administration of endotoxin, lidocaine-treated animals had significantly decreased plasma fibrinogen concentrations when compared to the other groups. 6 This study suggests that lidocaine, a local anaesthetic and a drug widely used for cardiac arrhythmias, might offer protection in endotoxin shock. PMID:361135

  2. Paraspinous Lidocaine Injection for Chronic Nonspecific Low Back Pain: A Randomized Controlled Clinical Trial

    PubMed Central

    Imamura, Marta; Imamura, Satiko Tomikawa; Targino, Rosa Alves; Morales-Quezada, León; Onoda Tomikawa, Luis C.; Onoda Tomikawa, Luis G.; Alfieri, Fabio M.; Filippo, Thais R.; da Rocha, Ivan D.; Neto, Raul Bolliger; Fregni, Felipe; Battistella, Linamara Rizzo

    2016-01-01

    In this large, sham-controlled, randomized trial, we examined the efficacy of the combination of standard treatment and paraspinous lidocaine injection compared with standard therapy alone in subjects with chronic low back pain. There is little research-based evidence for the routine clinical use of paraspinous lidocaine injection for low back pain. A total of 378 subjects with nonspecific chronic low back pain were randomized to 3 groups: paraspinous lidocaine injection, analgesics, and exercises (group 1, LID-INJ); sham paraspinous lidocaine injection, analgesics, and exercises (group 2, SH-INJ); and analgesics and exercises (group 3, STD-TTR). A blinded rater assessed the study outcomes at 3 time points: baseline, after treatment, and after 3 months of follow-up. There were increased frequency of pain responses and better low back functional scores in the LID-INJ group compared with the SH-INJ and STD-TTR groups. These effects remained at the 3-month follow-up but differed between all 3 groups. There were significant changes in pain threshold immediately after treatment, supporting the effects of this intervention in reducing central sensitization. Paraspinous lidocaine injection therapy is not associated with a higher risk of adverse effects compared with conventional treatment and sham injection. Its effects on hyperalgesia might correlate with changes in central sensitization. PMID:26828801

  3. Effect of charged lidocaine on static and dynamic properties of model bio-membranes.

    PubMed

    Yi, Zheng; Nagao, Michihiro; Bossev, Dobrin P

    2012-01-01

    The effect of the charged lidocaine on the structure and dynamics of DMPC/DMPG (mass fraction of 95/5) unilamellar vesicles has been investigated. Changes in membrane organization caused by the presence of lidocaine were detected through small angle neutron scattering experiments. Our results suggest that the presence of lidocaine in the vicinity of the headgroups of lipid membranes leads to an increase of the area per lipid molecule and to a decrease of membrane thickness. Such changes in membrane structure may induce disordering of the tail group. This scenario explains the reduction of the main transition temperature of lipid membranes, as the fraction of lidocaine per lipid molecules increases, which was evident from differential scanning calorimetry results. Furthermore neutron spin echo spectroscopy was used for the dynamics measurements and the results reveal that presence of charged lidocaine increases the bending elasticity of the lipid membranes in the fluid phase and slows the temperature-dependent change of bending elasticity across the main transition temperature.

  4. Determination and temperature effects of lidocaine (lignocaine) hydrochloride, epinephrine, methylparaben, 2,6-dimethylaniline, and p-hydroxybenzoic acid in USP lidocaine injection by ion-pair reversed-phase high pressure liquid chromatography

    SciTech Connect

    Smith, D.J.

    1981-05-01

    USP Lidocaine injection was assayed using ion-pair high pressure liquid chromatography with an octylsilane (RP-8) reversed-phase column packing and a mobile phase consisting of D-10-camphorsulfonic acid/methanol/acetic acid/water. The effect of temperature was investigated to determine the optimum temperature for separating the drug components and their degradation products. Lidocaine (lignocaine) hydrochloride, epinephrine, methylparaben, and p-hydroxybenzoic acid were separated at 50 degrees C. 2,6-Dimethylaniline was separated from lidocaine at 15 degrees C. An aliquot of the sample was injected directly into the liquid chromatograph, and after separation the compounds were quantitated by their spectrophotometric response at 254 nm (lidocaine) or 280 nm (lidocaine plus epinephrine).

  5. Determination and temperature effects of lidocaine (lignocaine) hydrochloride, epinephrine, methylparaben, 2,6-dimethylaniline, and p-hydroxybenzoic acid in USP lidocaine injection by ion-pair reversed-phase high pressure liquid chromatography.

    PubMed

    Smith, D J

    1981-05-01

    USP Lidocaine injection was assayed using ion-pair high pressure liquid chromatography with an octylsilane (RP-8) reversed-phase column packing and a mobile phase consisting of D-10-camphorsulfonic acid/methanol/acetic acid/water. The effect of temperature was investigated to determine the optimum temperature for separating the drug components and their degradation products. Lidocaine (lignocaine) hydrochloride, epinephrine, methylparaben, and p-hydroxybenzoic acid were separated at 50 degrees C. 2,6-Dimethylaniline was separated from lidocaine at 15 degrees C. An aliquot of the sample was injected directly into the liquid chromatograph, and after separation the compounds were quantitated by their spectrophotometric response at 254 nm (lidocaine) or 280 nm (lidocaine plus epinephrine).

  6. Topical lidocaine patch 5% for acute postoperative pain control.

    PubMed

    Gilhooly, D; McGarvey, B; O'Mahony, H; O'Connor, T C

    2011-02-08

    A 39-year-old para 3 woman presented for elective caesarean section (lower segment caesarean section (LSCS)) for breech presentation. The patient had a strong history of atopy and anaphylaxis to paracetamol, codeine, penicillin and latex. The patient was asthmatic, triggered by aspirin. Epidural anaesthesia was unsuccessful and LSCS was carried out under spinal anaesthesia. Postoperatively the patient was unwilling to take analgesic medication due to fear of an allergic reaction. Three 5% lidocaine patches were applied to the wound for postoperative analgesia. This reduced the patient's visual analogue scale pain score from 10/10 to 5/10 at rest and 10/10 to 7/10 with movement. Transcutaneous electrical nerve stimulation was added and this improved associated back pain, reducing the pain further to 2/10. This is the first description of lignocaine patch 5% for postoperative LSCS pain. It is suggested that this method of delivery of local anaesthetic, which is easy to apply and has minimal side effects, should be considered not as a sole agent but as part of a multimodal technique to address postoperative LSCS pain.

  7. Simultaneous micellar LC determination of lidocaine and tolperisone.

    PubMed

    Youngvises, Napaporn; Liawruangrath, Boonsom; Liawruangrath, Saisunee

    2003-03-26

    A micellar liquid chromatography (MLC) procedure was developed for the simultaneous separation and determination of lidocaine hydrochloride (LD HCl) and tolperisone hydrochloride (TP HCl) using a short-column C18 (12.5 mm x 4.6 mm, 5 microm), sodium dodecyl sulfate (SDS) with a small amount of isopropanol, and diode array detector. The optimum conditions for the simultaneous determination of both drugs were 0.075 mol l(-1) SDS-7.5% (v/v) isopropanol with a flow rate of 0.7 ml min(-1) and detection at 210 nm. The LOD (2S/N) of LD HCl was 0.73 ng 20 microl(-1), whereas that of TP HCl was 1.43 ng 20 microl(-1). The calibration curves for LD HCl and TP HCl were linear over the ranges 0.125-500 microg ml(-1) (r(2)=0.9999) and 1.00-500 microg ml(-1) (r(2)=0.9997), respectively. The %recoveries of both drugs were in the range 98-103% and the %RSD values were less than 2. The proposed method has been successfully applied to the simultaneous determination of TP HCl and LD HCl in various pharmaceutical preparations.

  8. Caspase-2 and microRNA34a/c regulate lidocaine-induced dorsal root ganglia apoptosis in vitro.

    PubMed

    Li, Yandong; Jia, Zhi; Zhang, Laizhu; Wang, Jianguo; Yin, Guangming

    2015-11-15

    Epidural administration of lidocaine may cause neurotoxicity in spinal cord dorsal root ganglia neurons (DRGNs). In this study, we explored the underling mechanisms of apoptotic pathways of lidocaine-induced apoptosis in DRGNs. Neonatal rat DRGNs were treated with lidocaine to induced apoptosis in vitro. Western blot showed caspase- (casp-) 2/3/9 proteins were all upregulated by lidocaine in DRGNs. However, inhibition of casp-2 protected lidocaine-induced apoptosis in DRGNs, whereas Casp3/9 inhibition did not. The possible upstream epigenetic regulators of casp-2, microRNA-34 (miR-34) family, including miR-34a/b/c, were evaluated by dual-luciferase reporter assay and qRT-PCR. We found miR-34a/c, but not miR-34b, were down-regulated in lidocaine-induced DRGN apoptosis. Subsequent upregulation of miR-34 family showed miR-34a/c were able to inhibit casp-2 and protect lidocaine-induced apoptosis in DRGNs, whereas miR-34b did not. Thus, out study shows that casp-2, in association with miR-34a/c was actively involved in lidocaine-induced apoptosis in DRGNs. Inhibiting casp-2 or upregulating miR-34a/c may provide novel meanings to protect local anesthetic-induced neurotoxicity.

  9. Endoplasmic reticulum stress is involved in the lidocaine-induced apoptosis in SH-SY5Y neuroblastoma cells.

    PubMed

    Li, Kehan; Han, Xuechang

    2015-05-01

    Lidocaine has been indicated to promote apoptosis and to promote endoplasmic reticulum (ER) stress. However, the mechanism underlining ER stress-mediated apoptosis is unclear. In the present study, we investigated the promotion to ER stress in the lidocaine-induced apoptosis in human neuroblastoma SH-SY5Y cells. Firstly, we confirmed that lidocaine treatment induced apoptosis in SH-SY5Y cells, time-dependently and dose-dependently, via MTT cell viability assay and annexin V/FITC apoptosis detection with a FACScan flow cytometer. And the anti-apoptosis Bcl-2 and Bcl-xL were downregulated, whereas the apoptosis-executive caspase 3 was promoted through Western blot assay and caspase 3 activity assay. Moreover, the ER stress-associated binding immunoglobulin protein (BiP), PKR-like ER kinase (PERK), activating transcription factor 4 (ATF4) and CCAAT/enhancer-binding protein homologous protein (CHOP) were also upregulated at both mRNA and protein levels by lidocaine treatment. On the other hand, downregulation of the ER stress-associated BiP by RNAi method not only blocked the lidocaine-promoted ER stress but also attenuated the lidocaine-induced SH-SY5Y cell apoptosis. In conclusion, the present study confirmed the involvement of ER stress in the lidocaine-induced apoptosis in human neuroblastoma SH-SY5Y cells. Our study provides a better understanding on the mechanism of lidocaine's neurovirulence.

  10. Continuous subcutaneous infusion of lidocaine for persistent hiccup in advanced cancer.

    PubMed

    Kaneishi, Keisuke; Kawabata, Masahiro

    2013-03-01

    Persistent hiccup can cause anorexia, weight loss, disabling sleep deprivation, anxiety, and depression. Therefore, relief of persistent hiccup is important for advanced cancer patients and their family. Most reports on this condition are case series reports advocating the use of baclofen, haloperidol, gabapentin, and midazolam. However, these medications are occasionally ineffective or accompanied by intolerable side effects. The sodium channel blocker lidocaine has been shown to be effective in treating a variety of disorders thought to involve neuropathic mechanisms. Intravenous administration of lidocaine is common but efficacy has also been reported for subcutaneous infusion. In advanced cancer patients, subcutaneous infusion is easy, advantageous, and accompanied by less discomfort. We report a case of severe and sustained hiccup caused by gastric cancer that was successfully treated with a continuous subcutaneous infusion of lidocaine (480 mg (24 ml)/day) without severe side effects.

  11. [Sensitization of bradycardia during final hypotension induced by serotonin in rats: effect of lidocaine].

    PubMed

    Valle, L B; Oliveira-Filho, R M; Armonia, P L; Nassif, M; Saraceni, G

    1975-10-01

    It was studied the sensibilizing effect of lidocaine (8.5 mg/kg, i.v.) on the ECG (heart rate, P-R interval, QRS complex and Q-T interval) of both intact and bilaterally vagotomised rats, in the nadir of the final hypotension determined by serotonine (60 mug/kg, i.v.). The results showed (1) a certain degree of selectivity of the vagi, and (2) the effects of serotonine either isolated or associated to lidocaine on P-R interval and heart rate were reinforced when intact animals were used. Although no significant alterations of Q-T were elicited by the drugs, lidocaine surprisingly enlarged the QRS complex in a more significant fashion for the intact than for the vagotomised animals.

  12. Analgesic efficacy of lidocaine and multimodal analgesia for chest tube removal: A randomized trial study1

    PubMed Central

    Pinheiro, Valdecy Ferreira de Oliveira; da Costa, José Madson Vidal; Cascudo, Marcelo Matos; Pinheiro, Ênio de Oliveira; Fernandes, Maria Angela Ferreira; de Araujo, Ivonete Batista

    2015-01-01

    Objective: to assess the analgesic efficacy of subcutaneous lidocaine and multimodal analgesia for chest tube removal following heart surgery. Methods: sixty volunteers were randomly allocated in two groups; 30 participants in the experimental group were given 1% subcutaneous lidocaine, and 30 controls were given a multimodal analgesia regime comprising systemic anti-inflammatory agents and opioids. The intensity and quality of pain and trait and state anxiety were assessed. The association between independent variables and final outcome was assessed by means of the Chi-squared test with Yates' correction and Fisher's exact test. Results: the groups did not exhibit significant difference with respect to the intensity of pain upon chest tube removal (p= 0.47). The most frequent descriptors of pain reported by the participants were pressing, sharp, pricking, burning and unbearable. Conclusion: the present study suggests that the analgesic effect of the subcutaneous administration of 1% lidocaine combined with multimodal analgesia is most efficacious. PMID:26625989

  13. [Prolonged epidural analgesia induced by clopheline in combination with lidocaine in obstetric analgesia].

    PubMed

    Semenikhin, A A; En Din Kim; Kurbanov, S D

    1998-01-01

    The study was carried out in 178 women without grave obstetrical or extragenital diseases. In group 1 labor pain was relieved by prolonged epidural anesthesia with 2% lidocaine solution (2-2.5 mg/kg), in group 2 prolonged epidural anesthesia with 1% lidocaine solution (1 mg/kg) and 0.01% clofelin (1 microgram/kg) was administered. Central hemodynamics, heart rhythm, external respiration function, uterine contractility, and fetal intrauterine status were assessed. The findings indicate that none of the methods had a negative impact on the vital parameters of women and newborns at any stage of anesthesia. However, a combination of epidural clofelin (1 microgram/kg) with lidocaine permits an appreciable decrease in the doses of both drugs without decreasing the efficacy of anesthesia. This method has a favorable effect on the course of labor: the mouth of the womb opens sooner at a lower uterine activity and there are no negative effects on the fetus and newborn.

  14. The analgesic effect of midazolam when added to lidocaine for intravenous regional anaesthesia*

    PubMed Central

    Kashefi, Parviz; Montazeri, Kamran; Honarmand, Azim; Safavi, Mohammadreza; Hosseini, Hashem Mirzaee

    2011-01-01

    BACKGROUND: Midazolam has analgesic properties. The aim of the present study was to assess the analgesic effect of midazolam when added to lidocaine in intravenous regional anesthesia (IVRA). METHODS: Sixty patients undergoing hand surgery were randomly allocated into two groups to receive 3 mg/kg 2% lidocaine diluted with saline to a total volume of 40 mL in the control group (group lidocaine saline ~ LS, n=30) or 50 μg/kg midazolam plus 3 mg/kg 2% lidocaine diluted with saline to a total volume of 40 mL in the midazolam group (group lidocaine midazolam ~ LM, n=30). Before and after the tourniquet application, hemodynamic variables, tourniquet pain, sedation, and analgesic use were recorded. RESULTS: Shortened sensory and motor block onset time [4.20 (0.84) vs. 5.94 (0.83) min, p = 0.001 and 6.99 (0.72) vs. 9.07 (0.99) min, p = 0.001 in LM and LS groups, respectively], prolonged sensory and motor block recovery times [8.41 (0.94) vs. 5.68 (0.90) min, p = 0.001 and 11.85 (1.18) vs. 7.06 (0.82) min, p = 0.001 in LM and LS groups, respectively], shortened visual analog scale (VAS) scores of tourniquet pain (p < 0.05), and improved quality of anesthesia were found in group LM (p < 0.05). VAS scores were lower in group LM in the postoperative period (p = 0.001). Postoperative analgesic requirements were significantly smaller in group LM (p = 0.001). CONCLUSIONS: The addition of 50 μg/kg midazolam to lidocaine for IVRA shortens the onset of sensory and motor block, and improves quality of anesthesia and perioperative analgesia without causing side effects. PMID:22973382

  15. The Effect of Lidocaine · HCl on the Fluidity of Native and Model Membrane Lipid Bilayers

    PubMed Central

    Park, Jun-Seop; Jung, Tae-Sang; Noh, Yang-Ho; Kim, Woo-Sung; Park, Won-Ick; Kim, Young-Soo; Chung, In-Kyo; Sohn, Uy Dong; Bae, Soo-Kyung

    2012-01-01

    The purpose of this study is to investigated the mechanism of pharmacological action of local anesthetic and provide the basic information about the development of new effective local anesthetics. Fluorescent probe techniques were used to evaluate the effect of lidocaine·HCl on the physical properties (transbilayer asymmetric lateral and rotational mobility, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex, and liposomes of total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. An experimental procedure was used based on selective quenching of 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer from the tryptophans of membrane proteins to Py-3-Py. Lidocaine·HCl increased the bulk lateral and rotational mobility of neuronal and model membrane lipid bilayes, and had a greater fluidizing effect on the inner monolayer than the outer monolayer. Lidocaine·HCl increased annular lipid fluidity in SPMV lipid bilayers. It also caused membrane proteins to cluster. The most important finding of this study is that there is far greater increase in annular lipid fluidity than that in lateral and rotational mobilities by lidocaine·HCl. Lidocaine·HCl alters the stereo or dynamics of the proteins in the lipid bilayers by combining with lipids, especially with the annular lipids. In conclusion, the present data suggest that lidocaine, in addition to its direct interaction with proteins, concurrently interacts with membrane lipids, fluidizing the membrane, and thus inducing conformational changes of proteins known to be intimately associated with membrane lipid. PMID:23269904

  16. Effect of PaCO2 and PaO2 on lidocaine and articaine toxicity.

    PubMed

    Barcelos, K C; Furtado, D P; Ramacciato, J C; Cabral, A M; Haas, D A

    2010-01-01

    Alterations in arterial PaCO₂ can influence local anesthetic toxicity. The objective of this study was to evaluate the effect of stress-induced changes in PaCO₂ and PaO₂ on the seizure threshold of lidocaine and articaine. Lidocaine (2% with 1 : 100,000 epinephrine) or articaine (4% with 1 : 100,000 epinephrine) was administered intravenously under rest or stress conditions to 36 rats separated into 4 groups. Propranolol and prazosin were administered preoperatively to minimize cardiovascular effects of epinephrine. Mean arterial pressure (MAP), heart rate (HR), and arterial pH, PaCO₂, and PaO₂ were measured. Results showed no differences in MAP, HR, or pH. Stress significantly increased the latency period for the first tonic-clonic seizure induced by a toxic dose of both lidocaine and articaine (P < .05). Seizures were brought on more rapidly by articaine. No significant difference between toxic doses of lidocaine and articaine was noted. Stress raised the seizure threshold dose for both drugs and significantly (P < .01) increased arterial PaO₂ from 94.0 ± 1.90 mm Hg to 113.0 ± 2.20 mm Hg, and reduced PaCO₂ from 36.0 ± 0.77 mm Hg to 27.0 ± 0.98 mm Hg. In conclusion, reduction in PaCO₂ and/or increase in PaO₂ raised the seizure threshold of lidocaine and articaine. This study also confirmed that lidocaine and articaine have equipotent central nervous system toxicity.

  17. Effect of PaCO2 and PaO2 on Lidocaine and Articaine Toxicity

    PubMed Central

    Barcelos, K.C; Furtado, D.P; Ramacciato, J.C; Cabral, A.M; Haas, D.A

    2010-01-01

    Alterations in arterial PaCO2 can influence local anesthetic toxicity. The objective of this study was to evaluate the effect of stress-induced changes in PaCO2 and PaO2 on the seizure threshold of lidocaine and articaine. Lidocaine (2% with 1 ∶ 100,000 epinephrine) or articaine (4% with 1 ∶ 100,000 epinephrine) was administered intravenously under rest or stress conditions to 36 rats separated into 4 groups. Propranolol and prazosin were administered preoperatively to minimize cardiovascular effects of epinephrine. Mean arterial pressure (MAP), heart rate (HR), and arterial pH, PaCO2, and PaO2 were measured. Results showed no differences in MAP, HR, or pH. Stress significantly increased the latency period for the first tonic-clonic seizure induced by a toxic dose of both lidocaine and articaine (P < .05). Seizures were brought on more rapidly by articaine. No significant difference between toxic doses of lidocaine and articaine was noted. Stress raised the seizure threshold dose for both drugs and significantly (P < .01) increased arterial PaO2 from 94.0 ± 1.90 mm Hg to 113.0 ± 2.20 mm Hg, and reduced PaCO2 from 36.0 ± 0.77 mm Hg to 27.0 ± 0.98 mm Hg. In conclusion, reduction in PaCO2 and/or increase in PaO2 raised the seizure threshold of lidocaine and articaine. This study also confirmed that lidocaine and articaine have equipotent central nervous system toxicity. PMID:20843225

  18. Digital Necrosis After Lidocaine and Epinephrine Injection in the Flexor Tendon Sheath Without Phentolamine Rescue.

    PubMed

    Zhang, Jacques X; Gray, Jason; Lalonde, Donald H; Carr, Nicholas

    2017-02-01

    The literature generally supports the safety of epinephrine injection in the digits, but recent case reports describe ischemic adverse events associated with the use of lidocaine and epinephrine in which phentolamine rescue was not performed. We present a case of finger necrosis and subsequent amputation in a patient after 1% lidocaine with 1:100,000 epinephrine was injected in the fat and flexor sheaths in the palm for a 3-finger trigger release. Phentolamine rescue was not performed. All surgeons who use epinephrine in the finger should be prepared to reverse vasoconstriction with phentolamine rescue if there is persistently inadequate perfusion of the fingertip.

  19. Modification of the peripheral nerve disturbance in ciguatera poisoning in rats with lidocaine.

    PubMed

    Cameron, J; Flowers, A E; Capra, M F

    1993-07-01

    Electrophysiological studies were performed on the ventral tail nerve of adult rats following intraperitoneal injection of a crude extract of ciguatoxin from known toxic fish flesh. Ciguatoxin induced significant slowing of both mixed and motor nerve conduction velocities and also significant reductions in both motor and mixed nerve amplitudes. Both absolute and supernormal periods were significantly prolonged together with an increase in the magnitude of the supernormal response. These electrophysiological disturbances were modified or blocked by intraperitoneal lidocaine. These findings suggest that lidocaine may have a potential therapeutic application in the treatment of the neurological disturbance in acute ciguatera poisoning in humans.

  20. Impact of tetrodotoxin application and lidocaine supplementation on equine jejunal smooth muscle contractility and activity of the enteric nervous system in vitro.

    PubMed

    Tappenbeck, K; Hoppe, S; Geburek, F; Feige, K; Huber, K

    2014-09-01

    By blocking the enteric nervous system (ENS) using tetrodotoxin (TTX), previous studies have documented the contractility-enhancing (CE) effects of lidocaine in equine intestinal smooth muscle (SM) at the level of SM cells and/or interstitial cells of Cajal (ICC). The present study examined the impact of ENS deactivation on CE lidocaine effects, and investigated the effects of lidocaine on ENS activity. TTX application did not affect the CE effects of lidocaine, indicating that these were not mediated by TTX-sensitive sodium channels. Application of TTX or ≥100 mg/L lidocaine reduced ENS activity. Although such concentrations of lidocaine exceed therapeutic blood concentrations, tissue concentrations may be higher with the potential to reduce ENS activity and impair intestinal motility in vivo. Improved understanding of underlying mechanisms is relevant for therapeutic use of lidocaine in horses with postoperative ileus.

  1. Effectiveness of pre-peritoneal continuous wound infusion with lidocaine for pain control following ovariohysterectomy in dogs.

    PubMed

    Morgaz, Juan; Muñoz-Rascón, Pilar; Serrano-Rodríguez, Juan Manuel; Navarrete, Rocío; Domínguez, Juan Manuel; Fernández-Sarmiento, José Andrés; Gómez-Villamandos, Rafael J; Serrano, Juan Manuel; Granados, María Del Mar

    2014-12-01

    This study compared the post-operative analgesic efficacy of continuous lidocaine administration with that of intramuscular (IM) methadone in dogs undergoing ovariohysterectomy. Thirty-eight dogs were divided randomly into two groups. Following surgery, the lidocaine group (L) received a continuous lidocaine infusion (2 mg/kg/h) through a wound catheter inserted in the pre-peritoneal space; the control group (C) received methadone (0.2 mg/kg IM). A dynamic and interactive visual analogue scale (DIVAS), the Scale-Form Glasgow Composite Measure Scale (CMPS-SF), mechanical wound thresholds, heart rate, respiratory rate and blood pressure were assessed pre-operatively and 2, 4, 6, 18, and 24 h after surgery. The presence of the wound catheter prevented the evaluator from remaining blinded to group allocations. Plasma lidocaine and cortisol levels were measured 2, 6, 18, and 24 h after surgery. There were no intergroup differences in any pain assessment scale scores at any time point. Stable intravenous lidocaine levels were observed. Four animals in the control group but none in the lidocaine group required rescue analgesia. There were no differences in complication rates between groups. Continuous locoregional lidocaine delivered via a wound catheter between the parietal peritoneum and abdominal muscle offers effective analgesia in dogs during ovariohysterectomy and appears to be a promising analgesic option in veterinary surgery.

  2. Pharmacokinetics of Lidocaine Hydrochloride Administered with or without Adrenaline for the Paravertebral Brachial Plexus Block in Dogs

    PubMed Central

    Troncy, Eric; Guillot, Martin; Varin, France

    2017-01-01

    Adrenaline is known to prolong the duration of local anesthesia but its effects on the pharmacokinetic processes of local anesthetic drugs are not fully understood. Our objective was to develop a compartmental model for quantification of adrenaline’s impact on the pharmacokinetics of perineurally-injected lidocaine in the dog. Dogs were subjected to paravertebral brachial plexus block using lidocaine alone or adrenalinated lidocaine. Data was collected through a prospective, randomised, blinded crossover protocol performed over three periods. Blood samples were collected during 180 minutes following block execution. Compartmental pharmacokinetic models were developed and their goodness-of-fit were compared. The lowering effects of adrenaline on the absorption of lidocaine were statistically determined with one-sided tests. A one-compartment disposition model with two successive zero-order absorption processes best fitted our experimental data. Adrenaline decreased the peak plasma lidocaine concentration by approximately 60% (P < 0.001), decreased this local anesthetic’s fast and slow zero-order absorption rates respectively by 50% and 90% (P = 0.046, and P < 0.001), which respective durations were prolonged by 90% and 1300% (P < 0.020 and P < 0.001). Lidocaine demonstrated a previously unreported atypical absorption profile following its paravertebral injection in dogs. Adrenaline decreased the absorption rate of lidocaine and prolonged the duration of its absorption. PMID:28068408

  3. Comparison of topical tetracaine, adrenaline, and cocaine anesthesia with lidocaine infiltration for repair of lacerations in children.

    PubMed

    Hegenbarth, M A; Altieri, M F; Hawk, W H; Greene, A; Ochsenschlager, D W; O'Donnell, R

    1990-01-01

    Local anesthetic infiltration is painful and frightening for children. We prospectively compared a topical alternative, TAC solution (tetracaine 0.5%, adrenaline 1:2,000, cocaine 11.8%), with 1% lidocaine infiltration for use in laceration repair in 467 children. Adequate anesthesia of facial and scalp wounds was achieved for 81% of TAC-treated wounds versus 87% of lidocaine-treated wounds (P = .005). TAC was less effective on extremity wounds; 43% had effective anesthesia compared with 89% of lidocaine-treated extremity wounds (P less than .0001). No systemic toxicity was observed. The incidence of wound infection was 2.2% for both TAC and lidocaine. Wound dehiscence occurred in seven TAC- and two lidocaine-treated facial or scalp wounds (4.5% vs 1.8%, NS) and in five TAC- and four lidocaine-treated extremity wounds (20% vs 17.4%, NS). The unusually high rate of dehiscence was due partially to recurrent trauma or coincident infection. TAC was well accepted by patients and parents. We encourage the careful use of TAC as a less painful alternative to lidocaine infiltration for selected scalp and facial lacerations in children.

  4. Effectiveness of lidocaine infusion for status epilepticus in childhood: a retrospective multi-institutional study in Japan.

    PubMed

    Hattori, Hideji; Yamano, Tsunekazu; Hayashi, Kitami; Osawa, Makiko; Kondo, Kyoko; Aihara, Masao; Haginoya, Kazuhiro; Hamano, Shinichiro; Izumi, Tatsurou; Kaneko, Kenichiro; Kato, Ikuko; Matsukura, Makoto; Minagawa, Kimio; Miura, Toshio; Ohtsuka, Yoko; Sugai, Kenji; Takahashi, Takao; Yamanouchi, Hideo; Yamamoto, Hitoshi; Yoshikawa, Hideto

    2008-09-01

    We evaluated the usefulness of intravenous lidocaine therapy for managing of status epilepticus (SE) during childhood in a retrospective multi-institutional study. Questionnaires were sent to 28 hospitals concerning patients admitted for SE who were managed with lidocaine, assessing patient characteristics, treatment protocols and efficacy. In 279 treated patients, 261 SE occurrences at ages between 1 month and 15 years were analyzed. SE was classified as showing continuous, clustered, or frequently repeated seizures. Considering efficacy and side effects in combination, the usefulness of lidocaine was classified into six categories: extremely useful, useful, slightly useful, not useful, associated with deterioration, or unevaluated. In 148 SE cases (56.7%), lidocaine was rated as useful or extremely useful. Multivariate analysis indicated lidocaine was to be useful in SE with clustered and frequently repeated seizures, and SE attributable to certain acute illnesses, such as convulsions with mild gastroenteritis. Efficacy was poor when SE caused by central nervous system (CNS) infectious disease. Standard doses (approximately 2mg/kg as a bolus, 2mg/kg/h as maintenance) produced better outcomes than lower or higher doses. Poor responders to the initial bolus injection of lidocaine were less likely to respond to subsequent continuous infusion than good initial responders. We recommend lidocaine for use in SE with clustered or frequently repeated seizures, and in SE associated with benign infantile convulsion and convulsions with mild gastroenteritis. Lidocaine should be initiated with a bolus of 2mg/kg. If SE is arrested by the bolus, continuous maintenance infusion should follow; treatment should proceed to different measures when SE shows a poor response to the initial bolus of lidocaine.

  5. A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity.

    PubMed

    Sheets, Patrick L; Jackson, James O; Waxman, Stephen G; Dib-Hajj, Sulayman D; Cummins, Theodore R

    2007-06-15

    Mutations in the TTX-sensitive voltage-gated sodium channel subtype Nav1.7 have been implicated in the painful inherited neuropathy, hereditary erythromelalgia. Hereditary erythromelalgia can be difficult to treat and, although sodium channels are targeted by local anaesthetics such as lidocaine (lignocaine), some patients do not respond to treatment with local anaesthetics. This study examined electrophysiological differences in Nav1.7 caused by a hereditary erythromelalgia mutation (N395K) that lies within the local anaesthetic binding site of the channel. The N395K mutation produced a hyperpolarized voltage dependence of activation, slower kinetics of deactivation, and impaired steady-state slow inactivation. Computer simulations indicate that the shift in activation is the major determinant of the hyperexcitability induced by erythromelalgia mutations in sensory neurons, but that changes in slow inactivation can modulate the overall impact on excitability. This study also investigated lidocaine inhibition of the Nav1.7-N395K channel. We show that the N395K mutation attenuates the inhibitory effects of lidocaine on both resting and inactivated Nav1.7. The IC50 for lidocaine was estimated at 500 microM for inactivated wild-type Nav1.7 and 2.8 mM for inactivated Nav1.7-N395K. The N395K mutation also significantly reduced use-dependent inhibition of lidocaine on Nav1.7 current. In contrast, a different hereditary erythromelalgia mutation (F216S), not located in the local anaesthetic binding site, had no effect on lidocaine inhibition of Nav1.7 current. Our observation of reduced lidocaine inhibition on Nav1.7-N395K shows that the residue N395 is critical for lidocaine binding to Nav1.7 and suggests that the response of individuals with hereditary erythromelalgia to lidocaine treatment may be determined, at least in part, by their specific genotype.

  6. Anesthetic efficacy of a combination of hyaluronidase and lidocaine with epinephrine in inferior alveolar nerve blocks.

    PubMed Central

    Ridenour, S.; Reader, A.; Beck, M.; Weaver, J.

    2001-01-01

    The purpose of this prospective, randomized, double-blind study was to determine the anesthetic efficacy of a buffered lidocaine with epinephrine solution compared to a combination buffered lidocaine with epinephrine plus hyaluronidase solution in inferior alveolar nerve blocks. Thirty subjects randomly received an inferior alveolar nerve block using 1 of the 2 solutions at 2 separate appointments using a repeated-measures design. Mandibular anterior and posterior teeth were blindly pulp tested at 4-minute cycles for 60 minutes postinjection. No response from the subject to the maximum output (80 reading) of the pulp tester was used as the criterion for pulpal anesthesia. Anesthesia was considered successful when 2 consecutive readings of 80 were obtained. A postoperative survey was used to measure pain and trismus. The results demonstrated 100% of the subjects had profound lip numbness with both solutions for inferior alveolar nerve blocks. The anesthetic success rates for individual teeth ranged from 20 to 80%. There were no significant differences (P > .05) between the 2 solutions. However, the combination lidocaine/hyaluronidase solution resulted in a significant increase in postoperative pain and trismus. It was concluded that adding hyaluronidase to a buffered lidocaine solution with epinephrine did not statistically increase the incidence of pulpal anesthesia in inferior alveolar nerve blocks and, because of its potential tissue damaging effect, it should not be added to local anesthetic solutions for inferior alveolar nerve blocks. PMID:11495405

  7. Protective effect of lidocaine during regional myocardial ischemia: an altered pathophysiologic response assessed by NADH fluorescence

    SciTech Connect

    Baron, D.W.; Walls, J.T.; Anderson, R.E.; Harrison, C.E. Jr.

    1982-07-01

    Studies were undertaken to determine the effects of lidocaine on ischemic myocardium, which was induced by coronary artery constriction in open-chested dogs. A real-time epicardial fluorescent technique to detect in vivo-reduced nicotinamide adenine dinucleotide (NADH) during 60 seconds of ischemia was used. Blood flow of ischemic myocardium was measured by using radioactive microspheres of 9 +/- 1 micrometers (mean +/- SE) and was compared with that of normal myocardium, shown by injection of alpha-zurine blue dye. Lidocaine effectively reduced peak NADH fluorescence by 18.6%, from 93.9 +/- 7.2 to 76.4 +/-4.1 mV (p less than 0.005). Lidocaine delayed the onset of fluorescence (2.2 +/- 0.2 versus 1.3 +/- 0.1 s p less than 0.002) and facilitated the recovery from ischemia (38.4 +/- 2.9 versus 54.8 +/- 2.9 s p less than 0.001). Increase in NADH concentration during ischemia correlated (r.0.76, p less than 0.006) with ischemic fluorescence. These findings were independent of altered hemodynamics or change in myocardial blood flow. Results indicate that lidocaine provides myocardial cellular protection during transient ischemia; there is an altered NADH fluorescent response to coronary artery occlusion.

  8. A fatal accidental subarachnoid injection of lidocaine and levobupivacaine during a lumbar paravertebral block.

    PubMed

    Busardò, Francesco Paolo; Tritapepe, Luigi; Montana, Angelo; Indorato, Francesca; Zaami, Simona; Romano, Guido

    2015-11-01

    Paravertebral block (PVB) is the technique of injecting a local anesthetic solution alongside the vertebral column, close to where the spinal nerves emerge, resulting in unilateral somatic and sympathetic nerve blockade. Here is reported a fatal case involving a 60-year-old woman with spondylitis arthropathy, who developed cardiac and respiratory arrest 40min after receiving an accidental subarachnoid injection (L5-S1 bilaterally) of depomedrol lidocaine and levobupivacaine. A complete autopsy including histological and toxicological analyses was performed in order to establish the cause of death. Liquid/liquid extraction (LLE) and GC-MS analysis were performed according to a previously published method. Lidocaine and bupivacaine were detected both in blood, at concentrations of 14.8mg/L and 13.3mg/L respectively, and in cerebrospinal fluid (CSF) at concentrations of 287.1mg/L and 464.2mg/L respectively. Both lidocaine and bupivacaine were also detected in the urine. The toxicological findings along with the autopsy allowed us to establish that the accidental subarachnoid injection of lidocaine and levobupivacaine had led to a progressive hypotension and normovolaemic shock caused by a severe ganglionic block, determining the patient's death.

  9. Regional lidocaine anesthesia without exsanguination for outpatient management of upper extremity fractures.

    PubMed Central

    Brown, G. A.; Hayes, W. M.; Cornwal, R.

    1995-01-01

    The use of small dose intravenous lidocaine without exsanguination for upper extremity fractures in children and adults is described. A twenty-plus year experience with this technique in the outpatient setting has shown it to be effective and safe. Attention to detail is essential and inadvertent tourniquet release must be avoided. Images Figure 1 PMID:7634037

  10. Test of a model of antiarrhythmic drug action. Effects of quinidine and lidocaine on myocardial conduction.

    PubMed

    Hondeghem, L; Katzung, B G

    1980-06-01

    The effects of quinidine and lidocaine on the maximum upstroke velocity (Vmax) of the ventricular myocardial action potential were compared with the effects predicted by a model over a wide range of driving rates, rhythm disturbances and holding potentials. These rate-, rhythm- and voltage-dependent effects were accurately predicted by the proposed model. The model was also able to predict several previously undocumented properties of the drugs: 1) If lidocaine decreases Vmax of a pulse train, the steady state is reached within a few action potentials. 2) The poststimulation recovery of Vmax in the presence of lidocaine or quinidine can occur in a multiexponential fashion, if the membrane potential is kept at the potential where both the fast (operating mainly at more negative membrane potentials) and the slow (operating at more positive potentials) recovery processes are operative. 3) Hyperpolarization markedly attenuates the rate-dependent drug effects. 4) Combinations of lidocaine and quinidine have a superadditive effect on the Vmax of early extrasystoles.

  11. Decreasing Effect of Lidocaine·HCl on the Thickness of the Neuronal and Model Membrane

    PubMed Central

    Park, Sung-Min; Park, Jong-Sun; Kim, Jae-Han; Baek, Jin-Hyun; Yoon, Tae-Gyun; Lee, Do-Keun; Ryu, Won-Hyang; Chung, In-Kyo; Sohn, Uy Dong

    2013-01-01

    This study examined the mechanism of action of a local anesthetic, lidocaine·HCl. Energy transfer between the surface fluorescent probe, 1-anilinonaphthalene-8-sulfonic acid, and the hydrophobic fluorescent probe, 1,3-di(1-pyrenyl) propane, was used to determine the effect of lidocaine·HCl on the thickness (D) of the synaptosomal plasma membrane vesicles (SPMV) isolated from the bovine cerebral cortex, and liposomes of the total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. The thickness (D) of the intact SPMV, SPMVTL and SPMVPL were 1.044±0.008, 0.914±0.005 and 0.890±0.003 (arbitrary units, n=5) at 37℃ (pH 7.4), respectively. Lidocaine·HCl decreased the thickness of the neuronal and model membrane lipid bilayers in a dose-dependent manner with a significant decrease in the thickness, even at 0.1 mM. The decreasing effect of lidocaine·HCl on the membrane thickness might be responsible for some, but not all of its anesthetic action. PMID:23946683

  12. Tolperisone: evaluation of the lidocaine-like activity by molecular modeling.

    PubMed

    Fels, G

    1996-04-01

    Tolperisone (1), a muscle relaxant with lidocaine-like activity, was compared to lidocaine (2) by molecular modeling methods. Conformational search analysis has been employed to find the global minima of these compounds along with numerous low energy conformations from which specific conformers were extracted that show good superimposition of the structural features important for protein binding. Two additional compounds, mepi- (3) and bupivacaine (4), were included in the analysis to validate the method as these ligands show very close structural and pharmacological relationship to lidocaine (2) and are assumed to bind to an identical site. As a result we find conformers of all four ligands that have exactly the same position and orientation of the potential sites for hydrogen bonding with the rest of the molecule showing close comparison of the three-dimensional geometry. Semiempirical calculations furthermore reveal good agreement of the electrostatic potentials of these conformations indicating similar interactions with a receptor. We conclude that tolperisone (1) and lidocaine (2) despite their chemical divergence can still attach to identical protein binding sites.

  13. Efficacy of Intravenous Lidocaine During Endoscopic Submucosal Dissection for Gastric Neoplasm: A Randomized, Double-Blind, Controlled Study.

    PubMed

    Kim, Ji Eun; Choi, Jong Bum; Koo, Bon-Nyeo; Jeong, Hae Won; Lee, Byung Ho; Kim, So Yeon

    2016-05-01

    Endoscopic submucosal dissection (ESD) is an advanced therapy for early gastric neoplasm and requires sedation with adequate analgesia. Lidocaine is a short-acting local anesthetic, and intravenous lidocaine has been shown to have analgesic efficacy in surgical settings. The aim of this study was to assess the effects of intravenous lidocaine on analgesic and sedative requirements for ESD and pain after ESD.Sixty-six patients scheduled for ESD randomly received either intravenous lidocaine as a bolus of 1.5 mg/kg before sedation, followed by continuous infusion at a rate of 2 mg/kg/h during sedation (lidocaine group; n = 33) or the same bolus and infusion volumes of normal saline (control group; n = 33). Sedation was achieved with propofol and fentanyl. The primary outcome was fentanyl requirement during ESD. We recorded hemodynamics and any events during ESD and evaluated post-ESD epigastric and throat pain.Fentanyl requirement during ESD reduced by 24% in the lidocaine group compared with the control group (105 ± 28 vs. 138 ± 37 μg, mean ± SD; P < 0.001). The lidocaine group reached sedation faster [40 (20-100) vs. 55 (30-120) s, median (range); P = 0.001], and incidence of patient movement during ESD decreased in the lidocaine group (3% vs. 26%, P = 0.026). Numerical rating scale for epigastric pain was significantly lower at 6 hours after ESD [2 (0-6) vs. 3 (0-8), median (range); P = 0.023] and incidence of throat pain was significantly lower in the lidocaine group (27% vs. 65%, P = 0.003). No adverse events associated with lidocaine were discovered.Administration of intravenous lidocaine reduced fentanyl requirement and decreased patient movement during ESD. Moreover, it alleviated epigastric and throat pain after ESD. Thus, we conclude that the use of intravenous adjuvant lidocaine is a new and safe sedative method during ESD.

  14. Assessment of membrane protection by /sup 31/P-NMR effects of lidocaine on calcium-paradox in myocardium

    SciTech Connect

    Sakai, Hirosumi; Yoshiyama, Minoru; Teragaki, Masakazu; Takeuchi, Kazuhide; Takeda, Takeda; Ikata, Mari; Ishikawa, Makoto; Miura, Iwao

    1989-01-01

    In studying calcium paradox, perfused rat hearts were used to investigate the myocardial protective effects of lidocaine. Intracellular contents of phosphates were measured using the /sup 31/P-NMR method. In hearts reexposed to calcium, following 3 minute calcium-free perfusion, a rapid contracture occurred, followed by rapid and complete disappearance of intracellular phosphates with no resumption of cardiac function. In hearts where lidocaine was administered from the onset of the calcium-free perfusion until 2 minutes following the onset of reexposure to calcium, both intracellular phosphates and cardiac contractility were maintained. Therefore, it can be said that cell membranes were protected by lidocaine.

  15. The effect of lidocaine, bupivacaine and ropivacaine in nasal packs on pain and hemorrhage after septoplasty.

    PubMed

    Karaman, Emin; Gungor, Gurcan; Alimoglu, Yalcin; Kilic, Erkan; Tarakci, Eylem; Bozkurt, Pervin; Enver, Ozgun

    2011-05-01

    We aimed to investigate the effects of local anesthetics soaked in Merocel nasal packs on hemorrhage and pain after septoplasty. The methodology includes a prospective double-blind study that was conducted in patients undergoing septoplasty because of nasal septal deviation. The study included 143 patients. The patients were divided into four groups. Each group received 1% lidocaine + 0.000625% adrenalin, 0.375% ropivacaine, 0.25% bupivacaine as study groups or 0.9% sodium chloride as a control group in their Merocel packs postoperatively. The local anesthetics or sodium chloride were reapplied at the eighth postoperative hour. Each patient was given a questionnaire where verbal analog score and amount of postoperative hemorrhage was noted. The statistical analysis was performed using two sided t test on each patient group at each time point. The results included the patients in the control group needing rescue drug most often. There was no statistically significant difference between bupivacaine and lidocaine plus adrenalin in the patients who requested rescue drug. The patients in the ropivacaine group requested rescue drug more frequently than the bupivacaine and lidocaine plus adrenalin groups. Bupivacaine group had significantly better pain scores versus control group at all intervals except for the first postoperative hour.The bupivacaine group had better pain scores versus ropivacaine and lidocaine plus adrenalin groups in the 4th, 8th and the 24th hours. The bupivacaine group had better pain scores versus lidocaine plus adrenalin in the 12th, 16th and the 20th hours. The ropivacaine group had significantly better pain scores versus control group in the 8th, 12th, 16th, 20th and 24th postoperative hours. The ropivacaine group scored better than lidocaine plus adrenalin group just in the 16th hour. The lidocaine plus adrenalin group had significantly better pain scores versus control group in 4th and 12th hours. There was no statistically significant

  16. A New Anaesthetic Protocol for Adult Zebrafish (Danio rerio): Propofol Combined with Lidocaine

    PubMed Central

    Valentim, Ana M.; Félix, Luís M.; Carvalho, Leonor; Diniz, Enoque; Antunes, Luís M.

    2016-01-01

    Background The increasing use of zebrafish model has not been accompanied by the evolution of proper anaesthesia for this species in research. The most used anaesthetic in fishes, MS222, may induce aversion, reduction of heart rate, and consequently high mortality, especially during long exposures. Therefore, we aim to explore new anaesthetic protocols to be used in zebrafish by studying the quality of anaesthesia and recovery induced by different concentrations of propofol alone and in combination with different concentrations of lidocaine. Material and Methods In experiment A, eighty-three AB zebrafish were randomly assigned to 7 different groups: control, 2.5 (2.5P), 5 (5P) or 7.5 μg/ml (7.5P) of propofol; and 2.5 μg/ml of propofol combined with 50, (P/50L), 100 (P/100L) or 150 μg/ml (P/150L) of lidocaine. Zebrafish were placed in an anaesthetic water bath and time to lose the equilibrium, reflex to touch, reflex to a tail pinch, and respiratory rate were measured. Time to gain equilibrium was also assessed in a clean tank. Five and 24 hours after anaesthesia recovery, zebrafish were evaluated concerning activity and reactivity. Afterwards, in a second phase of experiments (experiment B), the best protocol of the experiment A was compared with a new group of 8 fishes treated with 100 mg/L of MS222 (100M). Results In experiment A, only different concentrations of propofol/lidocaine combination induced full anaesthesia in all animals. Thus only these groups were compared with a standard dose of MS222 in experiment B. Propofol/lidocaine induced a quicker loss of equilibrium, and loss of response to light and painful stimuli compared with MS222. However zebrafish treated with MS222 recovered quickly than the ones treated with propofol/lidocaine. Conclusion In conclusion, propofol/lidocaine combination and MS222 have advantages in different situations. MS222 is ideal for minor procedures when a quick recovery is important, while propofol/lidocaine is best to

  17. Isoform-specific lidocaine block of sodium channels explained by differences in gating.

    PubMed

    Nuss, H B; Kambouris, N G; Marbán, E; Tomaselli, G F; Balser, J R

    2000-01-01

    When depolarized from typical resting membrane potentials (V(rest) approximately -90 mV), cardiac sodium (Na) currents are more sensitive to local anesthetics than brain or skeletal muscle Na currents. When expressed in Xenopus oocytes, lidocaine block of hH1 (human cardiac) Na current greatly exceeded that of mu1 (rat skeletal muscle) at membrane potentials near V(rest), whereas hyperpolarization to -140 mV equalized block of the two isoforms. Because the isoform-specific tonic block roughly parallels the drug-free voltage dependence of channel availability, isoform differences in the voltage dependence of fast inactivation could underlie the differences in block. However, after a brief (50 ms) depolarizing pulse, recovery from lidocaine block is similar for the two isoforms despite marked kinetic differences in drug-free recovery, suggesting that differences in fast inactivation cannot entirely explain the isoform difference in lidocaine action. Given the strong coupling between fast inactivation and other gating processes linked to depolarization (activation, slow inactivation), we considered the possibility that isoform differences in lidocaine block are explained by differences in these other gating processes. In whole-cell recordings from HEK-293 cells, the voltage dependence of hH1 current activation was approximately 20 mV more negative than that of mu1. Because activation and closed-state inactivation are positively coupled, these differences in activation were sufficient to shift hH1 availability to more negative membrane potentials. A mutant channel with enhanced closed-state inactivation gating (mu1-R1441C) exhibited increased lidocaine sensitivity, emphasizing the importance of closed-state inactivation in lidocaine action. Moreover, when the depolarization was prolonged to 1 s, recovery from a "slow" inactivated state with intermediate kinetics (I(M)) was fourfold longer in hH1 than in mu1, and recovery from lidocaine block in hH1 was similarly

  18. Effects of lidocaine and droxicainide on myocardial necrosis: a comparative study

    SciTech Connect

    Faria, D.B.; Cheung, W.M.; Ribeiro, L.G.; Maroko, P.R.

    1983-06-01

    Lidocaine has been shown to protect ischemic myocardium, but the degree of its effectiveness is not yet well established. Therefore, in this study, the effects of this drug on ultimate infarct size were examined quantitatively. Another member of the same class of drugs, droxicainide (ALS1249), DL-N-(2-hydroxyethyl)-pipecolinyl-2,6-dimethylanilide hydrochloride, is a new antiarrhythmic agent that has shown a good therapeutic index in the initial experimental studies. Accordingly, the effects of this drug on ultimate infarct size were examined and compared with those of lidocaine. Coronary artery occlusion was performed on 29 dogs. One minute later, technetium-99m labeled microspheres were injected into the left atrium for assessment of the hypoperfused zone (the zone at risk of infarction). Fifteen minutes after occlusion, the dogs were randomized into three groups: 9 dogs served as a control group, 10 were given lidocaine and 10 were given the same dosage of droxicainide. Six hours after occlusion, the dogs were sacrificed and the hearts cut into 3 mm thick slices and incubated in triphenyltetrazolium chloride to delineate the area of myocardial damage. Autoradiography of the same slices provided images of the areas of myocardial hypoperfusion. Thereafter, in each dog, the percent of hypoperfused area that evolved to necrosis was calculated. In control dogs, it was 85.6 +/- 2.0%; in lidocaine-treated dogs, 68.1 +/- 4.1% (p less than 0.01), a reduction of 20%; and in droxicainide-treated dogs, 50.1 +/- 5.3%, a reduction of 41% (p less than 0.001 versus control and p less than 0.005 versus lidocaine).

  19. Comparison of indomethacin suppository and lidocaine cream on post-episiotomy pain: A randomized trial

    PubMed Central

    Delaram, Masoumeh; Dadkhah, Narges-Khaton; Jafarzadeh, Loabat

    2015-01-01

    Background: One of the most important problems after episiotomy is perineal pain which is more severe on the first day of postpartum period. The aim of this study was to compare the analgesic effects of indomethacin suppository and lidocaine cream in the management of post-episiotomy pain. Materials and Methods: In a randomized, controlled trial, 60 primiparous women who had mediolateral episiotomy received 50 mg indomethacin suppository (n = 30) or 2% lidocaine cream (n = 30) in the postpartum period in Hajar Hospital in Shahrekord (Iran). The mean severity of post-episiotomy pain was assessed with the first complaint and at 6, 12, and 24 h after the delivery, and compared in the two groups. The visual analog scale (VAS) was used for pain recording and data were analyzed with independent-samples t-test, χ2, and Fisher's exact tests, and significance was defined as P < 0.05. Results: With the first complaint of pain, the mean intensity of pain was 4.9 (1.9) in the indomethacin group and 4.9 (1.8) in the lidocaine group, and the difference was not significant (P = 0.25). Six hours after birth, it was 3.3 (1.3) in the indomethacin group and 3.2 (1.9) in the lidocaine group, and there was not a significant difference between the two groups (P = 0.90). No significant difference was found between the two groups at 12 h after birth [2.3 (1.7) vs 2.5 (1.7); P = 0.59]. Also, the difference was not significant at 24 h after birth [1.5 (1.3) vs 1.8 (1.3); P = 0.31]. Conclusions: It was concluded from the study that indomethacin suppository and lidocaine cream have similar efficacy on episiotomy pain relief on the first day of postpartum period. PMID:26257799

  20. Case studies illustrating the management of trigeminal neuropathic pain using topical 5% lidocaine plasters

    PubMed Central

    Yilmaz, Zehra; Renton, Tara

    2013-01-01

    Chronic trigeminal pain, with its severe related functional problems, is difficult to treat. Treatment is often empirically based on medications used for other chronic pain conditions. Systemic sodium channel and calcium channel blocking agents may cause a multitude of complications that are often poorly tolerated by the patient. Aim: The aim of this case report was to assess the efficacy of topical 5% lidocaine plasters in reducing pain and reducing adjuvant medication in patients with orofacial neuropathic pain. Method: Fourteen patients with chronic orofacial pain conditions referred to the oral surgery department were instructed to wear 5% lidocaine plasters for 12 hours each day over the painful area. The conditions included post-surgical neuropathy (n = 10), multiple sclerosis-related pain (n = 1), persistent idiopathic facial pain (n = 1), Ramsay Hunt syndrome (post-herpetic neuralgia, n = 1) and trigeminal neuralgia (n = 1). Data were collected on patient demographics, pain levels and medication. Results: Pain levels improved in 12 out of 14 patients. Nine patients had a reduction in adjuvant medication, two of whom completely stopped adjuvant treatment. Conclusion: This case series demonstrates that of the use of 5% lidocaine plasters may play a useful role in the management of chronic trigeminal pain. A suggested novel approach for the management of orofacial pain, for clinicians, is presented. Summary points Management of chronic orofacial pain continues to be a major challenge to the clinician. Patients are often placed on a multitude of medications in an attempt to alleviate pain without success. Topical 5% lidocaine plasters, currently used for the management of post-herpetic neuralgia, offer the option of locally targeting trigeminal pain without the multiple side-effects of systemic medication. This case series demonstrates that lidocaine plasters decrease verbal pain scores in extraoral, trigeminal and neuropathic pain, and reduce the use of other

  1. Effects of Lidocaine, Dexmedetomidine or Their Combination on the Minimum Alveolar Concentration of Sevoflurane in Dogs

    PubMed Central

    MORAN-MUÑOZ, Rafael; IBANCOVICHI, J. A.; Gutierrez-BLANCO, Eduardo; ACEVEDO-ARCIQUE, Carlos M.; Victoria MORA, J. Mauro; TENDILLO, Francisco J.; SANTOS-GONZALEZ, Martin; YAMASHITA, Kazuto

    2014-01-01

    ABSTRACT The aim of this study was to determine the effects of lidocaine (LIDO) and dexmedetomidine (DEX) or their combination (LIDO–DEX), administered by constant-rate infusion (CRI), on the minimum alveolar concentration (MAC) of sevoflurane in dogs. Seven healthy mongrel dogs were used with a 2-week washout interval between treatments in this study. Anesthesia was induced with propofol and maintained with sevoflurane in oxygen, and MAC of sevoflurane was determined after 90 min equilibration period in the dogs (SEV-MACBASAL). Then, sevoflurane MAC was determined again in the dogs after 45 min equilibration period of one of the following treatments: an intravenous loading dose of lidocaine 2 mg/kg followed by 6 mg/kg/hr CRI (SEV-MACLIDO); an intravenous loading dose of dexmedetomidine 2 µg/kg followed by 2 µg/kg/hr CRI (SEV-MACDEX); or their combination (SEV-MACLIDO-DEX). These SEV-MACs were determined in duplicate. Data were analyzed using ANOVA and post hoc Tuckey test when appropriate. The SEV-MACBASAL was 1.82 ± 0.06%, SEV-MACLIDO was 1.38 ± 0.08%, SEV-MACDEX was 1.22 ± 0.10%, and SEV-MACLIDO-DEX was 0.78 ± 0.06%. The CRI administration of lidocaine, dexmedetomidine and their combination produced a significant reduction in the MAC of sevoflurane by 26.1 ± 9.0% (P<0.0001), 43.7 ± 11.8% (P<0.0002) and 54.4 ± 9.8% (P<0.0001), respectively. The MAC reduction was significantly greater after the CRI combination of lidocaine and dexmedetomidine when compared with lidocaine CRI (P<0.0001) or dexmedetomidine CRI treatments (P<0.025). PMID:24572631

  2. Intravenous administration of lidocaine directly acts on spinal dorsal horn and produces analgesic effect: An in vivo patch-clamp analysis

    PubMed Central

    Kurabe, Miyuki; Furue, Hidemasa; Kohno, Tatsuro

    2016-01-01

    Intravenous lidocaine administration produces an analgesic effect in various pain states, such as neuropathic and acute pain, although the underlying mechanisms remains unclear. Here, we hypothesized that intravenous lidocaine acts on spinal cord neurons and induces analgesia in acute pain. We therefore examined the action of intravenous lidocaine in the spinal cord using the in vivo patch-clamp technique. We first investigated the effects of intravenous lidocaine using behavioural measures in rats. We then performed in vivo patch-clamp recording from spinal substantia gelatinosa (SG) neurons. Intravenous lidocaine had a dose-dependent analgesic effect on the withdrawal response to noxious mechanical stimuli. In the electrophysiological experiments, intravenous lidocaine inhibited the excitatory postsynaptic currents (EPSCs) evoked by noxious pinch stimuli. Intravenous lidocaine also decreased the frequency, but did not change the amplitude, of both spontaneous and miniature EPSCs. However, it did not affect inhibitory postsynaptic currents. Furthermore, intravenous lidocaine induced outward currents in SG neurons. Intravenous lidocaine inhibits glutamate release from presynaptic terminals in spinal SG neurons. Concomitantly, it hyperpolarizes postsynaptic neurons by shifting the membrane potential. This decrease in the excitability of spinal dorsal horn neurons may be a possible mechanism for the analgesic action of intravenous lidocaine in acute pain. PMID:27188335

  3. Liquid-liquid miscibility gaps and hydrate formation in drug-water binary systems: pressure-temperature phase diagram of lidocaine and pressure-temperature-composition phase diagram of the lidocaine-water system.

    PubMed

    Ceolin, René; Barrio, Maria; Tamarit, Josep-Lluis; Veglio, Nestor; Perrin, Marc-Antoine; Espeau, Philippe

    2010-06-01

    The pressure-temperature (P-T) melting curve of lidocaine was determined (dP/dT = 3.56 MPa K(-1)), and the lidocaine-water system was investigated as a function of temperature and pressure. The lidocaine-water system exhibits a monotectic equilibrium at 321 K (ordinary pressure) whose temperature increases as the pressure increases until the two liquids become miscible. A hydrate, unstable at ordinary pressure, was shown to form, on increasing the pressure, from about 70 MPa at low temperatures (200-300 K). The thermodynamic conditions of its stability were inferred from the location of the three-phase equilibria involving the hydrate in the lidocaine-water pressure-temperature-mole fraction (P-T-x) diagram.

  4. Comparative effect of lidocaine and bupivacaine on glucose uptake and lactate production in the perfused working rat heart

    SciTech Connect

    Cronau, L.H. Jr.; Merin, R.G.; Aboulish, E.; Steenberg, M.L.; Maljorda, A.

    1986-03-01

    It has been suggested that at equivalent therapeutic concentrations, lidocaine and bupivacaine may have different cardiotoxic potency. In the isolated working rat heart preparation, the effect of a range of lidocaine and bupivacaine concentrations on glucose uptake and lactate production (LP) were observed. Insulin was added, 10 ..mu../L, to Ringer's solution containing /sup 3/H-labeled glucose to measure the glycolytic flux (GF). The effect of the local anesthetics on LP at the indicated concentrations were similar. Lidocaine appears to depress the glycolytic flux from exogenous glucose to a lesser degree. Bupivacaine, 10 mg/L, depresses VO/sub 2/ to a greater degree than does lidocaine, 40 mg/L.

  5. Peribulbar anesthesia for cataract surgery: Effect of lidocaine warming and alkalinization on injection pain, motor and sensory nerve blockade

    PubMed Central

    Jaichandran, Venkatakrishnan; Vijaya, Lingam; George, Ronnie Jacob; InderMohan, Bhanulakshmi

    2010-01-01

    Aim: To compare self-reported pain and efficacy of warmed, alkalinized, and warmed alkalinized lidocaine with plain 2% lidocaine at room temperature for peribulbar anesthesia in cataract surgery. Materials and Methods: Through a prospective, single-blinded, randomized, controlled clinical trial 200 patients were divided into four groups. They received either lidocaine at operating room temperature 18°C, control group (Group C), lidocaine warmed to 37°C (Group W), lidocaine alkalinized to a pH of 7.09 ± 0.10 (Group B) or lidocaine at 37°C alkalinized to a pH of 6.94 ± 0.05 (Group WB). All solutions contained Inj. Hyaluronidase 50 IU/ml. Pain was assessed using a 10-cm visual analog score scale. Time of onset of sensory and motor blockade and time to onset of postoperative pain were recorded by a blinded observer. Results: Mean pain score was significantly lower in Group B and WB compared with Group C (P < 0.001). Onset of analgesia was delayed in Group C compared with Group B (P = 0.021) and WB (P < 0.001). Mean time taken for the onset of complete akinesia and supplementation required for the block was significantly lower in Group B. Time of onset of pain after operation was significantly earlier in Group W compared with Group C (P = 0.036). Conclusion: Alkalinized lidocaine with or without warming produced less pain than lidocaine injected at room temperature. Alkalinization enhances the effect of warming for sensory nerve blockade, but warming does not enhance alkalinization, in fact it reduces the efficacy of alkalinized solution for blocking the motor nerves in the eye. PMID:20195031

  6. Lidocaine controls pain and allows safe wound bed preparation and debridement of digital ulcers in systemic sclerosis: a retrospective study.

    PubMed

    Braschi, Francesca; Bartoli, Francesca; Bruni, Cosimo; Fiori, Ginevra; Fantauzzo, Claudia; Paganelli, Lucia; De Paulis, Amato; Rasero, Laura; Matucci-Cerinic, M

    2017-01-01

    In Systemic Sclerosis (SSc), digital ulcers (DU) are painful, difficult to heal, and frequently infected. To reduce the risk of bacterial infection and to prevent chronicity, it is essential to carefully remove necrotic tissue from DU, with maximum patient comfort. Debridement, although very efficacious, is invasive and causes local pain: lidocaine is a local anesthetic commonly used as to fight pain during debridement procedures. The aim of the study was to evaluate the efficacy of lidocaine 4 % in pain control during debridement procedure of DU in SSc. One hundred eight DU characterized by pain Numeric Rating Scale (NRS) >3/10 before starting the procedure were treated with lidocaine 4 % (lidocaine cloridrate 200 mg in 5 ml of injecting solution). Pain was measured with NRS (0-10) before starting debridement, after 15 min of lidocaine application and at the end of the procedure. In DU, in respect to baseline (mean NRS 6.74 ± 2.96), pain after application of lidocaine 4 % for 15 min was significantly lower (mean NRS 2.83 ± 2.73) (p < 0.001). At the end of the procedure, pain control was still maintained and significantly lower (mean NRS 2.88 ± 2.65) in respect to baseline (p < 0.001). No systemic adverse event due to topical lidocaine were observed. In SSc, topical application of lidocaine 4 % significantly reduces pain, allowing a safe debridement procedure, thus improving the management of DU.

  7. Durability of Benefit From Repeated Intravenous Lidocaine Infusions in Fibromyalgia Patients: A Case Series and Literature Review

    PubMed Central

    Marks, David M.; Newhouse, Amy

    2015-01-01

    Fibromyalgia is a painful disorder with no curative treatments, and available medications typically provide partial relief of pain. Reported here is the effective use of serial intravenous lidocaine infusions for the chronic management of 3 patients with fibromyalgia. The details of the infusion procedure are described, and relevant literature is reviewed. Lidocaine infusions should be considered in fibromyalgia patients who are refractory to other treatments, and a positive response to 1 infusion may justify repeated infusions for chronic management. PMID:26835161

  8. Effect of lidocaine spray in pain management during office-based endometrial sampling: A randomised placebo-controlled trial.

    PubMed

    Aksoy, H; Aksoy, U; Ozyurt, S; Acmaz, G; Babayigit, M A; Yücel, B; Aydin, T

    2016-01-01

    Office-based endometrial sampling is the most frequently performed gynaecological procedure. The procedure is usually associated with pain and discomfort. Several anaesthetic and analgesic techniques (e.g., non-steroidal anti-inflammatory drugs, paracervical block, misoprostol and topical anaesthetics) are used for pain management during endometrial sampling. There is no comprehensive study using lidocaine in spray form; we sought to investigate the analgesic efficacy of 10% lidocaine spray in patients undergoing office-based endometrial biopsy. We conducted a prospective, randomised (lidocaine spray (n = 60) and placebo (n = 60), respectively), double-blind study. The mean pain score during procedure was 3.51 ± 1.51 in the lidocaine spray group and 5.11 ± 1.66 in the placebo group. Lidocaine spray treatment significantly lowered the pain scores compared with placebo (p < 0.001). Lidocaine spray can be accepted as a non-invasive, easy to apply and more comfortable anaesthetic method for office-based endometrial sampling.

  9. Effective Concentration of Lidocaine Plus Fentanyl for Caudal Block in Patients Undergoing Transrectal Ultrasound Guided Prostate Biopsy

    PubMed Central

    Wang, Jinguo; Zhou, Honglan; An, Wei; Gao, Yang

    2016-01-01

    Objective. This study determined the effective concentration (EC) of lidocaine plus 75 μg fentanyl for caudal block in patients undergoing transrectal ultrasound (TRUS) guided prostate biopsy. Methods. Consecutive male patients scheduled for TRUS guided prostate biopsy were enrolled. The mixed solution for caudal block contained lidocaine and 75 μg fentanyl, in total 20 mL. The concentration of lidocaine was determined using the up-and-down method, starting at 0.8% (a step size of 0.1%). A successful caudal block was defined by no pain perception during biopsy. The EC50 of lidocaine for successful caudal block was calculated and side effects were evaluated. Results. A total of 23 patients were recruited. The EC50 of lidocaine for successful caudal block was 0.53%. Conclusions. Lidocaine of 0.53% combined with 75 μg fentanyl resulted in excellent caudal block in 50% of male patients undergoing transrectal ultrasound guided prostate biopsy. PMID:27872761

  10. Use-dependent effects of lidocaine on conduction in canine myocardium: application of the modulated receptor hypothesis in vivo.

    PubMed

    Davis, J; Matsubara, T; Scheinman, M M; Katzung, B; Hondeghem, L H

    1986-07-01

    Lidocaine is a commonly used antiarrhythmic drug that causes use-dependent blockade of sodium channels in vitro and reduces conduction velocity in vitro and in vivo. According to the modulated receptor hypothesis of antiarrhythmic drug action, lidocaine has a low affinity for rested sodium channels but a high affinity for open and inactivated channels. In the present experiments, we characterized use-dependent conduction slowing and recovery from slowing by lidocaine in anesthetized dogs. The His-to-ventricular conduction interval was used as the indicator of conduction velocity. We found that prolongation of conduction time was greater as the stimulation frequency was increased. Moreover, on abruptly changing the stimulation frequency, a new steady-state conduction time was approached in two to three depolarizations. On discontinuation of stimulation, the conduction time of progressively less premature extrastimuli shortened exponentially with a terminal phase time constant of 152 +/- 115 msec. These effects by lidocaine were enhanced during acidosis and enhancement was reversed by correction of the acidosis. It is concluded that the effects in vivo of lidocaine on conduction under several conditions of rate, rhythm, and pH are similar to its effects on the maximum upstroke velocity of the action potential in vitro. Although these experiments were not designed to validate the modulated receptor hypothesis, it appears that the modulated receptor hypothesis can predict the effects of lidocaine on conduction in vivo.

  11. Ocular and systemic pharmacokinetics of lidocaine hydrochloride ophthalmic gel in rabbits after topical ocular administration.

    PubMed

    Liu, Bing; Ding, Li; Xu, Xiaowen; Lin, Hongda; Sun, Chenglong; You, Linjun

    2015-12-01

    Lidocaine hydrochloride ophthalmic gel is a novel ophthalmic preparation for topical ocular anesthesia. The study is aimed at evaluating the ocular and systemic pharmacokinetics of lidocaine hydrochloride 3.5 % ophthalmic gel in rabbits after ocular topical administration. Thirty-six rabbits were randomly placed in 12 groups (3 rabbits per group). The rabbits were quickly killed according to their groups at 0 (predose), 0.0833, 0.167, 0.333, 0.667, 1, 1.5, 2, 3, 4, 6, and 8 h postdose and then the ocular tissue and plasma samples were collected. All the samples were analyzed by a validated LC-MS/MS method. The test result showed that the maximum concentration (C max) of lidocaine in different ocular tissues and plasma were all achieved within 20 min after drug administration, and the data of C max were (2,987 ± 1814) μg/g, (44.67 ± 12.91) μg/g, (26.26 ± 7.19) μg/g, (11,046 ± 2,734) ng/mL, and (160.3 ± 61.0) ng/mL for tear fluid, cornea, conjunctiva, aqueous humor, and plasma, respectively. The data of the elimination half-life in these tissues were 1.5, 3.2, 3.5, 1.9, and 1.7 h for tear fluid, cornea, conjunctiva, aqueous humor, and plasma, respectively. The intraocular lidocaine levels were significantly higher than that in plasma, and the elimination half-life of lidocaine in cornea, conjunctiva, and aqueous humor was relatively longer than that in tear fluid and plasma. The high intraocular penetration, low systemic exposure, and long duration in the ocular tissues suggested lidocaine hydrochloride 3.5 % ophthalmic gel as an effective local anesthetic for ocular anesthesia during ophthalmic procedures.

  12. The relation between the duty cycle and anesthetic effect in lidocaine iontophoresis using alternating current.

    PubMed

    Wakita, Ryo; Nakajima, Atsushi; Haida, Yu; Umino, Masahiro; Fukayama, Haruhisa

    2011-01-01

    We assessed the effect of the duty cycle on the anesthetic effect during lidocaine alternating current (AC) iontophoresis. A solution of 2% lidocaine was delivered to the medial antecubital skin for 20 minutes using AC iontophoresis with a duty cycle of 60%, 70%, or 80%. The von Frey test was then performed to evaluate the anesthetic effect. In the groups treated with a duty cycle of 80% or 70% the touch thresholds (TT) were significantly elevated from 0 minutes to 30 minutes and from 0 minutes to 20 minutes. TT were significantly elevated at 0 minutes in the group treated with a 60% duty cycle. The anesthetic effect was significantly enhanced in a duty cycle-dependent manner.

  13. High pressure study of molecular dynamics of protic ionic liquid lidocaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Swiety-Pospiech, A.; Wojnarowska, Z.; Pionteck, J.; Pawlus, S.; Grzybowski, A.; Hensel-Bielowka, S.; Grzybowska, K.; Szulc, A.; Paluch, M.

    2012-06-01

    In this paper, we investigate the effect of pressure on the molecular dynamics of protic ionic liquid lidocaine hydrochloride, a commonly used pharmaceutical, by means of dielectric spectroscopy and pressure-temperature-volume methods. We observed that near Tg the pressure dependence of conductivity relaxation times reveals a peculiar behavior, which can be treated as a manifestation of decoupling between ion migration and structural relaxation times. Moreover, we discuss the validity of thermodynamic scaling in lidocaine HCl. We also employed the temperature-volume Avramov model to determine the value of pressure coefficient of glass transition temperature, dTg/dP|P = 0.1. Finally, we investigate the role of thermal and density fluctuations in controlling of molecular dynamics of the examined compound.

  14. Opiate refractory pain from an intestinal obstruction responsive to an intravenous lidocaine infusion.

    PubMed

    Bafuma, Patrick J; Nandi, Arun; Weisberg, Michael

    2015-10-01

    A 24-year-old female patient presented to our community emergency department (ED) for abdominal pain that had progressively worsened over the last 28 hours. Of note, 1 month prior to her presentation, the patient had a colostomy due to a rectal abscess and required stoma revision 5 days prior to her visit to our ED. The patient's pain was refractory to opiate analgesia in our ED, but experienced significant relief after an intravenous lidocaine infusion. Computer tomography of the abdomen and pelvis ultimately revealed a large bowel obstruction just proximal to the colostomy site. Historically, options for ED management of severe pain have been limited beyond narcotic analgesia. For patients whom are refractory to opiates in the ED, or for whom opiates are contraindicated, lidocaine infusions have shown promise for a variety of both acute and chronic painful conditions.

  15. Haemostatic effects of adrenaline-lidocaine subcutaneous infiltration at donor sites.

    PubMed

    Gacto, P; Miralles, F; Pereyra, J J; Perez, A; Martínez, E

    2009-05-01

    This study sought methods in burn surgery to reduce postoperative pain and blood loss at donor sites. A prospective, randomised, controlled, blinded trial included 56 people undergoing burn surgery, divided into two groups. Both groups received subcutaneous infiltration at donor sites, with either 1:500,000 adrenaline solution containing added lidocaine or with 0.45% normal saline (controls). Outcome measurements included amount of intraoperative bleeding, need for electrocautery, days the hydrocolloid dressing remained on donor sites, percentage of re-epithelialised skin at donor sites 1 week after surgery and viability of skin grafts. Results indicated that subcutaneous adrenaline-lidocaine infiltration at donor sites reduced intraoperative bleeding, decreased postoperative pain, shortened the duration of surgery and general anaesthesia and accelerated re-epithelialisation at the donor site. The overall graft take in both groups was similar.

  16. Development of an ANN optimized mucoadhesive buccal tablet containing flurbiprofen and lidocaine for dental pain.

    PubMed

    Hussain, Amjad; Syed, Muhammad Ali; Abbas, Nasir; Hanif, Sana; Arshad, Muhammad Sohail; Bukhari, Nadeem Irfan; Hussain, Khalid; Akhlaq, Muhammad; Ahmad, Zeeshan

    2016-06-01

    A novel mucoadhesive buccal tablet containing flurbiprofen (FLB) and lidocaine HCl (LID) was prepared to relieve dental pain. Tablet formulations (F1-F9) were prepared using variable quantities of mucoadhesive agents, hydroxypropyl methyl cellulose (HPMC) and sodium alginate (SA). The formulations were evaluated for their physicochemical properties, mucoadhesive strength and mucoadhesion time, swellability index and in vitro release of active agents. Release of both drugs depended on the relative ratio of HPMC:SA. However, mucoadhesive strength and mucoadhesion time were better in formulations, containing higher proportions of HPMC compared to SA. An artificial neural network (ANN) approach was applied to optimise formulations based on known effective parameters (i.e., mucoadhesive strength, mucoadhesion time and drug release), which proved valuable. This study indicates that an effective buccal tablet formulation of flurbiprofen and lidocaine can be prepared via an optimized ANN approach.

  17. Lidocaine spray alone is similar to spray plus viscous solution for pharyngeal observation during transoral endoscopy: a clinical randomized trial

    PubMed Central

    Hayashi, Tomoyuki; Asahina, Yoshiro; Waseda, Yohei; Kitamura, Kazuya; Kagaya, Takashi; Seike, Takuya; Okada, Kazuhiro; Inada, Yuki; Takabatake, Hisashi; Orita, Noriaki; Yanase, Yuko; Yamashita, Tatsuya; Ninomiya, Itasu; Yoshimura, Kenichi; Kaneko, Shuichi

    2017-01-01

    Background and study aims It is important to examine the pharynx during upper gastrointestinal endoscopy. Pharyngeal anesthesia using topical lidocaine is generally used as pretreatment. In Japan, lidocaine viscous solution is the anesthetic of choice, but lidocaine spray is applied when the former is considered insufficient. However, the relationship between the extent of pharyngeal anesthesia and accuracy of observation is unclear. We compared the performance of lidocaine spray alone versus lidocaine spray combined with lidocaine viscous solution for pharyngeal observation during transoral endoscopy. Patients and methods In this prospective, double-blinded, randomized clinical trial conducted between January and March 2015, 327 patients were randomly assigned to lidocaine spray alone (spray group, n = 157) or a combination of spray and viscous solution (combination group, n = 170). We compared the number of pharyngeal observable sites (non-inferiority test), pain by visual analogue scale, observation time, and the number of gag reflexes between the two groups. Results The mean number of images of suitable quality taken at the observable pharyngeal sites in the spray group was 8.33 (95 % confidence interval [CI]: 7.94 – 8.72) per patient, and 8.77 (95 % CI: 8.49 – 9.05) per patient in the combination group. The difference in the number of observable pharyngeal sites was – 0.44 (95 % CI: – 0.84 to – 0.03, P = 0.01). There were no differences in pain, observation time, or number of gag reflexes between the 2 groups. Subgroup analysis of the presence of sedation revealed no differences between the two groups for the number of pharyngeal observation sites and the number of gag reflexes. However, the number of gag reflexes was higher in the spray group compared to the combination group in a subgroup analysis that looked at the absence of sedation. Conclusions Lidocaine spray for pharyngeal anesthesia was not

  18. Efficacy of lidocaine on preventing incidence and severity of pain associated with propofol using in pediatric patients

    PubMed Central

    Lang, Bing-chen; Yang, Chun-song; Zhang, Ling-li; Zhang, Wen-sheng; Fu, Yu-zhi

    2017-01-01

    Abstract Background: Propofol injection pain was considered as one conundrum during clinical anesthesia. The systematic review about the effect of lidocaine in reducing injection pain among children has not been established. The aim of the study was to systematically evaluate the efficacy and safety of such intervention. Methods: The literature search was performed from the inception to the May 31, 2016 in PubMed, Ovid EMBASE, and Cochrane database. All randomized controlled trials that using lidocaine for propofol injection pain in children were enrolled. The primary outcome included the incidence of injection pain and the incidence of propofol injection pain in different degrees. The data were combined to calculate the relative ratio and relevant 95% confidence interval. A meta-analysis was performed following the guidelines of the Cochrane Reviewer's Handbook and the PRISMA statement. Results: Data from the included 11 studies indicated that the incidence of injection pain was lower in lidocaine group than the incidence in saline control group and in propofol lipuro (medium- and long-chain triglycerides) group (pain occurrence: 22.1% in lidocaine vs 66.8% in saline, RR with 95% 0.34 [0.26, 0.43], I2 = 38%; 30.5% in lidocaine vs 46.9% in propofol lipuro, RR with 95% 0.68 [0.46, 1.00], I2 = 9%). There was no difference between lidocaine and ketamine/alfentanil both in reducing pain occurrence and in reducing pain severity (pain occurrence: 29.7% in lidocaine vs 25.8% in ketamine, RR with 95% 1.47 [0.16, 13.43], I2 = 94%; 31.0% in lidocaine vs 30.7% in alfentanil, RR with 95% 1.01 [0.69, 1.46], I2 = 11%). And the reported side effects revealed that the safety of lidocaine in pediatric patients was acceptable. Conclusion: Compared with ketamine and alfentanil, lidocaine would be served as one more effective treatment in consideration of its well-matched efficacy, acceptable accessibility, and reasonable safety. However, more high-quality evidences in

  19. Anesthetic effects of clove oil and lidocaine-HCl on marine medaka (Oryzias dancena).

    PubMed

    Park, In-Seok; Park, Sung Jun; Gil, Hyun Woo; Nam, Yoon Kwon; Kim, Dong Soo

    2011-02-01

    Fish may be anesthetized for various experimental and practical purposes, primarily to immobilize them in order to facilitate handling. Marine medaka (Oryzias dancena) is a teleost fish used in marine ecotoxicology studies. Despite the importance of anesthesia in handling experimental fish, the effects of anesthesia in marine medaka have not yet been investigated. In this study, the authors evaluated the anesthetic effects (time required for anesthesia to take effect and recovery time) of two anesthetic agents, clove oil and lidocaine-HCl, on marine medaka. They anesthetized fish at different water temperatures (23 °C, 26 °C and 29 °C) and using different concentrations of clove oil (50 ppm, 75 ppm, 100 ppm, 125 ppm, 150 ppm and 175 ppm) or lidocaine-HCl (300 ppm, 400 ppm, 500 ppm, 600 ppm, 700 ppm and 800 ppm). The time required for anesthesia to take effect decreased significantly as both anesthetic concentration and water temperature increased for both clove oil and lidocaine-HCl. To anesthetize marine medaka within approximately 1 min, the optimal concentrations for clove oil were 125 ppm at 23 °C, 100 ppm at 26 °C and 75 ppm at 29 °C and for lidocaine-HCl were 800 ppm at 23 °C and 700 ppm at both 26 °C and 29 °C. The authors also compared anesthetic effects in marine medaka of different sizes. Both anesthetic exposure time and recovery time were significantly shorter for smaller fish than for larger fish. These results provide a useful foundation for the laboratory handling of marine medaka.

  20. Lidocaine inhibits the invasion and migration of TRPV6-expressing cancer cells by TRPV6 downregulation

    PubMed Central

    Jiang, Yuan; Gou, Hui; Zhu, Jiang; Tian, Si; Yu, Lehua

    2016-01-01

    It is well known that local anesthetics have a broad spectrum of pharmacological actions, acting as nerve blocks, and treating pain and cardiac arrhythmias via blocking of the sodium channel. The use of local anesthetics could reduce the possibility of cancer metastasis and recurrence following surgical tumor excision. The purpose of the present study was to investigate the inhibitory effect of lidocaine upon the invasion and migration of transient receptor potential cation channel subfamily V member 6 (TRPV6)-expressing cancer cells. Human breast cancer MDA-MB-231 cells, prostatic cancer PC-3 cells and ovarian cancer ES-2 cells were treated with lidocaine. Cell viability was quantitatively determined by MTT assay. The migration of the cells was evaluated using the wound healing assay, and the invasion of the cells was assessed using a Transwell assay. Calcium (Ca2+) measurements were performed using a Fluo-3 AM fluorescence kit. The expression of TRPV6 mRNA and protein in the cells was determined by quantitative-polymerase chain reaction and western blot analysis, respectively. The results suggested that lidocaine inhibits the cell invasion and migration of MDA-MB-231, PC-3 and ES-2 cells at lower than clinical concentrations. The inhibitory effect of lidocaine on TRPV6-expressing cancer cells was associated with a reduced rate of calcium influx, and could occur partly as a result of the downregulation of TRPV6 expression. The use of appropriate local anesthetics may confer potential benefits in clinical practice for the treatment of patients with TRPV6-expressing cancer. PMID:27446413

  1. The efficacy and safety of intravenous lidocaine for analgesia in the older adult: a literature review

    PubMed Central

    Daykin, Harriet

    2016-01-01

    Opioids remain the mainstay of analgesia for the treatment of moderate to severe acute pain. Even in the young, the use of opioids can be associated with an increased incidence of post-operative complications such as respiratory depression, vomiting, pruritus, excessive sedation, slowing of gastrointestinal function, and urinary retention. The need to manage acute pain in the older patient is becoming more common as the population ages, and increasingly older patients are undergoing more major surgery. Medical conditions are more common in older people and can result in the requirement of systemic analgesia for fractures, malignancy, nociceptive or neuropathic pain and peripheral vascular disease. Effective pain control can be difficult in older patients as there is a higher incidence of coexistent diseases, polypharmacy and age-related changes in physiology, pharmacodynamics and pharmacokinetics. Consequently, due to the fear of respiratory depression in older people, this leads to inadequate doses of opioid being given for the treatment of their pain. Lidocaine has analgesic, anti-hyperalgesic and anti-inflammatory properties and is metabolized by the liver which is limited by perfusion, and heart failure or drugs can alter this, affecting its clearance. Therefore, there are concerns regarding safety in older patients as plasma concentrations have both intersubject and intrasubject variability. The aim of this literature review is to assess the efficacy and safety of intravenous lidocaine as an adjuvant in pain management for the older patient. In total, 12 studies fulfilled the criteria. Lidocaine infusions were found to reduce pain scores and be opioid sparing in abdominal and urological surgery, in patients with opioid-refractory malignancy pain, neuropathic pain and critical limb ischaemia. Patients with malignancy were more likely to develop adverse effects, but no patients required treatment for lidocaine toxicity. PMID:28386401

  2. Hyaluron Filler Containing Lidocaine on a CPM Basis for Lip Augmentation: Reports from Practical Experience.

    PubMed

    Fischer, Tanja C; Sattler, Gerhard; Gauglitz, Gerd G

    2016-06-01

    Lip augmentation with hyaluronic acid fillers is established. As monophasic polydensified hyaluronic acid products with variable density, CPM-HAL1 (Belotero Balance Lidocaine, Merz Aesthetics, Raleigh, NC) and CPM-HAL2 (Belotero Intense Lidocaine, Merz Aesthetics, Raleigh, NC) are qualified for beautification and particularly natural-looking rejuvenation, respectively. The aim of this article was to assess the handling and outcome of lip augmentation using the lidocaine-containing hyaluronic acid fillers, CPM-HAL1 and CPM-HAL2. Data were documented from patients who received lip augmentation by means of beautification and/or rejuvenation using CPM-HAL1 and/or CPM-HAL2. Observation period was 4 months, with assessment of natural outcome, evenness, distribution, fluidity, handling, malleability, tolerability, as well as patient satisfaction and pain. A total of 146 patients from 21 German centers participated. Physicians rated natural outcome and evenness as good or very good for more than 95% of patients. Distribution, fluidity, handling, and malleability were assessed for both fillers as good or very good in more than 91% of patients. At every evaluation point, more than 93% of patients were very or very much satisfied with the product. A total of 125 patients (85.6%) experienced transient injection-related side effects. Pain intensity during the procedure was mild (2.72 ± 1.72 on the 0-10 pain assessment scale) and abated markedly within 30 minutes (0.42 ± 0.57). Lip augmentation with hyaluronic acid fillers produced a long-term cosmetic result. Due to the lidocaine content, procedural pain was low and transient. Accordingly, a high degree of patient satisfaction was achieved that was maintained throughout the observation period.

  3. Methemoglobin levels in generally anesthetized pediatric dental patients receiving prilocaine versus lidocaine.

    PubMed

    Gutenberg, Lauren L; Chen, Jung-Wei; Trapp, Larry

    2013-01-01

    The purpose of this study was to measure and compare peak methemoglobin levels and times to peak methemoglobin levels following the use of prilocaine and lidocaine in precooperative children undergoing comprehensive dental rehabilitation under general anesthesia. Ninety children, 3-6 years of age, undergoing dental rehabilitation under general anesthesia were enrolled and randomly assigned into 3 equal groups: group 1, 4% prilocaine plain, 5 mg/kg; group 2, 2% lidocaine with 1:100,000 epinephrine, 2.5 mg/kg; and group 3, no local anesthetic. Subjects in groups 1 and 2 were administered local anesthetic prior to restorative dental treatment. Methemoglobin levels (SpMET) were measured and recorded throughout the procedure using a Masimo Radical-7 Pulse Co-Oximeter (Masimo Corporation, Irvine, Calif, RDS-1 with SET software with methemoglobin interface). Data were analyzed using chi-square, one-way analysis of variance (ANOVA), and Pearson correlation (significance of P < .05). Group 1 had a significantly higher mean peak SpMET level at 3.55% than groups 2 and 3 at 1.63 and 1.60%, respectively. The mean time to peak SpMET was significantly shorter for group 3 at 29.50 minutes than that of group 1 at 62.73 and group 2 at 57.50 minutes. Prilocaine, at 5 mg/kg in pediatric dental patients, resulted in significantly higher peak SpMET levels than lidocaine and no local anesthetic. In comparison to no local anesthetic, the administration of prilocaine and lidocaine caused peak SpMET levels to occur significantly later in the procedure.

  4. Cardiovascular alterations after injection of 2% lidocaine with norepinephrine 1:50,000 (xylestesin) in rats.

    PubMed

    Faraco, Fatima Neves; Armonia, Paschoal Laercio; Malamed, Stanley F

    2007-01-01

    The purpose of the present study is to determine the cardiovascular effects produced by intravascular injection of 2% lidocaine with 20 microg/mL of norepinephrine on systolic, diastolic, and mean arterial pressures and heart rate of rats at the following times: control period, during the injection (first 15 seconds), during the first minute, and at the end of 1, 2, 3, 4, 5, 10, 15, 20, 25, and 30 minutes after drug administration. The study was performed on 13 male Wistar rats with weights between 200 grams and 220 grams that were awake during the recording of these parameters. The dose administered was proportional to 1 cartridge of local anesthetic (1.8 mL) in an average-size human, which is equivalent to 0.51 mg/kg of lidocaine hydrochloride and 0.51 microg/kg of norepinephrine hydrochloride. The average time of injection was 15.7 seconds. The results of this study showed significant increases in systolic, diastolic, and mean arterial pressure and a noticeable decrease in heart rate. The greatest variation occurred in the systolic blood pressure. The greatest alterations occurred during injection and within the first minute following administration of the anesthetic solution. We would anticipate these changes in the parameters analyzed to be clinically significant. Thus, dentists using 2% lidocaine with norepinephrine 20 mug/mL should be very careful to avoid intravascular injection.

  5. Pheniramine Maleate is more effective than Lidocaine on Fentanyl Induced Cough

    PubMed Central

    Ozmen, Ozgur; Kara, Duygu; Karaman, Emine Uzlas; Karakoc, Fatma; Karakaya, Muhammet Ahmet; Arslan, Zakir

    2016-01-01

    Objective: Fentanyl is frequently used during anesthesia induction. The use of fentanyl can cause cough through different mechanisms. Here, we aimed to investigate effects of pheniramine maleate (PM), an antihistaminic agent, and compare it with lidocaine on fentanyl induced cough. Methods: This is a randomized double-blind prospective clinical study of ASA I-II, 120 patients scheduled for elective abdominal surgery. Patients were administered drugs intravenously and randomly allocated into three groups: Group C (2 ml 0.9 % normal saline), Group L (1mg/kg lidocaine), and Group F (PM 45.5 mg). 90 seconds after administration, 2µ/kg fentanyl was applied in three seconds to all patients. Severity of cough (mild: 1-2, moderate: 3-5, severe> 5), time of the cough and vital parameters were recorded 90 seconds after fentanyl injection. Results: Eight patients (25%) in Group C had fentanyl induced cough whereas three patients (7.5%) in Group L and one patient (2.5%) in Group F experienced this phenomenon. There was statistically significant difference between Group F and Group C (p<0.05); however, differences between Group L and Group C or Group F and Group L were not statistically significant (p>0.05). Conclusions: Pheniramine Maleate 45.5 mg is better that placebo and as effective as lidocaine to prevent fentanyl induced cough. PMID:27375720

  6. Pain behaviour after castration of piglets; effect of pain relief with lidocaine and/or meloxicam.

    PubMed

    Kluivers-Poodt, M; Zonderland, J J; Verbraak, J; Lambooij, E; Hellebrekers, L J

    2013-07-01

    Behavioural responses and the effect of lidocaine and meloxicam on behaviour of piglets after castration were studied. A total of 144 piglets of 2 to 5 days of age were allocated to one of six treatments: castration (CAST), castration with lidocaine (LIDO), castration with meloxicam (MELO), castration with lidocaine and meloxicam (L + M), handling (SHAM) and no handling (NONE). Behaviour was observed for 5 days after the procedure, growth until weaning was recorded and characteristics of the castration wound noted. MELO piglets showed significantly (P < 0.05) more no pain-related behaviour than CAST and LIDO at the afternoon after castration, and were not significantly different from SHAM and NONE. LIDO piglets showed an increase (P < 0.001) in tail wagging, lasting for 3 days. This increase was not seen in L + M piglets. The occurrence of several behaviours changed with age, independent of treatment. A treatment effect on growth was not found. Wound healing was rapid in all treatments, but thickening of the heal was observed in several piglets, suggesting perturbation in the cicatrization process. Our study showed a pain-relieving effect of meloxicam after castration. Local anaesthesia resulted in piglets performing more tail wagging during the first few days after castration, which was prevented by administering meloxicam in combination with local anaesthesia.

  7. Lidocaine, Dexmedetomidine and Their Combination Reduce Isoflurane Minimum Alveolar Concentration in Dogs

    PubMed Central

    Acevedo-Arcique, Carlos M.; Ibancovichi, José A.; Chavez, Julio R.; Gutierrez-Blanco, Eduardo; Moran-Muñoz, Rafael; Victoria-Mora, José M.; Tendillo-Cortijo, Francisco; Santos-González, Martín; Sanchez-Aparicio, Pedro

    2014-01-01

    The effects of intravenous (IV) lidocaine, dexmedetomidine and their combination delivered as a bolus followed by a constant rate infusion (CRI) on the minimum alveolar concentration of isoflurane (MACISO) in dogs were evaluated. Seven healthy adult dogs were included. Anaesthesia was induced with propofol and maintained with isoflurane. For each dog, baseline MAC (MACISO/BASAL) was determined after a 90-minute equilibration period. Thereafter, each dog received one of the following treatments (loading dose, CRI): lidocaine 2 mg kg−1, 100 µg kg−1 minute−1; dexmedetomidine 2 µg kg−1, 2 µg kg−1 hour−1; or their combination. MAC was then determined again after 45- minutes of treatment by CRI. At the doses administered, lidocaine, dexmedetomidine and their combination significantly reduced MACISO by 27.3% (range: 12.5–39.2%), 43.4% (33.3–53.3%) and 60.9% (46.1–78.1%), respectively, when compared to MACISO/BASAL. The combination resulted in a greater MACISO reduction than the two drugs alone. Their use, at the doses studied, provides a clinically important reduction in the concentration of ISO during anaesthesia in dogs. PMID:25232737

  8. Use of adrenalin with lidocaine in hand surgery☆☆☆

    PubMed Central

    de Freitas Novais Junior, Ronaldo Antonio; Bacelar Costa, Jorge Ribamar; de Morais Carmo, Jose Mauricio

    2014-01-01

    Objective Because of the received wisdom within our setting that claims that local anesthesia should not be used with adrenalin in hand surgery; we conducted a study using lidocaine with adrenalin, to demonstrate its safety, utility and efficacy. Methods We conducted a prospective study in which, in wrist, hand and finger surgery performed from July 2012 onwards, we used local anesthesia comprising a 1% lidocaine solution with adrenalin at 1:100,000. We evaluated the quantity of bleeding, systemic alterations, signs of arterial deficit and complications, among other parameters. We described the infiltration techniques for specific procedures individually. Results We operated on 41 patients and chose to describe separately the raising of a lateral microsurgical flap on the arm, which was done without excessive bleeding and within the usual length of time. In only three cases was there excessive bleeding or use of bipolar tweezers. No systemic alterations were observed by the anesthesiologists or any complications relating to ischemia and necrosis in the wounds or in the fingers, and use of tourniquets was not necessary in any case. Conclusions Use of lidocaine with adrenalin in hand surgery was shown to be a safe local anesthetic technique, without complications relating to necrosis. It provided efficient exsanguination of the surgical field and made it possible to perform the surgical procedures without using a pneumatic tourniquet, thereby avoiding its risks and benefiting the patient through lower sedation. PMID:26229844

  9. Articaine versus lidocaine for third molar surgery: A randomized clinical study

    PubMed Central

    Santos, Thiago-de-S; Santos, Jadson-A.; Maia, Marcelo-C; Mendonça, Carla-G

    2012-01-01

    Objective: Pain reduction has been the subject of continuous research in the field of oral and maxillofacial surgery since postoperative pain with ranging of intensity and duration may affects the patient submitted in an oral surgical procedure. The aim of present study was to compare the analgesic effectiveness between two different anesthetic solutions (articaine and lidocaine) in third molar surgery. Study Design: A prospective, randomized and clinical study with patients submitted to third molar surgery at two distinct times. The visual analogue scale, the McGill Pain Questionnaire and the analgesic consumption record were used to measure the pain after each surgical time. Results: Duration of surgery, latency, the amount of anesthetic used and analgesic consumption showed clinical differences with highlights of articaine, though statistical significance was not observed (P<0.05). The pain scores indicated similar anesthetic efficacy with both solutions. Conclusion: In the present study no significant differences were observed between lidocaine and articaine in the control of postoperative pain. Key words: Articaine, lidocaine, pain control, lower third molar. PMID:22157664

  10. Controlled release of lidocaine hydrochloride from the surfactant-doped hybrid xerogels.

    PubMed

    Wu, Zhijian; Joo, Hyeonwoo; Lee, Tai Gyu; Lee, Kangtaek

    2005-06-02

    We investigate the controlled release of lidocaine hydrochloride from the doped silica-based xerogels. In the xerogel preparation, tetraethoxysilane (TEOS), methyltriethoxysilane (MTES), and propyltriethoxysilane (PTES) are used as precursors, and a nonionic surfactant Igepal CO 720 is used as a dopant. The experimental results suggest that the release of lidocaine hydrochloride can be easily controlled by partially substituting TEOS with the organosilanes, and/or by adding the dopant. Adding the organosilane precursors lowers the release of both the drug and the surfactant in the order of TEOS, MTES/TEOS, and PTES/TEOS xerogels. The release from the PTES/TEOS xerogels is much lower than that from the other xerogels. The release of lidocaine hydrochloride is obviously suppressed by the addition of Igepal CO 720, while the release of Igepal CO 720 is slightly promoted by the addition of the drug. The overall release process is found to be diffusion-controlled, and the release behaviors can be well explained by considering the effects of the textual properties of the xerogels and the interactions among the drug, the surfactant, and the xerogel matrices.

  11. Cardiovascular Alterations After Injection of 2% Lidocaine With Norepinephrine 1:50,000 (Xylestesin) in Rats

    PubMed Central

    Faraco, Fatima Neves; Armonia, Paschoal Laercio; Malamed, Stanley F

    2007-01-01

    The purpose of the present study is to determine the cardiovascular effects produced by intravascular injection of 2% lidocaine with 20 μg/mL of norepinephrine on systolic, diastolic, and mean arterial pressures and heart rate of rats at the following times: control period, during the injection (first 15 seconds), during the first minute, and at the end of 1, 2, 3, 4, 5, 10, 15, 20, 25, and 30 minutes after drug administration. The study was performed on 13 male Wistar rats with weights between 200 grams and 220 grams that were awake during the recording of these parameters. The dose administered was proportional to 1 cartridge of local anesthetic (1.8 mL) in an average-size human, which is equivalent to 0.51 mg/kg of lidocaine hydrochloride and 0.51 μg/kg of norepinephrine hydrochloride. The average time of injection was 15.7 seconds. The results of this study showed significant increases in systolic, diastolic, and mean arterial pressure and a noticeable decrease in heart rate. The greatest variation occurred in the systolic blood pressure. The greatest alterations occurred during injection and within the first minute following administration of the anesthetic solution. We would anticipate these changes in the parameters analyzed to be clinically significant. Thus, dentists using 2% lidocaine with norepinephrine 20 μg/mL should be very careful to avoid intravascular injection. PMID:17579502

  12. Comparison of Bupivacaine and Lidocaine Use for Postoperative Pain Control in Endodontics

    PubMed Central

    Moradi, Saeed; Naghavi, Neda

    2010-01-01

    INTRODUCTION: Many patients suffer from mild, moderate or severe pain during or after root canal therapy. Theoretically, post-operative pain control can be achieved by using long-acting local anesthetics. The aim of this study was to evaluate the efficacy of a long acting anesthesia, bupivacaine, on preventing post-operative pain associated with endodontic treatment, and to compare it with lidocaine. MATERIALS AND METHODS: This study was a double blind and randomized clinical trial on 30 patients' anterior maxillary teeth. The patients were divided into two groups of fifteen. One group was administered lidocanine (2% with 1:100000 epinephrine) local anesthesia and the other group was given bupivacaine (0.5% without epinephrine). The pain in patients were compared using the visual analogue scale (VAS) at definite times i.e. before treatment, during treatment and 2,4,6,8,10,12,24,36 and 48 hours after operation. Data were analyzed using One-way ANOVA tests. RESULTS: Bupivacaine significantly decreased postoperative pain compared to lidocaine. Postoperative pain was directly related to preoperative pain. Women reported more pain, though significant difference in postoperative pain report was not found between different ages. CONCLUSION: In conclusion, a single dose of bupivacaine 0.5% used in infiltration anesthesia could be more effective in reduction or prevention of post-operative endodontic pain compared with lidocaine. PMID:24778680

  13. Lidocaine blockage of basolateral potassium channels in the amphibian urinary bladder.

    PubMed Central

    Van Driessche, W

    1986-01-01

    1. Basolateral membranes of the frog urinary bladder were investigated after increasing the cationic conductance of the apical membrane by the incorporation of nystatin. 2. K+ currents were recorded in the presence of a mucosa to serosa oriented K+ gradient (SO4(2-) Ringer solution). Nystatin caused a rapid rise of the short-circuit current (Isc) followed by a slow increase over a period of 1-2 h. 3. Impedance analysis showed that the apical membrane resistance was drastically reduced by nystatin. The slow increase in Isc was accompanied by a progressive increase in basolateral conductance. 4. The transepithelial current and conductance recorded in the presence of nystatin could be depressed with lidocaine added to the mucosal and serosal solution. The effects of lidocaine were completely reversible. 5. Noise analysis showed that lidocaine induced additional fluctuations in Isc. The spectrum of these fluctuations was of the Lorentzian type. This noise component is caused by the random interruption of the current through the basolateral K+ channels. The Lorentzian parameters were used to calculate the microscopic parameters of the basolateral K+ channels. PMID:2442354

  14. Potentiation of epidural lidocaine by co-administering tramadol by either intramuscular or epidural route in cats.

    PubMed

    Hermeto, Larissa C; DeRossi, Rafael; Marques, Beatriz C; Jardim, Paulo H A

    2015-07-01

    This study investigated the analgesic and systemic effects of intramuscular (IM) versus epidural (EP) administration of tramadol as an adjunct to EP injection of lidocaine in cats. Six healthy, domestic, shorthair female cats underwent general anesthesia. A prospective, randomized, crossover trial was then conducted with each cat receiving the following 3 treatments: EP injection of 2% lidocaine [LEP; 3.0 mg/kg body weight (BW)]; EP injection of a combination of lidocaine and 5% tramadol (LTEP; 3.0 and 2.0 mg/kg BW, respectively); or EP injection of lidocaine and IM injection of tramadol (LEPTIM; 3.0 and 2.0 mg/kg BW, respectively). Systemic effects, spread and duration of analgesia, behavior, and motor blockade were determined before treatment and at predetermined intervals afterwards. The duration of analgesia was 120 ± 31 min for LTEP, 71 ± 17 min for LEPTIM, and 53 ± 6 min for LEP (P < 0.05; mean ± SD). The cranial spread of analgesia obtained with LTEP was similar to that with LEP or LEPTIM, extending to dermatomic region T13-L1. Complete motor blockade was similar for the 3 treatments. It was concluded that tramadol produces similar side effects in cats after either EP or IM administration. Our findings indicate that EP and IM tramadol (2 mg/kg BW) with EP lidocaine produce satisfactory analgesia in cats. As an adjunct to lidocaine, EP tramadol provides a longer duration of analgesia than IM administration. The adverse effects produced by EP and IM administration of tramadol were not different. Further studies are needed to determine whether EP administration of tramadol could play a role in managing postoperative pain in cats when co-administered with lidocaine after painful surgical procedures.

  15. Neonatal bilateral lidocaine administration into the ventral hippocampus caused postpubertal behavioral changes: An animal model of neurodevelopmental psychopathological disorders.

    PubMed

    Blas-Valdivia, Vanessa; Cano-Europa, Edgar; Hernández-García, Adelaida; Ortiz-Butrón, Rocio

    2009-01-01

    Our aim was to investigate if neonatal bilateral administration of lidocaine into the ventral hippocampus would cause behavioral changes related to schizophrenia. A neonatal ventral-hippocampal lesion (nVH lesion) was made with lidocaine in Wistar male pups. Two groups were formed, the first received lidocaine (4 mug/0.3 muL) and the second an equal volume of vehicle. At day 35 and 56, both groups were tested for social contact, immobility caused by clamping the neck and dorsal immobility, locomotor activity in an open field, and tail flick (TF) latency after a painful heat stimulus. All animals were then killed. Coronal cuts (7 mum) of the brain were obtained and each brain section was stained with cresyl violet-eosin. The animals which received the nVH lesion with lidocaine had decreased social interaction at both ages. The rats with lesions, only at day 58 postnatal, increased their distance traveled and ambulatory time, with a decrease in their nonambulatory and reset time. The rats with lesions had a longer duration of immobility caused by clamping the neck and a longer dorsal immobility at both days 34 and 57 compared to control rats. The lidocaine-treated group spent less time to deflect the tail compared to the control group at postpubertal age. The neonatal bilateral administration of lidocaine into the ventral hippocampus caused some alterations, such as chromatin condensation, nucleolus loss, and cell shrinkage, but glial proliferation was not seen. Neonatal bilateral lidocaine administration into the ventral hippocampus caused postpubertal behavioral changes.

  16. Potentiation of epidural lidocaine by co-administering tramadol by either intramuscular or epidural route in cats

    PubMed Central

    Hermeto, Larissa C.; DeRossi, Rafael; Marques, Beatriz C.; Jardim, Paulo H.A.

    2015-01-01

    This study investigated the analgesic and systemic effects of intramuscular (IM) versus epidural (EP) administration of tramadol as an adjunct to EP injection of lidocaine in cats. Six healthy, domestic, shorthair female cats underwent general anesthesia. A prospective, randomized, crossover trial was then conducted with each cat receiving the following 3 treatments: EP injection of 2% lidocaine [LEP; 3.0 mg/kg body weight (BW)]; EP injection of a combination of lidocaine and 5% tramadol (LTEP; 3.0 and 2.0 mg/kg BW, respectively); or EP injection of lidocaine and IM injection of tramadol (LEPTIM; 3.0 and 2.0 mg/kg BW, respectively). Systemic effects, spread and duration of analgesia, behavior, and motor blockade were determined before treatment and at predetermined intervals afterwards. The duration of analgesia was 120 ± 31 min for LTEP, 71 ± 17 min for LEPTIM, and 53 ± 6 min for LEP (P < 0.05; mean ± SD). The cranial spread of analgesia obtained with LTEP was similar to that with LEP or LEPTIM, extending to dermatomic region T13–L1. Complete motor blockade was similar for the 3 treatments. It was concluded that tramadol produces similar side effects in cats after either EP or IM administration. Our findings indicate that EP and IM tramadol (2 mg/kg BW) with EP lidocaine produce satisfactory analgesia in cats. As an adjunct to lidocaine, EP tramadol provides a longer duration of analgesia than IM administration. The adverse effects produced by EP and IM administration of tramadol were not different. Further studies are needed to determine whether EP administration of tramadol could play a role in managing postoperative pain in cats when co-administered with lidocaine after painful surgical procedures. PMID:26130854

  17. Comparison Between Intraperitoneal and Intravenous Lidocaine for Postoperative Analgesia After Elective Abdominal Hysterectomy, a Double-Blind Placebo Controlled Study

    PubMed Central

    Samimi, Saghar; Taheri, Arman; Davari Tanha, Fatemeh

    2015-01-01

    Objective: To compare the efficacy of intravenous and intraperitoneal injection of lidocaine and normal saline in relieving postoperative pain after elective abdominal hysterectomy. Materials and methods: For this double-blind randomized controlled study 109 patients undergoing elective abdominal hysterectomy were randomly allocated to three groups :1) IV group (intravenous injection group) received intravenous lidocaine %2 bolus 1.5mg/kg 30 min before incision and then a continuous lidocaine infusion of 2mg/kg and before the wound closure an intraperitoneal injection of N/S , 2) IP group (intraperitoneal group) received intravenous N/S and intraperitoneal lidocaine 3mg/kg , 3) P group (placebo, N/S) received both intravenous and intraperitoneal N/S. The pain scores (VAS) at rest, total morphine consumption , the time to first need for rescue analgesic ,incidence of lidocaine related adverse effects and nausea and vomiting were recorded at 0,2,4,8,12 and 24 hrs postoperatively. Results: The VAS scores were significantly lower in IP and IV groups compared with placebo (p = 0.001). Total consumption of morphine (p = 0.001) and time to firs request of recue analgesic (p = 0.001) were lower too in IP and IV groups.Incidence of vomiting was comparable between groups (p < 0.05) but nausea was higher in control group (p > 0.05).There were not notable lidocaine-related adverse effects. IP and IV groups were not statistically different for all investigated variables. Conclusion: This study showed lidocaine administration both intravenously and intraperitoneally are effective in reducing the postoperative pain and also have opioid sparing effect and can be safely used in elective abdominal hysterectomy without any major adverse effects. PMID:27047566

  18. Tachyphylaxis associated with repeated epidural injections of lidocaine is not related to changes in distribution or the rate of elimination from the epidural space

    SciTech Connect

    Mogensen, T.; Simonsen, L.; Scott, N.B.; Henriksen, J.H.; Kehlet, H. )

    1989-08-01

    The relationship between tachyphylaxis (measured as a decrease in the rate of regression of sensory levels of analgesia) during repeated epidural injections of lidocaine and both the distribution of lidocaine within the epidural space (as measured by spread of simultaneous injection of the tracer technetium-99m diethylenetriaminepentaacetate (99mTc-DTPA)) and elimination of lidocaine from the epidural space (as measured by serum concentrations of lidocaine) was investigated in 18 patients undergoing minor surgery during lumbar epidural analgesia. Twelve patients received four injections of 20 mL of 2% lidocaine at 2-hr intervals. Epidural distribution was assessed by injection of 99mTc-DTPA diluted in saline on the preoperative day and diluted in an equal volume of 2% lidocaine on the morning before surgery and again after the fourth injection of lidocaine 6 hr later. The distribution of 99mTc-DTPA in the epidural space was unchanged during the three measurements despite significant tachyphylaxis in both sensory analgesia and motor blockade (11 of 12 patients had sensory analgesia 2 hr after the first injection in contrast to only 3 of 12 patients during the third injection). In another six patients 20 mL of 2% lidocaine were injected three times at 2-hr intervals before surgery, with measurements of serum concentrations of lidocaine after the first and last injections. Despite tachyphylaxis (no patient had sensory analgesia 2 hr after the third injection), there was no difference in the rate of disappearance of lidocaine from the epidural space as assessed by plasma lidocaine concentration curves during the first and third injection (0.5 +/- 0.1 and 0.3 +/- 0.04 microgram.mL-1.min-1, respectively).

  19. Transcervical intrauterine levobupivacaine or lidocaine infusion for pain control during endometrial biopsy

    PubMed Central

    Kosus, Nermin; Kosus, Aydın; Demircioglu, Ruveyda I; Simavli, Serap A; Derbent, Aysel; Keskin, Esra Aktepe; Turhan, Nilgun O

    2014-01-01

    BACKGROUND: Endometrial biopsy is a common procedure for the investigation of many gynecological disorders including abnormal uterine bleeding, postmenopausal bleeding, abnormal cytology and infertility. Most women experience some degree of discomfort and pain during the procedure. Pain may occur during dilation of the cervix for insertion of the catheter and during endometrial biopsy, which further aggravates pain by inducing uterine contraction. OBJECTIVES: To determine pain levels during endometrial biopsy by comparing intrauterine instillation of levobupivacaine or lidocaine with placebo in a randomized, double-blinded trial in pre- and postmenopausal women. METHODS: Ninety patients were allocated to either control or experimental groups before endometrial biopsy. The trial medication was intra-uterine anesthesia, either 5 mL 0.9% saline (control group), or 5 mL 0.5% levobupivacaine or 2% lidocaine (experimental groups). Resident doctors used the same endometrial biopsy technique to minimize the risk of technical variation. All tissue specimens were sent for cytopathological examination. The pathologists, who were blinded to the study solution, analyzed all tissue specimens. The primary outcome measure was pain experienced during the procedure. Pain was assessed using a 10 cm visual analogue pain scale. All observed adverse effects were recorded until the patients were discharged. RESULTS: Pain scores of the intrauterine lidocaine and levobupivacaine groups were found to be significantly lower than the control group. There was no difference between the levobupivacaine and lidocaine groups with regard to pain scores. There was a moderately positive correlation between pain scores and endometrial thickness. No complications were observed due to the procedure. Most of the biopsy results were proliferative and secretory endometrium. Insufficient material causing inconclusive results was observed mostly in the control group. CONCLUSION: Transcervical intrauterine

  20. Functional consequences of lidocaine binding to slow-inactivated sodium channels

    PubMed Central

    1996-01-01

    Na channels open upon depolarization but then enter inactivated states from which they cannot readily reopen. After brief depolarizations, native channels enter a fast-inactivated state from which recovery at hyperpolarized potentials is rapid (< 20 ms). Prolonged depolarization induces a slow-inactivated state that requires much longer periods for recovery (> 1 s). The slow-inactivated state therefore assumes particular importance in pathological conditions, such as ischemia, in which tissues are depolarized for prolonged periods. While use- dependent block of Na channels by local anesthetics has been explained on the basis of delayed recovery of fast-inactivated Na channels, the potential contribution of slow-inactivated channels has been ignored. The principal (alpha) subunits from skeletal muscle or brain Na channels display anomalous gating behavior when expressed in Xenopus oocytes, with a high percentage entering slow-inactivated states after brief depolarizations. This enhanced slow inactivation is eliminated by coexpressing the alpha subunit with the subsidiary beta 1 subunit. We compared the lidocaine sensitivity of alpha subunits expressed in the presence and absence of the beta 1 subunit to determine the relative contributions of fast-inactivated and slow-inactivated channel block. Coexpression of beta 1 inhibited the use-dependent accumulation of lidocaine block during repetitive (1-Hz) depolarizations from -100 to - 20 mV. Therefore, the time required for recovery from inactivated channel block was measured at -100 mV. Fast-inactivated (alpha + beta 1) channels were mostly unblocked within 1 s of repolarization; however, slow-inactivated (alpha alone) channels remained blocked for much longer repriming intervals (> 5 s). The affinity of the slow- inactivated state for lidocaine was estimated to be 15-25 microM, versus 24 microM for the fast-inactivated state. We conclude that slow- inactivated Na channels are blocked by lidocaine with an affinity

  1. [Effect of intravenous infusion with lidocaine on rapid recovery of laparoscopic cholecystectomy].

    PubMed

    Chen, X Z; Lou, Q B; Sun, C C; Zhu, W S; Li, J

    2017-03-28

    Objective: To investigate the effect of intravenous infusion with lidocaine on rapid recovery of laparoscopic cholecystectomy. Methods: This study was a prospective randomized controlled trial. From February to August 2016 in Affiliated Yiwu Hospital of Wenzhou Medical University, 60 patients scheduled for laparoscopic cholecystectomy under general anesthesia were involved and randomly divided into control group (n=30) and lidocaine group (n=30). Patients in lidocaine group received lidocaine 1.5 mg/kg intravenously before induction and followed by 2.0 mg·kg(-1)·h(-1) to the end of surgery. Patients in control group received equal volumes of saline intravenously. Anesthesia induction in both groups were given intravenous midazolam 0.03 mg/kg, sufentanil 0.2 μg/kg, propofol 2.0 mg/kg and cisatracuium 0.2 mg/kg. Anesthesia was maintained with propofol 0.05-0.20 mg·kg(-1)·min(-1) and remifentanil 0.1-0.5 μg·kg(-1)·min(-1) for laryngeal mask airway which bispectral index (BIS) value maintained at 40-60. BIS, heart rate(HR) and mean arterial pressure(MAP) were recorded before anesthesia induction, before and immediately after laryngeal mask implantation, intraoperative 30 min and anesthesia awake. Pain scores were assessed using visual analogue scales (VAS) at postoperation immediately, 30 min during postanesthesia care unit (PACU), 2, 6, 12, and 24 h after surgery. The time of PACU retention, postoperative ambulation, first intestine venting and discharge were recorded. The dosage of propofol and remifentanil, the frequency of sufentanil used, the incidence of postoperative nausea and vomiting were also recorded. Patient satisfaction was evaluated by using Simple Restoration Quality Score (QoR-9). Results: BIS values before and after laryngeal mask implantation in lidocaine group were 50.50±3.47 and 54.63±1.25 respectively, which was lower than those in control group(54.30±4.78, 55.80±2.33; t=3.542, 2.423, all P<0.05). The VAS score at postoperation

  2. Muscle-Type Nicotinic Receptor Modulation by 2,6-Dimethylaniline, a Molecule Resembling the Hydrophobic Moiety of Lidocaine

    PubMed Central

    Alberola-Die, Armando; Fernández-Ballester, Gregorio; González-Ros, José M.; Ivorra, Isabel; Morales, Andrés

    2016-01-01

    To identify the molecular determinants responsible for lidocaine blockade of muscle-type nAChRs, we have studied the effects on this receptor of 2,6-dimethylaniline (DMA), which resembles lidocaine’s hydrophobic moiety. Torpedo marmorata nAChRs were microtransplanted to Xenopus oocytes and currents elicited by ACh (IACh), either alone or co-applied with DMA, were recorded. DMA reversibly blocked IACh and, similarly to lidocaine, exerted a closed-channel blockade, as evidenced by the enhancement of IACh blockade when DMA was pre-applied before its co-application with ACh, and hastened IACh decay. However, there were marked differences among its mechanisms of nAChR inhibition and those mediated by either the entire lidocaine molecule or diethylamine (DEA), a small amine resembling lidocaine’s hydrophilic moiety. Thereby, the IC50 for DMA, estimated from the dose-inhibition curve, was in the millimolar range, which is one order of magnitude higher than that for either DEA or lidocaine. Besides, nAChR blockade by DMA was voltage-independent in contrast to the increase of IACh inhibition at negative potentials caused by the more polar lidocaine or DEA molecules. Accordingly, virtual docking assays of DMA on nAChRs showed that this molecule binds predominantly at intersubunit crevices of the transmembrane-spanning domain, but also at the extracellular domain. Furthermore, DMA interacted with residues inside the channel pore, although only in the open-channel conformation. Interestingly, co-application of ACh with DEA and DMA, at their IC50s, had additive inhibitory effects on IACh and the extent of blockade was similar to that predicted by the allotopic model of interaction, suggesting that DEA and DMA bind to nAChRs at different loci. These results indicate that DMA mainly mimics the low potency and non-competitive actions of lidocaine on nAChRs, as opposed to the high potency and voltage-dependent block by lidocaine, which is emulated by the hydrophilic DEA

  3. A comparative evaluation of 4% articaine and 2% lidocaine in mandibular buccal infiltration anesthesia: A clinical study

    PubMed Central

    Maruthingal, Sunith; Mohan, Dennis; Maroli, Ramesh Kumar; Alahmari, Ali; Alqahtani, Ahmed; Alsadoon, Mohammed

    2015-01-01

    Background: To compare 4% articaine and 2% lidocaine local anesthetics in achieving pulpal anesthesia of the lower first permanent molar teeth objectively, and to assess and compare lip and lingual mucosa numbness subjectively. Materials and Methods: All subjects received 1.7 ml of any one anesthetic in the mucobuccal fold adjacent to mandibular first molar teeth; the same individuals received the second infiltration at least 1 week after the first. Later, comparisons for pulpal anesthesia, lip and lingual mucosa numbness between these two anesthetics solutions were made. Results: Articaine showed significant results with P = 0.006 in achieving pulpal anesthesia objectively, when compared with lidocaine. Articaine also showed very high significant results subjectively with P = 0.0006 in achieving lip numbness, when compared with lidocaine. But the results in achieving lingual mucosa numbness with articaine subjectively was not significant with P = 0.01, when compared with lidocaine. Conclusion: Endodontic and operative treatments are one of the most common oral non-surgical procedures done under local anesthesia. The diversity of anesthetic substances currently available on the market requires dental professionals to assess the drug both by its pharmacokinetic and also by its clinical characteristics during dental treatments. Our study used 4% articaine, which is available in the market, for comparison with 2% lidocaine. Further studies are required to use an equal concentration of solutions to achieve more accurate results. PMID:26759799

  4. Efficacy of caudal epidural injection of lidocaine, xylazine and xylazine plus hyaluronidase in reducing discomfort produced by electroejaculation in bulls.

    PubMed

    Pagliosa, Ronaldo C; Derossi, Rafael; Costa, Deiler S; Faria, Fabio J C

    2015-11-01

    To test the hypothesis that epidural administration of lidocaine, xylazine or xylazine plus hyaluronidase provides reduced pain and stress during electroejaculation in bulls, eight 30-month-old Nellore bulls received saline solution (control), 2% lidocaine, 2% xylazine or 2% xylazine plus hyaluronidase injected into the first intercoccygeal (Co1-Co2) epidural space in randomized order. Heart rate, respiratory rate, mean arterial pressure, analgesia, animal behavior and motor blockade were evaluated before treatment and at predetermined intervals during and after treatment. Pain and stress were scored subjectively, and semen quality was evaluated. The onset of anesthetic action was significantly faster with lidocaine (3.0 ± 1.2 min) than with xylazine or xylazine plus hyaluronidase (8.9 ± 1.5 and 5.5 ± 2.6 min, P=0.021 and P=0.012, respectively), and the onset of anesthesia with xylazine plus hyaluronidase was significantly faster than that with xylazine alone (P=0.032). Treatment with xylazine or xylazine plus hyaluronidase resulted in less discomfort than treatment with lidocaine, as indicated by animal behavior. Changes in heart rate, respiratory rate and arterial pressure were within acceptable limits. Penile protrusion and semen emission occurred in all animals during all four treatments. Our results suggest that xylazine plus hyaluronidase reduced discomfort during electroejaculation more effectively than xylazine or lidocaine alone. Further experiments are necessary to determine whether electroejaculation with xylazine plus hyaluronidase is feasible for obtaining semen from Nellore bulls unaccustomed to being handled or restrained.

  5. Botulinum toxin type A reconstituted in lidocaine with epinephrine for facial rejuvenation: results of a participant satisfaction survey.

    PubMed

    Kim, Alex; Jung, Jeong; Pak, Alexis

    2013-07-01

    To assess the feasibility, safety, and lack of inferiority of reconstituting botulinum toxin type A (BTX-A) in 1% lidocaine hydrochloride with epinephrine 1:100,000, 181 participants were asked to complete a satisfaction survey 3 to 6 months after treatment with the reconstituted formulation for facial rejuvenation. The addition of lidocaine was believed to achieve an immediate paralyzing effect on the injected muscles, and the addition of epinephrine was hypothesized to minimize diffusion to adjacent muscles. Participants were treated in the areas of the forehead and glabella, as well as the orbicularis oculi, orbicularis oris, and procerus muscles, in varying doses (10-60 U). Fifty-eight percent (91/157) of participants reported being more satisfied with BTX-A reconstituted in 1% lidocaine with epinephrine 1:100,000, with 85.7% (78/91) of these participants reporting that the immediate results made the formulation superior; 35.7% (56/157) were indifferent and 6.4% (10/157) reported that the modified formulation did not work better. The injection of BTX-A reconstituted in 1% lidocaine with epinephrine 1:100,000 presented no increased adverse effects (AEs), no decrease in pharmacologic potency, immediate feedback to the clinician, and higher satisfaction for the participants who previously had been treated with BTX-A reconstituted in unpreserved saline. Botulinum toxin type A reconstituted in 1% lidocaine with epinephrine 1:100,000 may increase the duration and efficacy of this widely used toxin.

  6. Differential response of DPI-modified cardiac Na+ channels to antiarrhythmic drugs: no flicker blockade by lidocaine.

    PubMed

    Benz, I; Kohlhardt, M

    1992-03-01

    Elementary Na+ currents were recorded in cell-attached patches from short-time cultured neonatal cardiocytes in order to test the hypothesis whether the open state of DPI-modified, noninactivating cardiac Na+ channels is basically sensitive to blocking drug molecules such as antiarrhythmics. Lidocaine (300 mumol/liter) effectively reduced the open probability of cardiac Na+ channels and, at a stimulation rate of 1 Hz, depressed the reconstructed macroscopic peak INa to 40 +/- 3.5% of the predrug value. The same drug concentration failed to influence DPI-modified Na+ channels. Their open state proved almost insensitive to lidocaine. tau open decreased only slightly to 85 +/- 2%. Still more importantly, the number of transitions between the conducting and a nonconducting configuration did not increase. At -40 mV, lidocaine may interfere with the open state with an association rate constant of 1.3 x 10(5) mol-1 sec-1 which is about two orders of magnitude smaller than the rate constant obtained with propafenone or prajmalium. Moreover, propafenone (10-20 mumol/liter) or prajmalium (30 mumol/liter) led to a tremendous increase in the number of transitions between the open and a nonconducting configuration. Lidocaine also failed to evoke a fast flicker blockade with reaction kinetics in the microsecond range. It is concluded that DPI-modified cardiac Na+ channels discriminate between lidocaine and other antiarrhythmic drugs. As a tentative explanation, this might be indicative for multiple binding sites for those drugs in cardiac Na+ channels.

  7. Electroencephalographic Changes Associated with Antinociceptive Actions of Lidocaine, Ketamine, Meloxicam, and Morphine Administration in Minimally Anaesthetized Dogs

    PubMed Central

    Hui Cheng, Chen; Meng, Goh Yong; Fakurazi, Sharida; Kaka, Asmatullah; Behan, Atique Ahmed

    2015-01-01

    Effects of ketamine and lidocaine on electroencephalographic (EEG) changes were evaluated in minimally anaesthetized dogs, subjected to electric stimulus. Six dogs were subjected to six treatments in a crossover design with a washout period of one week. Dogs were subjected to intravenous boluses of lidocaine 2 mg/kg, ketamine 3 mg/kg, meloxicam 0.2 mg/kg, morphine 0.2 mg/kg and loading doses of lidocaine 2 mg/kg followed by continuous rate infusion (CRI) of 50 and 100 mcg/kg/min, and ketamine 3 mg/kg followed by CRI of 10 and 50 mcg/kg/min. Electroencephalogram was recorded during electrical stimulation prior to any drug treatment (before treatment) and during electrical stimulation following treatment with the drugs (after treatment) under anaesthesia. Anaesthesia was induced with propofol and maintained with halothane at a stable concentration between 0.85 and 0.95%. Pretreatment median frequency was evidently increased (P < 0.05) for all treatment groups. Lidocaine, ketamine, and morphine depressed the median frequency resulting from the posttreatment stimulation. The depression of median frequency suggested evident antinociceptive effects of these treatments in dogs. It is therefore concluded that lidocaine and ketamine can be used in the analgesic protocol for the postoperative pain management in dogs. PMID:25695060

  8. Comparison of lidocaine and saline for epidural top-up during combined spinal-epidural anesthesia in volunteers.

    PubMed

    Trautman, W J; Liu, S S; Kopacz, D J

    1997-03-01

    This study was designed to determine the efficacy of saline as an epidural top-up to prolong spinal anesthesia during combined spinal-epidural anesthesia (CSEA). Eight volunteers received three separate CSEAs with intrathecal lidocaine (50 mg). After two-segment regression, each subject received either a saline (10 mL), lidocaine 1.5% (10 mL), or control sham (0.5 mL saline) epidural injection in a randomized, double-blind, triple cross-over fashion. Sensory block was assessed by pinprick and tolerance to transcutaneous electrical stimulation (TES) equivalent to surgical stimulation at the knee and ankle. Motor strength was assessed with iso-metric force dynamometry. Data were analyzed with a repeated measures analysis of variance and a paired t-test. Sensory block to pinprick was prolonged in the thoracolumbar dermatomes only by lidocaine (P < 0.05). Neither lidocaine nor saline prolonged the duration of tolerance to TES at the tested sites. Instead, saline decreased the duration of tolerance to TES by 20 and 24 min at the knee and ankle (P < 0.05). Recovery from motor block at the quadriceps was prolonged by an epidural injection of lidocaine (P < 0.05). We conclude that when 10 mL of epidural saline is administered after two-segment regression, it is an ineffective top-up and may decrease the duration of spinal anesthesia during CSEA.

  9. A prospective, randomized, double-blind study of the anesthetic efficacy of sodium bicarbonate buffered 2% lidocaine with 1:100,000 epinephrine in inferior alveolar nerve blocks.

    PubMed

    Whitcomb, Michael; Drum, Melissa; Reader, Al; Nusstein, John; Beck, Mike

    2010-01-01

    The authors, using a crossover design, randomly administered, in a double-blind manner, inferior alveolar nerve (IAN) blocks using a buffered 2% lidocaine with 1:100,000 epinephrine/sodium bicarbonate formulation and an unbuffered 2% lidocaine with 1:100,000 epinephrine formulation at 2 separate appointments spaced at least 1 week apart. An electric pulp tester was used in 4-minute cycles for 60 minutes to test for anesthesia of the first and second molars, premolars, and lateral and central incisors. Anesthesia was considered successful when 2 consecutive 80 readings were obtained within 15 minutes, and the 80 reading was continuously sustained for 60 minutes. For the buffered 2% lidocaine with 1:100,000 epinephrine/sodium bicarbonate formulation, successful pulpal anesthesia ranged from 10-71%. For the unbuffered 2% lidocaine with 1:100,000 epinephrine formulation, successful pulpal anesthesia ranged from 10-72%. No significant differences between the 2 anesthetic formulations were noted. The buffered lidocaine formulation did not statistically result in faster onset of pulpal anesthesia or less pain during injection than did the unbuffered lidocaine formulation. We concluded that buffering a 2% lidocaine with 1:100,000 epinephrine with sodium bicarbonate, as was formulated in the current study, did not statistically increase anesthetic success, provide faster onset, or result in less pain of injection when compared with unbuffered 2% lidocaine with 1:100,000 epinephrine for an IAN block.

  10. Efficacy and safety of post-cesarean section incisional infiltration with lidocaine and epinephrine versus lidocaine alone in reducing postoperative pain: A randomized controlled double-blinded clinical trial

    PubMed Central

    Tharwat, Ahmed A.; Yehia, Amr H.; Wahba, Karim A.; Ali, Abd-Elrhman G.

    2016-01-01

    Objective Aim was to assess the efficacy and safety of incisional infiltration of lidocaine and epinephrine vs. lidocaine only to reduce postcesarean section (C/S) pain. Material and Methods It was a prospective, randomized, controlled, double-blinded clinical trial that was conducted in two tertiary hospitals in Egypt and included 153 women undergoing C/S under general anesthesia. They were randomly divided into the following two groups: Group I (control group, number=78), in which the wound was infiltrated before skin closure with 20 mL of 2% lidocaine, and Group II (study group, number=75), in which the wound was infiltrated before skin closure with 20 mL of 2% lidocaine and epinephrine. The primary outcomes were the time to first analgesic (TFA) request (minutes) and the postoperative pain scores that were measured using a visual analogue scale (VAS). The secondary outcomes included the duration of C/S, onset of mobilization, onset of breastfeeding, duration of hospital stay, local or systemic side effects of lidocaine and epinephrine, postoperative pyrexia, and postoperative wound infection. Results The pain score determined using VAS after 1 and 2 h was significantly decreased in Group II than in Group I. However, at 4.8 and 16 h, these results were significantly reversed in Group II than in Group I. The cumulative postoperative opioid consumption was significantly less in Group II than in Group I (50 vs. 90 mg). The onset of mobilization, onset of breastfeeding, and duration of hospital stay was significantly shorter in Group II than in Group I, whereas the TFA request was significantly longer in Group II. Conclusion Administering epinephrine with 2% lidocaine prolongs the anesthetic effect and reduces the opioid analgesic dose postoperatively required, thereby enhancing patient recovery. PMID:27026771

  11. Intra-articular administration of lidocaine plus adrenaline in dogs: Pharmacokinetic profile and evaluation of toxicity in vivo and in vitro.

    PubMed

    Di Salvo, A; Chiaradia, E; della Rocca, G; Mancini, F; Galarini, R; Giusepponi, D; De Monte, V; Cagnardi, P; Marenzoni, M L; Bufalari, A

    2016-02-01

    The aim of this study was to evaluate the safety of intra-articular (IA) lidocaine plus adrenaline for improving peri-operative analgesia in anaesthetized dogs undergoing arthroscopy of the elbow. A solution of lidocaine (L) 1.98% plus adrenaline 1:100.000 was administered via the IA route and its safety evaluated in terms of cardio-, neuro-, and chondro-toxicity. No bradycardia or hypotension was recorded from induction to the last observational time point. Signs of toxicity of the nervous system could have been masked by the general anaesthesia but lidocaine concentrations detected in the blood were lower than those thought to be capable of producing toxicity. The assessment of in vitro chondrotoxicity showed a dose- and time-dependent effect of lidocaine on the viability of articular cells. Adrenaline appeared to reduce the chondrotoxicity of 1% lidocaine, following an exposure of up to 30 min.

  12. Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use

    PubMed Central

    Soares da Silva, Luiz Francisco Jones; do Carmo, Flavia Almada; de Almeida Borges, Vinicius Raphael; Monteiro, Lidiane Mota; Rodrigues, Carlos Rangel; Cabral, Lúcio Mendes; de Sousa, Valeria Pereira

    2011-01-01

    Inclusions of lidocaine hydrochloride in cyclodextrins were prepared to obtain stable complexes compatible for association with chlorhexidine in a new gel formulation for use in urogenital applications. Two cyclodextrins, β-cyclodextrin and methyl-β-cyclodextrin, were used for encapsulating lidocaine hydrochloride through solubilization and kneading techniques. The lidocaine–cyclodextrin complexes were characterized by ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The results revealed that the techniques generated good yields of inclusion products that maintained the functional properties of lidocaine. In addition, the inclusion products obtained improved the compatibility of lidocaine hydrochloride with chlorhexidine in solution and a gel formulation. The gel formulation displayed desirable rheological and physicochemical properties. The results presented here are the first description of the inclusion of lidocaine with cyclodextrins, which improves compatibility with chlorhexidine in formulations for simultaneous delivery. PMID:21822378

  13. Effects of lidocaine constant rate infusion on sevoflurane requirement, autonomic responses, and postoperative analgesia in dogs undergoing ovariectomy under opioid-based balanced anesthesia.

    PubMed

    Columbano, Nicolò; Secci, Fabio; Careddu, Giovanni M; Sotgiu, Giovanni; Rossi, Gabriele; Driessen, Bernd

    2012-08-01

    The effects of constant rate infusion (CRI) of lidocaine on sevoflurane (SEVO) requirements, autonomic responses to noxious stimulation, and postoperative pain relief were evaluated in dogs undergoing opioid-based balanced anesthesia. Twenty-four dogs scheduled for elective ovariectomy were randomly assigned to one of four groups: BC, receiving buprenorphine without lidocaine; FC, receiving fentanyl without lidocaine; BL, receiving buprenorphine and lidocaine; FL, receiving fentanyl and lidocaine. Dogs were anesthetized with intravenous (IV) diazepam and ketamine and anesthesia maintained with SEVO in oxygen/air. Lidocaine (2mg/kg plus 50 μg/kg/min) or saline were infused in groups BL/FL and BC/FC, respectively. After initiation of lidocaine or saline CRI IV buprenorphine (0.02 mg/kg) or fentanyl (4 μg/kg plus 8 μg/kg/h CRI) were administered IV in BC/BL and FC/FL, respectively. Respiratory and hemodynamic variables, drug plasma concentrations, and end-tidal SEVO concentrations (E'SEVO) were measured. Behaviors and pain scores were subjectively assessed 1 and 2h post-extubation. Lidocaine CRI produced median drug plasma concentrations <0.4 μg/mL during peak surgical stimulation. Lidocaine produced a 14% decrease in E'SEVO in the BL (P<0.01) but none in the FL group and no change in cardio-pulmonary responses to surgery or postoperative behaviors and pain scores in any group. Thus, depending on the opioid used, supplementing opioid-based balanced anesthesia with lidocaine (50 μg/kg/min) may not have any or only a minor impact on anesthetic outcome in terms of total anesthetic dose, autonomic responses to visceral nociception, and postoperative analgesia.

  14. Comparison of Transcutaneous Electrical Nerve Stimulation and Lidocaine on Episiotomy Complication in Primiparous Women: A Randomized Clinical Trial

    PubMed Central

    Rezaeyan, Maryam; Geranmayeh, Mehrnaz; Direkvand-Moghadam, Ashraf

    2017-01-01

    Introduction: Transcutaneous electrical nerve stimulation (TENS) through the skin is a nonpharmacological method of pain relief. The present study aimed to compare TENS and lidocaine on episiotomy complication in primiparous women. Material and Methods: In a randomized, controlled clinical trial, 80 participants were included from March to July 2011 at the antenatal clinic and postdelivery ward in the Social Security Organization Hospital, Khorramabad, Lorestan, Iran. Data were collected using a demographic questionnaire, visual analog scale and redness, edema, ecchymosis, discharge, and approximation scales. The participants were randomized into two groups with equal number of participants. All participants received 5 cc of local infiltration of 1% lidocaine before episiotomy, and TENS electrodes were placed on He Gu and Shenmen points during the crowning of fetal head. The TENS group received TENS with 100; 250 μs, the output range of 15–20 mm amplifier from crowning of first stage of labor to the end of the episiotomy repairing. The lidocaine group received 10 cc of local infiltration of 1% lidocaine before episiotomy repair while did not receive TENS electrodes. The pain intensity during and after episiotomy repair was recorded. Results: TENS and lidocaine have similar effects on pain relief at the episiotomy cutting, the start of the episiotomy repair, and at end of the episiotomy repair; however, the pain relief of both the interventions was different during the episiotomy repair. The effect of TENS in reducing edema was statistically significant (P = 0.001). Conclusions: TENS and lidocaine are effective for the episiotomy complications during and after episiotomy repair. PMID:28382054

  15. Drug delivery and transmission of lidocaine using iontophoresis in combination with direct and alternating currents.

    PubMed

    Inoue, Takutoshi; Sugiyama, Tomoaki; Ikoma, Toshiyuki; Shimazu, Hideaki; Wakita, Ryo; Fukayama, Haruhisa

    2016-01-01

    The present study investigates how effectively lidocaine ions are transported across a cellophane membrane through the application of either a direct current (DC) or alternating current (AC). The cellophane membrane was set on a parallelplate- type acrylic cell with platinum electrodes at both ends, filled with a donor cell of a 1 % aqueous solution of lidocaine and a receptor cell with distilled water. Lidocaine concentrations were measured for 60 min while the following voltages were applied, with changes every 10 min: 3 V DC and 7.5 V sine wave AC; frequency at 1 kHz. As a result, lidocaine concentrations in the receptor cell increased in a time-dependent manner. Significant increases in lidocaine concentrations were observed in groups where the voltage combination consisted of DC 30 min/AC 30 min, DC 50 min/AC 10 min, DC 60 min and AC 10 min/DC 50 min, compared with the passive diffusion group or in groups where voltage application was performed for 20, 30 , 40, 50 and 60 min. Significant increases were also observed in groups where the voltage combination consisted of A C 6 0 min, D C 10 min/AC 5 0 min, AC 3 0 min/ DC 30 min and AC 50 min/DC 10 min, compared with the passive diffusion group or in groups where voltage application was performed for 40, 50 and 60 min. These results suggest that lidocaine was delivered more rapidly with DC than with AC, and that its ions are transported faster when voltage is switched from DC to AC than from AC to DC, which is presumably due to the contribution of electrorepulsion by DC voltage application and the vibration energy infiltration mechanism owning to AC. Iontophoresis in combination with DC and AC was found to enable highly efficient drug delivery that shares the benefits of both forms of current application.

  16. Lidocaine infusion adjunct to total intravenous anesthesia reduces the total dose of propofol during intraoperative neurophysiological monitoring.

    PubMed

    Sloan, Tod B; Mongan, Paul; Lyda, Clark; Koht, Antoun

    2014-04-01

    Total intravenous anesthesia (TIVA) with propofol and opioids is frequently utilized for spinal surgery where somatosensory evoked potentials (SSEP) and motor evoked potentials (tcMEP) are monitored. Lidocaine infusions can contribute to antinociception and unconsciousness, thus allowing for a reduction in the total dose of propofol. We examined our recent experience with lidocaine infusions to quantify this effect. After institutional review board approval, we conducted a retrospective review of propofol usage in propofol-opioid TIVA (with and without lidocaine) for spine cases monitored with SSEP and tcMEP over a 7 months period. The propofol infusion rate, cortical amplitudes of the SSEP (median nerve, posterior tibial nerve), amplitudes and stimulation voltage of the tcMEP (adductor pollicis brevis, tibialis anterior) were evaluated. The savings of propofol and sufentanil were estimated based on utilization in 50 milliliter (ml) bottles and 5 ml ampules, respectively. 129 cases were evaluated. Propofol infusion rates were reduced with lidocaine infusion from an average of 115-99 μg/kg/min (p = 0.00038) and sufentanil infusions from an average of 0.36-0.29 μg/kg/h (p = 0.0059). This reduction in propofol infusion was also seen when the cases were divided into anterior cervical, posterior cervical, or posterior thoraco-lumbar procedures. No significant differences in the cortical SSEP or tcMEP amplitudes or the tcMEP stimulation voltages used were observed. No complications were associated with the use of the lidocaine infusion. The total estimated drug savings included 104 50 ml bottles of propofol and 5 5 ml ampules of sufentanil. These cases indicate that a lidocaine infusion can be effectively utilized in spine surgery with SSEP and tcMEP monitoring as a means to reduce propofol and sufentanil usage without a negative effect on the monitoring.

  17. Presentation of Neurolytic Effect of 10% Lidocaine after Perineural Ultrasound Guided Injection of a Canine Sciatic Nerve: A Pilot Study

    PubMed Central

    Asif, Asma; Kataria, Sandeep

    2016-01-01

    Background Phenol and alcohol have been used to ablate nerves to treat pain but are not specific for nerves and can damage surrounding soft tissue. Lidocaine at concentrations > 8% injected intrathecal in the animal model has been shown to be neurotoxic. Tests the hypothesis that 10% lidocaine is neurolytic after a peri-neural blockade in an ex vivo experiment on the canine sciatic nerve. Methods Under ultrasound, one canine sciatic nerve was injected peri-neurally with 10 cc saline and another with 10 cc of 10% lidocaine. After 20 minutes, the sciatic nerve was dissected with gross inspection. A 3 cm segment was excised and preserved in 10% buffered formalin fixative solution. Both samples underwent progressive dehydration and infusion of paraffin after which they were placed on paraffin blocks. The sections were cut at 4 µm and stained with hemoxylin and eosin. Microscopic review was performed by a pathologist from Henry Ford Hospital who was blinded to which experimental group each sample was in. Results The lidocaine injected nerve demonstrated loss of gross architecture on visual inspection while the saline injected nerve did not. No gross changes were seen in the surrounding soft tissue seen in either group. The lidocaine injected sample showed basophilic degeneration with marked cytoplasmic vacuolation in the nerve fibers with separation of individual fibers and endoneurial edema. The saline injected sample showed normal neural tissue. Conclusions Ten percent lidocaine causes rapid neurolytic changes with ultrasound guided peri-neural injection. The study was limited by only a single nerve being tested with acute exposure. PMID:27413480

  18. TRPA1 insensitivity of human sural nerve axons after exposure to lidocaine.

    PubMed

    Docherty, Reginald J; Ginsberg, Lionel; Jadoon, Saqiba; Orrell, Richard W; Bhattacharjee, Anupam

    2013-09-01

    TRPA1 is an ion channel of the TRP family that is expressed in some sensory neurons. TRPA1 activity provokes sensory symptoms of peripheral neuropathy, such as pain and paraesthesia. We have used a grease gap method to record axonal membrane potential and evoked compound action potentials (ECAPs) in vitro from human sural nerves and studied the effects of mustard oil (MO), a selective activator of TRPA1. Surprisingly, we failed to demonstrate any depolarizing response to MO (50, 250 μM) in any human sural nerves. There was no effect of MO on the A wave of the ECAP, but the C wave was reduced at 250 μM. In rat saphenous nerve fibres MO (50, 250 μM) depolarized axons and reduced the C wave of the ECAP but had no effect on the A wave. By contrast, both human and rat nerves were depolarized by capsaicin (0.5 to 5 μM) or nicotine (50 to 200 μM). Capsaicin caused a profound reduction in C fibre conduction in both species but had no effect on the amplitude of the A component. Lidocaine (30 mM) depolarized rat saphenous nerves acutely, and when rat nerves were pretreated with 30 mM lidocaine to mimic the exposure of human nerves to local anaesthetic during surgery, the effects of MO were abolished whilst the effects of capsaicin were unchanged. This study demonstrates that the local anaesthetic lidocaine desensitizes TRPA1 ion channels and indicates that it may have additional mechanisms for treating neuropathic pain that endure beyond simple sodium channel blockade.

  19. Infiltration with lidocaine and adrenaline instead of normal saline does not improve the septoplasty procedure.

    PubMed

    Gungor, Volkan; Baklaci, Deniz; Kum, Rauf Oguzhan; Yilmaz, Yavuz Fuat; Ozcan, Muge; Unal, Adnan

    2016-08-01

    The aim of this study was to determine whether infiltration of local anesthetics with adrenaline improved septoplasty procedure when compared to normal saline. Eight-two patients undergoing septoplasty were randomized into two groups. In group 1, septal mucoperichondrium was infiltrated with lidocaine with adrenaline, and normal saline was used in group 2. Presence of intra-operative septal mucosal injuries, the amount of bleeding, arterial blood pressure, operation time as well as the quality of the surgical field and the convenience of finding the correct surgical plane as determined by the surgeon using a 5-point scale were compared between two groups. There were no significant differences for the amount of blood loss, mean arterial pressure, operation time, or scores for convenience of finding the correct surgical plane between the two groups. There was no significant difference for intra-operative simple (P = 0.631) and total (simple+severe) (P = 0.649) septal mucoperichondrial injuries between groups 1 and 2, either. However, severe mucoperichondrial injury rate was higher in the patients infiltrated with lidocaine and adrenaline (P = 0.026), and the quality of the surgical field was worse in the patients injected with normal saline (P = 0.0179). Infiltration of septal mucoperichondrium with lidocaine and adrenaline instead of normal saline was not advantageous in terms of objective parameters tested, including bleeding amount and duration of surgery as well as the of the total mucosal injury rate in septoplasty procedure.

  20. Comparative study between 2 different doses of pregabalin and lidocaine on pain following propofol injection

    PubMed Central

    Choi, Eunkyung; Kim, Donggyeong; Jeon, Younghoon

    2016-01-01

    Abstract Background: Propofol, an intravenous anesthetic, often causes pain on injection, which can be very distressful to patients. We investigated the analgesic effect of pregabalin on pain following propofol injection, compared with lidocaine. Methods: In a randomized, double-blind, prospective trial, 120 patients were randomized into 3 groups of 40 each; who received oral placebo and intravenous lidocaine 40 mg with venous occlusion for 1 minute (group L, n = 40), oral pregabalin 75 mg and intravenous normal saline with venous occlusion for 1 minute (group LP, n = 40), and oral pregabalin 150 mg and intravenous normal saline with venous occlusion for 1 minute (group HP, n = 40) as pretreatment, followed by administration of 1% propofol 0.5 mg/kg. Pain intensity was measured on a 4-point scale (0 = no, 1 = mild, 2 = moderate, and 3 = severe pain). Any side effects associated with pretreatment substances were recorded during the first 24 hours after surgery. Results: A total of 120 patients completed this trial. Demographic data were similar between groups. The incidence of pain following propofol injection was significantly reduced in group HP (50%) and group L (55%) compared with group LP (92.5%) (P < 0.05, respectively). The incidences of moderate pain in group HP (12.5%) and group L (15%) were significantly decreased compared with group LP (37.5%; both, P < 0.05). There were no significant differences in the incidence of side effects such as headache and dizziness between groups. Conclusion: Pretreatment with oral pregabalin 150 mg and intravenous lidocaine 40 mg with venous occlusion equally reduced pain from propofol injection. PMID:28002316

  1. Intraoperative intravenous lidocaine exerts a protective effect on cell-mediated immunity in patients undergoing radical hysterectomy.

    PubMed

    Wang, Huan-Liang; Yan, Hong-Dan; Liu, Ya-Yang; Sun, Bao-Zhu; Huang, Rui; Wang, Xiao-Shuang; Lei, Wei-Fu

    2015-11-01

    Surgical procedures cause a decrease in lymphocyte proliferation rate, an increase in apoptosis and shifts the balance of T‑helper (Th)1/Th2 cells towards anti‑cell‑mediated immunity (CMI) Th2 dominance, which is relevant to the immunosuppressive effects of CMI, postoperative septic complications and the formation of tumor metastasis. Previous studies have revealed that lidocaine exhibits antibacterial actions; regulating inflammatory responses, reducing postoperative pain and affecting the duration spent in hospital. Thus, the present study hypothesized that lidocaine may exert a protective effect on the CMI of patients undergoing surgery for the removal of a primary tumor. A total of 30 adult female patients diagnosed with cervical cancer were recruited to the present study and were randomized into two groups. The lidocaine group received an intravenous bolus dose of 1.5 mg/kg lidocaine, followed by continuous infusion at 1.5 mg/kg/h until discharge from the operating room. The control group received the same volume of normal saline. A 10 ml sample of venous blood was drawn, and the lymphocytes were isolated using Ficoll‑paque 1 day prior to surgery, at discharge from the operating room and 48 h post‑surgery. The proliferation rate of the lymphocytes was assessed using a Cell Counting Kit‑8 assay and was found to be higher in the lidocaine group. The early apoptosis of lymphocytes was attenuated following lidocaine treatment at 48 h post‑surgery, as detected using flow cytometry with Annexin V‑fluorescein isothiocyanate/propidium iodide staining. The level of interferon (IFN)‑γ in the serum at 48 h was significantly decreased following surgery in the control group, compared with the pre‑surgical values (3.782 ± 0.282, vs. 4.089 ± 0.339 pg/ml, respectively) and the ratio of IFN‑γ to interleukin‑4 was well preserved in the lidocaine group. In conclusion, the present study demonstrated that the intraoperative systemic administration of

  2. Comparison of two different doses of lidocaine on the pain sensation during transrectal ultrasound-guided prostate biopsy

    PubMed Central

    Ateş, Ferhat; Dursun, Furkan; Malkoç, Ercan; Yılmaz, Ömer; Soydan, Hasan; Şen, Hüseyin; Başal, Şeref; Zekey, Fatih; Karademir, Kenan

    2016-01-01

    Objective To compare two different doses of lidocaine used for periprostatic nerve block on pain perception during transrectal ultrasound (TRUS) guided prostate biopsy. Material and methods A total of 288 patients with elevated prostate specific antigen (PSA) levels and/or abnormal digital rectal examination who underwent TRUS-guided prostate biopsy were included in the study. The patients were divided into 3 groups: Group 1 (n=103) prostate biopsy were performed after administering perianal intrarectal application of 10 mL 2% lidocaine gel, Group 2 (n=98) 2 mL of 2% lidocaine injection on each side following rectal installation of lidocaine gel and Group 3 (n=87) 4 mL of 2% lidocaine injection on each side after rectal instillation of lidocaine gel. Patients’ pain scores during biopsy procedure were reported using visual analogue score (VAS). Independent sample t test, ANOVA test and Tukey test were used for statistical evaluation. Results The mean age, prostate volume and PSA level were 65.6±8.4 years, 58.2±34.8 mL, and 11.8±3.4 ng/mL respectively. There were no statistically significant differences in baseline characteristics between the groups. The mean VAS scores were 2.4±1.8 in Group 1, 2.5±1.9 in Group 2 and 1.6±1.6 in Group 3. Patients in Group 3, reported significant pain reduction compared with patients in Groups 1 and 2 (p=0.002, and 0.001, respectively). However, there was no statistically significant difference in VAS scores between Groups 1 and 2 (p=0.815). Conclusion According to our results we recommend the use of perianal intrarectal lidocain gel application, and periprostatic nerve block with injection of 4 ml 2% lidocaine per side combination in TRUS-guided prostate biopsies. Further large-scale randomized control studies are needed to validate these finding. PMID:27635288

  3. Effects of a concentrated lidocaine solution on the acute phase stress response to dehorning in dairy calves.

    PubMed

    Doherty, T J; Kattesh, H G; Adcock, R J; Welborn, M G; Saxton, A M; Morrow, J L; Dailey, J W

    2007-09-01

    The objective of this study was to more fully define the surgical stress response to dehorning by heat cauterization in dairy calves by measuring behavioral, hormonal, inflammatory, and immunological markers of stress and to determine whether a nerve block of the surgical site with a concentrated solution of lidocaine (5%) reduces the degree of stress. Thirty-two 10- to 12-wk-old female Holstein calves were randomly allotted to 1 of 4 treatments: 5% lidocaine followed by dehorning, 2% lidocaine followed by dehorning, saline followed by dehorning, or 5% lidocaine followed by sham dehorning. Plasma cortisol concentration was measured in blood samples collected via a jugular catheter at -0.5, 0, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 9, 12, 24, 48, and 72 h. Various other blood constituents were measured in samples collected at -0.5, 12, 24, 48, and 72 h. Feeding, drinking, scratching, grooming, rubbing, licking, and inactivity behaviors were observed in the standing and recumbent positions using a 10-min scan sampling method analyzed on a time period and daily basis for 72 h following the dehorning procedure. The frequency of vocalization, kicking, and lying in the chute during the dehorning procedure were also assessed. The overall plasma cortisol concentrations were higher in calves subjected to dehorning than in control calves. Compared with the control group, the saline-treated calves had a higher cortisol concentration at 30 and 60 min postdehorning. Plasma cortisol concentrations were higher in all groups at 30 min postdehorning than at other sampling times. The percentage of circulating neutrophils and the neutrophil:lymphocyte ratio were increased in the saline and 2% lidocaine group. Total plasma protein, fibrinogen, and alpha1-acid glycoprotein concentrations were similar among treatments. The behavioral response to dehorning, as manifested by kicking while in the chute, was greater in the saline and 2% lidocaine group than in the control or 5% lidocaine

  4. Allergic reaction to epinephrine preparation in 2% lidocaine: two case reports.

    PubMed Central

    Kohase, Hikaru; Umino, Masahiro

    2004-01-01

    We report 2 cases of hypersensitivity to an epinephrine preparation in local anesthetics which were found by skin tests for local anesthetics. Both patients had uncomfortable episodes to local anesthetics at dental treatment. In both cases, the skin tests showed positive reactions to 2% lidocaine with 1:80,000 epinephrine. Furthermore drug lymphocyte stimulation test revealed positive reaction to epinephrine hydrochloride, epinephrine bitartrate in case 1, whereas in case 2, the drug lymphocyte stimulation test showed positive response to epinephrine bitartrate. Attention should be paid to exogenous epinephrine preparations that have the potential to induce hypersensitivity during dental treatment. PMID:15675262

  5. Simultaneous programmed temperature GLC assay of phenol, chloroxylenol, and lidocaine hydrochloride in topical antiseptic cream.

    PubMed

    Palermo, P J; Lundberg, J B

    1978-11-01

    A simultaneous programmed temperature GLC assay for the active ingredients in a topical antiseptic cream is described. The sample is extracted directly using a dimethyl sulfoxide solution of p-cresol, 4-chlorophenol, and 2-amino-4-phenylthiazole as internal standards for phenol, chloroxylenol, and lidocaine hydrochloride, respectively. The resulting solution is chromatographed by temperature programming on an OV-225 column from 90 to 225 degrees. The internal standard calculation is accomplished using peak heights or peak areas. The relative standard deviation of all assays is less than 2%.

  6. Tolerability of 2.5% Lidocaine/Prilocaine Hydrogel in Children Undergoing Cryotherapy for Molluscum Contagiosum.

    PubMed

    Gobbato, André A M; Babadópulos, Tainah; Gobbato, Cintia A R S; Moreno, Ronilson A; Gagliano-Jucá, Thiago; De Nucci, Gilberto

    2016-05-01

    The tolerability of a 2.5% lidocaine/prilocaine hydrogel (Nanorap, Biolab Indústria Farmacêutica Ltd., Sao Paulo, Brazil) was evaluated in 20 children ages 2 to 11 years undergoing cryotherapy for molluscum contagiosum (MC). The product was well tolerated, with only two children presenting with eczema at the application site. These adverse reactions were considered unlikely to be related to the test product, because a patch test was negative in one of the individuals and the other event occurred in only one of the two treated areas. Nanorap is an efficacious and well-tolerated option for topical anesthesia in children undergoing cryotherapy for MC.

  7. Comparison of the Effect of Lidocaine versus a Lidocaine-Bupivacaine Combination in a Periprostatic Nerve Block Undergoing Transrectal Ultrasound-Guided Prostate Biopsy: A Double-Blind Randomized Controlled Trial

    PubMed Central

    Yilmaz, Ali H.; Ziypak, Elif; Ziypak, Tevfik; Aksoy, Mehmet; Adanur, Senol; Kocakgol, Hüseyin; Demirdogen, Saban O.; Polat, Ozkan

    2016-01-01

    Introduction To determine whether a combination of the long acting local anesthetic, bupivacaine, and lidocaine is better than lidocaine alone in the long-term pain control, which is a short-acting anesthetic. Materials and Methods In group 1, periprostatic nerve block was applied to both neurovascular areas with 2% lidocaine (5 ml) in an isotonic solution (5 ml). In group 2, the combination of 2% lidocaine (5 ml) and 5mg/ml bupivacaine (5 ml) was used for the PPNB. Results In the first 30 minutes the mean VAS scores of groups 1 and 2 were 2.1 ± 0.2 and 1.2 ± 0.1, respectively (p = 0.002). VAS scores of group II determined at 1, 2, 4, 6, and 8 hours after the biopsy were significantly lower since it was (p < 0.05). Conclusion While periprostatic nerve block for late phase pain control, applying a combination of a long-acting local anesthetic, such as bupivacaine, is effective in terms of pain control and patient comfort. PMID:27867334

  8. Comparative study on anesthetic potency depending on concentrations of lidocaine and epinephrine: assessment of dental local anesthetics using the jaw-opening reflex.

    PubMed Central

    Ohkado, S.; Ichinohe, T.; Kaneko, Y.

    2001-01-01

    Anesthetic potency of a local anesthetic on the dental pulp was investigated by increasing or decreasing the concentration of lidocaine and that of epinephrine. An electromyogram of the digastric muscle in Japan White male rabbits was recorded during the jaw-opening reflex induced by electrical stimulation of the dental pulp. Probit analysis was used for the determination of the 50% effective volume (ED50) values of the anesthetic. The anesthetics used were plain 2% lidocaine solution (2Lid-0 group), 2% lidocaine solution with 12.5 microgram/mL of epinephrine (2Lid-1/8 group), 2% lidocaine solution with 6.25 microgram/mL of epinephrine (2Lid-1/16 group), and 4% lidocaine solution with 5 microgram/mL of epinephrine (4Lid-1/20 group). No anesthetic effect was shown in the 2Lid-0 group. The 2Lid-1/8 group indicated adequate anesthetic potency with the smallest dosage at all observation periods. The potency in the 2Lid-1/16 group was 0.3-0.5 times, and that in the 4Lid-1/20 group was 0.3-0.4 times as much as the 2Lid-1/8 group. The decrease in epinephrine concentration produced the decrease in the anesthetic potency on the dental pulp independent of lidocaine concentration. These results suggest that the increase in lidocaine concentration may not compensate the decrease in epinephrine concentration. PMID:11495400

  9. Biodegradable nanofiber-membrane for sustainable release of lidocaine at the femoral fracture site as a periosteal block: In vitro and in vivo studies in a rabbit model.

    PubMed

    Chou, Ying-Chao; Cheng, Yi-Shiun; Hsu, Yung-Heng; Yu, Yi-Hsun; Liu, Shih-Jung

    2016-04-01

    The aim of this study was to evaluate the efficacy of a biodegradable, lidocaine-embedded, nanofibrous membrane for the sustainable analgesic release onto fragments of a segmental femoral fracture site. Membranes of three different lidocaine concentrations (10%, 30%, and 50%) were produced via an electrospinning technique. In vitro lidocaine release was assessed by high-performance liquid chromatography. A femoral segmental fracture, with intramedullary Kirschner-wire fixation and polycaprolactone stent enveloping the fracture site, was set-up in a rabbit model for in vivo assessment of post-operative recovery of activity. Eighteen rabbits were randomly assigned to three groups (six rabbits per group): group A comprised of rabbits with femoral fractures and underwent fixation; group B comprised of a comparable fracture model to that of group A with the implantation of lidocaine-loaded nanofibers; and group C, the control group, received only anesthesia. The following variables were measured: change in body weight, food and water intake before and after surgery, and total activity count post-surgery. All membranes eluted effective levels of lidocaine for more than 3 weeks post-surgery. Rabbits in group B showed faster recovery of activity post-operatively, compared with those in group A, which confirmed the pain relief efficacy of the lidocaine-embedded nanofibers. Nanofibers with sustainable lidocaine release have adequate efficacy and durability for pain relief in rabbits with segmental long bone fractures.

  10. Buccal Injection of 2% Lidocaine With Epinephrine for the Removal of Maxillary Third Molars

    PubMed Central

    Yadav, Sunil; Verma, Ajay; Sachdeva, Akash

    2013-01-01

    The aim of the study was to demonstrate if 2% lidocaine hydrochloride with 1 : 200,000 epinephrine could provide palatal anesthesia in maxillary tooth removal with a single buccal injection. The subjects included in the clinical study were those requiring extraction of the maxillary third molar of either side. For the purpose of comparison, the sample was randomly divided into 2 main groups: group 1 (study group) included 100 subjects who were to receive a single injection before extraction, and group 2 (control group) included 100 subjects who were to receive a single buccal injection and a single palatal injection before extraction. After 5 minutes the extraction was performed. All patients were observed for Faces Pain Scale during extraction and asked for the same on a 100-mm visual analog scale after extraction. According to visual analog scale and Faces Pain Scale scores, when maxillary third molar removal without palatal injection (study group) and with palatal injection (control group) were compared the difference was not statistically significant (P > .05). Removal of maxillary third molars without palatal injection is possible by depositing 2 mL of 2% lidocaine hydrochloride with 1 : 200,000 epinephrine to the buccal vestibule of the tooth. PMID:24010986

  11. Anesthetic Efficacy of 3 Volumes of Lidocaine With Epinephrine in Maxillary Infiltration Anesthesia

    PubMed Central

    Brunetto, Paula Cristina; Ranali, José; Bovi Ambrosano, Gláucia Maria; de Oliveira, Patrícia Cristine; Groppo, Francisco Carlos; Meechan, John Gerard; Volpato, Maria Cristina

    2008-01-01

    The objective of this randomized double-blind investigation was to compare the anesthetic efficacy and injection discomfort of 3 volumes of 2% lidocaine with 1∶100,000 epinephrine for maxillary infiltration anesthesia. A total of 25 subjects received 0.6, 0.9, and 1.2 mL of the anesthetic buccal to an upper canine. Test teeth were assessed with electrical stimulation to determine onset and duration of pulpal anesthesia; soft tissue anesthesia and injection discomfort were assessed by pin-prick test and visual analog scale (VAS). Data were analyzed by 2-way analysis of variance (ANOVA), Friedman, and chi-square tests (α  =  5%). The 1.2 mL dose induced faster onset of pulpal anesthesia, a higher success rate, and a longer duration of soft tissue/pulpal anesthesia than were achieved with the other doses (P < .05). No differences in injection discomfort were observed between treatments. It is concluded that maxillary infiltration anesthesia with lidocaine and epinephrine has a faster onset, a greater success rate, and a longer duration when a volume of 1.2 mL is used than when volumes less than 1.0 mL are used. PMID:18547150

  12. Reduction in radiation-induced brain injury by use of pentobarbital or lidocaine protection

    SciTech Connect

    Oldfield, E.H.; Friedman, R.; Kinsella, T.; Moquin, R.; Olson, J.J.; Orr, K.; DeLuca, A.M. )

    1990-05-01

    To determine if barbiturates would protect brain at high doses of radiation, survival rates in rats that received whole-brain x-irradiation during pentobarbital- or lidocaine-induced anesthesia were compared with those of control animals that received no medication and of animals anesthetized with ketamine. The animals were shielded so that respiratory and digestive tissues would not be damaged by the radiation. Survival rates in rats that received whole-brain irradiation as a single 7500-rad dose under pentobarbital- or lidocaine-induced anesthesia was increased from between from 0% and 20% to between 45% and 69% over the 40 days of observation compared with the other two groups (p less than 0.007). Ketamine anesthesia provided no protection. There were no notable differential effects upon non-neural tissues, suggesting that pentobarbital afforded protection through modulation of ambient neural activity during radiation exposure. Neural suppression during high-dose cranial irradiation protects brain from acute and early delayed radiation injury. Further development and application of this knowledge may reduce the incidence of radiation toxicity of the central nervous system (CNS) and may permit the safe use of otherwise unsafe doses of radiation in patients with CNS neoplasms.

  13. Nystatin and lidocaine pastilles for the local treatment of oral mucositis.

    PubMed

    Silva, Filipa Cosme; Marto, Joana M; Salgado, Ana; Machado, Paula; Silva, Alexandra N; Almeida, António J

    2017-03-01

    Oral mucositis (OM) is a common adverse reaction to radiotherapy and chemotherapy in oncology. Its treatment requires oral formulations that enhance therapy compliance, improve administration and ensure drug effectiveness. Solid dosage forms that act by slow dissolution, such as pastilles, are an effective alternative to mouthwashes, for their versatility, ease of administration and extended residence time in the oral cavity. The present work describes the development and stability studies of an innovative formulation of nystatin and lidocaine pastilles for the treatment of oral mucositis. Full pharmaceutical quality testing was carried out, including disintegration and dissolution testing, texture profile analysis, grittiness and an antifungal activity testing. A soft pastille formulation containing 0.25% lidocaine and 78,000 IU nystatin was obtained, presenting suitable pharmaceutical characteristics, as a disintegration time of 17 ± 2 min, dissolution rate and microbiological and physicochemical for 30 days when stored at 2-8 °C under light protection. Palatability was also evaluated, being well accepted by a panel of 38 healthy volunteers. This formulation allows an accurate drug dosing by the prescriber, while enabling the patients to control the retention time of the drugs in the oral cavity and consequently manage their pain treatment.

  14. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis.

    PubMed

    Pandit, Ashlesha P; Pol, Vaibhav V; Kulkarni, Vinit S

    2016-01-01

    The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 3(2) factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y 1) and drug release (Y 2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure.

  15. Effects of lidocaine and adrenaline combination on postoperative edema and ecchymosis in rhinoplasty.

    PubMed

    Gun, R; Yorgancılar, E; Yıldırım, M; Bakır, S; Topcu, I; Akkus, Z

    2011-07-01

    Nasal osteotomies are the most important cause of periorbital edema and ecchymosis. Injection of lidocaine and adrenaline is recommended to reduce bleeding. Whilst the lidocaine and adrenaline combination (LAC) is claimed to reduce postoperative ecchymosis and edema, this effect remains to be proven conclusively. This study, on 48 patients, was designed to investigate the effects of LAC injection on postoperative edema/ecchymosis in rhinoplasty. LAC was applied at a random side prior to the lateral osteotomy. The opposite side was used as a control. The relationship between edema/ecchymosis and the degree of LAC on the injected and uninjected sides was evaluated on the first, third and seventh day postoperatively. The relationships between edema and ecchymosis with operation time and intraoperative systolic blood pressure were also evaluated. Bleeding was reduced on the side treated with LAC (p=0.050). The degrees of edema/ecchymosis increased with increases in the duration of operation and the systolic blood pressure on the first postoperative day for the LAC-applied side (p<0.05). This correlation was not observed on the opposite side (p>0.05). Application of LAC reduces bleeding during rhinoplasty and pain control postoperatively but reduced edema and ecchymosis should not be expected following LAC application.

  16. Effect of a trial pharmaceutical solution on reversing sensations after using lidocain: An animal study

    PubMed Central

    Haghighat, Abbas; Davoudi, Amin; Minaiyan, Mohsen; Molai, Meghdad; Afshar, Abdolreza; Basiri, Keyvan

    2015-01-01

    Introduction: Local anesthesia has a paramount role in any branches of medical sciences specially dentistry. Soft tissue irritations and lips biting are adverse side-effects in some cases. This study tried out to represent a new pharmaceutical solution in returning sensations faster. Materials and Methods: Five New Zealand laboratory rabbits were anesthetized with 1 cc Ketamine and Xilosine intramuscularly in thigh site. Electrodes were attached to the palms and wrists. Then, 0.2 cc lidocain 2% was injected in forearm origin in order to block median proximal nerve in both forelegs. The nerves conduction study (NCS) was recorded before and after lidocain injection, plus 30 min and once again 1 h after calcium gloconate 10%, dextrose 50%, citric acid solution injection. The recorded data were analyzed using Wilcoxon test and using SPSS software (version 11.5) at significant level of 0.05. Results: The NCS of left and right forearms was 1.4 ± 1.35 mV and 0.48 ± 0.45 mV. According to the statistical test, there was no significant difference between two groups (P > 0.05). Conclusion: Calcium gloconate 10%, dextrose 50%, citric acid solution did not reverse the effect of anesthetic drugs. Possible reasons were pressure to the nerves, which were caused by drug volume, and low sample size. PMID:25886425

  17. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis

    PubMed Central

    Pandit, Ashlesha P.; Pol, Vaibhav V.; Kulkarni, Vinit S.

    2016-01-01

    The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y1) and drug release (Y2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure. PMID:27034908

  18. The effect of lidocaine on regional blood flows and cardiac output in the non-stressed and the stressed foetal lamb.

    PubMed

    Friesen, C; Yarnell, R; Bachman, C; Meatheral, R; Biehl, D

    1986-03-01

    Lidocaine has been used in obstetrical anaesthesia for many years but there are still concerns about possible adverse affects of this drug on the foetus in utero. To examine in greater detail the effects of lidocaine in the foetus, the following two-part study was done. In Part A, seven pregnant ewes were surgically prepared with maternal and foetal arterial and venous catheters. After recovery from surgery lidocaine was infused intravenously, initially into the ewe and then into both ewe and foetus. Blood lidocaine concentrations were monitored and foetal regional blood flows were determined by the radioactive microsphere method. In Part B, 14 ewes were prepared as in Part A with the addition of an inflatable loop around the umbilical cord. During each study the loop was inflated to partially compress the cord and produce foetal acidosis. In all animals this cord compression was maintained for 30 minutes. In seven animals a lidocaine infusion was given, to examine the effect of lidocaine in the acidotic foetus. Organ blood flows were measured and cardiac outputs calculated. The normal foetuses in Part A showed no change in organ blood flow or cardiac output with arterial lidocaine concentrations of 1.5-3.4 mg X ml-1. In the acidotic foetuses, lidocaine concentrations of 1.4-1.5 mg X ml-1 produced a tachycardia and an increase in cerebral blood flow compared to the control acidotic foetuses. There were no other significant changes. We conclude that arterial lidocaine concentrations of less than 3.5 mg X ml-1 do not produce significant alterations in organ blood flow in normal foetal lambs.(ABSTRACT TRUNCATED AT 250 WORDS)

  19. Comparison of Gating Properties and Use-Dependent Block of Nav1.5 and Nav1.7 Channels by Anti-Arrhythmics Mexiletine and Lidocaine.

    PubMed

    Wang, Ying; Mi, Jianxun; Lu, Ka; Lu, Yanxin; Wang, KeWei

    2015-01-01

    Mexiletine and lidocaine are widely used class IB anti-arrhythmic drugs that are considered to act by blocking voltage-gated open sodium currents for treatment of ventricular arrhythmias and relief of pain. To gain mechanistic insights into action of anti-arrhythmics, we characterized biophysical properties of Nav1.5 and Nav1.7 channels stably expressed in HEK293 cells and compared their use-dependent block in response to mexiletine and lidocaine using whole-cell patch clamp recordings. While the voltage-dependent activation of Nav1.5 or Nav1.7 was not affected by mexiletine and lidocaine, the steady-state fast and slow inactivation of Nav1.5 and Nav1.7 were significantly shifted to hyperpolarized direction by either mexiletine or lidocaine in dose-dependent manner. Both mexiletine and lidocaine enhanced the slow component of closed-state inactivation, with mexiletine exerting stronger inhibition on either Nav1.5 or Nav1.7. The recovery from inactivation of Nav1.5 or Nav1.7 was significantly prolonged by mexiletine compared to lidocaine. Furthermore, mexiletine displayed a pronounced and prominent use-dependent inhibition of Nav1.5 than lidocaine, but not Nav1.7 channels. Taken together, our findings demonstrate differential responses to blockade by mexiletine and lidocaine that preferentially affect the gating of Nav1.5, as compared to Nav1.7; and mexiletine exhibits stronger use-dependent block of Nav1.5. The differential gating properties of Nav1.5 and Nav1.7 in response to mexiletine and lidocaine may help explain the drug effectiveness and advance in new designs of safe and specific sodium channel blockers for treatment of cardiac arrhythmia or pain.

  20. Lidocaine concentration in mandibular bone after subperiosteal infiltration anesthesia decreases with elevation of periosteal flap and irrigation with saline.

    PubMed

    Ogawa, Sachie; Watanabe, Masahiro; Kawaai, Hiroyoshi; Tada, Hitoshi; Yamazaki, Shinya

    2014-01-01

    It has been reported that the action of infiltration anesthesia on the jawbone is attenuated significantly by elevation of the periosteal flap with saline irrigation in clinical studies; however, the reason is unclear. Therefore, the lidocaine concentration in mandibular bone after subperiosteal infiltration anesthesia was measured under several surgical conditions. The subjects were 48 rabbits. Infiltration anesthesia by 0.5 mL of 2% lidocaine with 1 : 80,000 epinephrine (adrenaline) was injected into the right mandibular angle and left mandibular body, respectively. Under several surgical conditions (presence or absence of periosteal flap, and presence or absence of saline irrigation), both mandibular bone samples were removed at a fixed time after subperiosteal infiltration anesthesia. The lidocaine concentration in each mandibular bone sample was measured by high-performance liquid chromatography. As a result, elevation of the periosteal flap with saline irrigation significantly decreased the lidocaine concentration in the mandibular bone. It is suggested that the anesthetic in the bone was washed out by saline irrigation. Therefore, supplemental conduction and/or general anesthesia should be utilized for long operations that include elevation of the periosteal flap with saline irrigation.

  1. Validation of a Thin-Layer Chromatography for the Determination of Hydrocortisone Acetate and Lidocaine in a Pharmaceutical Preparation

    PubMed Central

    Dołowy, Małgorzata; Kulpińska-Kucia, Katarzyna; Pyka, Alina

    2014-01-01

    A new specific, precise, accurate, and robust TLC-densitometry has been developed for the simultaneous determination of hydrocortisone acetate and lidocaine hydrochloride in combined pharmaceutical formulation. The chromatographic analysis was carried out using a mobile phase consisting of chloroform + acetone + ammonia (25%) in volume composition 8 : 2 : 0.1 and silica gel 60F254 plates. Densitometric detection was performed in UV at wavelengths 200 nm and 250 nm, respectively, for lidocaine hydrochloride and hydrocortisone acetate. The validation of the proposed method was performed in terms of specificity, linearity, limit of detection (LOD), limit of quantification (LOQ), precision, accuracy, and robustness. The applied TLC procedure is linear in hydrocortisone acetate concentration range of 3.75 ÷ 12.50 μg·spot−1, and from 1.00 ÷ 2.50 μg·spot−1 for lidocaine hydrochloride. The developed method was found to be accurate (the value of the coefficient of variation CV [%] is less than 3%), precise (CV [%] is less than 2%), specific, and robust. LOQ of hydrocortisone acetate is 0.198 μg·spot−1 and LOD is 0.066 μg·spot−1. LOQ and LOD values for lidocaine hydrochloride are 0.270 and 0.090 μg·spot−1, respectively. The assay value of both bioactive substances is consistent with the limits recommended by Pharmacopoeia. PMID:24526880

  2. Effects of lidocaine injections into the lateral parabrachial nucleus on dipsogenic and pressor response to central angiotensin 2 in rats

    NASA Technical Reports Server (NTRS)

    Menani, Jose Vanderlei; Beltz, Terry G.

    1995-01-01

    This study investigated the effects of bilateral injections of the local anesthetic, lidocaine, into the lateral parabrachial nucleus (LPBN) on the dipsogenic and pressor responses induced by intracerebroventricular (i.c.v.) injection of angiotensin 2 (ANG 2). Centrally injected ANG 2 (50 ng/1 microliter) induced water intake ( IO.2 +/- 0.8 ml/h) and pressor responses (22 +/- 1 mmHg). Prior bilateral injection of 10% lidocaine (200 nl) into the LPBN increased the water intake (14.2 +/- 1.4 ml/h), but did not change the pressor response (17 +/- 1 mmHg) to i.c.v. ANG 2. Lidocaine alone injected into the LPBN also induced a pressor response (23 +/- 3 mmHg). These results showing that bilateral LPBN injection of lidocaine increase water intake induced bv i.c.v. ANG 2 are consistent with electrolytic and neurotoxic lesion studies and suggest that the LPBN is associated with inhibitory mechanisms controlling water intake induced by ANG 2. These results also provide evidence that it is feasible to reversibly anesthetize this brain area to facilitate fluid-related ingestive behavior.

  3. Effect of intraoperative intravenous lidocaine on postoperative pain and return of bowel function after laparoscopic abdominal gynecologic procedures.

    PubMed

    Grady, Philip; Clark, Nathaniel; Lenahan, John; Oudekerk, Christopher; Hawkins, Robert; Nezat, Greg; Pellegrini, Joseph E

    2012-08-01

    Abdominal surgery has a high incidence of postoperative pain and dysfunctional gastrointestinal motility. This study investigated the effect of a continuous intraoperative infusion of lidocaine on patients undergoing laparoscopic gynecologic surgery. In this double-blind, placebo-controlled investigation, 50 subjects were randomly assigned to control and experimental groups. Both groups received an intravenous lidocaine bolus of 1 mg/kg on induction. The experimental group received a continuous lidocaine infusion of 2 mg/kg/h, initiated following induction and discontinued 15 to 30 minutes before skin closure. Controls received a placebo infusion. Patients in the experimental group had lower postoperative day 3 pain scores using a verbal analog scale (P = .02). Morphine equivalent dose at second request for pain treatment in the postoperative anesthesia care unit was lower in the experimental group (P = .02). There was a statistically significant difference in time interval from surgical start to return of first flatus between the groups (P = .02). Data were analyzed using descriptive and inferential statistics. A P value less than .05 was considered significant. These study results are consistent with previous research suggesting that intraoperative lidocaine infusion may improve postoperative pain levels and may shorten the time to return of bowel function.

  4. Clinical assessment of epidural analgesia induced by xylazine-lidocaine combination accompanied by xylazine sedation in calves

    PubMed Central

    2005-01-01

    The aim of the present study was to investigate whether epidural administration of a xylazine-lidocaine combination accompanied by xylazine sedation would provide satisfactory analgesia for some surgical procedures on 10 calves admitted to the Department of Veterinary Surgery, University of Kafkas with perineal urolithiasis (n:2), rectovaginal fistula (n:1), atresia ani (n:2), omphalophlebitis (n:2), omphaloarteritis (n:1) and umbilical hernia (n:2). Following intramuscular injection of xylazine at a dose of 0.05 mg/kg for sedation, xylazine-lidocaine combination (0.2 mg/kg lidocaine + 0.02 mg/kg xylazine + 5 ml 0.9% NaCl) was administrated into the lumbosacral (L6-S1), sacrococcygeal (S5-Co1) or intercoccygeal (Co1-Co2) space. Heart rate, respiratory rate and rectal temperature were recorded prior to and during analgesia at 5, 10, 15, 30 and 60 minutes. Furthermore, depth and duration of analgesia were evaluated during surgical intervention. The study revealed that the combination of epidural xylazine-lidocaine with xylazine sedation was highly satisfactory for surgery of the lower urinary tract and the perineal region, but it was less so for surgery of the umbilical area. PMID:21851664

  5. [The effect of antihypertensive drugs on the anaesthetic effect of lidocaine in hypertensive patients who need dental treatment].

    PubMed

    Grădinaru, Irina; Grădinaru, Marilena; Ghiciuc, Cristina Mihaela; Nechifor, M; Tatarciuc, Monica; Dimitriu, G; Doloca, A

    2005-01-01

    The study evaluated the influence of atenolol/nifedipine on the local anaesthesia with lidocaine in 64 patients with essential arterial hypertension following dietetic regimen and divided in: control group (21 patients), atenolol-treated group (21 patients with atenolol therapy) and nifedipine-treated group (22 patients with nifedipine therapy). Atenolol/nifedipine was administrated three hours before anaesthesia (1.5 mg lidocaine/kg body weight) applied on Spix Spina. The atenolol/nifedipine influence on the anaesthetic intensity was evaluated both by the patient and dentist using scales for the appreciation of pain intensity (Visual Analogue Scale, Numerical Rating Scale) at 0 minutes (before anaesthesia), 5, 10, 20, 30, 60 minutes (moments for the determination of lidocaine plasmatic concentrations). There were no statistically significant differences between the values appreciated by the patient and dentist. Our data demonstrated a significant decrease of pain intensity in patients treated with atenolol/nifedipine. Very good inverse correlation was found between lidocaine concentrations and pain intensity.

  6. The Local Pharmacokinetics of 3H-Ropivacaine and 14C-Lidocaine After Maxillary Infiltration Anesthesia in Rats

    PubMed Central

    Kimi, Hiromi; Yamashiro, Mikiko; Hashimoto, Shuichi

    2012-01-01

    The effects of infiltration anesthesia with ropivacaine on the dental pulp are considered to be weak. This may be partly associated with its permeation into the oral tissue. With the objective of investigating the local pharmacokinetics of ropivacaine and lidocaine following infiltration anesthesia, we injected 3H-ropivacaine or 14C-lidocaine to the palatal mucosa in rats, measured distributions of radioactivity in the maxilla, and compared the local pharmacokinetics of these agents. The animals were sacrificed at various times and the maxillas were removed. The palatal mucosa and maxillary nerve were resected, and the bone was divided into 6 portions. We measured radioactivity in each tissue and calculated the level of each local anesthetic (n  =  8). Lidocaine diffused to the surrounding tissue immediately after the injection, whereas ropivacaine tended to remain in the palatal mucosa for a longer period. Lidocaine showed a higher affinity for the maxillary bone than ropivacaine. There was a correlation between the distribution level of local anesthetics in the maxillary bone and that in the maxillary nerve. The lower-level effects of infiltration anesthesia with ropivacaine on the dental pulp may be because ropivacaine has a high affinity for soft tissue, and its transfer to bone is slight. PMID:22822994

  7. The local pharmacokinetics of ³H-ropivacaine and ¹⁴C-lidocaine after maxillary infiltration anesthesia in rats.

    PubMed

    Kimi, Hiromi; Yamashiro, Mikiko; Hashimoto, Shuichi

    2012-01-01

    The effects of infiltration anesthesia with ropivacaine on the dental pulp are considered to be weak. This may be partly associated with its permeation into the oral tissue. With the objective of investigating the local pharmacokinetics of ropivacaine and lidocaine following infiltration anesthesia, we injected (3)H-ropivacaine or (14)C-lidocaine to the palatal mucosa in rats, measured distributions of radioactivity in the maxilla, and compared the local pharmacokinetics of these agents. The animals were sacrificed at various times and the maxillas were removed. The palatal mucosa and maxillary nerve were resected, and the bone was divided into 6 portions. We measured radioactivity in each tissue and calculated the level of each local anesthetic (n  =  8). Lidocaine diffused to the surrounding tissue immediately after the injection, whereas ropivacaine tended to remain in the palatal mucosa for a longer period. Lidocaine showed a higher affinity for the maxillary bone than ropivacaine. There was a correlation between the distribution level of local anesthetics in the maxillary bone and that in the maxillary nerve. The lower-level effects of infiltration anesthesia with ropivacaine on the dental pulp may be because ropivacaine has a high affinity for soft tissue, and its transfer to bone is slight.

  8. Intra-articular administration of lidocaine in anaesthetized dogs: pharmacokinetic profile and safety on cardiovascular and nervous systems.

    PubMed

    Di Salvo, A; Bufalari, A; De Monte, V; Cagnardi, P; Marenzoni, M L; Catanzaro, A; Vigorito, V; Della Rocca, G

    2015-08-01

    The intra-articular administration of lidocaine is a frequent practice in human orthopaedic surgical procedures, but an eventual absorption of the drug into the bloodstream can lead to toxicity, mainly concerning the central nervous system and the cardiovascular systems. The purpose of this study was to determine the pharmacokinetic profile and the safety, in terms of cardiovascular and CNS toxicity, of lidocaine after intra-articular administration to anesthetized dogs undergoing arthroscopy. Lidocaine 2% was administered to eight dogs before surgery in differing amounts, depending on the volume of the joints involved, and blood samples were taken at predetermined time points. The maximum serum concentration of lidocaine ranged from 0.50 to 3.01 μg/mL (mean ± SD: 2.18 ± 0.91 μg/mL), and the time to reach it was 28.75 ± 15.74 min. No signs of cardiac toxicity were detected during the entire procedure, and possible signs of CNS toxicity were masked by the anaesthesia. However, concentrations reported in literature as responsible for neurotoxicity in dog were achieved in three of eight investigated subjects. Pending further studies, veterinarians should consider the possibility of side effects occurring following the intra-articular administration of local anaesthetics.

  9. The effects of adding epinephrine or xylazine to lidocaine solution for lumbosacral epidural analgesia in fat-tailed sheep.

    PubMed

    Rostami, Maryam; Vesal, Nasser

    2012-03-02

    This blinded, randomised experimental study was designed to compare the analgesic effects of lumbosacral epidural administration of lidocaine-epinephrine or lidocaine-xylazine combinations in fat-tailed sheep. Nine healthy fat-tailed male lambs (mean ± s.d. age, 4.6 ± 0.4 months; weight, 24.6 kg ± 2.5 kg) were randomly allocated into four groups of six sheep: lidocaine 2% (LID), lidocaine-epinephrine 5 µg/mL (LIDEP), lidocaine-xylazine 0.05 mg/kg (LIDXY) or bupivacaine 0.5% (BUP). The onset and duration of flank, perineum and hindlimb anaesthesia and the onset and duration of hindlimb paralysis were recorded. Epidural administration of LID, LIDEP, LIDXY or BUP produced anaesthesia within 6.6 min, 7.6 min, 3.4 min and 8.4 min, respectively. The mean onset of anaesthesia in the LIDXY group was significantly shorter compared with the BUP group (p = 0.02). The mean duration of anaesthesia was 107.9 min, 190.4 min, 147.6 min and 169.7 min for LID, LIDEP, LIDXY and BUP, respectively. The onset of hindlimb paralysis was faster in the LIDXY group than in the BUP group; however, the duration of hindlimb paralysis was shorter in LIDXY compared with LIDEP. Epidural administration of LIDEP or LIDXY provides a comparable duration of local anaesthesia without any adverse effects in fat-tailed sheep. Epidural LIDXY did not appear to be advantageous over epidural LIDEP.

  10. Echinacea/sage or chlorhexidine/lidocaine for treating acute sore throats: a randomized double-blind trial

    PubMed Central

    2009-01-01

    Background The aim of this trial was to assess the relative efficacy of a sage/echinacea spray and a chlorhexidine/lidocaine spray in the treatment of acute sore throats. Methods This was a multicenter, randomized, double-blind, double-dummy controlled trial carried out in eleven general practices in Switzerland. A total of 154 patients (133 analyzed in per protocol collective) at least 12 years old with acute sore throat present for not more than 72 hours prior to inclusion and with a throat score ≥6 participated in the study. They used either an echinacea/sage spray or a chlorhexidine/lidocaine spray with two puffs every 2 hours, in a double-dummy blinded manner, up to 10 times daily until they were symptom-free, for a maximum of 5 days. The main outcome measures was the comparison of response rates during the first three days. A response was defined as a decrease of at least 50% of the total symptoms compared to baseline. Results The echinacea/sage treatment exhibited similar efficacy to the chlorhexidine/lidocaine treatment in reducing sore throat symptoms during the first 3 days (P(x < Y) = .5083). Response rates after 3 days were 63.8% in the echinacea/sage group and 57.8% in the chlorhexidine/lidocaine group. For all secondary parameters, such as time to becoming symptom free, throat pain, and global assessments of efficacy by the physician and patient, no difference between the two treatments was seen. They were both very well tolerated. Conclusion An echinacea/sage preparation is as efficacious and well tolerated as a chlorhexidine/lidocaine spray in the treatment of acute sore throats. PMID:19748859

  11. Comparison of the efficacy of intrauterine lidocaine, paracervical block and oral etodolac for decreasing pain in endometrial biopsy

    PubMed Central

    Güler, Ayşe; Şahin, H. Güler; Küçükaydın, Zehra; Erdemoğlu, Evrim

    2010-01-01

    Objective To compare the effectiveness of paracervical block, intrauterine lidocaine and oral etodolac in decreasing the pain caused by pipelle endometrial sampling. A secondary goal of this study was to determine the adverse effects and compare possible effects of these methods on pulse and blood pressure. Material and Methods The study was performed between April 2006 and October 2006 in the Obstetrics and Gynecology Department of Van Yüzüncü Yıl University Research Hospital. One-hundred twenty patients were randomized into four groups: 1. Group: Paracervical block was performed with 3 ml 2% prilocaine solution. 2. Group: Five ml of 2% lidocaine solution was instilled through the endocervix into the uterine cavity. 3. Group: Subjects received 400 mg oral etodolac tablet 1–1.5 hour before the procedure. 4. Group: No method of anesthesia was used in the control group. Endometrial sampling was performed with pipelle. Severity of pain during the procedure was scored by the subjects according to the “6-point Verbal Rating Scale (VRS)”. Blood pressure and pulse rate were measured before, during and 30 minutes after the procedure. Results Pain scores in intrauterine lidocaine group (2nd group) were found statistically significantly lower than the other three groups (p<0.05). Conclusion Intrauterine lidocaine anesthesia technique decreases pain in endometrial sampling with pipelle more efficiently than paracervical block or oral etodolac. While indication of menorrhagia and endometrial thickness more than 5 mm increased pain scores, intrauterine lidocaine application or paracervical block decreased the scores significantly (p<0.05). PMID:24591932

  12. Relaxation of tracheal smooth muscle independent on functional epithelium cells induced by lidocaine, bupivacaine and isomers in rats.

    PubMed

    Lautner, Roberto Q; Zapata-Sudo, Gisele; Sudo, Roberto T

    2009-05-21

    Lidocaine is a local anesthetic which has been used to protect spasm reaction during tracheal intubation and bronchoscopy. We compared the potency of lidocaine, bupivacaine (RS(+/-)-bupivacaine) and isomers (S(-)-bupivacaine and R(+)-bupivacaine) to promote relaxation of tracheal smooth muscle. Relaxation of airways smooth muscle can be dependent on the release of relaxing factors by epithelium such as prostanoids and nitric oxide (NO). Possible mechanisms involved in the tracheal smooth muscle relaxation induced by these local anesthetics were evaluated in preparation in which the epithelium layer was intact or denuded. Bupivacaine and its isomers were approximately six to eleven-fold more potent than lidocaine to promote relaxation on acetylcholine-induced contraction in tracheal rings. The concentration of lidocaine, RS(+/-)-bupivacaine, S(-)-bupivacaine and R(+)-bupivacaine necessary to produce a 50% reduction of maximal contraction to acetylcholine (IC(50)) in tracheal rings with intact epithelium was 1.25+/-0.01, 0.11+/-0.01, 0.15+/-0.01, 0.19+/-0.01 mM, respectively. Removal of epithelium or exposure to N(G)-nitro-L-arginine methyl ester, indomethacin did not alter the IC(50). However, calcium influx of depolarized tracheal smooth muscle was inhibited by lidocaine, bupivacaine and isomers. S(-)-bupivacaine reduced by 78.8+/-7.4% the calcium influx followed by RS(+/-)-bupivacaine (41.8+/-6.7%) and R(+)-bupivacaine (25.6+/-9.5%). In conclusion, local anesthetic action was stereoselective and partially dependent on blockade of Ca(2+) influx to muscular cells. The isomer S(-)-bupivacaine is more potent and less toxic which could represent a valuable clinical advantage to use as broncholitic agent.

  13. Transplacental Distribution of Lidocaine and Its Metabolite in Peridural Anesthesia Administered to Patients With Gestational Diabetes Mellitus

    PubMed Central

    Duarte, Luciana de Barros; Cavalli, Ricardo de Carvalho; Carvalho, Daniela Miarelli; Filgueira, Gabriela Campos de Oliveira; Marques, Maria Paula; Lanchote, Vera Lucia; Duarte, Geraldo

    2015-01-01

    Background: Neonatal effects of drugs administered to mothers before delivery depend on the quantity that crosses the placental barrier, which is determined by the pharmacokinetics of the drug in the mother, fetus, and placenta. Diabetes mellitus can alter the kinetic disposition and the metabolism of drugs. This study investigated the placental transfer of lidocaine and its metabolite monoethylglycinexylidide (MEGX) in pregnant women with gestational diabetes mellitus (GDM) submitted to peridural anesthesia. Patients and Methods: A total of 10 normal pregnant women (group 1) and 6 pregnant women with GDM (group 2) were studied, all at term. The patients received 200 mg 2% lidocaine hydrochloride by the peridural locoregional route. Maternal blood samples were collected at the time of delivery and, after placental expulsion, blood samples were collected from the intervillous space, umbilical artery, and vein for determination of lidocaine and MEGX concentrations and analysis of the placental transfer of the drug. Results: The following respective lidocaine ratios between the maternal and the fetal compartments were obtained for groups 1 and 2: umbilical vein/maternal peripheral blood, 0.60 and 0.46; intervillous space/maternal blood, 1.01 and 0.88; umbilical artery/umbilical vein, 0.77 and 0.91; and umbilical vein/intervillous space, 0.53 and 0.51. The following MEGX ratios for groups 1 and 2 were, respectively, fetal/maternal, 0.43 and 0.97; intervillous space/maternal blood, 0.64 and 0.90; umbilical artery/umbilical vein, 1.09 and 0.99; and umbilical vein/intervillous space, 0.55 and 0.78. Conclusion: Gestational diabetes mellitus did not affect the transplacental transfer of lidocaine but interfered with the transfer of MEGX, acting as a mechanism facilitating the transport of the metabolite. PMID:25563756

  14. Pregabalin, the lidocaine plaster and duloxetine in patients with refractory neuropathic pain: a systematic review

    PubMed Central

    2010-01-01

    Background Patients frequently fail to receive adequate pain relief from, or are intolerant of, first-line therapies prescribed for neuropathic pain (NeP). This refractory chronic pain causes psychological distress and impacts patient quality of life. Published literature for treatment in refractory patients is sparse and often published as conference abstracts only. The aim of this study was to identify published data for three pharmacological treatments: pregabalin, lidocaine plaster, and duloxetine, which are typically used at 2nd line or later in UK patients with neuropathic pain. Methods A systematic review of the literature databases MEDLINE, EMBASE and CCTR was carried out and supplemented with extensive conference and grey literature searching. Studies of any design (except single patient case studies) that enrolled adult patients with refractory NeP were included in the review and qualitatively assessed. Results Seventeen studies were included in the review: nine of pregabalin, seven of the lidocaine plaster, and one of duloxetine. No head-to-head studies of these treatments were identified. Only six studies included treatments within UK licensed indications and dose ranges. Reported efficacy outcomes were not consistent between studies. Pain scores were most commonly assessed in studies including pregabalin; trials of pregabalin and the lidocaine plaster reported the proportion of responders. Significant improvements in the total, sensory and affective scores of the Short-form McGill Pain Questionnaire, and in function interference, sleep interference and pain associated distress, were associated with pregabalin treatment; limited or no quality of life data were available for the other two interventions. Limitations to the review are the small number of included studies, which are generally small, of poor quality and heterogeneous in patient population and study design. Conclusions Little evidence is available relevant to the treatment of refractory

  15. C-fiber spontaneous discharge evoked by chronic inflammation is suppressed by a long-term infusion of lidocaine yielding nanogram per milliliter plasma levels.

    PubMed

    Xiao, Wen Hua; Bennett, Gary J

    2008-07-01

    Nociceptors innervating inflamed tissue acquire an abnormal spontaneous discharge that is believed to be at least part of the reason for the persistent spontaneous pain, allodynia, and hyperalgesia that accompany inflammation. Recent studies suggest that patients with chronic inflammatory pain may obtain an analgesic effect with transdermal application of lidocaine that yields very low plasma levels (130-225 ng/ml). The aim of this study was to investigate whether a 7-day exposure to such low plasma levels of lidocaine had an effect on inflammation-evoked spontaneous discharge in the rat. Seven days after a hind-paw injection of Complete Freund's Adjuvant (CFA), we confirmed the presence of myositis, pain hypersensitivity, and a significant increase in the incidence of spontaneous discharge in A-fibers and C-fibers innervating both muscle and skin. We then compared the incidence of spontaneous discharge in muscle and cutaneous fibers in CFA-injected animals treated with a 7-day infusion of saline or lidocaine. The lidocaine infusion yielded a plasma level of 210 ng/ml. The muscle C-fiber discharge was completely inhibited by the lidocaine infusion and the cutaneous C-fiber discharge was suppressed by 50%. Lidocaine infusion had no effect on the incidence of spontaneous discharge in muscle or cutaneous A-fibers. Lidocaine infusion reduced mechano-hyperalgesia but had no effect on mechano-allodynia or heat-hyperalgesia. We conclude that the analgesic effects seen clinically with transdermal lidocaine administration yielding low plasma levels may be due to a systemic drug action on spontaneously active C-fibers.

  16. Buffered lidocaine and bupivacaine mixture – the ideal local anesthetic solution?

    PubMed Central

    Best, Corliss A; Best, Alyssa A; Best, Timothy J; Hamilton, Danielle A

    2015-01-01

    The use of injectable local anesthetic solutions to facilitate pain-free surgery is an integral component of many procedures performed by the plastic surgeon. In many instances, a solution that has both rapid onset and prolonged duration of analgesia is optimal. A combination of lidocaine and bupivacaine, plain or with epinephrine, is readily available in most Canadian health care settings where such procedures are performed, and fulfills these criteria. However, commercially available solutions of both medications are acidic and cause a burning sensation on injection. Buffering to neutral pH with sodium bicarbonate is a practical method to mitigate the burning sensation, and has the added benefit of increasing the fraction of nonionized lipid soluble drug available. The authors report on the proportions of the three drugs to yield a neutral pH, and the results of an initial survey regarding the use of the combined solution with epinephrine in hand surgery. PMID:26090348

  17. Hypoesthesia after IAN block anesthesia with lidocaine: management of mild to moderate nerve injury

    PubMed Central

    Moon, Sungjoo; Lee, Seung-Jong; Kim, Euiseong

    2012-01-01

    Hypoesthesia after an inferior alveolar nerve (IAN) block does not commonly occur, but some cases are reported. The causes of hypoesthesia include a needle injury or toxicity of local anesthetic agents, and the incidence itself can cause stress to both dentists and patients. This case presents a hypoesthesia on mental nerve area followed by IAN block anesthesia with 2% lidocaine. Prescription of steroids for a week was performed and periodic follow up was done. After 1 wk, the symptoms got much better and after 4 mon, hypoesthesia completely disappeared. During this healing period, only early steroid medication was prescribed. In most cases, hypoesthesia is resolved within 6 mon, but being aware of etiology and the treatment options of hypoesthesia is important. Because the hypoesthesia caused by IAN block anesthesia is a mild to moderate nerve injury, early detection of symptom and prescription of steroids could be helpful for improvement of the hypoesthesia. PMID:23430216

  18. Guest:host interactions of lidocaine and prilocaine with natural cyclodextrins: Spectral and molecular modeling studies

    NASA Astrophysics Data System (ADS)

    Rajendiran, N.; Mohandoss, T.; Saravanan, J.

    2014-11-01

    Inclusion complex formation of two local anesthetics drugs (lidocaine (LC) and prilocaine (PC)) with α- and β-cyclodextrins (CDs) in aqueous solution were studied by absorption, fluorescence, time-resolved fluorescence and molecular modeling methods. The formation of inclusion complexes was confirmed by 1H NMR, FTIR, differential scanning calorimetry, SEM, TEM and X-ray diffractometry. Both drugs formed 1:1 inclusion complex and exhibit biexponential decay in water whereas triexponential decay in the CD solution. Nanosized self-aggregated particles of drug: CD complexes were found by TEM. Both experimental and theoretical studies revealed that the phenyl ring with the amide group of the drug is encapsulated in the hydrophobic CD nanocavity. Investigations of energetic and thermodynamic properties confirmed the stability of the inclusion complexes. van der Waals interactions are mainly responsible for enthalpy driven complex formation of LC and PC with CDs.

  19. Solid-phase synthesis of lidocaine and procainamide analogues using backbone amide linker (BAL) anchoring.

    PubMed

    Shannon, Simon K; Peacock, Mandy J; Kates, Steven A; Barany, George

    2003-01-01

    New solid-phase strategies have been developed for the synthesis of lidocaine (1) and procainamide (2) analogues, using backbone amide linker (BAL) anchoring. Both sets were prepared starting from a common resin-bound intermediate, followed by four general steps: (i) attachment of a primary aliphatic or aromatic amine to the solid support via reductive amination (as monitored by a novel test involving reaction of 2,4-dinitrophenylhydrazine with residual aldehyde groups); (ii) acylation of the resultant secondary amine; (iii) displacement of halide with an amine; and (iv) trifluoroacetic acid-mediated release from the support. A manual parallel strategy was followed to provide 60 novel compounds, of which two dozen have not been previously described. In most cases, initial crude purities were >80%, and overall isolated yields were in the 40-88% range.

  20. The lidocaine metabolite N-ethylglycine has antinociceptive effects in experimental inflammatory and neuropathic pain

    PubMed Central

    Werdehausen, Robert; Mittnacht, Sebastian; Bee, Lucy A.; Minett, Michael S.; Armbruster, Anja; Bauer, Inge; Wood, John N.; Hermanns, Henning; Eulenburg, Volker

    2015-01-01

    Abstract Glycine transporter 1 (GlyT1) plays a crucial role in regulating extracellular glycine concentrations and might thereby constitute a new drug target for the modulation of glycinergic inhibition in pain signaling. Consistent with this view, inhibition of GlyT1 has been found to induce antinociceptive effects in various animal pain models. We have shown previously that the lidocaine metabolite N-ethylglycine (EG) reduces GlyT1-dependent glycine uptake by functioning as an artificial substrate for this transporter. Here, we show that EG is specific for GlyT1 and that in rodent models of inflammatory and neuropathic pain, systemic treatment with EG results in an efficient amelioration of hyperalgesia and allodynia without affecting acute pain. There was no effect on motor coordination or the development of inflammatory edema. No adverse neurological effects were observed after repeated high-dose application of EG. EG concentrations both in blood and spinal fluid correlated with an increase of glycine concentration in spinal fluid. The time courses of the EG and glycine concentrations corresponded well with the antinociceptive effect. Additionally, we found that EG reduced the increase in neuronal firing of wide-dynamic-range neurons caused by inflammatory pain induction. These findings suggest that systemically applied lidocaine exerts antihyperalgesic effects through its metabolite EG in vivo, by enhancing spinal inhibition of pain processing through GlyT1 modulation and subsequent increase of glycine concentrations at glycinergic inhibitory synapses. EG and other substrates of GlyT1, therefore, may be a useful therapeutic agent in chronic pain states involving spinal disinhibition. PMID:25932687

  1. Masking the bitter taste of injectable lidocaine HCl formulation for dental procedures.

    PubMed

    Wei, Yangjie; Nedley, Michael P; Bhaduri, Sarit B; Bredzinski, Xavier; Boddu, Sai H S

    2015-04-01

    Several attempts have been made to mask the bitter taste of oral formulations, but none have been made for injectable formulations. This study aims to mask the bitter taste of dental lidocaine HCl (LID) injection using hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium saccharin. Inclusion complexes of LID and HP-β-CD were prepared by the solution method in 1:1 and 1:2 M ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (pH 8, 9, and 10). Freeze-dried inclusion complexes were characterized using differential scanning calorimetry (DSC), X-ray, Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), and in vitro release. Injectable formulations were prepared using inclusion complexes and characterized for stability and for taste using an Alpha MOS ASTREE electronic tongue (ETongue). The association constants of HP-β-CD with lidocaine-free base and its ionized form were found to be 26.23 ± 0.00025 and 0.8694 ± 0.00045 M(-1), respectively. Characterization studies confirmed the formation of stable inclusion complexes of LID and HP-β-CD. Injectable formulations were found to be stable for up to 6 months at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-β-CD (1:1 and 1:2 M ratios) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 M ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.

  2. Permeation and block of TRPV1 channels by the cationic lidocaine derivative QX-314.

    PubMed

    Puopolo, Michelino; Binshtok, Alexander M; Yao, Gui-Lan; Oh, Seog Bae; Woolf, Clifford J; Bean, Bruce P

    2013-04-01

    QX-314 (N-ethyl-lidocaine) is a cationic lidocaine derivative that blocks voltage-dependent sodium channels when applied internally to axons or neuronal cell bodies. Coapplication of external QX-314 with the transient receptor potential vanilloid 1 protein (TRPV1) agonist capsaicin produces long-lasting sodium channel inhibition in TRPV1-expressing neurons, suggestive of QX-314 entry into the neurons. We asked whether QX-314 entry occurs directly through TRPV1 channels or through a different pathway (e.g., pannexin channels) activated downstream of TRPV1 and whether QX-314 entry requires the phenomenon of "pore dilation" previously reported for TRPV1. With external solutions containing 10 or 20 mM QX-314 as the only cation, inward currents were activated by stimulation of both heterologously expressed and native TRPV1 channels in rat dorsal root ganglion neurons. QX-314-mediated inward current did not require pore dilation, as it activated within several seconds and in parallel with Cs-mediated outward current, with a reversal potential consistent with PQX-314/PCs = 0.12. QX-314-mediated current was no different when TRPV1 channels were expressed in C6 glioma cells, which lack expression of pannexin channels. Rapid addition of QX-314 to physiological external solutions produced instant partial inhibition of inward currents carried by sodium ions, suggesting that QX-314 is a permeant blocker. Maintained coapplication of QX-314 with capsaicin produced slowly developing reduction of outward currents carried by internal Cs, consistent with intracellular accumulation of QX-314 to concentrations of 50-100 μM. We conclude that QX-314 is directly permeant in the "standard" pore formed by TRPV1 channels and does not require either pore dilation or activation of additional downstream channels for entry.

  3. Simultaneous determination of tolperisone and lidocaine by high performance liquid chromatography.

    PubMed

    Liawruangrath, S; Liawruangrath, B; Pibool, P

    2001-12-01

    A reversed phase high performance liquid chromatographic (RP-HPLC) method for the simultaneous determination of tolperisone (TP) and lidocaine (LD) has been developed. The drugs were separated on a column (4.60 x 250 mm(2)) Spherisorb ODS (5 microm) using 5.5% triethylamine in 70/30 v/v acetonitrile/water as mobile phase 0.7 ml min(-1)and UV detection at 254 nm. The detection limits for Tolperisone hydrochloride (TP-HCl) and lidocaine hydrochloride (LD-HCl) were 0.20 ng/20 microl and 100 ng/20 microl and the quantitation limits were 0.50 ng/20 microl and 250 ng/20 microl, respectively. Linear calibration curves over the ranges of 1-10, 10-100 and 150-500 microg ml(-1) for TP-HCl and 10-500 microg ml(-1) for LD-HCl were established. Different calibration slopes were found for TP probably owing to changes in refractive index due to increase in TP concentration. The average recoveries of the added TP in the samples (TP-HCl tablets and injection liquid). A solutions spiked with standard TP-HCl were 99.9 and 99.7% with the RSD (n=11) of 0.66 and 0.67%, respectively. The average recovery of the added LD in the sample (injection) spiked with standard LD-HCl was 98.9% with the RSD (n=11) of 0.59%. The proposed method has been applied to the determination of TP-HCl and LD-HCl in commercial products available in Thailand. Comparative determination of TP by UV spectrophotometry and LD by colorimetry were also carried out. The results obtained by both methods were in good agreement of those obtained by the proposed method verified by using t-test. The proposed RP-HPLC method is simple, accurate, reproducible and suitable for routine analysis.

  4. The conformational stability, solvation and the assignments of the experimental infrared, Raman, (1)H and (13)C NMR spectra of the local anesthetic drug lidocaine.

    PubMed

    Badawi, Hassan M; Förner, Wolfgang; Ali, Shaikh A

    2015-05-05

    The structure, vibrational and (1)H and (13)C NMR spectra of the local anesthetic drug lidocaine were investigated by the B3LYP/6-311G(∗∗) calculations. The molecule was predicted to have the non-planar cis (NCCN∼0°) structures being about 2-6kcal/mol lower in energy than the corresponding trans (NCCN∼180°) forms. The calculated NCCN (9.6°) and CNCC (-132.2°) torsional angles were in a good qualitative agreement with the reported X-ray angles (3.1 and 13.0°, -102.67 and -77.9°, respectively, for H-bonded dimers). The Gibbs energy of solution of lidocaine in formamide, water, dimethylsulfoxide, acetonitrile, methanol, ethanol and chloroform solutions was estimated at the B3LYP level. The predicted affinity of lidocaine toward the alcohols, acetonitrile and chloroform solutions was in excellent agreement with the reported experimental solubility of the drug in organic solvents. The analysis of the observed vibrational spectra is consistent with the presence of lidocaine in only one conformation at room temperature. The (1)H and (13)C NMR spectra of lidocaine were interpreted by experimental and DFT calculated chemical shifts of the drug. The RMSD between experimental and theoretical (1)H and (13)C chemical shifts for lidocaine is 0.47 and 8.26ppm, respectively.

  5. Lidocaine self-sacrificially improves the skin permeation of the acidic and poorly water-soluble drug etodolac via its transformation into an ionic liquid.

    PubMed

    Miwa, Yasushi; Hamamoto, Hidetoshi; Ishida, Tatsuhiro

    2016-05-01

    Poor transdermal penetration of active pharmaceutical ingredients (APIs) impairs both bioavailability and therapeutic benefits and is a major challenge in the development of transdermal drug delivery systems. Here, we transformed a poorly water-soluble drug, etodolac, into an ionic liquid in order to improve its hydrophobicity, hydrophilicity and skin permeability. The ionic liquid was prepared by mixing etodolac with lidocaine (1:1, mol/mol). Both the free drug and the transformed ionic liquid were characterized by differential scanning colorimetry (DSC), infrared spectroscopy (IR), and saturation concentration measurements. In addition, in vitro skin-permeation testing was carried out via an ionic liquid-containing patch (Etoreat patch). The lidocaine and etodolac in ionic liquid form led to a relatively lower melting point than either lidocaine or etodolac alone, and this improved the lipophilicity/hydrophilicity of etodolac. In vitro skin-permeation testing demonstrated that the Etoreat patch significantly increased the skin permeation of etodolac (9.3-fold) compared with an etodolac alone patch, although an Etoreat patch did not increase the skin permeation of lidocaine, which was consistent with the results when using a lidocaine alone patch. Lidocaine appeared to self-sacrificially improve the skin permeation of etodolac via its transformation into an ionic liquid. The data suggest that ionic liquids composed of approved drugs may substantially expand the formulation preparation method to meet the challenges of drugs which are characterized by poor rates of transdermal absorption.

  6. The conformational stability, solvation and the assignments of the experimental infrared, Raman, 1H and 13C NMR spectra of the local anesthetic drug lidocaine

    NASA Astrophysics Data System (ADS)

    Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.

    2015-05-01

    The structure, vibrational and 1H and 13C NMR spectra of the local anesthetic drug lidocaine were investigated by the B3LYP/6-311G∗∗ calculations. The molecule was predicted to have the non-planar cis (NCCN ∼ 0°) structures being about 2-6 kcal/mol lower in energy than the corresponding trans (NCCN ∼ 180°) forms. The calculated NCCN (9.6°) and CNCC (-132.2°) torsional angles were in a good qualitative agreement with the reported X-ray angles (3.1 and 13.0°, -102.67 and -77.9°, respectively, for H-bonded dimers). The Gibbs energy of solution of lidocaine in formamide, water, dimethylsulfoxide, acetonitrile, methanol, ethanol and chloroform solutions was estimated at the B3LYP level. The predicted affinity of lidocaine toward the alcohols, acetonitrile and chloroform solutions was in excellent agreement with the reported experimental solubility of the drug in organic solvents. The analysis of the observed vibrational spectra is consistent with the presence of lidocaine in only one conformation at room temperature. The 1H and 13C NMR spectra of lidocaine were interpreted by experimental and DFT calculated chemical shifts of the drug. The RMSD between experimental and theoretical 1H and 13C chemical shifts for lidocaine is 0.47 and 8.26 ppm, respectively.

  7. Lidocaine-prilocaine cream reduces catheter-related bladder discomfort in male patients during the general anesthesia recovery period: A prospective, randomized, case-control STROBE study.

    PubMed

    Mu, Li; Geng, Li-Cheng; Xu, Hui; Luo, Man; Geng, Jing-Miao; Li, Li

    2017-04-01

    Urethral catheterization is a predictor of agitation during the general anesthesia recovery period. The aim of this study was to determine the effect of intraurethral 5% lidocaine and 25 mg/g prilocaine cream in reducing catheter-related bladder discomfort (CRBD) in male patients during the general anesthesia recovery period. Adult male patients undergoing elective operations that required urinary catheterization under general anesthesia were enrolled and assigned randomly to 2 groups. In the lidocaine-prilocaine cream group (n = 72), approximately 5 g of topical cream was spread in the preputial sac, the glans, the meatus, and on the urinary catheter surface before urinary catheterization. In the control group (n = 74), the urinary catheter was lubricated with lidocaine gel. The incidence and severity of CRBD were assessed 15, 30, 45, and 60 minutes postoperatively. We found that the incidence of CRBD in the lidocaine-prilocaine cream group was significantly lower than in the control group. Multivariate logistic regression analysis showed that lidocaine-prilocaine cream applications reduced moderate or severe CRBD. Thirty minutes postoperation was the most frequent time point for the incidence of CRBD. Application of lidocaine-prilocaine cream on the surface of the urinary catheter is an efficient and safe method to reduce the incidence and severity of CRBD.

  8. Evaluation of the efficacy and safety of a lidocaine and tetracaine (7%/7%) cream for induction of local dermal anesthesia for facial soft tissue augmentation with hyaluronic Acid.

    PubMed

    Cohen, Joel L; Gold, Michael H

    2014-10-01

    Injection of dermal fillers for soft tissue augmentation is a minimally invasive cosmetic procedure with growing popularity. However, patients often express concern about pain with such procedures. A topical anesthetic cream formulated with lidocaine/tetracaine 7%7% was approved by the United States Food and Drug Administration in 2006 and recently reintroduced to the market for use during superficial dermatological procedures. A Phase 3 study was conducted to assess the efficacy and safety of lidocaine/tetracaine 7%7% cream versus placebo cream when used to induce local dermal anesthesia during injections with hyaluronic acid. Mean visual analog scale scores significantly favored lidocaine/tetracaine 7%7% cream. A significant percent of subjects also indicated that lidocaine/tetracaine 7%7% cream provided adequate pain relief and that they would use lidocaine/tetracaine 7%7% cream again. Investigators also rated lidocaine/tetracaine 7%7% cream significantly better than placebo cream for providing adequate pain relief and on the assessment of pain scale. Lidocaine/tetracaine 7%7% cream was safe and well tolerated with most subjects reporting no erythema, edema, or blanching. No related adverse events were reported with lidocaine/tetracaine 7%7% cream; one related adverse event of erythema was reported with placebo cream. The results of this study indicate that lidocaine/tetracaine 7%7% cream is efficacious and safe at providing pain relief for soft tissue augmentation with hyaluronic acid.

  9. Antimicrobial effect of continuous lidocaine infusion in a Staphylococcus aureus-induced wound infection in a mouse model.

    PubMed

    Lu, Cheng-Wei; Lin, Tzu-Yu; Shieh, Jiann-Shing; Wang, Ming-Jiuh; Chiu, Kuan-Ming

    2014-11-01

    Continuous infusion of local anesthetics in surgical wounds has been shown to be an effective technique for postoperative analgesia. To investigate the potential antimicrobial effect of continuous local anesthetic infusion, we adapted a mouse model of surgical wound infection to examine effects on antibacterial response. Forty male BALB/c mice were randomized into 2 groups. An incision wound was made over the dorsal flank and instilled with Staphylococcus aureus. An osmotic pump was then implanted to deliver either 0.9% NaCl or 2% lidocaine continuously. Each wound was cultured postoperatively at 2 days, and the colony count of S. aureus was determined. Results showed that the number of colony-forming units of S. aureus measured in wounds treated with lidocaine displayed a nearly 10-fold reduction compared to the wounds in the saline group (P=0.009). The demonstrated antibacterial activity indicates that local anesthetic infusion may play a role in prophylaxis for surgical wound infections.

  10. Evaluation of gentamicin and lidocaine release profile from gum acacia-crosslinked-poly(2-hydroxyethylmethacrylate)-carbopol based hydrogels.

    PubMed

    Singh, Baljit; Dhiman, Abhishek

    2017-01-27

    In this manuscript an attempt has been made to incorporate both, antibiotic agent 'gentamicin' and pain relieving agent 'lidocaine' into the gum acacia-poly(2-hydroxyethylmethacrylate)-carbopol based hydrogel for wound dressing application. Drug release, gel strength, network parameter, antimicrobial activity and biodegradation properties of hydrogel have been evaluated. Porous microstructure of the hydrogel was observed in cryo-SEM images. The hydrogel showed mesh size 37.29 nm, cross-link density 2.19× 10-5 mol/cm3, molecular weight between two cross-links 60.25× 10-3 g/mol and gel strength 0.625±0.112 N in simulated wound fluid. The hydrogels were evaluated as a drug carrier for model drugs gentamicin and lidocaine. The release of these drugs occurred through Fickian diffusion mechanism and release profile of the drugs was best fitted in first order kinetic model.

  11. Sterilisation of hybrid Galapagos tortoises (Geochelone nigra) for island restoration. Part 2: phallectomy of males under intrathecal anaesthesia with lidocaine.

    PubMed

    Rivera, S; Divers, S J; Knafo, S E; Martinez, P; Cayot, L J; Tapia-Aguilera, W; Flanagan, J

    2011-01-22

    Lidocaine intrathecal anaesthesia was used to perform phallectomies in 15 hybrid Galapagos tortoises (Geochelone nigra) in a field setting as part of a conservation and ecosystem restoration project in the Galapagos Islands. The intrathecal injection was performed in the dorsal intercoccygeal region of the tail. Once the tail and hindlimbs were relaxed and the phallus was easily exteriorised, phallectomy was performed in a routine manner. All the animals recovered well from the procedure and were walking 30 to 60 minutes after surgery. No adverse effects were noted as a result of lidocaine intrathecal anaesthesia. One of the larger animals had evidence of haemorrhage from the surgical site 48 hours postoperatively. All tortoises continued to make full recoveries and were released on to the island of Pinta in May 2010.

  12. The Effect of Intravenous Lidocaine on Brain Activation During Non-Noxious and Acute Noxious Stimulation of the Forepaw: A Functional Magnetic Resonance Imaging Study in the Rat

    PubMed Central

    Luo, Zhongchi; Yu, Mei; Smith, S. David; Kritzer, Mary; Du, Congwu; Ma, Yu; Volkow, Nora D.; Glass, Peter S.; Benveniste, Helene

    2009-01-01

    BACKGROUND Lidocaine can alleviate acute as well as chronic neuropathic pain at very low plasma concentrations in humans and laboratory animals. The mechanism(s) underlying lidocaine’s analgesic effect when administered systemically is poorly understood but clearly not related to interruption of peripheral nerve conduction. Other targets for lidocaine’s analgesic action(s) have been suggested, including sodium channels and other receptor sites in the central rather than peripheral nervous system. To our knowledge, the effect of lidocaine on the brain’s functional response to pain has never been investigated. Here, we therefore characterized the effect of systemic lidocaine on the brain’s response to innocuous and acute noxious stimulation in the rat using functional magnetic resonance imaging (fMRI). METHODS Alpha-chloralose anesthetized rats underwent fMRI to quantify brain activation patterns in response to innocuous and noxious forepaw stimulation before and after IV administration of lidocaine. RESULTS Innocuous forepaw stimulation elicited brain activation only in the contralateral primary somatosensory (S1) cortex. Acute noxious forepaw stimulation induced activation in additional brain areas associated with pain perception, including the secondary somatosensory cortex (S2), thalamus, insula and limbic regions. Lidocaine administered at IV doses of either 1 mg/kg, 4 mg/kg or 10 mg/kg did not abolish or diminish brain activation in response to innocuous or noxious stimulation. In fact, IV doses of 4 mg/kg and 10 mg/kg lidocaine enhanced S1 and S2 responses to acute nociceptive stimulation, increasing the activated cortical volume by 50%–60%. CONCLUSION The analgesic action of systemic lidocaine in acute pain is not reflected in a straightforward interruption of pain-induced fMRI brain activation as has been observed with opioids. The enhancement of cortical fMRI responses to acute pain by lidocaine observed here has also been reported for cocaine. We

  13. Characterisation and in vitro stability of low-dose, lidocaine-loaded poly(vinyl alcohol)-tetrahydroxyborate hydrogels.

    PubMed

    Abdelkader, D H; Osman, M A; El-Gizawy, S A; Faheem, A M; McCarron, P A

    2016-03-16

    Poly(vinyl alcohol) hydrogels cross-linked with the tetrahydroxyborate anion possess textural and rheological properties that can be used as novel drug-loaded vehicles for application to traumatic wounds. However, addition of soluble drug substances causes concentration-dependent phase separation and rheological changes. The aim of this work was to investigate the effect of adding a local anaesthetic, but keeping the concentration low in an attempt to prevent these changes. Cross-linked hydrogels prepared from three grades of poly(vinyl alcohol) were characterised rheologically. Temperature sweep studies showed an elevated complex viscosity upon moving from 25°C to 80°C, which remained high for 48 h following completion of the cycle. Adhesion to model dermal surfaces achieved a maximum of 2.62 N cm(-2) and were greater than that observed to epidermal substrates, with a strong dependence on the rate of detachment used during testing. An optimised formulation (6% w/w PVA (31-50; 99) and 2% w/w THB) containing lidocaine hydrochloride loaded to an upper maximum concentration of 1.5% w/w was assessed for phase separation and drug crystallisation. After six months, crystallisation was present in formulations containing 0.7% and 1.5% lidocaine HCl. Changes in pH in response to increases in lidocaine loading were low. Drug release was shown to operate via a non-Fickian process for all three concentrations, with 60% occurring after approximately 24h. It can be concluded that using a low concentration of lidocaine hydrochloride in hydrogels based on poly(vinyl alcohol) will result in crystallisation. Furthermore, these hydrogels are unlikely to induce rapid anaesthesia due to the low loading and slow release kinetics.

  14. Intravenous lidocaine for effective pain relief after a laparoscopic colectomy: a prospective, randomized, double-blind, placebo-controlled study.

    PubMed

    Ahn, EunJin; Kang, Hyun; Choi, Geun Joo; Park, Yong Hee; Yang, So Young; Kim, Beom Gyu; Choi, Seung Won

    2015-03-01

    A perioperative intravenous lidocaine infusion has been reported to decrease postoperative pain. The goal of this study was to evaluate the effectiveness of intravenous lidocaine in reducing postoperative pain for laparoscopic colectomy patients. Fifty-five patients scheduled for an elective laparoscopic colectomy were randomly assigned to 2 groups. Group L received an intravenous bolus injection of lidocaine 1.5 mg/kg before intubation, followed by 2 mg/kg/h continuous infusion during the operation. Group C received the same dosage of saline at the same time. Postoperative pain was assessed at 2, 4, 8, 12, 24, and 48 hours after surgery by using the visual analog scale (VAS). Fentanyl consumption by patient-controlled plus investigator-controlled rescue administration and the total number of button pushes were measured at 2, 4, 8, 12, 24, and 48 hours after surgery. In addition, C-reactive protein (CRP) levels were checked on the operation day and postoperative days 1, 2, 3, and 5. VAS scores were significantly lower in group L than group C until 24 hours after surgery. Fentanyl consumption was lower in group L than group C until 12 hours after surgery. Moreover, additional fentanyl injections and the total number of button pushes appeared to be lower in group L than group C (P < 0.05). The CRP level tended to be lower in group L than group C, especially on postoperative day 1 and 2 and appeared to be statistically significant. The satisfaction score was higher in group L than group C (P = 0.024). Intravenous lidocaine infusion during an operation reduces pain after a laparoscopic colectomy.

  15. Multiple open channel states revealed by lidocaine and QX-314 on rat brain voltage-dependent sodium channels

    PubMed Central

    1996-01-01

    We have recently reported that brain sodium channels display periods with high (low-Kd) and low (high-Kd) levels of lidocaine-induced open channel block (Salazar, B.C., D.O. Flash, J.L. Walewski, and E. Recio- Pinto. 1995. Brain Res. 699:305-314). In the present study, we further characterize this phenomenon by studying the effects of the permanently charged lidocaine analogue, QX-314. We found that the detection of high- and low-Kd periods does not require the presence of the uncharged form of lidocaine. The level of block, for either period, at various QX-314 concentrations indicated the presence of a single local anesthetic binding site. Increasing the concentration of QX-314 decreased the lifetime of the high-Kd periods while it increased the lifetime of the low-Kd periods. These results could be best fitted to a model with two open channel conformations that display different local anesthetic Kd values (low and high Kd), and in which the channel area defining the local anesthetic Kd consists of multiple interacting regions. Amplitude distribution analysis showed that changes in the Kd values reflected changes in the kon rates, without changes in the koff rates. Both lidocaine and QX-314 were found to be incapable of blocking small- channel subconductance states (5-6 pS). Changes in the local anesthetic kon rates for blocking the fully open state and the lack of local anesthetic block of the small subconductance state are consistent with the presence of channel conformational changes involving the intracellular permeation pathway leading to the local anesthetic binding site. PMID:8783074

  16. The influence of lidocaine topical anesthesia during transesophageal echocardiography on blood methemoglobin level and risk of methemoglobinemia.

    PubMed

    Filipiak-Strzecka, Dominika; Kasprzak, Jarosław D; Wiszniewska, Marta; Walusiak-Skorupa, Jolanta; Lipiec, Piotr

    2015-04-01

    Methemoglobinemia is a relatively rare, but potentially life-threating medical condition, which may be induced by application of topical anaesthetic agents commonly used during endoscopic procedure. The aim of our study was to assess the influence of lidocaine used prior to transesophageal echocardiography (TEE) on the blood level of methemoglobin in vivo. Additionally we attempted to establish the occurrence rate of clinically evident lidocaine-induced methemoglobinemia on the basis of data collected in our institution. We retrospectively analyzed patient records from 3,354 TEEs performed in our echocardiographic laboratory over the course of 13 years in search for clinically evident methemoglobinemia cases. Additionally, 18 consecutive patients referred for TEE were included in the prospective part of our analysis. Blood samples were tested before and 60 min after pre-TEE lidocaine anesthesia application. Information concerning concomitant conditions and pharmacotherapy were also obtained. In 3,354 patients who underwent TEE in our institution no cases of clinically evident methemoglobinemia occurred. In the prospective part of the study, none of 18 patients [16 (89 %) men, mean age 63 ± 13] was diagnosed with either clinical symptoms of methemoglobinemia or exceeded normal blood concentration of methemoglobin. Initial mean methemoglobin level was 0.5 ± 0.1 % with mild, statistically (but not clinically) significant rise to 0.6 ± 0.1 % after 60 min (p = 0.02). Among the analyzed factors only the relation between the proton pump inhibitors intake and methemoglobin blood level rise was identified as statistically relevant (p = 0.03). In adults, pre-TEE lidocaine anesthesia with recommended dosage results in significant increase in methemoglobin blood level, which however does not exceed normal values and does not result in clinically evident methemoglobinemia.

  17. Nematocyst discharge in Pelagia noctiluca (Cnidaria, Scyphozoa) oral arms can be affected by lidocaine, ethanol, ammonia and acetic acid.

    PubMed

    Morabito, Rossana; Marino, Angela; Dossena, Silvia; La Spada, Giuseppa

    2014-06-01

    Nematocyst discharge and concomitant delivery of toxins is triggered to perform both defence and predation strategies in Cnidarians, and may lead to serious local and systemic reactions in humans. Pelagia noctiluca (Cnidaria, Scyphozoa) is a jellyfish particularly abundant in the Strait of Messina (Italy). After accidental contact with this jellyfish, not discharged nematocysts or even fragments of tentacles or oral arms may tightly adhere to the human skin and, following discharge, severely increase pain and the other adverse consequences of the sting. The aim of the present study is to verify if the local anesthetic lidocaine and other compounds, like alcohols, acetic acid and ammonia, known to provide pain relief after jellyfish stings, may also affect in situ discharge of nematocysts. Discharge was induced by a combined physico-chemical stimulation of oral arms by chemosensitizers (such as N-acetylated sugars, aminoacids, proteins and nucleotides), in the presence or absence of 1% lidocaine, 70% ethanol, 5% acetic acid or 20% ammonia, followed by mechanical stimulation by a non-vibrating test probe. The above mentioned compounds failed to induce discharge per se, and dramatically impaired the chemosensitizer-induced discharge response. We therefore suggest that prompt local treatment of the stung epidermis with lidocaine, acetic acid, ethanol and ammonia may provide substantial pain relief and help in reducing possible harmful local and systemic adverse reaction following accidental contact with P. noctiluca specimens.

  18. Adenosine, lidocaine, and Mg2+ (ALM): From cardiac surgery to combat casualty care--Teaching old drugs new tricks.

    PubMed

    Dobson, Geoffrey Phillip; Letson, Hayley Louise

    2016-01-01

    New frontline drugs and therapies are urgently required to protect the body from primary and secondary injuries. We review more than 10 years of work on adenosine, lidocaine, and magnesium (ALM) and its possible significance to civilian and military medicine. Adenosine is an endogenous nucleoside involved in nucleotide production, adenosine triphosphate turnover, and restoration of supply and demand imbalances. Lidocaine is a local anesthetic and Class 1B antiarrhythmic, and magnesium is essential for ionic regulation and cellular bioenergetics. Individually, each plays important roles in metabolism, immunomodulation, inflammation, and coagulation. The original idea to combine all three was as a "polarizing" cardioplegia, an idea borrowed from natural hibernators. Two recent prospective, randomized human trials have demonstrated its safety and superiority in myocardial protection over high-potassium "depolarizing" solutions. The next idea came from witnessing how the human heart spontaneously reanimated after complex operations with little inotropic support. At high doses, ALM arrests the heart, and at lower doses, it resuscitates the heart. In rat and pig models, we have shown that ALM intravenous bolus and infusion "drip" protects against acute regional myocardial ischemia, lethal arrhythmias, cardiac arrest, compressible and noncompressible blood loss and shock, endotoxemia, and sepsis. Individually, adenosine, lidocaine, or magnesium fails to protect. Protection is afforded in part by reducing inflammation, correcting coagulopathy, and lowering energy demand. We propose a unifying hypothesis involving improved central, cardiovascular and endothelium coupling to maintain sufficient tissue oxygenation and reduce primary and secondary "hit" complications. As with any new drug innovation, translation into humans is challenging.

  19. Randomized clinical trial of multimodal physiotherapy treatment compared to overnight lidocaine ointment in women with provoked vestibulodynia: Design and methods.

    PubMed

    Morin, Mélanie; Dumoulin, Chantale; Bergeron, Sophie; Mayrand, Marie-Hélène; Khalifé, Samir; Waddell, Guy; Dubois, Marie-France

    2016-01-01

    Provoked vestibulodynia (PVD) is a highly prevalent and debilitating condition yet its management relies mainly on non-empirically validated interventions. Among the many causes of PVD, there is growing evidence that pelvic floor muscle (PFM) dysfunctions play an important role in its pathophysiology. Multimodal physiotherapy, which addresses these dysfunctions, is judged by experts to be highly effective and is recommended as a first-line treatment. However, the effectiveness of this promising intervention has been evaluated through only two small uncontrolled trials. The proposed bi-center, single-blind, parallel group, randomized controlled trial (RCT) aims to evaluate the efficacy of multimodal physiotherapy and compare it to a frequently used first-line treatment, topical overnight application of lidocaine, in women with PVD. A total of 212 women diagnosed with PVD according to a standardized protocol were eligible for the study and were randomly assigned to either multimodal physiotherapy or lidocaine treatment for 10weeks. The primary outcome measure is pain during intercourse (assessed with a numerical rating scale). Secondary measures include sexual function, pain quality, psychological factors (including pain catastrophizing, anxiety, depression and fear of pain), PFM morphology and function, and patients' global impression of change. Assessments are made at baseline, post-treatment and at the 6-month follow-up. This manuscript presents and discusses the rationale, design and methodology of the first RCT investigating physiotherapy in comparison to a commonly prescribed first-line treatment, overnight topical lidocaine, for women with PVD.

  20. Comparison of Topical Anesthetics for Radiofrequency Ablation of Achrocordons: Eutectic Mixture of Lignocaine/Prilocaine versus Lidocaine/Tetracaine.

    PubMed

    Gahalaut, Pratik; Mishra, Nitin; Chauhan, Sandhya; Rastogi, Madhur Kant

    2014-01-01

    Introduction. Topical application of local anesthetics is currently considered to be the easiest, most effective, and convenient way for treatment of patients who may be undergoing superficial dermatosurgical procedures. Materials and Methods. This study compares the anesthetic potential of 2.5% lidocaine and 2.5% prilocaine topical cream with 7% lignocaine and 7% tetracaine combination cream for radio ablative dermatosurgery when applied, under occlusion, for 30 minutes. 40 subjects of achrocordons were enrolled in this split-side randomized trial. Result. The pain severity experienced by subjects in terms of visual analogue scale score was significantly lesser for lignocaine/tetracaine combination cream as compared to lidocaine/prilocaine combination. Conclusion. This small study proves the efficacy of lidocaine/tetracaine combination as a topical anesthetic cream when applied for a short time interval of 30 minutes. This will help a dermatosurgeon to perform various dermatological procedures in a better and efficient manner with a shorter waiting period for analgesia to set in.

  1. Usefulness of applying lidocaine in esophagogastroduodenoscopy performed under sedation with propofol

    PubMed Central

    de la Morena, Felipe; Santander, Cecilio; Esteban, Carlos; de Cuenca, Beatriz; García, Juan Antonio; Sánchez, Javier; Moreno, Ricardo

    2013-01-01

    AIM: To determine whether topical lidocaine benefits esophagogastroduoduenoscopy (EGD) by decreasing propofol dose necessary for sedation or procedure-related complications. METHODS: The study was designed as a prospective, single centre, double blind, randomised clinical trial and was conducted in 2012 between January and May (NCT01489891). Consecutive patients undergoing EGD were randomly assigned to receive supplemental topical lidocaine (L; 50 mg in an excipient solution which was applied as a spray to the oropharynx) or placebo (P; taste excipients solution without active substance, similarly delivered) prior to the standard propofol sedation procedure. The propofol was administered as a bolus intravenous (iv) dose, with patients in the L and P groups receiving initial doses based on the patient’s American Society of Anaesthesiologists (ASA) classification (ASA I-II: 0.50-0.60 mg/kg; ASA III-IV: 0.25-0.35 mg/kg), followed by 10-20 mg iv dose every 30-60 s at the anaesthetist’s discretion. Vital signs, anthropometric measurements, amount of propofol administered, sedation level reached, examination time, and the subjective assessments of the endoscopist’s and anaesthetist’s satisfaction (based upon a four point Likert scale) were recorded. All statistical tests were performed by the Stata statistical software suite (Release 11, 2009; StataCorp, LP, College Station, TX, United States). RESULTS: No significant differences were found between the groups treated with lidocaine or placebo in terms of total propofol dose (310.7 ± 139.2 mg/kg per minute vs 280.1 ± 87.7 mg/kg per minute, P = 0.15) or intraprocedural propofol dose (135.3 ± 151.7 mg/kg per minute vs 122.7 ± 96.5 mg/kg per minute, P = 0.58). Only when the L and P groups were analysed with the particular subgroups of female, < 65-year-old, and lower anaesthetic risk level (ASA I-II) was a statistically significant difference found (L: 336.5 ± 141.2 mg/kg per minute vs P: 284.6 ± 91.2 mg

  2. A comparison of Stone Cone versus lidocaine jelly in the prevention of ureteral stone migration during ureteroscopic lithotripsy

    PubMed Central

    Bastawisy, Mohamed; Gameel, Tarek; Radwan, Mohamed; Ramadan, Ahmed; Alkathiri, Mutie; Omar, Adel

    2011-01-01

    Background: Intracorporeal lithotripsy modalities and stone removal devices have been created to facilitate endoscopic management of ureteral stones. These devices, along with improved techniques, have resulted in stone-free rates greater than 95% with low morbidity. However, problems remain that preclude consistent 100% stone-free rates with endoscopic treatment of ureteral calculi. Retrograde migration during ureteroscopic procedures remains a significant problem. Objectives: The aim of this study was to compare the Stone Cone device and instillation of lubricating lidocaine jelly as two methods to prevent retrograde stone migration during ureteroscopic lithotripsy. Patients and methods: This study included patients suffering from ureteral stones that were treated with intracorporeal lithotripsy using the pneumatic Lithoclast. These patients were divided into two groups. In group I, the Stone Cone device was used, while in group II, lidocaine jelly 2% concentration was used. Results: This study included 40 patients with a mean age of 38.6 ± 9.3 years (20 patients in each group). There was no significant difference between the groups with regards to stone site, size or state of the upper urinary tract by excretory urography. The pneumatic Lithoclast allowed successful fragmentation of all calculi into small fragments. Upward stone migration did not occur in patients in the Stone Cone group, while in the lidocaine jelly group it occurred in three patients (15%). The operative time in the Stone Cone group ranged between 30 and 55 minutes (mean, 41.8 ± 5.3), while in the lidocaine jelly group it ranged between 40 and 71 minutes (mean, 51.4 ± 3.4), and this difference was statistically significant (p < 0.05). Conclusion: The Stone Cone is safe and efficient in preventing proximal stone migration during ureteroscopic pneumatic lithotripsy. It maintained continuous ureteral access and demonstrated a statistically significant advantage over the

  3. A comparison of intraoral injection discomfort produced by plain and epinephrine-containing lidocaine local anesthetic solutions: a randomized, double-blind, split-mouth, volunteer investigation.

    PubMed Central

    Meechan, J. G.; Day, P. F.

    2002-01-01

    The authors report a clinical trial designed to compare the discomfort produced by plain and epinephrine-containing lidocaine solutions during local anesthesia in the maxilla. Twenty-four healthy volunteers were recruited; each received buccal and palatal infiltrations on each side of the maxilla in the premolar region. The solutions were 2% lidocaine and 2% lidocaine with 1:80,000 epinephrine. Allocation to side was randomized and operator and volunteer were blinded to the identity of the solutions. Volunteers recorded injection discomfort on a 100-mm visual analogue scale (VAS). Volunteers were included in the trial if a score of at least 30 mm was recorded for at least 1 of the matched pair of injections. Differences between treatments were measured using Student's paired t test. Twelve volunteers recorded a VAS score of at least 30 mm for 1 or both buccal injections, and 17 volunteers reached this score for palatal injections. Buccal injection pain was less when the plain solution was used (P = .04) and was not influenced by the order of the injection. Palatal injection discomfort did not differ between the solutions; however, the second palatal injection was more uncomfortable than the first palatal injection (P = .046). These results suggest that plain lidocaine produces less discomfort than lidocaine with epinephrine when administered into the maxillary premolar buccal sulcus in individuals who report moderate pain during this injection. Palatal injection discomfort does not differ between these solutions. PMID:15384291

  4. A comparative evaluation of anesthetic efficacy of articaine 4% and lidocaine 2% with anterior middle superior alveolar nerve block and infraorbital nerve block: An in vivo study

    PubMed Central

    Saraf, Suma Prahlad; Saraf, Prahlad Annappa; Kamatagi, Laxmikant; Hugar, Santosh; Tamgond, Shridevi; Patil, Jayakumar

    2016-01-01

    Background: The ideal maxillary injection should produce a rapid onset of profound pulpal anesthesia for multiple teeth from a single needle penetration. The main objective is to compare the efficacy of articaine 4% and lidocaine 2% and to compare anterior middle superior alveolar nerve block (AMSANB) and infraorbital nerve block (IONB) for anesthesia of maxillary teeth. Materials and Methods: Forty patients undergoing root canal treatment of maxillary anteriors and premolars were included and randomly divided into four groups of ten each. Group I: patients receiving AMSANB with articaine, Group II: Patients receiving IONB with articaine, Group III: Patients receiving AMSANB with lidocaine, Group IV: Patients receiving IONB with lidocaine. The scores of onset of anesthesia and pain perception were statistically analyzed. Results: Onset of action was fastest for articaine with AMSANB and slowest for lidocaine with IONB by Tukey's test. A significant change was observed in the electrical pulp test readings at onset and at 30 min by paired t-test. All patients experienced mild pain during the procedure recorded by visual analog scale. Conclusion: Articaine 4% proved to be more efficacious than lidocaine 2%, and AMSANB was more advantageous than IONB in securing anesthesia of maxillary anteriors and premolars. PMID:27994313

  5. Methemoglobin and sulfhemoglobin formation due to benzocaine and lidocaine in macaques

    SciTech Connect

    Martin, D.G.; Woodard, C.L.; Gold, M.B.; Watson, C.E.; Baskin, S.I.

    1993-05-13

    Benzocaine (BNZ) and lidocaine (LC) are commonly used topical (spray) anesthetics approved for use in humans. BNZ has structural similarities to methemoglobin (MHb) forming drugs that are current candidates for cyanide prophylaxis, while LC has been reported to increase MHb in man. We therefore, compared MHb and sulfhemoglobin (SHb) production in three groups of Macaques (Macaca mulata, Chinese rhesus and Indian rhesus, and Macaca nemistrina, Pig-tailed Macaques) after exposure to BNZ and LC. Formation of SHb, unlike MHb, is not thought to be reversible and is considered to be toxic. MHb and SHb levels were measured periodically on a CO-Oximeter. All rhesus (n=8) were dosed intratrachealy/intranasaly with 56 mg and 280 mg BNZ and with 40 mg of LC in a randomized cross-over design. Pig-tailed macaques (n=6) were dosed with BNZ intranasaly 56 mg and with 40 mg of LC. Since no differences in the peak MHb or time to peak (mean +/- SD) were observed among the three macaque subspecies, the data were pooled. LC did not cause MHb or SHb formation above baseline in any monkey.

  6. Kinetic effects of quaternary lidocaine block of cardiac sodium channels: a gating current study

    PubMed Central

    1994-01-01

    The interaction of antiarrhythmic drugs with ion channels is often described within the context of the modulated receptor hypothesis, which explains the action of drugs by proposing that the binding site has a variable affinity for drugs, depending upon whether the channel is closed, open, or inactivated. Lack of direct evidence for altered gating of cardiac Na channels allowed for the suggestion of an alternative model for drug interaction with cardiac channels, which postulated a fixed affinity receptor with access limited by the conformation of the channel (guarded receptor hypothesis). We report measurement of the gating currents of Na channels in canine cardiac Purkinje cells in the absence and presence of QX-222, a quaternary derivative of lidocaine, applied intracellularly, and benzocaine, a neutral local anesthetic. These data demonstrate that the cardiac Na channel behaves as a modulated rather than a guarded receptor in that drug-bound channels gate with altered kinetics. In addition, the results suggest a new interpretation of the modulated receptor hypothesis whereby drug occupancy reduces the overall voltage- dependence of gating, preventing full movement of the voltage sensor. PMID:8169596

  7. Pharmacokinetics of oxytetracycline after intramuscular administration with lidocaine in sheep, comparison with a conventional formulation.

    PubMed

    Moreno, L; Serrano, J M; Guimerá, M E; Carceles, C M

    1998-01-01

    The pharmacokinetic behaviour of oxytetracycline (OTC) was studied in 11 sheep after intravenous and intramuscular administration at a single dosage of 20 mg kg(-1) bodyweight. A conventional formulation was injected by the intravenous route and two different preparations were administered by the intramuscular route: a conventional formulation (T-100) and an aqueous solution of OTC with lidocaine (1 per cent) (OTC-L). The objective was to determine whether there are differences between both formulations in the disposition kinetics of OTC after intramuscular administration to sheep. After intravenous administration of the conventional formulation, plasma oxytetracycline concentrations were best fitted to an open two-compartment model. Mean apparent volume of distribution was 0.77+/-0.02 litre kg(-1) and the harmonic mean half-life was three hours. The OTC transfer process between central and peripheral compartments was fast and that did not influence the elimination process. After intramuscular administrations of both formulations, half-lives were longer than after intravenous administration (mean values of 14.1 and 58.2 hours for T-100 and OTC-L respectively). In both cases, a biphasic absorption, a 'flip-flop' model and a complete bioavailability were found. OTC-L provided therapeutic plasma concentrations over 0.5 microg ml(-1) (the minimum inhibitory concentration for most susceptible pathogens) for a longer period of time than T-100 (72 hours compared with 36 or 48 hours).

  8. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats.

    PubMed

    Li, Zhuo; Chai, Yunfei; Gong, Chunyu; Du, Guizhi; Liu, Jin; Yang, Jing

    2013-07-01

    This study was designed to develop a simple and effective model of tail nerve block without general anaesthesia and surgical incision, to assist in exploring and studying new local anaesthetics. Tail nerves of adult, male Sprague-Dawley rats were blocked by injecting 1% lidocaine and 0.5% bupivacaine, respectively. To evaluate the tail nerve block model, the effects of tail nerve blocks induced by two classical local anaesthetics were assessed and compared by recording disappearance and recovery time of thermal and mechanical nociception. The results showed that thermal and mechanical nociception of the tail disappeared after application of local anaesthetics but were unchanged by normal saline. No abnormal results were found in both the 3-day observation period and the pathological study, and pain thresholds of all rats recovered fully. We have thus developed an easily operated, reliable and reversible model of tail nerve block for conscious rats that can be used to evaluate efficacy, safety and pharmacokinetics of new local anaesthetics and additives.

  9. RAGE deficiency attenuates the protective effect of Lidocaine against sepsis-induced acute lung injury.

    PubMed

    Zhang, Zhuo; Zhou, Jie; Liao, Changli; Li, Xiaobing; Liu, Minghua; Song, Daqiang; Jiang, Xian

    2017-04-01

    Lidocaine (Lido) is reported to suppress inflammatory responses and exhibit a therapeutic effect in models of cecal ligation and puncture (CLP)-induced acute lung injury (ALI). The receptor for advanced glycation end product (RAGE) exerts pro-inflammatory effects by enhancing pro-inflammatory cytokine production. However, the precise mechanism by which Lido confers protection against ALI is not clear. ALI was induced in RAGE WT and RAGE knockout (KO) rats using cecal ligation and puncture (CLP) operations for 24 h. The results showed that Lido significantly inhibited CLP-induced lung inflammation and histopathological lung injury. Furthermore, Lido significantly reduced CLP-induced upregulation of HMGB1 and RAGE expression and activation of the NF-κB and MAPK signaling pathways. With the use of RAGE KO rats, we demonstrate here that RAGE deficiency attenuates the protective effect of Lido against CLP-induced lung inflammatory cell infiltration and histopathological lung injury. These results suggest that RAGE deficiency attenuates the protective effect of Lido against CLP-induced ALI by attenuating the pro-inflammatory cytokines production.

  10. Transretroperitoneal CT-guided Embolization of Growing Internal Iliac Artery Aneurysm after Repair of Abdominal Aortic Aneurysm: A Transretroperitoneal Approach with Intramuscular Lidocaine Injection Technique

    SciTech Connect

    Park, Joon Young Kim, Shin Jung Kim, Hyoung Ook; Kim, Yong Tae; Lim, Nam Yeol Kim, Jae Kyu; Chung, Sang Young Choi, Soo Jin Na Lee, Ho Kyun

    2015-02-15

    This study was designed to evaluate the efficacy and safety of CT-guided embolization of internal iliac artery aneurysm (IIAA) after repair of abdominal aortic aneurysm by transretroperitoneal approach using the lidocaine injection technique to iliacus muscle, making window for safe needle path for three patients for whom CT-guided embolization of IIAA was performed by transretroperitoneal approach with intramuscular lidocaine injection technique. Transretroperitoneal access to the IIAA was successful in all three patients. In all three patients, the IIAA was first embolized using microcoils. The aneurysmal sac was then embolized with glue and coils without complication. With a mean follow-up of 7 months, the volume of the IIAAs remained stable without residual endoleaks. Transretroperitoneal CT-guided embolization of IIAA using intramuscular lidocaine injection technique is effective, safe, and results in good outcome.

  11. Increase in volume of dental local anaesthetic solution while maintaining the tissue lidocaine and adrenaline concentration does not increase acute postoperative pain after gingivectomy.

    PubMed

    Hanvold, K I; Vigen, E C; Jorkjend, L; Aass, A M; Skoglund, L A

    2008-04-01

    A randomised, single-blind, within-patient, crossover study was done in 45 patients (29 women and 16 men, mean age 49 years, range 37-71) who had bilateral "identical" gingivectomies. On one occasion a standard volume of local anaesthetic containing 2% lidocaine and 1/80,000 adrenaline was infiltrated into the mucosal tissue before operation. On the other, double the standard volume with 1% lidocaine and 1/160,000 adrenaline was infiltrated. The intensity of postoperative pain was recorded by the patients on a 100 mm visual analogue scale every hour for an 11-hour observation period. The time courses and the sum of pain intensity after injection of the double and standard volumes did not differ significantly. Doubling the volume of local anaesthetic while maintaining the total lidocaine and adrenaline concentration that was infiltrated does not influence the intensity of acute pain after gingivectomy.

  12. Clinical effects of carticaine, a new local anesthetic. A survey and a double-blind investigation comparing carticaine with lidocaine in epidural analgesia.

    PubMed

    Brinklov, M M

    1977-01-01

    Carticaine, a new local anesthetic of the amide type, differs from those previously known in that it contains a thiophene ring. The physico-chemical properties of the compound, its pharmacology and its toxicology are reviewed from the litererture. A controlled, double-blind investigation in which carticaine was compared with lidocaine for the purpose of throwing light on the effect of the new local anesthetic in epidural analgesia is presented. Carticaine and lidocaine 2% with adrenaline 1:200 000 were used in the investigation. It was not possible to show any stastically significant difference as regards latency, spread, duration, or motor blockade obtained with the two substances. Marked differences in the type of side effects or their frequency were not noted. From this investigation and a scrutiny of the published clinical studies on the effect of carticaine, it is concluded that its clinical properties are comparable to those of lidocaine.

  13. Inhibitory gene expression of the Cav3.1 T-type calcium channel to improve neuronal injury induced by lidocaine hydrochloride.

    PubMed

    Wen, Xianjie; Xu, Shiyuan; Zhang, Qingguo; Li, Xiaohong; Liang, Hua; Yang, Chenxiang; Wang, Hanbing; Liu, Hongzhen

    2016-03-15

    Cav3.1 is a low-voltage-activated (LVA) calcium channel that plays a key role in regulating intracellular calcium ion levels. In this study, we observed the effects of lidocaine hydrochloride on the pshRNA-CACNA1G-SH-SY5Y cells that silenced Cav3.1 mRNA by RNA interference, and investigated the roles of p38 MAPK in these effects. We constructed the pNC-puro-CACNA1G-SH-SY5Y cells and pshRNA-CACNA1G -SH-SY5Y cells by the RNA interference. All the cells were cultured with or without 10mM lidocaine hydrochloride for 24 h. The cell morphology, cell viability, Cav3.1 and p38 protein expression, cell apoptosis rate and intracellular calcium ion concentration were detected. We found that all cells treated with 10mM lidocaine hydrochloride for 24 h showed cellular rounding, axonal regression, and cellular floating. Compared with the cells in SH-SY5Y+Lido group and NC+Lido group, those in the RNAi+Lido group showed similar changes, but of smaller magnitude. Additionally, following lidocaine hydrochloride all cells displayed increased Cav3.1 and p38 MAPK protein, apoptosis rate, and intracellular calcium ion levels; however,these changes in the RNAi+Lido group were less pronounced than in the SH-SY5Y+Lido and NC+Lido groups. The cell viability decreased following lidocaine hydrochloride treatment, but viability of the cells in the RNAi+Lido group was higher than in the SH-SY5Y+Lido and NC+Lido groups. The results showed that Cav3.1 may be involved in neuronal injury induced by lidocaine hydrochloride and that p38 MAPK phosphorylation was reduced upon Cav3.1 gene silencing.

  14. Fast-onset lidocaine block of rat NaV1.4 channels suggests involvement of a second high-affinity open state.

    PubMed

    Gingrich, Kevin J; Wagner, Larry E

    2016-06-01

    Local anesthetics (LAs) block resting, open, and inactivated states of voltage-gated Na(+) channels where inactivated states are thought to bind with highest affinity. However, reports of fast-onset block occurring over milliseconds hint at high-affinity block of open channels. Movement of voltage-sensor domain IV-segment 4 (DIVS4) has been associated with high affinity LA block termed voltage-sensor block (VSB) that also leads to a second open state. These observations point to a second high-affinity open state that may underlie fast-onset block. To test for this state, we analyzed the modulation of Na(+) currents by lidocaine and its quaternary derivative (QX222) from heterologously expressed (Xenopus laevis oocytes) rat skeletal muscle μ1 NaV1.4 (rSkM1) with β1 (WT-β1), and a mutant form (IFM-QQQ mutation in the III-IV interdomain, QQQ) lacking fast inactivation, in combination with Markov kinetic gating models. 100 μM lidocaine induced fast-onset (τonset≈2 ms), long-lived (τrecovery≈120 ms) block of WT-β1 macroscopic currents. Lidocaine blocked single-channel and macroscopic QQQ currents in agreement with our previously described mechanism of dual, open-channel block (DOB mechanism). A DOB kinetic model reproduced lidocaine effects on QQQ currents. The DOB model was extended to include trapping fast-inactivation and activation gates, and a second open state (OS2); the latter arising from DIVS4 translocation that precedes inactivation and exhibits high-affinity, lidocaine binding (apparent Kd=25 μM) that accords with VSB (DOB-S2VSB mechanism). The DOB-S2VSB kinetic model predicted fast-onset block of WT-β1. The findings support the involvement of a second, high-affinity, open state in lidocaine modulation of Na(+) channels.

  15. Evaluating the Effect of Lidocaine on the Interactions of C-reactive Protein with Its Aptamer and Antibody by Dynamic Force Spectroscopy.

    PubMed

    Li, Zhiping; Wang, Qing; Yang, Xiaohai; Wang, Kemin; Du, Shasha; Zhang, Hua; Gao, Lei; Zheng, Yan; Nie, Wenyan

    2017-03-21

    Effects of medicine on the biomolecular interaction have been given extensive attention in biochemistry and biomedicine because of the complexity of the environment in vivo and the increasing opportunity of exposure to medicine. Herein, the effect of lidocaine on the interactions of C-reactive protein (CRP) with its aptamer and antibody under different temperature was investigated through dynamic force spectroscopy (DFS). The results revealed that lidocaine could reduce the binding probabilities and binding affinities of the CRP-aptamer and the CRP-antibody. An interesting discovery was that lidocaine had differential influences on the dynamic force spectra of the CRP-aptamer and the CRP-antibody. The energy landscape of the CRP-aptamer turned from two activation barriers to one after the treatment of lidocaine, while the one activation barrier in energy landscape of the CRP-antibody almost remained unchanged. In addition, similar results were obtained for 25 and 37 °C. In accordance with the result of molecular docking, the reduction of binding probabilities might be due to the binding of lidocaine on CRP. Additionally, the alteration of the dissociation pathway of the CRP-aptamer and the change of binding affinities might be caused by the conformational change of CRP, which was verified through synchronous fluorescence spectroscopy. Furthermore, differential effects of lidocaine on the interactions of CRP-aptamer and CRP-antibody might be attributed to the different dissociation processes and binding sites of the CRP-aptamer and the CRP-antibody and different structures of the aptamer and the antibody. This work indicated that DFS provided information for further research and comprehensive applications of biomolecular interaction, especially in the design of biosensors in complex systems.

  16. Determination of lidocaine and its two N-desethylated metabolites in dog and horse plasma by high-performance liquid chromatography combined with electrospray ionization tandem mass spectrometry.

    PubMed

    Maes, A; Weiland, L; Sandersen, C; Gasthuys, F; De Backer, P; Croubels, S

    2007-06-01

    A sensitive method for the quantification of lidocaine and its metabolites, monoethylglycinexylidide (MEGX) and glycinexylidide (GX), in animal plasma using high-performance liquid chromatography combined with electrospray ionization mass spectrometry is described. The sample preparation includes a liquid-liquid extraction with methyl tert-butylmethyl ether after addition of 2M sodium hydroxide. Ethylmethylglycinexylidide (EMGX) is used as an internal standard. For chromatographic separation, an ODS Hypersil column was used. Isocratic elution was achieved with 0.01 M ammonium acetate and acetonitrile as mobile phases. Good linearity was observed in the range of 2.5-1000 ng ml(-1) for lidocaine in both dog and horse plasma. For MEGX, linear calibration curves were obtained in the range of 5-1000 ng ml(-1) and 20-1000 ng ml(-1) for dog and horse plasma, respectively. In dog and horse plasma good linearity was observed in the range of 200-1500 ng ml(-1) for GX. The limit of quantification (LOQ) in dog plasma for lidocaine, MEGX and GX was set at 2.5 ng ml(-1), 20 ng ml(-1) and 200 ng ml(-1), respectively. For horse plasma a limit of quantification of 2.5 ng ml(-1), 5 ng ml(-1) and 200 ng ml(-1) was achieved for lidocaine, MEGX and GX, respectively. In dog plasma, the limit of detection (LOD) was found to be 0.8 ng ml(-1), 2.3 ng ml(-1) and 55 ng ml(-1) for lidocaine, MEGX and GX, respectively. In horse plasma the LOD's found for lidocaine, MEGX and GX, were 1.1 ng ml(-1), 0.5 ng ml(-1) and 13 ng ml(-1), respectively. The method was shown to be of use in pharmacokinetic studies after application of a transdermal patch in dogs and after an intravenous infusion in horses.

  17. Lidocaine versus ropivacaine for postoperative continuous paravertebral nerve blocks in patients undergoing laparoscopic bowel surgery: a randomized, controlled, double-blinded, pilot study

    PubMed Central

    Ghisi, Daniela; Fanelli, Andrea; Jouguelet-Lacoste, Julie; La Colla, Luca; Auroux, Anne-Sophie; Chelly, Jacques E

    2015-01-01

    Background and objectives Lidocaine could provide many advantages in continuous regional anesthesia techniques, including faster onset, greater titratability, and lower cost than long-acting local anesthetics. This prospective, randomized, double-blinded, pilot study is therefore intended to compare lidocaine to ropivacaine in bilateral continuous paravertebral blocks using a multimodal approach for postoperative pain management following laparoscopic bowel surgery. Methods Thirty-five ASA I–III consecutive patients undergoing elective laparoscopic bowel surgery and bilateral thoracic paravertebral continuous blocks were analyzed: bilateral thoracic paravertebral infusions of ropivacaine 0.2% (Group Ropi, n=18) or lidocaine 0.25% (Group Lido, n=17) were started at 7 mL/h in the postanesthesia care unit. For each patient, we collected numerical rating scores (NRS) for pain at rest and during movement at baseline, at postanesthesia care unit discharge, at 24 hours and 48 hours after the end of surgery, as well as hydromorphone patient-controlled analgesia requirements, local anesthetic consumption, side effects, postoperative complications, and functional outcomes. Results No effect of group distribution on NRS scores for pain at rest or at movement (P=0.823 and P=0.146), nor on hydromorphone (P=0.635) or local anesthetic consumption (P=0.063) was demonstrated at any analyzed time point. Hospital length of stay and spontaneous ambulation were comparable between groups (P=0.636 and P=0.148). In the context of a multimodal approach, the two drugs showed comparable safety profiles. Discussion Lidocaine 0.25% and ropivacaine 0.2% provided similar analgesic profiles after elective abdominal surgeries, without any difference in terms of functional outcomes. The easier titratability of lidocaine together with its lower cost induced our clinical practice to definitely switch from ropivacaine to lidocaine for postoperative bilateral paravertebral continuous infusions. PMID

  18. Application of lidocaine jelly on chest tubes to reduce pain caused by drainage catheter after coronary artery bypass surgery.

    PubMed

    Kang, Hyun; Chung, Yoon Sang; Choe, Ju Won; Woo, Young Cheol; Kim, Sang Wook; Park, Soon J; Hong, Joonhwa

    2014-10-01

    The objective of this study was to assess the effect of lidocaine jelly application to chest tubes on the intensity and duration of overall pain, chest tube site pain and the required analgesics for postoperative pain relief in coronary artery bypass graft (CABG) patients. For patients in group L, we applied sterile 2% lidocaine jelly on the chest tubes just before insertion, and for patients in group C, we applied normal saline. Overall visual analogue scale (VAS), maximal pain area with their VAS were documented postoperatively, and the frequency that button of patient-controlled analgesia was pressed (FPB) and total fentanyl consumption were assessed. The number of patients who complained that tube site was the most painful site was significantly higher in group C than in group L (85% vs. 30% at extubation, P<0.001). The overall VAS score was significantly higher in group C than in group L (39.14±12.49 vs. 27.74±13.76 at extubation, P=0.006). After all of the tubes were removed, the VAS score decreased more in group C (5.74±4.77, P<0.001) than in group L (3.05±2.48, P<0.001). FPB and total fentanyl consumption were significantly higher in group C than in group L (73.00, 59.00-78.00 vs. 34.00, 31.00-39.25, P<0.001; 2,214.65±37.01 vs. 1,720.19±361.63, P<0.001, respectively). Lidocaine jelly application is a very simple way to reduce postoperative pain by reducing chest tube site pain after CABG. (Clinical Trials Registry No. ACTRN 12611001215910).

  19. Effects of sympathetic stimulation on use dependence of lidocaine, mexiletine, and quinidine in an intact canine model.

    PubMed

    Newman, D; Herre, J M; Chin, M; Scheinman, M M; Franz, M; Katzung, B

    1992-02-01

    The use- or rate-dependent effects of a continuous infusion of lidocaine (n = 6, serum level 3.1 +/- 0.34 micrograms/mL), mexiletine (n = 8, serum level 7.08 +/- 0.90 micrograms/mL), and quinidine (n = 6, serum level 6.8 +/- 1.22 micrograms/mL) were studied in an open chest canine preparation. A use-dependent effect on conduction was assessed by measuring the change in the His to surface ventricular activation (HV) time at differing atrial paced rates during drug infusion. Global sympathetic activation was achieved by nondecentralized left stellate ganglion stimulation (4-10 Hz, 6-12 V, 2 ms) and use dependence at the same cycle lengths was compared. Repolarization times were measured from epicardial monophasic action potentials recorded from the anterior left ventricle throughout the study. There was no significant change in the HV time during control studies with or without left stellate stimulation. Use-dependent slowing of conduction was seen in all studies during drug infusion. This was evident at cycle lengths of 300-190 ms for quinidine and at cycle lengths less than 250 ms for lidocaine and mexiletine. Stellate stimulation attenuated use dependence in all studies. This effect was significant from cycle lengths of 300-190 ms for lidocaine and quinidine and at cycle lengths shorter than 230 ms for mexiletine (p less than 0.05). Stellate stimulation significantly reduced use-dependent prolongation of the HV interval by an average of 60%. During stellate stimulation there was a nonsignificant trend towards cycle length independent shortening of action potential duration both at baseline and in the presence of drugs.(ABSTRACT TRUNCATED AT 250 WORDS)

  20. Comparing Clonidine and Lidocaine on Attenuation of Hemodynamic Responses to Laryngoscopy and Tracheal Intubation in Controlled Hypertensive Patients: A Randomized, Double-Blinded Clinical Trial

    PubMed Central

    Soltani Mohammadi, Sussan; Maziar, Alireza; Saliminia, Alireza

    2016-01-01

    Background: Hemodynamic fluctuations in response to laryngoscopy and tracheal intubation and their potential hazards have been well-recognized, especially in hypertensive patients. Many drugs in various combinations have been used to attenuate these adverse responses. Objectives: We conducted a study to compare lidocaine with clonidine on the attenuation of hemodynamic responses to laryngoscopy and tracheal intubation, in controlled hypertensive patients undergoing general anesthesia. Patients and Methods: Eighty-six patients of American society of anesthesiologists (ASA) class II, who were aged 18 to 65-years-old and were scheduled for elective surgeries under general anesthesia, were included. The patients were randomly divided into two equal groups. The clonidine group received 0.2 mg oral clonidine 90 minutes before surgery and the lidocaine group received a placebo tablet at the same time. All patients in both groups were anesthetized with the same technique, including: intravenous fentanyl 3 mcg/kg, sodium thiopental 5 mg/kg, and atracurium 0.5 mg/kg. The lidocaine group received 1.5 mg/kg lidocaine but the clonidine group received the same volume of saline ninety seconds before intubation. Hemodynamic parameters were recorded before intubation and 1, 3, 5, and 10 minutes after endotracheal intubation. Results: There were no significant differences between the two groups’ hemodynamic parameters, including heart rate and systolic, diastolic, and mean arterial blood pressures at the measured points. There were also no significant differences within each group in hemodynamic responses at the measured points (P > 0.05). Twenty patients in the clonidine and three patients in the lidocaine group complained of mouth dryness (P = 0.001). Fourteen patients in the clonidine and four patients in the lidocaine group had bradycardia (P = 0.008). Nineteen patients in the clonidine and six patients in the lidocaine group had orthostatic hypotension (P = 0

  1. In vivo priming and ex vivo activation of equine neutrophils in black walnut extract-induced equine laminitis is not attenuated by systemic lidocaine administration.

    PubMed

    Loftus, John P; Williams, Jarred M; Belknap, James K; Black, Samuel J

    2010-11-15

    Laminitis is a crippling disease of horses characterized by an inflammatory response in the tissue that suspends the axial skeleton within the hoof. Pain is a common feature of laminitic pathology and its management is an important component of the treatment regime for this disease. Systemic lidocaine administration is commonly utilized to manage pain in equine laminitis; however, the potential anti-inflammatory effects of this drug during the treatment of equine laminitis have not been investigated. Here, we sought to determine if lidocaine concentrations achieved in the plasma (therapeutic concentrations) of horses systemically administered lidocaine are capable of attenuating neutrophil activation and associated inflammation. To identify markers of activation, purified neutrophils were stimulated in vitro with LPS or recombinant equine IL-8 (reqIL-8) and surface expression of CD13 and CD18 was ascertained by immunofluorescent staining. Activation with LPS or reqIL-8 in vitro induced an elevated expression of CD13 as well as a putative conformational change in CD18 detected by elevated staining with a sub-saturating concentration of anti-CD18 mAb. Lidocaine attenuated the activation-induced changes in CD13 and CD18 expression only when used at 30-70 times therapeutic concentrations. For in vivo analyses, horses were administered black walnut extract (BWE) to induce laminitis and either systemic lidocaine (n=6) or saline (n=6) as a control. Whole blood was collected and incubated with or without reqIL-8. Following which, leukocytes were stained for CD13 and CD18. Protein was extracted from laminar tissue and subjected to gelatin zymography to measure matrix metalloproteinase-9 (MMP-9) accumulation. Results obtained show that changes in neutrophil size, granularity/complexity, CD13 surface expression and CD18 staining intensity occurred over time post BWE administration irrespective of lidocaine treatment in response to incubation alone or with 100 ng/ml of reqIL-8

  2. Absorption of Iontophoresis-Driven 2% Lidocaine With Epinephrine in the Tissues at 5 mm Below the Surface of the Skin

    PubMed Central

    Draper, David O.; Coglianese, Mark; Castel, Chris

    2011-01-01

    Context: In a recent study, we were unable to measure lidocaine in the human calf at a 5-mm depth via iontophoresis. We surmised that this might be due to a lack of epinephrine in the compound. Because epinephrine is a vasoconstrictor, it might allow the drug to pass beyond the capillaries and be delivered to the deeper tissues. Objective: To determine if iontophoresis could deliver lidocaine with epinephrine 5 mm under the surface of human skin, as measured by microdialysis. Design: Descriptive laboratory study. Setting: Therapeutic modalities research laboratory. Patients or Other Participants: Ten volunteers (5 males, 5 females; age, 15–28 years) with less than 5 mm of adipose tissue in the area we measured and with no allergies to lidocaine participated. The measurement area had been free of any injury, swelling, or infection for at least 3 months before the study. Intervention(s): We inserted a microdialysis probe 0.5 cm under the skin of the right lower leg. Next, microdialysis was performed through this area for 60 minutes, which allowed local skin blood flow to return to baseline. We then performed iontophoresis at 40 mA/min using 2 mL of 2% lidocaine. Iontophoresis was performed over this area for 10.5 minutes to collect the lidocaine samples. After this stage, the electrode was left in place for another 50 minutes for a total of 60 minutes. Main Outcome Measure(s): The samples of the drug were analyzed via reverse-phase high-performance liquid chromatography (RP-HPLC) in the chemistry department. Results: The RP-HPLC analysis confirmed the presence of lidocaine in all 10 participants. The mean concentration of lidocaine detected at the 5-mm depth was calculated as 3.63 mg/mL (greater than 18% of delivered concentration). Conclusions: We found that 2% lidocaine can be delivered up to 5 mm below the surface of the skin when the drug compound contains epinephrine and when passive delivery occurs for at least 50 minutes after the active delivery has

  3. Lidocaine injection of pericranial myofascial trigger points in the treatment of frequent episodic tension-type headache

    PubMed Central

    2013-01-01

    Background The present study aimed to evaluate the efficacy of local lidocaine injections into the myofascial trigger points (TPs) located at the pericranial muscles in patients with episodic tension-type headache (ETTH). Methods The study included 108 patients with frequent ETTH that were randomized into 4 groups. One injection of saline (NaCl 0.9%) was administered to group 1 (n = 27), 1 injection of lidocaine (0.5%) was administered to group 2 (n = 27), group 3 (n = 27) received 5 injections of saline (NaCl 0.9%), and group 4 (n = 27) received 5 injections of lidocaine (0.5%); on alternate days 2 mL for each muscle was injected into the frontal, temporal, masseter, sternocleidomastoid, semispinalis capitis, trapezius and splenius capitis muscles bilaterally. The frequency of painful days per month (FPD) and the patients’ visual analogue scales (VAS) were evaluated before treatment, and 2, 4 and 6 months after treatment. Results Mean age of the patients was 36.28 ± 9.41 years (range: 18–54 years). FPD scores improved significantly in group 2, 3 and 4 at 2 months posttreatment compared to pre- treatment (all P < 0.05), and also VAS scores improved significantly in group 2 and 4 at 2 months posttreatment (P < 0.05) but this improvement insisted at the 6 month only in group 4. Group 2 had better VAS and FPD than group 1 only at 2. and 4. months after treatment (for VAS P < 0.0121, P = 0.0232; for FPD P = 0.0003, P = 0.0004, respectively). Group 4 had better scores than group 3 at the 2., 4. and 6. months after treatment in both parameters (all P < 0.05). Group 2 had better scores than group 1 in FPD at the 2. and 4. months posttreatment (P = 0.0003, P = 0.0004, respectively), but not at the 6. month. Conclusion Local lidocaine injections into the myofascial TPs located in the pericranial muscles could be considered as an effective alternative treatment for ETTH. PMID:23698019

  4. Lidocaine Injections Targeting CA3 Hippocampus Impair Long-Term Spatial Memory and Prevent Learning-Induced Mossy Fiber Remodeling

    PubMed Central

    Holahan, Matthew R.; Routtenberg, Aryeh

    2010-01-01

    Learning a spatial location induces remodeling of the mossy fiber terminal field (MFTF) in the CA3 subfield of the dorsal hippocampus (Holahan et al., 2006; Ramirez-Amaya et al., 2001; Rekart et al., 2007a). These fibers appear to grow from the stratum lucidum (SL) into distal stratum oriens (dSO). Is this axonal growth dependent on ‘repeated and persistent’ neural activity in the CA3 region during training? To address this issue, we targeted local inactivation of the MFTF region in a post-training, consolidation paradigm. Male Wistar rats, bilaterally implanted with chronic indwelling cannulae aimed at the MFTF CA3 region, were trained on a hidden platform water maze task (10 trials per day for 5 days). Immediately after the 10th trial on each training day, rats were injected with lidocaine (4% w/V; 171 mM; n = 7) or phosphate-buffered saline (PBS; n = 7). Behavioral measures of latency, path length and thigmotaxis were recorded, as was directional heading. A retention test (probe trial) was given 7 days after the last training day and brains were subsequently processed for MFTF distribution (Timm’s stain) and cannula location. Lidocaine treatment was found to block the learning-associated structural remodeling of the MFTF that was reported previously and observed in the PBS-injected controls. During training, the lidocaine group showed elevated latencies and a misdirected heading to locate the platform on the first trial of each training day. On the 7-day retention probe trial, the lidocaine-injected group showed poor retention indicated by the absence of a search bias in the area where the platform had been located during training. These data suggest that reduction of neuronal activity in the CA3 region impairs long-term storage of spatial information. As this was associated with reduced MFTF structural remodeling, it provides initial anatomical and behavioral evidence for an activity – dependent, presynaptic growth model of memory. PMID:20865723

  5. [In vitro effects of the alkalinization of 0.25% bupivacaine and 2% lidocaine].

    PubMed

    Berrada, R; Chassard, D; Bryssine, S; Berthier, S; Bryssine, B; Boulétreau, P

    1994-01-01

    Recent clinical studies have suggested that alkalinization of local anaesthetic agents may shorten the onset time and lengthen their duration of action. In clinical practice, sodium bicarbonate 1.4 and 4.2% are often added to local anaesthetic agents to obtain these effects. We evaluated pH changes of 4 local anaesthetic solutions commonly used for obstetrical epidural anaesthesia, in order to develop titration curves with sodium bicarbonate 1.4 and 4.2%. Local anaesthetic agents tested included lidocaine 2% and bupivacaine 0.25% with and without epinephrine. Each one was divided in 10 mL aliquots, and supplemented with 25 micrograms of sufentanil (1 mL). The pH measurement were made with a pH-meter P 500 with a combined electrode (TBC 12/HS) in the standard solution and after incremental addition of 0.5 mL of 1.4 or 4.2% sodium bicarbonate. The percentage of the free form of local anaesthetic was calculated for each step, using the Henderson-Hasselbalch equation. Results showed that alkalinization is not beneficial with epinephrine free solutions. Increasing volumes of sodium bicarbonate, buffered the acidic effect of sodium bisulfite present in solutions containing epinephrine, and increased the percentage of the free form of local anaesthetic to the level of epinephrine free solutions. From this pH point upwards, the gain is poor and precipitates are generated. This study suggests that 1 mL of 4.2% sodium bicarbonate for 10 mL of local anaesthetic solution is the best theorical choice for alkalinization of a local anaesthetic associated with epinephrine.

  6. Lidocaine-Prilocaine Cream as Analgesia for IUD Insertion: A Prospective, Randomized, Controlled, Triple Blinded Study

    PubMed Central

    Tavakolian, Samira; Doulabi, Mahbobeh Ahmadi; Baghban, Alireza Akbarzade; Mortazavi, Alireza; Ghorbani, Maryam

    2015-01-01

    Introduction: Copper IUD is a long term and reversible contraception which equals tubal ligation in terms of sterilization. One of the barriers to using this contraception method is the fear and the pain associated with its insertion. Eutectic mixture of local anesthetics (EMLA) 5% is a local anesthetic that contains 25 mg lidocaine and 25 mg of prilocaine per gram. Application of topical analgesic cream to the cervix for laser surgery, hysteroscopy and hysterosalpingography is known Aims: this study aimed to determine the effect of EMLA on IUD insertion pain. Methods: This triple blind clinical trial was conducted on 92 women in a clinic in Hamedan in 2012. After applying the cream on the cervix, pain in three steps, after using Tenaculum, after inserting hystrometr and after inserting IUD and removing IUD insertion tube were assessed with visual analog scale and were compared in EMLA group and placebo group Statistical analysis used to determine and compare the pain of independent t tests, Mann-Whitney U test and repeated measures analysis of variance and chi-square tests to determine the homogeneity of variables and Fisher’s exact test was used Results: Insertion hystrometr was determined as the most painful IUD insertion. The mean pain at step 2 (inserting hystrometr) was (3/11±2/53) in EMLA group, (5/23±2/31) in placebo group. EMLA cream significantly reduced the pain after using tenaculum (P<0/001), pain inserting Hystrometr (P< 0/001) and pain at IUD insertion and removing insertion tube (P< 0/001) Conclusions: Topical Application of EMLA 5% cream as a topical anesthetic on the cervix before insertion IUD reduced the pain during this procedure. PMID:25946948

  7. Nanostructured lipid carriers as robust systems for topical lidocaine-prilocaine release in dentistry.

    PubMed

    Ribeiro, Lígia N M; Franz-Montan, Michelle; Breitkreitz, Márcia C; Alcântara, Ana C S; Castro, Simone R; Guilherme, Viviane A; Barbosa, Raquel M; de Paula, Eneida

    2016-10-10

    In dental practice, local anesthesia causes pain, fear, and stress, and is frequently the reason that patients abandon treatment. Topical anesthetics are applied in order to minimize the discomfort caused by needle insertion and injection, and to reduce the symptoms of superficial trauma at the oral mucosa, but there are still no efficient commercially available formulations. Factorial design is a multivariate data analysis procedure that can be used to optimize the manufacturing processes of lipid nanocarriers, providing valuable information and minimizing development time. This work describes the use of factorial design to optimize a process for the preparation of nanostructured lipid carriers (NLC) based on cetyl palmitate and capric/caprylic triglycerides as structural lipids and Pluronic 68 as the colloidal stabilizer, for delivery of the local anesthetics lidocaine and prilocaine (both at 2.5%). The factors selected were the excipient concentrations, and three different responses were followed: particle size, polydispersity index and zeta potential. The encapsulation efficiency of the most effective formulations (NLC 2, 4, and 6) was evaluated by the ultrafiltration/centrifugation method. The formulations that showed the highest levels of encapsulation were tested using in vitro release kinetics experiments with Franz diffusion cells. The NLC6 formulation exhibited the best sustained release profile, with 59% LDC and 66% PLC released after 20h. This formulation was then characterized using different techniques (IR-ATR, DSC, DRX, TEM, and NTA) to obtain information about its molecular organization and its physicochemical stability, followed during 14months of storage at 25°C. This thorough pre-formulation study represents an important advance towards the development of an efficient pre-anesthetic for use in dentistry.

  8. Use-dependent block of cardiac sodium channels by quaternary derivatives of lidocaine.

    PubMed

    Gintant, G A; Hoffman, B F

    1984-02-01

    Modulation of the reduction of fast inward sodium current by local anesthetics due to changes in electrical activity has been termed use-dependent block ( Courtney 1975). To determine the mechanisms responsible for use-dependent block of cardiac sodium channels and to compare use-dependent block in cardiac and nerve preparations, we investigated use-dependent block of cardiac sodium channels by the quaternary lidocaine analogues QX -314 and QX -222 (two agents previously studied in nerve). We used canine cardiac Purkinje fibers, and assessed changes in the fast inward sodium current using changes in the maximum rate of rise of the action potential upstroke (Vmax). Two microelectrode voltage clamp and current clamp techniques were used to control membrane potential prior to stimulated upstrokes . Use-dependent block was not affected by shortening the action potential duration during rapid stimulation. Partial recovery from use-dependent block was observed during rapid stimulation with brief depolarizing prepulses terminating immediately prior to the upstroke. Similar prepulses also prevented the development of use-dependent block following an abrupt increase in the stimulation rate. Hyperpolarizing prepulses during rapid stimulation caused recovery from use-dependent block; recovery was greater and more rapid with increasingly negative prepulses . Hyperpolarization during periods of electrical quiescence also caused greater recovery. These results, interpreted using the modulated receptor hypothesis ( Hille 1977; Hondeghem and Katzung 1977), suggest that use-dependent block of cardiac sodium channels by quaternary local anesthetics is due to drug association with the inactivated sodium channel receptor which occurs only after these drugs gain access to the receptor site through open sodium channels.

  9. Coupled obturator neurotomies and lidocaine intrathecal infusion to treat bilateral adductor spasticity and drug-refractory pain.

    PubMed

    Carrillo-Ruiz, José D; Andrade, Pablo; Godínez-Cubillos, Nora; Montes-Castillo, María L; Jiménez, Fiacro; Velasco, Ana L; Castro, Guillermo; Velasco, Francisco

    2010-09-01

    Spastic diplegia is present in three-fourths of children with cerebral palsy, interfering with gait and frequently accompanied by severe pain. The authors report the case of a 28-year-old woman with history of perinatal hypoxia, who presented with cerebral palsy and severe spastic diplegia (Ashworth Scale Score 4, Tardieu Scale Score 5) and was confined to a wheelchair. She complained of pain in the left hip and knee with mixed neuropathic and somatic components. She consistently rated pain intensity as 10 of 10 on a visual analog scale, and her symptoms were resistant to multiple treatments. The patient underwent selective bilateral adductor myotomies and the implantation of an infusion pump for intrathecal lidocaine application. Postoperative control of pain and spasticity was dramatic (scores of 0 on the Ashworth, Tardieu, and visual analog scales) and persisted throughout a follow-up period of 36 months. This is the first report in the literature of combined selective neurotomies for the treatment of spasticity and chronic lidocaine subarachnoid infusion to treat associated pain. This therapy could represent an alternative to treat spasticity associated with neuropathic and somatic pain.

  10. Local anesthesia of genital mucosa with a lidocaine/prilocaine combination cream before laser therapy of human papillomavirus lesions.

    PubMed

    Monsonego, J; Semaille, C

    2000-12-01

    The objective was to assess the efficacy of the lidocaine 2. 5%/prilocaine 2.5% combination cream during CO2 laser vaporisation treatment of human papillomavirus-related anogenital lesions. The cream was applied 1 to 30 min beforehand. Patients assessed pain using a visual analogue scale. Regardless of the site and lesion surface area, anaesthesia was greatest when the cream was applied 5 to 15 min before treatment. Extra-cervical lesions (vagina, vulva, perineum, anus) were globally less painful than cervical lesions. Lesion surface area is a decisive factor in pre-operative anaesthesia. Small surface-area lesions (< 1 cm2) had significantly greater anaesthesia than larger surface area-lesions (> 5 cm2) (p<0.00001). The study cream proved particularly useful for complete anaesthesia in ambulatory treatment of anal (70%) and urethral (60%) mucosa lesions compared to the uterine cervix (p = 0.03). In terms of anaesthetic efficacy and cost-related benefits, the lidocaine/prilocaine cream is an effective and interesting alternative to locoregional intra-lesional anaesthesia or even to general anaesthesia, for excision and destruction of human papillomavirus-related anogenital lesions.

  11. Reduction of the minimum alveolar concentration of isoflurane in dogs using a constant rate of infusion of lidocaine-ketamine in combination with either morphine or fentanyl.

    PubMed

    Aguado, Delia; Benito, Javier; Gómez de Segura, Ignacio A

    2011-07-01

    The objective of this study was to determine the effects of a constant rate of infusion of lidocaine and ketamine in combination with either morphine or fentanyl on the minimum alveolar concentration of isoflurane (MAC(ISO)) during ovariohysterectomy in dogs. Female dogs (n=44) were premedicated with acepromazine and midazolam. Anaesthesia was induced with propofol and maintained with isoflurane. Dogs received ketamine (0.6 mg/kg/h) and lidocaine (3 mg/kg/h) together with morphine (0.24 mg/kg/h; MLK) or fentanyl (0.0036 mg/kg/h; FLK). The control group received Ringer's lactate solution. A skin incision was used as the noxious stimulus. The MAC(ISO) value was obtained with Dixon's up-and-down method. MAC(ISO) was 0.7±0.0 vol.% in the control group, 0.3±0.0 vol.% in the MLK group (45% MAC reduction) and 0.0±0.0 vol.% in the FLK group (97% MAC reduction). A combination of fentanyl with lidocaine and ketamine decreased the MAC(ISO) in dogs; this decrease was more pronounced than that produced by morphine, lidocaine and ketamine.

  12. Risk-benefit stratification as a guide to lidocaine prophylaxis of primary ventricular fibrillation in acute myocardial infarction: an analytic review.

    PubMed Central

    Goldman, L.; Batsford, W. P.

    1979-01-01

    Early investigators suggested that ventricular fibrillation without heart failure in acute myocardial infarction was reliably preceded by warning arrhythmias, and that suppression of such arrhythmias with intravenous lidocaine could avoid the need for resuscitation. While the efficacy and safety of lidocaine have been substantiated, the reliability of warning arrhythmias as predictors for primary ventricular fibrillation has not. We present data showing that the risk of primary ventricular fibrillation is most dependent on the patient's age and the interval since the onset of his symptoms, rather than on the presence of warning arrhythmias. We have estimated that lidocaine prophylaxis would have to be given to about 12 patients in the highest risk group (patients under age 50 and within six hours of the onset of symptoms), compared to about 400 patients in the lowest risk group (patients above age 70 and more than 24 hours since the onset of symptoms), to prevent one episode of primary ventricular fibrillation in each group. We propose that these risk stratifications, as adapted to the conditions in specific hospitals, provide the most rational approach to lidocaine prophylaxis of primary ventricular fibrillation. PMID:392960

  13. Safety and performance of cohesive polydensified matrix hyaluronic acid fillers with lidocaine in the clinical setting – an open-label, multicenter study

    PubMed Central

    Kühne, Ulrich; Esmann, Jørgen; von Heimburg, Dennis; Imhof, Matthias; Weissenberger, Petra; Sattler, Gerhard

    2016-01-01

    Cohesive polydensified matrix (CPM®) hyaluronic acid fillers are now available with or without lidocaine. The aim of this study was to investigate the safety and performance of CPM® fillers with lidocaine in the clinical setting. In an open-label, prospective, postmarketing study, 108 patients from seven sites in Germany and Denmark were treated with one or more lidocaine-containing CPM® fillers. Performance was assessed using the Merz Aesthetics Scales® (MAS). Pain was rated on an 11-point visual analog scale. Patients’ and physicians’ satisfaction as well as adverse events were recorded. Improvements of ≥1-point on MAS immediately after and 17 days posttreatment were observed in ~90% of patients compared with baseline. All investigators assessed ejection force, product positioning, and performance as similar or superior to the respective nonlidocaine products. Overall, 94% of investigators were satisfied with the esthetic outcomes and were willing to continue using the products. All patients except one were satisfied with the results, and all were willing to repeat the treatment. Mean pain scores were low during (<3.0) and after injection (<0.6). Except for one case of bruising, all adverse events were mild to moderate. CPM® fillers with lidocaine are safe and effective for a wide range of esthetic facial indications. PMID:27799807

  14. Infusion of lidocaine into the dorsal hippocampus before or after the shock training phase impaired conditioned freezing in a two-phase training task of contextual fear conditioning.

    PubMed

    Chang, Shih-Dar; Chen, Der-Yow; Liang, K C

    2008-02-01

    Learning in a contextual fear conditioning task involves forming a context representation and associating it with a shock. The dorsal hippocampus (DH) is implicated in representing the context, but whether it also has a role in associating the context and shock is unclear. To address this issue, male Wistar rats were trained on the task by a two-phase training paradigm, in which rats learned the context representation on day 1 and then reactivated it to associate with the shock on day 2; conditioned freezing was tested on day 3. Lidocaine was infused into the DH at various times in each of the two training sessions. Results showed that intra-DH infusion of lidocaine shortly before or after the context training session on day 1 impaired conditioned freezing, attesting to the DH involvement in context representation. Intra-DH infusion of lidocaine shortly before or after the shock training session on day 2 also impaired conditioned freezing. This deficit was reproduced by infusing lidocaine or APV (alpha-amino-5-phosphonovaleric acid) into the DH after activation of the context memory but before shock administration. The deficit was not due to drug-induced state-dependency, decreased shock sensitivity or reconsolidation failure of the contextual memory. These results suggest that in contextual fear conditioning integrity of the DH is required for memory processing of not only context representation but also context-shock association.

  15. Effects of Addition of Systemic Tramadol or Adjunct Tramadol to Lidocaine Used for Intravenous Regional Anesthesia in Patients Undergoing Hand Surgery

    PubMed Central

    Yektaş, Abdulkadir; Gümüş, Funda; Karayel, Abdulhalim; Alagöl, Ayşin

    2016-01-01

    Intravenous regional anesthesia (IVRA) is used in outpatient hand surgery as an easily applicable and cost-effective technique with clinical advantages. The present study aimed to investigate the effects of addition of systemic tramadol or adjunct tramadol to lidocaine for IVRA in patients undergoing hand surgery. American Society of Anesthesiologists (ASA) I-II patients (n = 60) who underwent hand surgery were included. For this purpose, only lidocaine (LDC), lidocaine+adjunct tramadol (LDC+TRA group), or lidocaine+systemic tramadol (LDC+SysTRA group) was administered to the patients for IVRA and the groups were compared in terms of onset and recovery time of sensory and motor blocks, quality of anesthesia, and the degree of intraoperative and postoperative pain. The onset time of sensorial block was significantly shorter in the LDC+TRA group than that in the LDC+SysTRA group. The motor block recovery time was significantly shorter in the LDC+SysTRA group than that in the LDC+TRA and LDC groups. Administration of tramadol as an adjunct showed some clinical benefits by providing a shorter onset time of sensory and motor block, decreasing pain and analgesic requirement, and improving intraoperative conditions during IVRA. It was determined that systemic tramadol administration had no superiority. PMID:27313608

  16. Cardiorespiratory and antinociceptive effects of two different doses of lidocaine administered to horses during a constant intravenous infusion of xylazine and ketamine

    PubMed Central

    2013-01-01

    Background This study investigated the antinociceptive effects of a constant rate infusion (CRI) of lidocaine during xylazine and ketamine anesthesia in horses and aimed to correlate these effects with cardiorespiratory variables, bispectral index (BIS) and plasma lidocaine concentrations. Six adult crossbred mares weighing 320–400 kg were anesthetized on three different occasions. Sedation was performed with xylazine (0.75 mg/kg IV) and anesthetic induction with guaifenesin (75 mg/kg IV) and ketamine (2 mg/kg IV). Anesthesia was maintained with 37.5 μg/kg/min of xylazine and 87.5 μg/kg/min of ketamine both administered intravenously for 75 min. The three treatments consisted of: lidocaine (loading dose: 5 mg/kg, CRI: 100 μg/kg/min; THL); lidocaine (loading dose: 2.5 mg/kg; CRI: 50 μg/kg/min: TLL); and saline (TS); all given 15 min after induction and maintained for 1 h. Antinociception was measured by response to electrical stimulation and bispectral index (BIS) was recorded during anesthesia. Parametric and non-parametric data were compared using ANOVA followed by Student-Newman-Keuls and Friedman tests, respectively. Results Plasma lidocaine concentrations peaked at the end of lidocaine loading dose and was greater in THL (9.61 ± 2.75 μg/mL) vs TLL (4.50 ± 3.34 μg/mL). Electrical noxious stimulation caused purposeful movement in all horses from TS, but no response in THL. The BIS was decreased in THL only and was less when compared to the other treatments throughout anesthesia. Blood pressure, PaO2 and PaCO2 increased and heart rate (HR), respiratory rate (RR), pH, total plasma protein and temperature decreased during anesthesia in all treatments. PaCO2 and HR were greater and RR and pH less in THL compared to TLL and TS at 30 min during anesthesia. All recoveries were considered excellent. Time to standing was longer after THL (60 ± 20 min) than following TLL and TS (32 ± 17 and 30 ± 15 min, respectively

  17. Pharmacokinetics of lidocaine and bupivacaine following subarachnoid administration in surgical patients: simultaneous investigation of absorption and disposition kinetics using stable isotopes

    SciTech Connect

    Burm, A.G.; Van Kleef, J.W.; Vermeulen, N.P.; Olthof, G.; Breimer, D.D.; Spierdijk, J.

    1988-10-01

    The pharmacokinetics of lidocaine and bupivacaine following subarachnoid administration were studied in 12 surgical patients using a stable isotope method. After subarachnoid administration of the agent to be evaluated, a deuterium-labelled analogue was administered intravenously. Blood samples were collected for 24 h. Plasma concentrations of the unlabelled and the deuterium-labelled local anesthetics were determined using a combination of capillary gas chromatography and mass fragmentography. Bi-exponential functions were fitted to the plasma concentration-time data of the deuterium-labelled local anesthetics. The progression of the absorption was evaluated using deconvolution. Mono- and bi-exponential functions were then fitted to the fraction absorbed versus time data. The distribution and elimination half-lives of the deuterium-labelled analogues were 25 +/- 13 min (mean +/- SD) and 121 +/- 31 min for lidocaine and 19 +/- 10 min and 131 +/- 33 min for bupivacaine. The volumes of the central compartment and steady-state volumes of distribution were: lidocaine 57 +/- 10 l and 105 +/- 25 l, bupivacaine 25 +/- 6 l and 63 +/- 22 l. Total plasma clearance values averaged 0.97 +/- 0.21 l/min for lidocaine and 0.56 +/- 0.14 l/min for bupivacaine. The absorption of lidocaine could be described by a single first order absorption process, characterized by a half-life of 71 +/- 17 min in five out of six patients. The absorption of bupivacaine could be described adequately assuming two parallel first order absorption processes in all six patients. The half-lives, characterizing the fast and slow absorption processes of bupivacaine, were 50 +/- 27 min and 408 +/- 275 min, respectively. The fractions of the dose, absorbed in the fast and slow processes, were 0.35 +/- 0.17 and 0.61 +/- 0.16, respectively.

  18. The quest for effective pain control during suture adjustment after strabismus surgery: a study evaluating supplementation of 2% lidocaine with 0.4% ropivacaine

    PubMed Central

    Palte, Howard D; Cavuoto, Kara M; Sundararaman, Lalitha; Gayer, Steven; Schiffman, Joyce; Capo, Hilda

    2015-01-01

    Purpose To determine whether the addition of 0.4% ropivacaine to the standard 2% lidocaine peribulbar anesthetic block improves pain scores during suture adjustment in patients undergoing strabismus surgery with adjustable sutures. Methods Prospective, double-blind study of 30 adult patients aged 21–84 years scheduled for elective strabismus surgery with adjustable sutures. Patients were divided into two groups of 15 patients each based on the local anesthetic. Group A received 2% lidocaine and Group B received 2% lidocaine/0.4% ropivacaine. Pain was assessed using the visual analog scale (VAS) preoperatively and at 2, 4, and 6 hours postoperatively. The Lancaster red-green test was used to measure ocular motility at the same time points. Results The pain scores in the two groups were low and similar at all measurement intervals. The VAS for Group A versus Group B at 2 hours (1.7 versus 2.4, P=0.5) and 4 hours (3.5 versus 3.7, P=0.8) showed no benefit from the addition of ropivacaine. At 6 hours, the VAS (3.7 versus 2.7) was not statistically significant, but the 95% confidence interval indicated that ropivacaine may provide some benefit. A repeated measures ANOVA did not find a statistically significant difference in VAS scores over time (P=0.9). In addition, the duration of akinesia was comparable in both groups (P=0.7). Conclusion We conclude that the 50:50 mixture of 2% lidocaine with 0.4% ropivacaine as compared to 2% lidocaine in peribulbar anesthetic blocks in adjustable-suture strabismus surgery does not produce significant improvements in pain control during the postoperative and adjustment phases. In addition, ropivacaine did not impair return of full ocular motility at 6 hours, which is advantageous in adjustable-suture strabismus surgery. PMID:25609996

  19. Inhibitory effect of lidocaine on pain and itch using formalin-induced nociception and 5′-guanidinonaltrindole-induced scratching models in mice: behavioral and neuroanatomical evidence

    PubMed Central

    Inan, Saadet; Dun, Nae J.; Cowan, Alan

    2009-01-01

    The aim of this study was to establish the effect of lidocaine, a local anesthetic, on pain and itch using formalin-induced nociception and kappa opioid antagonist-induced scratching models in mice. We investigated if local intradermal pretreatment (at −10 min) with lidocaine N-ethyl bromide (lidocaine, 2%, 0.1 ml) antagonizes behavioral responses and prevents c-fos expression induced by pain and itch. Male, Swiss Webster mice (25–30 g, n=6–10) were used. Formalin (5%, 20 µl, s.c.) or saline was administered to the right dorsal hindpaw and the time spent licking this paw was recorded at 0–10 min and 20–35 min. For itching, mice were challenged with 5′- guanidinonaltrindole (GNTI, 0.3 mg/kg, s.c., behind the neck) or saline and the number of neck-directed scratches with hindpaws was counted for 30 min. C-fos immunohistochemistry was performed in lumbar (for pain) and cervical (for scratching) spinal sections 2 h after respective treatments. We found that lidocaine (a) antagonizes both formalin-induced pain and GNTI-induced scratching and (b) prevents c-fos expression evoked by pain (medial side of the superficial layer and deeper layers of the dorsal horn) and itch (lateral side of the superficial layer of the dorsal horn). Additionally, GNTI caused c-fos activation in mice wearing an Elizabethan collar (to prevent scratching of the neck) suggesting that GNTI provokes c-fos expression by inducing an itch sensation. Our results highlight the antipruritic properties of lidocaine and argue for its comprehensive clinical testing against pruritic states. PMID:19549515

  20. Functional Connectivity of the Default Mode Network and Its Association With Pain Networks in Irritable Bowel Patients Assessed via Lidocaine Treatment

    PubMed Central

    Letzen, Janelle E.; Craggs, Jason G.; Perlstein, William M.; Price, Donald D.; Robinson, Michael E.

    2013-01-01

    The default mode network (DMN), a group of brain regions implicated in passive thought processes, has been proposed as a potentially informative neural marker to aid in novel treatment development. However, the DMN’s internal connectivity and its temporal relationship (ie, functional network connectivity) with pain-related neural networks in chronic pain conditions is poorly understood, as is the DMN’s sensitivity to analgesic effects. The current study assessed how DMN functional connectivity and its temporal association with 3 pain-related networks changed after rectal lidocaine treatment in irritable bowel syndrome patients. Eleven females with irritable bowel syndrome underwent a rectal balloon distension paradigm during functional magnetic resonance imaging in 2 conditions: natural history (ie, baseline) and lidocaine. Results showed increased DMN connectivity with pain-related regions during natural history and increased within-network connectivity of DMN structures under lidocaine. Further, there was a significantly greater lag time between 2 of the pain networks, those involved in cognitive and in affective pain processes, comparing lidocaine to natural history. These findings suggest that 1) DMN plasticity is sensitive to analgesic effects, and 2) reduced pain ratings via analgesia reflect DMN connectivity more similar to pain-free individuals. Findings show potential implications of this network as an approach for understanding clinical pain management techniques. Perspective This study shows that lidocaine, a peripheral analgesic, significantly altered DMN connectivity and affected its relationship with pain-related networks. These findings suggest that the DMN, which is hypothesized to represent non-goal-oriented activity, is sensitive to analgesic effects and could be useful to understand pain treatment mechanisms. PMID:23743257

  1. Inhibitory effect of lidocaine on pain and itch using formalin-induced nociception and 5'-guanidinonaltrindole-induced scratching models in mice: behavioral and neuroanatomical evidence.

    PubMed

    Inan, Saadet; Dun, Nae J; Cowan, Alan

    2009-08-15

    The aim of this study was to establish the effect of lidocaine, a local anesthetic, on pain and itch using formalin-induced nociception and kappa opioid antagonist-induced scratching models in mice. We investigated if local intradermal pretreatment (at -10 min) with lidocaine N-ethyl bromide (lidocaine, 2%, 0.1 ml) antagonizes behavioral responses and prevents c-fos expression induced by pain and itch. Male, Swiss Webster mice (25-30 g, n=6-10) were used. Formalin (5%, 20 microl, s.c.) or saline was administered to the right dorsal hindpaw and the time spent licking this paw was recorded at 0-10 min and 20-35 min. For itching, mice were challenged with 5'-guanidinonaltrindole (GNTI, 0.3mg/kg, s.c., behind the neck) or saline and the number of neck-directed scratches with hindpaws was counted for 30 min. C-fos immunohistochemistry was performed in lumbar (for pain) and cervical (for scratching) spinal sections 2h after the respective treatments. We found that lidocaine (a) antagonizes both formalin-induced pain and GNTI-induced scratching and (b) prevents c-fos expression evoked by pain (medial side of the superficial layer and deeper layers of the dorsal horn) and itch (lateral side of the superficial layer of the dorsal horn). Additionally, GNTI caused c-fos activation in mice wearing an Elizabethan collar (to prevent scratching of the neck) suggesting that GNTI provokes c-fos expression by inducing an itch sensation. Our results highlight the antipruritic properties of lidocaine and argue for its comprehensive clinical testing against pruritic states.

  2. Anesthetic efficacy of a combination of 0.5 M mannitol plus 36.8 mg of lidocaine with 18.4 μg epinephrine in maxillary infiltration: a prospective, randomized, single-blind study.

    PubMed

    Younkin, Kevin; Reader, Al; Drum, Melissa; Nusstein, John; Beck, Mike

    2014-01-01

    The purpose of this prospective, randomized, single-blind study was to determine the anesthetic efficacy of lidocaine with epinephrine compared to lidocaine with epinephrine plus 0.5 M mannitol in maxillary lateral incisor infiltrations. Forty-one subjects randomly received 2 maxillary lateral infiltrations consisting of a 1.84-mL solution of 36.8 mg lidocaine with 18.4 μg epinephrine (control solution) and a 2.90-mL solution of 36.8 mg lidocaine with 18.4 μg epinephrine (1.84 mL) plus 0.5 M mannitol (1.06 mL) in 2 separate appointments spaced at least 1 week apart. The maxillary lateral incisor was blindly electric pulp-tested in 2-minute cycles for 60 minutes postinjection. No response from the subject to the maximum output (a reading of 80) of the pulp tester was used as the criterion for pulpal anesthesia. Total percent pulpal anesthesia was defined as the total of all pulpal anesthesia readings (at output of 80) over the 60-minute test period. Pain during solution deposition and postoperative pain were also measured. The results demonstrated that a 2.90-mL solution of 36.8 mg lidocaine with 18.4 μg epinephrine (1.84 mL) plus 0.5 M mannitol (1.06 mL) was not statistically significantly superior to a 1.84-mL solution of 36.8 mg lidocaine with 18.4 μg epinephrine. The pain of solution deposition was lower with the lidocaine/mannitol formulation. Postoperative pain was not statistically significantly different between the lidocaine/mannitol formulation and the lidocaine formulation without mannitol. We concluded that adding 0.5 M mannitol to a lidocaine with epinephrine formulation was not significantly more effective in achieving a greater percentage of total pulpal anesthesia (as defined in this study) than a lidocaine formulation without mannitol in the maxillary lateral incisor.

  3. A Prospective, Randomized, Double-Blind Study of the Anesthetic Efficacy of Sodium Bicarbonate Buffered 2% Lidocaine With 1 : 100,000 Epinephrine in Inferior Alveolar Nerve Blocks

    PubMed Central

    Whitcomb, Michael; Drum, Melissa; Reader, Al; Nusstein, John; Beck, Mike

    2010-01-01

    Abstract The authors, using a crossover design, randomly administered, in a double-blind manner, inferior alveolar nerve (IAN) blocks using a buffered 2% lidocaine with 1 : 100,000 epinephrine/sodium bicarbonate formulation and an unbuffered 2% lidocaine with 1 : 100,000 epinephrine formulation at 2 separate appointments spaced at least 1 week apart. An electric pulp tester was used in 4-minute cycles for 60 minutes to test for anesthesia of the first and second molars, premolars, and lateral and central incisors. Anesthesia was considered successful when 2 consecutive 80 readings were obtained within 15 minutes, and the 80 reading was continuously sustained for 60 minutes. For the buffered 2% lidocaine with 1 : 100,000 epinephrine/sodium bicarbonate formulation, successful pulpal anesthesia ranged from 10–71%. For the unbuffered 2% lidocaine with 1 : 100,000 epinephrine formulation, successful pulpal anesthesia ranged from 10–72%. No significant differences between the 2 anesthetic formulations were noted. The buffered lidocaine formulation did not statistically result in faster onset of pulpal anesthesia or less pain during injection than did the unbuffered lidocaine formulation. We concluded that buffering a 2% lidocaine with 1 : 100,000 epinephrine with sodium bicarbonate, as was formulated in the current study, did not statistically increase anesthetic success, provide faster onset, or result in less pain of injection when compared with unbuffered 2% lidocaine with 1 : 100,000 epinephrine for an IAN block. PMID:20553136

  4. Percutaneous Injection of Lidocaine Within the Carotid Body Area in Carotid Artery Stenting: An 'Old-New' Technique

    SciTech Connect

    Mourikis, Dimitrios; Chatoupis, Konstantinos; Katsenis, Konstantinos; Vlahos, Lampros; Chatziioannou, Achilles

    2008-07-15

    Severe bradycardia is a common untoward effect during balloon angioplasty when performing carotid artery stenting. Therefore atropine injection even before dilatation and the presence of an anesthesiologist are advocated in all patients. In the surgical literature, injection of a local anesthetic agent into the carotid sinus before carotid endarterectomy was performed in an attempt to ameliorate perioperative hemodynamic instability. This study was undertaken to test the hypothesis that percutaneous infiltration of the carotid sinus with local anesthetic immediately before balloon dilatation reduces bradycardia and ameliorates the need for atropine injection or the presence of an anesthesiologist. Infiltration of the carotid sinus with 5 ml of 1% lidocaine, 3 min before dilatation, was performed in 30 consecutive patients. No one exhibited any significant rhythm change that required atropine injection. The anesthesiologist did not face any hemodynamic instability during the carotid artery stenting procedure.

  5. Lidocaine 5% patch for localized neuropathic pain: progress for the patient, a new approach for the physician

    PubMed Central

    Hans, Guy; Robert, Dominique; Verhulst, Johanna; Vercauteren, Marcel

    2010-01-01

    Neuropathic pain (NeP) syndromes remain a difficult-to-treat medical entity. Despite a growing number of pharmacological and invasive analgesic therapies the results remain less than optimal because of insufficient analgesic efficacy and/or occurrence of pronounced side effects. Current guidelines propose the use of multimodal and balanced pharmacological therapies, focused on the underlying pathophysiological mechanisms (mechanistic approach). Lidocaine 5% patches are a new treatment option currently licensed for the treatment of postherpetic neuralgia. However, these patches can also be used for the treatment of different types of superficial NeP syndromes, such as diabetic polyneuropathy. Their therapeutic success, however, largely depends on the correct identification of appropriate patients and pain syndromes. This manuscript outlines the correct identification of patients and proper use of these patches in order to ensure as much as possible the therapeutic efficacy of this new treatment option. PMID:22291487

  6. Effects of tocainide and lidocaine on the transmembrane action potentials as related to external potassium and calcium concentrations in guinea-pig papillary muscles.

    PubMed

    Oshita, S; Sada, H; Kojima, M; Ban, T

    1980-10-01

    Effects of lidocaine and tocainide on transmembrane potentials were studied in isolated guinea-pig papillary muscles, superfused with modified Tyrode's solution containing either 5.4, 2.7, 10.0 or 8.1 mmol/l potassium concentration, [K]0. The last solution applied contained either 1.8 (normal [Ca]0) or 7.2 mmol/l [Ca]0 (high [Ca]0. The concentrations of lidocaine and tocainide used were 18.5, 36.9 and 73.9 mumol/l and 43.7, 87.5 and 174.9 mumol/l in 5.4 mmol/l [K]0 solution and 36.9 and 87.5 mumol/l in the other solutions, respectively. At the driving rate of 1 Hz in 5.4 mmol/l "K]0 solution, both drugs produced dose-dependently a reduction of maximum rate of rise of action potential (Vmax), together with a prolongation of the relative refractory period. Vmax decreased progressively as the driving rate was increased from 1 Hz (for lidocaine) and from 0.25 Hz (for tocainide) to 5 Hz. This action was accentuated dose-dependently. A slow component (time constant tau = 232 ms for lidocaine, 281--303 ms for tocainide) and slower component (tau = 2.1--3.8 s for tocainide) of the recovery (reactivation) of Vmax were observed in premature responses at 0.25 Hz and in the first response after interruption of the basic driving rate at 1 Hz. All these effects were accentuated with rising [K]0 and attenuated in the high [Ca]0 solution. Both drugs abbreviated the action potential duration at 50% (APD50) and 90% (APD90) levels at 5.4, 8.1 and 10.0 mmol/l [K]0 but not at 2.7 mmol/l [K]0 nor a high [Ca]0 at 1 Hz. These [K]0-dependent effects of lidocaine on Vmax were successfully simulated by the model proposed by Hondeghem and Katzung (1977), with a slight change in parameter values. The mode of interaction of lidocaine with sodium channels in the open, closed and rested states was deduced from these results.

  7. Drug-induced vasodilation in an in vitro and in vivo study: the effects of nicardipine, papaverine, and lidocaine on the rabbit carotid artery.

    PubMed

    Evans, G R; Gherardini, G; Gürlek, A; Langstein, H; Joly, G A; Cromeens, D M; Sukumaran, A V; Williams, J; Kilbourn, R G; Wang, B; Lundeberg, T

    1997-11-01

    Extreme arterial vasoconstriction (vasospasm) is a common problem encountered in microvascular surgery. An ideal pharmacologic tool able to counteract ischemia during microsurgery should be easy to apply and exert its action both locally and distally in the microcirculation of the flap. We have compared in vitro and in vivo vascular properties of nicardipine, papaverine, and lidocaine in the rabbit carotid artery. In vitro, rings from the rabbit carotid artery (n = 7) were bathed in Krebs-Ringers solution and stretched progressively to an optimal tension of 3.7 to 4.2 g. The specimens were contracted with norepinephrine (1 microM), and a cumulative dose response curve was established. In vivo, microvascular anastomoses were performed bilaterally in the rabbit carotid artery in 35 animals using 9-0 nylon suture and standard microsurgical techniques. During and after the anastomoses, nicardipine (0.1, 0.01 mg topical, or 0.1 mg/hour IV), papaverine (30 mg/cc topical), and lidocaine (2% with and without epinephrine) were applied (blinded) at the anastomotic site in five rabbits each. Heparinized sodium chloride was used as topical irrigation for control and to clean the anastomosis. Blood flow changes were monitored continuously with the transonic Doppler for 30 minutes after the procedure. The systemic blood pressure was also monitored in a group of pilot experiments. A documented decrease in blood flow was noted in all animals after the microvascular anastomosis. Nicardipine and papaverine evoked a concentration-dependent relaxation to precontracted rings to norepinephrine. Nicardipine was greater than papaverine in inducing relaxation. Lidocaine demonstrated a biphasic response with low concentrations potentiating contraction. Systemic nicardipine and papaverine significantly increased the blood flow in the rabbit carotid artery. Topical application of nicardipine and lidocaine did not significantly alter the blood flow; however, the application of nicardipine

  8. A double blind, randomised placebo controlled trial of topical 2% viscous lidocaine in improving oral intake in children with painful infectious mouth conditions

    PubMed Central

    2011-01-01

    Background Painful infectious mouth conditions are a common presentation to emergency departments. Although self limiting, painful ulcerative lesions and inflamed mucosa can decrease oral intake and can lead to dehydration. Oral analgesia is of limited efficacy and is often refused by the patient. Despite widespread use of oral 2% viscous lidocaine for many years, there is little evidence for its efficacy as an analgesic and in aiding oral intake in children with painful infectious mouth conditions. This study aims to establish the effectiveness of 2% viscous lidocaine in increasing oral intake in these children by comparing it with placebo. Methods/Design This study is a randomised double-blind placebo controlled trial of children between 6 months and 8 years of age with painful infectious mouth conditions defined as gingivostomatitis (herpetic or non herpetic), ulcerative pharyngitis, herpangina and hand foot and mouth disease as assessed by the treating clinician in association with a history of poor oral fluid intake. It will be conducted at a single tertiary paediatric emergency department in Melbourne Australia. 20 patients have already been randomised to receive 2% lidocaine or placebo in a pilot study to determine the sample size in a preplanned adaptive design. A further 80 patients will be randomised to receive either 2% lidocaine or placebo. The placebo agent is identical to lidocaine in terms of appearance, flavour and smell. All clinical and research staff involved, patients and their parents will be blinded to treatment allocation. The primary endpoint is the amount of fluid ingested by each child, expressed in ml/kg, within 60 minutes from the time of administration of the study mixture. Secondary endpoints are the proportion of patients ingesting 5 ml/kg and 10 ml/kg at 30 and 60 minutes after drug administration and the incidence of adverse events. Longer term outcomes will include the proportion of patients requiring hospital admission and length

  9. Biocompatible lidocaine and prilocaine loaded-nanoemulsion system for enhanced percutaneous absorption: QbD-based optimisation, dermatokinetics and in vivo evaluation.

    PubMed

    Negi, Poonam; Singh, Bhupinder; Sharma, Gajanand; Beg, Sarwar; Katare, Om Prakash

    2015-01-01

    Barrier properties of the skin and physicochemical properties of the drugs are the main hiccups in delivering local anaesthetic molecules topically. The present work endeavours for systematic optimisation and evaluation of nanoemulsions (NEs) of local anaesthetic drugs, lidocaine and prilocaine, employing the systematic approach of Quality by Design. A 3(3) Box-Behnken design was employed for systematic optimisation of the factors obtained from screening studies employing Plackett-Burman design and risk assessment studies. The superior permeation rates, and higher concentrations of the drugs in skin layers from the optimised NE carriers, were achieved in permeation and dermatokinetic studies, when compared to marketed cream. Furthermore, rapid onset of action was demonstrated by the NE system in rabbit eye corneal reflex model and biocompatibility was confirmed from the absence of any marked skin change(s) in the normal skin histology. The developed NE systems demonstrated it as a promising carrier for topical delivery of lidocaine and prilocaine.

  10. Efficacy of Articaine and Lidocaine for Buccal Infiltration of First Maxillary Molars with Symptomatic Irreversible Pulpitis: A Randomized Double-blinded Clinical Trial

    PubMed Central

    Hosseini, Hamid Reza; Parirokh, Masoud; Nakhaee, Nouzar; V. Abbott, Paul; Samani, Syamak

    2016-01-01

    Introduction: The aim of the present study was to compare the efficacy of 2% lidocaine to 4% articaine in buccal infiltration of maxillary first molars with irreversible pulpitis. Moreover, the effect of root length on success of anesthesia irrespective of the type of anesthetic agent was assessed. Methods and Materials: Fifty patients suffering from painful maxillary first molars with irreversible pulpitis received an infiltration injection of either 4% articaine with 1:100000 epinephrine or 2% lidocaine with 1:80000 epinephrine. Each patient recorded their pain score in response to a cold test on a Heft-Parker visual analogue scale (VAS) before commencing the treatment, 5 min following injection, during access preparation, after pulp exposure and during root canal instrumentation. No or mild pain at any stage was considered a success. Data were analyzed using the multivariate logistic regression analysis, chi-square and t tests. Results: Finally, 47 out of 50 patients were eligible to be included in this study. The anesthetic success rates in the lidocaine and articaine groups were 56.52% and 66.67%, respectively and the difference was not significant (P=0.474). Irrespective of the anesthetic agent, the length of the palatal root (Odds Ratio=0.24, P=0.007) had an adverse effect on anesthetic success. There was an association between longer palatal root length and anesthetic failure. Conclusion: No significant difference was found between 2% lidocaine and 4% articaine in terms of anesthetic success in maxillary first molars with irreversible pulpitis. The length of the palatal root had a significant negative influence on anesthetic success. PMID:27141212

  11. Reduction of painful area as new possible therapeutic target in post-herpetic neuropathic pain treated with 5% lidocaine medicated plaster: a case series

    PubMed Central

    Casale, Roberto; Di Matteo, Maria; Minella, Cristina E; Fanelli, Guido; Allegri, Massimo

    2014-01-01

    Post-herpetic neuralgia (PHN) is neuropathic pain persisting after an acute episode of herpes zoster, and is associated with severe pain and sensory abnormalities that adversely affect the patient’s quality of life and increase health care costs. Up to 83% of patients with PHN describe localized neuropathic pain, defined as “a type of neuropathic pain characterized by consistent and circumscribed area(s) of maximum pain”. Topical treatments have been suggested as a first-line treatment for localized neuropathic pain. Use of 5% lidocaine medicated plaster could reduce abnormal nervous peripheral discharge and via the plaster could have a “protective” function in the affected area. It has been suggested that use of this plaster could reduce pain as well as the size of the painful area. To evaluate this possible outcome, we retrospectively reviewed eight patients with PHN, treated using 5% lidocaine medicated plaster. During a follow-up period of 3 months, we observed good pain relief, which was associated with a 46% reduction in size of the painful area after one month (from 236.38±140.34 cm2 to 128.80±95.7 cm2) and a 66% reduction after 3 months (81.38±59.19 cm2). Our study cohort was composed mainly of elderly patients taking multiple drugs to treat comorbidities, who have a high risk of drug–drug interactions. Such patients benefit greatly from topical treatment of PHN. Our observations confirm the effectiveness of lidocaine plasters in the treatment of PHN, indicating that 5% lidocaine medicated plaster could reduce the size of the painful area. This last observation has to be confirmed and the mechanisms clarified in appropriate larger randomized controlled trials. PMID:25018649

  12. Seizures and Methemoglobinemia After Topical Application of Eutectic Mixture of Lidocaine and Prilocaine on a 3.5-Year-Old Child with Molluscum Contagiosum and Atopic Dermatitis.

    PubMed

    Cho, Yong Se; Chung, Bo Young; Park, Chun Wook; Kim, Hye One

    2016-09-01

    A eutectic mixture of lidocaine and prilocaine (EMLA) is used topically to provide local anesthesia for a variety of painful superficial procedures. Although the side effects of EMLA are usually mild and transient local reactions, potentially life-threatening complications can occur. We report a case of generalized seizures and methemoglobinemia after topical application of EMLA for curettage of molluscum contagiosum lesions in a 3.5-year-old girl with atopic dermatitis.

  13. An improved model for the binding of lidocaine and structurally related local anaesthetics to fast-inactivated voltage-operated sodium channels, showing evidence of cooperativity

    PubMed Central

    Leuwer, Martin; Haeseler, Gertrud; Hecker, Hartmut; Bufler, Johannes; Dengler, Reinhard; Aronson, Jeffrey K

    2003-01-01

    The interaction of lidocaine-like local anaesthetics with voltage-operated sodium channels is traditionally assumed to be characterized by tighter binding of the drugs to depolarized channels. As inactivated and drug-bound channels are both unavailable on depolarization, an indirect approach is required to yield estimates for the dissociation constants from channels in inactivated states. The established model, originally described by Bean et al., describes the difference in affinity between resting and inactivated states in terms of the concentration dependence of the voltage shift in the availability curve. We have tested the hypothesis that this model, which assumes a simple Langmuir relationship, could be improved by introducing a Hill-type exponent, which would take into account potential sources of cooperativity. Steady-state block by lidocaine was studied in heterologously (HEK 293) expressed human skeletal muscle sodium channels and compared with experimental data previously obtained for 2,6-dimethylphenol, 3,5-dimethyl-4-chlorophenol, and 4-chlorophenol. Cells were clamped to membrane potentials from −150 to −5 mV, and a subsequent test pulse was used to assess the number of channels available to open. All compounds shifted the voltage dependence of channel availability in the direction of negative prepulse potentials. Prediction of the concentration dependence of the voltage shift in the availability curve was improved by the modified model, as shown by a marked reduction in the residual sum of squares. For all compounds, the Hill-type exponent was significantly greater than one. These results could be interpreted in the light of the contemporary hypothesis that lidocaine functions as an allosteric gating effector to enhance sodium channel inactivation by strengthening the latch mechanism of inactivation, which is considered to be a particle-binding process allosterically coupled to activation. Alternatively, they could be interpreted by postulating

  14. An improved model for the binding of lidocaine and structurally related local anaesthetics to fast-inactivated voltage-operated sodium channels, showing evidence of cooperativity.

    PubMed

    Leuwer, Martin; Haeseler, Gertrud; Hecker, Hartmut; Bufler, Johannes; Dengler, Reinhard; Aronson, Jeffrey K

    2004-01-01

    1. The interaction of lidocaine-like local anaesthetics with voltage-operated sodium channels is traditionally assumed to be characterized by tighter binding of the drugs to depolarized channels. As inactivated and drug-bound channels are both unavailable on depolarization, an indirect approach is required to yield estimates for the dissociation constants from channels in inactivated states. The established model, originally described by Bean et al., describes the difference in affinity between resting and inactivated states in terms of the concentration dependence of the voltage shift in the availability curve. We have tested the hypothesis that this model, which assumes a simple Langmuir relationship, could be improved by introducing a Hill-type exponent, which would take into account potential sources of cooperativity. 2. Steady-state block by lidocaine was studied in heterologously (HEK 293) expressed human skeletal muscle sodium channels and compared with experimental data previously obtained for 2,6-dimethylphenol, 3,5-dimethyl-4-chlorophenol, and 4-chlorophenol. Cells were clamped to membrane potentials from -150 to -5 mV, and a subsequent test pulse was used to assess the number of channels available to open. 3. All compounds shifted the voltage dependence of channel availability in the direction of negative prepulse potentials. Prediction of the concentration dependence of the voltage shift in the availability curve was improved by the modified model, as shown by a marked reduction in the residual sum of squares. 4. For all compounds, the Hill-type exponent was significantly greater than one. These results could be interpreted in the light of the contemporary hypothesis that lidocaine functions as an allosteric gating effector to enhance sodium channel inactivation by strengthening the latch mechanism of inactivation, which is considered to be a particle-binding process allosterically coupled to activation. Alternatively, they could be interpreted by

  15. Effect of paracetamol, dexketoprofen trometamol, lidocaine spray, and paracervical block application for pain relief during suction termination of first-trimester pregnancy.

    PubMed

    Açmaz, Gökhan; Aksoy, Hüseyin; Özoğlu, Nil; Aksoy, Ülkü; Albayrak, Evrim

    2013-01-01

    The aim of the study was to investigate the analgesic efficacy of preoperative oral dexketoprofen trometamol, intravenous paracetamol, lidocaine spray, and paracervical block with ultracaine on curettage procedure. A total of 111 subjects with the request of pregnancy termination between 5 and 7 weeks of gestation were included in the study. The first group (control group) consisted of 20 participants without medication. The second group consisted of 25 participants receiving 2 puffs of lidocaine sprays on cervical mucosa. The third group consisted of 20 participants receiving oral 25 mg dexketoprofen trometamol. The fourth group consisted of 23 participants receiving 1000 mg intravenous paracetamol and the fifth group consisted of 23 participants receiving paracervical block with ultracaine. Paracervical block reduced pain score significantly in both intraoperative and postoperative periods. All analgesic procedures were significantly effective for reducing pain in postoperative period. Paracervical block may be the best method for reducing pain scores in intraoperative and postoperative periods during curettage procedure. All analgesic procedures such as lidocaine, paracetamol, ultracaine, and paracervical block with ultracaine can be used for reducing pain score in postoperative period. This trial is registered with NCT01947205.

  16. Effect of lidocaine and quinidine on steady-state characteristics and recovery kinetics of (dV/dt)max in guinea pig ventricular myocardium.

    PubMed

    Chen, C M; Gettes, L S; Katzung, B G

    1975-07-01

    We studied the effects of quinidine and lidocaine on the steady-state relationship between membrane potential and the maximum rate of rise of the action potential, (dV/dt)max, and on the recovery kinetics of (dV/dt)max in guinea pig papillary muscles. The steady-state relationships were determined in fibers stimulated at 0.2/sec and depolarized with KCl. Recovery kinetics were determined at various resting membrane potentials by assessing (dV/dt)max in progressively earlier premature action potentials. Lidocaine caused a dose-dependent decrease in (dV/dt)max, shifted the curve defining the steady-state relationship along the voltage axis in the direction of more negative potentials, and slowed the recovery kinetics of (dV/dt)max. Quinidine caused a dose-dependent decrease in (dV/dt)max but did not alter the shape of the curves defining either the steady-state relationship or the recovery kinetics of (dV/dt)max. Both drugs depressed membrane responsiveness as determined in premature action potentials originating from incompletely repolarized fibers. Our study indicates that the mechanisms whereby quinidine and lidocaine influence (dV/dt)max are different. It is possible that this difference may underlie some of the differences in the clinical effects of these two drugs.

  17. High-Throughput Analysis of Lidocaine in Pharmaceutical Formulation by Capillary Zone Electrophoresis Using Multiple Injections in a Single Run

    PubMed Central

    Valese, Andressa C.; Spudeit, Daniel A.; Dolzan, Maressa D.; Bretanha, Lizandra C.; Micke, Gustavo A.

    2016-01-01

    This paper reports the development of a subminute separation method by capillary zone electrophoresis in an uncoated capillary using multiple injection procedure for the determination of lidocaine in samples of pharmaceutical formulations. The separation was performed in less than a minute leading to doing four injections in a single run. The cathodic electroosmotic flow contributed to reducing the analyses time. The background electrolyte was composed of 20 mmol L−1 2-amino-2-(hydroxymethyl)-1,3-propanediol and 40 mmol L−1 2-(N-morpholino)ethanesulfonic acid at pH 6.1. The internal standard used was benzylamine. Separations were performed in a fused uncoated silica capillary (32 cm total length, 23.5 cm effective length, and 50 μm internal diameter) with direct UV detection at 200 nm. Samples and standards were injected hydrodynamically using 40 mbar/3 s interspersed with spacer electrolyte using 40 mbar/7 s. The electrophoretic system was operated under constant voltage of 30 kV with positive polarity on the injection side. The evaluation of some analytical parameters of the method showed good linearity (r2 > 0.999), a limit of detection 0.92 mg L−1, intermediate precision better than 3.2% (peak area), and recovery in the range of 92–102%. PMID:27069712

  18. Management of pain from heel lance with lidocaine-prilocaine (EMLA) cream: is it safe and efficacious in preterm infants?

    PubMed

    Stevens, B; Johnston, C; Taddio, A; Jack, A; Narciso, J; Stremler, R; Koren, G; Aranda, J

    1999-08-01

    Hospitalized preterm infants undergo multiple painful heel lances. A two-phase, randomized, controlled trial was undertaken to determine the safety and efficacy of lidocaine-prilocaine 5% cream (EMLA, Astra Pharmaceuticals, L.P, Westborough, MA) for relieving pain from heel lance. One hundred twenty infants were randomly assigned to receive 0.5 g of EMLA or placebo cream for 30 minutes (Phase 1) or 60 minutes (Phase 2) before a routine heel lance. Efficacy was assessed using the Premature Infant Pain Profile (PIPP). Safety was determined by methemoglobin concentration 8 hours after EMLA application and by clinical signs of methemoglobinemia. No significant differences existed on PIPP scores between EMLA and placebo groups in Phase 1 (p < .480) or Phase 2 (p < .831). No infant had any clinical signs of methemoglobinemia. The mean methemoglobin concentration was 1.19% (.47). Approximately 10% of infants had minor skin reactions, and approximately 20% of EMLA-treated infants had blanching at the application site. The authors conclude that EMLA is safe but not efficacious for relieving pain from heel lance in preterm infants.

  19. Anesthetic efficacy of the Gow-Gates injection and maxillary infiltration with articaine and lidocaine for irreversible pulpitis.

    PubMed

    Sherman, Michael G; Flax, Michael; Namerow, Kenneth; Murray, Peter E

    2008-06-01

    The aim of this randomized, double-blinded study was to compare the anesthetic efficacy of 4% articaine with 1:100,000 epinephrine (AE) with 2% lidocaine with 1:100,000 epinephrine (LE) for Gow-Gates blocks and maxillary infiltrations in patients experiencing irreversible pulpitis in mandibular and maxillary posterior teeth. Forty patients diagnosed with irreversible pulpitis of a posterior tooth randomly received either AE or LE by using a Gow-Gates injection or maxillary infiltration. Endodontic access was initiated after no response to Endo-ice 15 minutes after solution deposition. Success was defined as none to mild pain on a visual analogue scale after access. Chi-square and analysis of variance statistical tests were used to analyze the data. Successful endodontic treatment substantially reduced the assessment of pulpitis pain by patients (analysis of variance, P < .0001). Overall anesthetic success in both dental arches was 87.5%. Anesthetic success was not influenced by tooth arch (chi(2), P > .7515) or gender (chi(2), P > .1115). AE proved to be as effective but not superior to LE (P > .6002). These results demonstrated the similar anesthetic effectiveness of AE and LE when used during the endodontic treatment of teeth diagnosed with irreversible pulpitis.

  20. Clinical improvement of secondary focal limb dystonia in neurodegenerative disease following a five-day lidocaine infusion: a case report.

    PubMed

    Irwin, D; Revuelta, G; Lippa, C F

    2009-02-15

    Dystonia associated with neurodegenerative disease has minimal effective treatment options and can be devastating to a patient's ability to perform tasks of daily living. We present a case of a 55 year-old man who had progressive symptoms of an atypical asymmetric parkinsonian neurodegenerative disease. This patient presented with a dystonic left upper extremity that was refractory to treatment. In an attempt to treat worsening pain associated with the dystonia, he was given a five-day lidocaine infusion for associated pain and within 24 h had improvement in mobility of his dystonic extremity. Dystonia was measured by the Burke-Fahn-Marsden (BFM) dystonia rating and disability scales on hospital day five and at an eight week follow up visit. These scores were compared with scores derived from his previous pre-treatment neurologic examination. The BFM dystonia scale score was initially 16 and improved to 12 on both immediate post-treatment and eight-week follow-up. The BFM disability score improved from 16 to 6 post treatment and to 8 on follow-up appointment. Most importantly, the patient could feed and dress himself for the first time in several years. No adverse events of treatment were encountered. Treatment effect lasted three months with a slow return to baseline motor function. This case report raises interesting questions regarding the mechanism of dystonia in neurodegenerative disease and suggests the afferent sensory system as a potential target for therapeutics.

  1. Effects of Liposomes Charge on Extending Sciatic Nerve Blockade of N-ethyl Bromide of Lidocaine in Rats

    NASA Astrophysics Data System (ADS)

    Yin, Qinqin; Ke, Bowen; Chen, Xiaobing; Guan, Yikai; Feng, Ping; Chen, Guo; Kang, Yi; Zhang, Wensheng; Nie, Yu

    2016-12-01

    N-methyl bromide of lidocaine (QX-314) is a potential local anaesthetic with compromised penetration through cell membranes due to its obligated positive charge. Liposomes have been widely used for drug delivery with promising efficacy and safety. Therefore we investigated the local anaesthetic effects and tissue reactions of QX-314 in combination with anionic, cationic or neutral liposomes in rat sciatic nerve block model, and explored the effects of these liposomes on cellular entry of QX-314 in human embryonic kidney 293 cells. The results demonstrated that anionic liposomes substantially prolonged the duration of sensory (25.7 ± 8.3 h) and motor (41.4 ± 6.1 h) blocks of QX-314, while cationic and neutral ones had little effects. Tissue reactions from QX-314 with anionic liposomes were similar to those with commonly used local anaesthetic bupivacaine. Consistent with in vivo results, the anionic liposomes produced the greatest promotion of cellular entry of QX-314 in a time-dependent manner. In conclusion, ultra-long lasting nerve blocks were achieved by a mixture of QX-314 and anionic liposomes with a satisfactory safety profile, indicating a potential approach to improve postoperative pain management. The liposome-induced enhancement in cellular uptake of QX-314 may underlie the in vivo effects.

  2. Development of a HPLC-MS/MS method for the simultaneous determination of nifedipine and lidocaine in human plasma.

    PubMed

    Grigoriev, Alexander; Nikitina, Alexandra; Yaroshenko, Irina; Sidorova, Alla

    2016-11-30

    The method for simultaneous determination of nifedipine (NIF) and lidocaine (LID) in human plasma by one-step sample preparation has been developed for the first time. Due to the photosensitivity of nifedipine and its low plasma concentrations a precise and reliable method was required. The method involved liquid-liquid extraction (methyl tert-butyl ether, MTBE), and 10μL of the resulting sample was analyzed by HPLC-MS/MS. Chromatographic separation was achieved on an YMC-Triart C18 HPLC column (100×2.0mm; S-5μm 12nm). The mobile phase was methanol:water, 60:40 (v/v) and contained 0.15% acetic acid. The linearity of the method was established in the concentration ranges of 0.5-50ng/mL for NIF and 1.0-500ng/mL for LID. Photodestruction of NIF under ambient light was evaluated. The validated method was successfully applied to analyze human plasma samples after rectal application of the drug (1g) containing 2.0% LID and 0.3% NIF.

  3. Effects of Liposomes Charge on Extending Sciatic Nerve Blockade of N-ethyl Bromide of Lidocaine in Rats

    PubMed Central

    Yin, Qinqin; Ke, Bowen; Chen, Xiaobing; Guan, Yikai; Feng, Ping; Chen, Guo; Kang, Yi; Zhang, Wensheng; Nie, Yu

    2016-01-01

    N-methyl bromide of lidocaine (QX-314) is a potential local anaesthetic with compromised penetration through cell membranes due to its obligated positive charge. Liposomes have been widely used for drug delivery with promising efficacy and safety. Therefore we investigated the local anaesthetic effects and tissue reactions of QX-314 in combination with anionic, cationic or neutral liposomes in rat sciatic nerve block model, and explored the effects of these liposomes on cellular entry of QX-314 in human embryonic kidney 293 cells. The results demonstrated that anionic liposomes substantially prolonged the duration of sensory (25.7 ± 8.3 h) and motor (41.4 ± 6.1 h) blocks of QX-314, while cationic and neutral ones had little effects. Tissue reactions from QX-314 with anionic liposomes were similar to those with commonly used local anaesthetic bupivacaine. Consistent with in vivo results, the anionic liposomes produced the greatest promotion of cellular entry of QX-314 in a time-dependent manner. In conclusion, ultra-long lasting nerve blocks were achieved by a mixture of QX-314 and anionic liposomes with a satisfactory safety profile, indicating a potential approach to improve postoperative pain management. The liposome-induced enhancement in cellular uptake of QX-314 may underlie the in vivo effects. PMID:27924842

  4. Comparison of injection pain, heart rate increase, and postinjection pain of articaine and lidocaine in a primary intraligamentary injection administered with a computer-controlled local anesthetic delivery system.

    PubMed Central

    Nusstein, John; Berlin, Jeffrey; Reader, Al; Beck, Mike; Weaver, Joel M.

    2004-01-01

    The purpose of this prospective, randomized, double-blind study was to compare the pain of injection, heart rate increase, and postinjection pain of the intraligamentary injection of 4% articaine with 1:100,000 epinephrine and 2% lidocaine with 1:100,000 epinephrine administered with a computer-controlled local anesthetic delivery system. Using a crossover design, intraligamentary injections of 1.4 mL of 4% articaine with 1:100,000 epinephrine and 1.4 mL of 2% lidocaine with 1:100,000 epinephrine were randomly administered on the mesial and distal aspects of the mandibular first molar with a computer-controlled local anesthetic delivery system in a double-blind manner at 2 separate appointments to 51 subjects. The results demonstrated the incidence of moderate pain was 14%-27% with needle insertion, with 0%-4% reporting severe pain. For solution deposition, moderate pain was reported 8%-18% of the time, with no reports of severe pain. There were no significant differences between the articaine and lidocaine solutions. Regarding heart rate changes, neither anesthetic solution resulted in a significant increase in heart rate over baseline readings. On day 1 postinjection, there was a 31% incidence of moderate/severe pain with the articaine solution and 20% incidence of moderate/severe pain with the lidocaine solution. The moderate/severe pain ratings decreased over the next 2 days. There were no significant differences between the articaine and lidocaine solutions. We concluded that the intraligamentary injection of 4% articaine with 1:100,000 epinephrine was similar to 2% lidocaine with 1:100,000 epinephrine for injection pain and postinjection pain in the mandibular first molar when administered with a computer-controlled local anesthetic delivery system. For both anesthetic solutions, heart rate did not significantly increase with the intraligamentary injection using the computer-controlled local anesthetic system. PMID:15675261

  5. The 5% Lidocaine-Medicated Plaster: Its Inclusion in International Treatment Guidelines for Treating Localized Neuropathic Pain, and Clinical Evidence Supporting its Use.

    PubMed

    Baron, Ralf; Allegri, Massimo; Correa-Illanes, Gerardo; Hans, Guy; Serpell, Michael; Mick, Gerard; Mayoral, Victor

    2016-12-01

    When peripheral neuropathic pain affects a specific, clearly demarcated area of the body, it may be described as localized neuropathic pain (LNP). Examples include postherpetic neuralgia and painful diabetic neuropathy, as well as post-surgical and post-traumatic pain. These conditions may respond to topical treatment, i.e., pharmaceutical agents acting locally on the peripheral nervous system, and the topical route offers advantages over systemic administration. Notably, only a small fraction of the dose reaches the systemic circulation, thereby reducing the risk of systemic adverse effects, drug-drug interactions and overdose. From the patient's perspective, the analgesic agent is easily applied to the most painful area(s). The 5% lidocaine-medicated plaster has been used for several years to treat LNP and is registered in approximately 50 countries. Many clinical guidelines recommend this treatment modality as a first-line option for treating LNP, particularly in frail and/or elderly patients and those receiving multiple medications, because the benefit-to-risk ratios are far better than those of systemic analgesics. However, some guidelines make only a weak recommendation for its use. This paper considers the positioning of the 5% lidocaine-medicated plaster in international treatment guidelines and how they may be influenced by the specific criteria used in developing them, such as the methodology employed by randomized, placebo-controlled trials. It then examines the body of evidence supporting use of the plaster in some prevalent LNP conditions. Common themes that emerge from clinical studies are: (1) the excellent tolerability and safety of the plaster, which can increase patients' adherence to treatment, (2) continued efficacy over long-term treatment, and (3) significant reduction in the size of the painful area. On this basis, it is felt that the 5% lidocaine-medicated plaster should be more strongly recommended for treating LNP, either as one component

  6. Electro-Oxidation Mechanism and Direct Square-Wave Voltammetric Determination of Lidocaine With a Carbon-Paste Electrode

    PubMed Central

    Rahbar, Nadereh; Ramezani, Zahra; Babapour, Ahmad

    2015-01-01

    Background Lidocaine hydrochloride (LH) is one of the most extensively used local anesthetics and peripheral analgesics. Availability of a simple and sensitive assay method for this analyte in pharmaceutical preparations as well as development of new voltammetric detectors that can be applied in chromatographic systems for determination of this analyte in biological samples are of great importance. Objectives In this study, a square-wave voltammetric (SWV) determination of LH at a bare carbon-paste electrode (CPE) was reported. Moreover, the oxidation mechanism for LH molecule at this electrode was investigated. Materials and Methods The SW voltammogram of LH solution at CPE showed a well-defined peak between +0.80 and +0.88 V depending on a scan rate in potassium nitrate (KNO3) solution. Different chemical and instrumental parameters influencing the voltammetric response, such as the pH level and scan rate were optimized for LH determination. Results A linear range of 8.0 - 1000.0 μmol L-1 (r2 = 0.999) was obtained. The limit of detection (LOD) was 0.29 μmol L-1. The relative standard deviations of 2.1% obtained for 0.8 800 μmol L-1 solution of LH indicated a reasonable reproducibility of the method. Conclusions The results of this study show that LH in different pharmaceutical preparations could be determined with good reliability. In addition, the results reveal that the equal numbers of electrons and protons are involved in the oxidation of LH and the irreversible oxidation of an analyte was performed via amine groups of LH molecule. PMID:25866720

  7. A Randomized Clinical Trial of Jet Injected Lidocaine (J tip) to Reduce Venipuncture Pain for Young Children

    PubMed Central

    Lunoe, Maren M; Drendel, Amy L; Levas, Michael N; Weisman, Steven J; Dasgupta, Mahua; Hoffmann, Raymond G; Brousseau, David C

    2016-01-01

    Background The J tip uses air instead of a needle to push lidocaine into the skin. No studies have investigated its use for venipuncture in young children. Objective Determine if J tip decreased venipuncture pain in young children compared to vapocoolant spray. Methods Children ages 1 to 6 years were randomized into 3 groups: Intervention – J tip, Control –vapocoolant spray, and Sham –vapocoolant spray and “pop” of an empty J tip. The procedure was videotaped and scored using the FLACC tool at three times; Baseline - before approach, Device - J tip deployment and Venipuncture - venipuncture. The FLACC tool was scored 0(none) to 10(severe). Comparisons of pain scores over time were made using the Generalized Estimating Equation. Venipuncture success and adverse effects were assessed and compared using Χ2. Results 205 children enrolled; Intervention=96, Control=53, Sham=56. There were no between group differences in baseline characteristics. There was no mean change in pain scores from Device to Venipuncture in the Intervention group (0.25, 95% CI (−0.31, 0.82) but there was an increase in pain in the Control (2.82, 95% CI (1.91, 3.74) and Sham (1.68, 95% CI (0.83, 2.52) groups. This change was greater for the Control and Sham compared to the Intervention group. There was no difference in venipuncture success between groups. No severe adverse events occurred. Minor adverse events were the same between groups. Conclusion Use of the J tip for children ages 1 to 6 years reduced venipuncture pain compared to vapocoolant spray or sham treatment. PMID:25935844

  8. Application of statistical experimental design to study the formulation variables influencing the coating process of lidocaine liposomes.

    PubMed

    González-Rodríguez, M L; Barros, L B; Palma, J; González-Rodríguez, P L; Rabasco, A M

    2007-06-07

    In this paper, we have used statistical experimental design to investigate the effect of several factors in coating process of lidocaine hydrochloride (LID) liposomes by a biodegradable polymer (chitosan, CH). These variables were the concentration of CH coating solution, the dripping rate of this solution on the liposome colloidal dispersion, the stirring rate, the time since the liposome production to the liposome coating and finally the amount of drug entrapped into liposomes. The selected response variables were drug encapsulation efficiency (EE, %), coating efficiency (CE, %) and zeta potential. Liposomes were obtained by thin-layer evaporation method. They were subsequently coated with CH according the experimental plan provided by a fractional factorial (2(5-1)) screening matrix. We have used spectroscopic methods to determine the zeta potential values. The EE (%) assay was carried out in dialysis bags and the brilliant red probe was used to determine CE (%) due to its property of forming molecular complexes with CH. The graphic analysis of the effects allowed the identification of the main formulation and technological factors by the analysis of the selected responses and permitted the determination of the proper level of these factors for the response improvement. Moreover, fractional design allowed quantifying the interactions between the factors, which will consider in next experiments. The results obtained pointed out that LID amount was the predominant factor that increased the drug entrapment capacity (EE). The CE (%) response was mainly affected by the concentration of the CH solution and the stirring rate, although all the interactions between the main factors have statistical significance.

  9. Use of 5% lidocaine medicated plaster to treat localized neuropathic pain secondary to traumatic injury of peripheral nerves

    PubMed Central

    Correa-Illanes, Gerardo; Roa, Ricardo; Piñeros, José Luis; Calderón, Wilfredo

    2012-01-01

    Objective The efficacy of 5% lidocaine medicated plaster (LMP) has previously been demonstrated in post-traumatic localized neuropathic pain. This study evaluated the use of LMP in localized neuropathic pain secondary to traumatic peripheral nerve injury. Patients and methods This prospective observational study enrolled patients with traumatic injuries to peripheral nerves that were accompanied by localized neuropathic pain of more than 3 months duration. Demographic variables, pain intensity (measured using the numeric rating scale; NRS), answers to the Douleur Neuropathique 4 (DN4) questionnaire, and the size of the painful area were recorded. Results Nineteen patients were included, aged (mean ± standard deviation) 41.4 ± 15.7 years. Nerve injuries affected the upper (eight patients) or lower (11 patients) limbs. The mean duration of pain before starting treatment with LMP was 22.6 ± 43.5 months (median 8 months). Mean baseline values included: NRS 6.7 ± 1.6, painful area 17.8 ± 10.4 cm2 (median 18 cm2), and DN4 score 6.7 ± 1.4. The mean duration of treatment with LMP was 19.5 ± 10.0 weeks (median 17.4 weeks). Mean values after treatment were: NRS 2.8 ± 1.5 (≥3 point reduction in 79% of patients, ≥50% reduction in 57.9% of patients) and painful area 2.1 ± 2.3 cm2 (median 1 cm2, ≥50% reduction in 94.7% of patients). Functional improvement after treatment was observed in 14/19 patients (73.7%). Conclusion LMP effectively treated traumatic injuries of peripheral nerves which presented with chronic localized neuropathic pain, reducing both pain intensity and the size of the painful area. PMID:23152700

  10. Enhancement of the 1-Octanol/Water Partition Coefficient of the Anti-Inflammatory Indomethacin in the Presence of Lidocaine and Other Local Anesthetics.

    PubMed

    Tateuchi, Ryo; Sagawa, Naoki; Shimada, Yohsuke; Goto, Satoru

    2015-07-30

    Side effects and excessive potentiation of drug efficacy caused by polypharmacy are becoming important social issues. The apparent partition coefficient of indomethacin (log P'IND) increases in the presence of lidocaine, and this is used as a physicochemical model for investigating polypharmacy. We examined the changes in log P'IND caused by clinically used local anesthetics-lidocaine, tetracaine, mepivacaine, bupivacaine, and dibucaine-and by structurally similar basic drugs-procainamide, imipramine, and diltiazem. The quantitative structure-activity relationship study of log P'IND showed that the partition coefficient values (log PLA) and the structural entropic terms (ΔSobs, log f) of the additives affect log P'IND. These results indicate that the local anesthetics and structurally similar drugs function as phase-transfer catalysts, increasing the membrane permeability of indomethacin via heterogeneous intermolecular association. Therefore, we expect that the potency of indomethacin, an acidic nonsteroidal anti-inflammatory drug, will be increased by concurrent administration of the other drugs.

  11. Analysis of lidocaine and its major metabolite, monoethylglycinexylidide, in elk velvet antler by liquid chromatography with UV detection and confirmation by electrospray ionization tandem mass spectrometry.

    PubMed

    Bagonluri, Mukasa T; Woodbury, Murray R; Reid, R Stephen; Boison, Joe O

    2005-04-06

    A sensitive liquid chromatographic (LC) method with UV detection was developed for the determination of residues of lidocaine (LID) and its major metabolite, monoethylglycinexylidide (MEGX), in elk velvet antler. The drugs were extracted from alkaline velvet antler homogenates, cleaned up on a C(18) solid-phase extraction cartridge, and separated on an Inertsil ODS-3 (3.0 x 250 mm, 5 microm) column using an isocratic mobile phase made up of 0.05 M phosphate buffer (pH 4.0)/acetonitrile (88:12, v/v) at a flow rate of 1.0 mL/min. The limits of quantification for LID and its major metabolite, MEGX, were 10 and 20 ng/g, respectively. The method was validated and used to measure the concentration of residues of LID and MEGX in elk velvet antlers harvested after either LID anesthesia or application of a drug-free control method (electro-anesthesia, EA). No LID or MEGX residues were detected in any of the antlers harvested after EA application. No MEGX residues were detected in any of the velvet antlers harvested after LID application, but residues of LID ranging in concentration from 68 to 4300 ng/g were detected in the three sections of the velvet antlers harvested after LID administration. LC-tandem mass spectrometry was used to confirm the presence of lidocaine detected in the velvet antlers.

  12. The behavioral assessment and alleviation of pain associated with castration in beef calves treated with flunixin meglumine and caudal lidocaine epidural anesthesia with epinephrine.

    PubMed

    Currah, Jan M; Hendrick, Steven H; Stookey, Joseph M

    2009-04-01

    The objectives of this study were 1) to determine the effects of flunixin megulmine in combination with caudal epidural anesthesia as a postoperative analgesic in beef calves following surgical castration, and 2) to consider stride length and pedometry as potential behavioral assessment tools for detecting postcastration pain. Surgical castration was performed in 101 beef calves randomly assigned to 3 treatment subgroups: 1) castration without anesthesia (SURG); 2) castration following lidocaine with epinephrine caudal epidural anesthesia (SURG + EPI); 3) castration following lidocaine with epinephrine caudal epidural anesthesia and flunixin meglumine (SURG + EPI + F). Several outcomes, including pedometer counts, changes in stride length, subjective visual assessment of pain, instantaneous scan sampling of the calves' postoperative activities, and the amount of movement and vocalization during the castration procedure, were measured to identify and quantify pain. The results indicated that stride length and the number of steps taken by calves after castration appear to be good measures of pain. Significant differences found between treatment groups for stride length and visual assessments suggest that flunixin meglumine can be considered to provide visible pain relief up to 8 hours postcastration.

  13. Spatial cognition and memory: a reversible lesion with lidocaine into the anteromedial/posterior parietal cortex (AM/PPC) affects differently working and long-term memory on two foraging tasks.

    PubMed

    Espina-Marchant, Pablo; Pinto-Hamuy, Teresa; Bustamante, Diego; Morales, Paola; Robles, Luis; Herrera-Marschitz, Mario

    2006-01-01

    Place memory is relevant for exploration and forage behaviour. When food supply is dispersed, a win-shift has advantage over a win-stay strategy. In the Olton Octagonal Maze, the rat follows a win-shift strategy using working memory. However, in the Olton 4x4 version, the rat follows a win-stay strategy, using both working and long-term memories. It has been suggested that the neocortex is required for the resolution of tasks demanding long-term, but not for that demanding working memory alone. The role of anteromedial/posterior parietal cortex (AM/PPC) was investigated here, using a reversible lesion induced by intracerebral lidocaine infusion. Long-Evans rats were implanted with guide cannulae into the AM/PPC and trained in an Olton 4x4 maze, counting working and long-term memory errors after a delay. Then, the animals were infused with lidocaine or saline during the delay phase and tested for three days. Another series of animals, treated as before, was tested in an Olton Octagonal Maze and subjected to the same injection schedule. In the Olton 4x4 Maze, lidocaine produced a significant increase in working and long-term memory errors, compared to saline and post-lidocaine conditions. In contrast, in the Olton Octagonal Maze, lidocaine did not induce any effect on working memory errors. Thus, AM/PPC is required when both working with previous information and long-term memories are needed, but not when only working memory is required, as it happens under ethological conditions. Whenever food supply is dispersed, a win-shift strategy is preferable.

  14. Pharmacokinetics of Lidocaine Hydrochloride Metabolized by CYP3A4 in Chinese Han Volunteers Living at Low Altitude and in Native Han and Tibetan Chinese Volunteers Living at High Altitude.

    PubMed

    Zhang, Juanling; Zhu, Junbo; Yao, Xingchen; Duan, Yabin; Zhou, Xuejiao; Yang, Meng; Li, Xiangyang

    2016-01-01

    To investigate the pharmacokinetics of lidocaine hydrochloride metabolized by cytochrome P450 3A4 (CYP3A4) in Chinese Han volunteers living at low altitude (LA) and in native Han and Tibetan Chinese volunteers living at high altitude, lidocaine hydrochloride 10 mg was given by intramuscular injection to 3 groups: Han volunteers living at LA, and native Han and Tibetan volunteers living at a high altitude. Blood samples were collected before the (baseline) study drug was given and at 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0 h after study drug administration. Lidocaine hydrochloride in plasma was determined by RP-HPLC. Pharmacokinetics parameters of lidocaine hydrochloride showed that there were no significant difference between the native Han and Tibetan volunteers, but the t(1/2) was 29.8 and 29.8% higher in 2 groups, respectively, than in the LA group. To study related mechanism, the effects of exposure to chronic high-altitude hypoxia (CHH) on the activity and expression of CYP3A1 were examined in rats. Rats were divided into LA, chronic moderate altitude hypoxia, and CHH groups. CHH caused significant decreases in the activity and protein and mRNA expression of rat CYP3A1 in vivo. This study found significant changes in the disposition of lidocaine hydrochloride in native healthy Tibetan and Han Chinese subjects living at a high altitude in comparison to healthy Han Chinese subjects living at LA, it might be due to significant decreases in the activity and protein and mRNA expression of CYP3A4 under CHH condition.

  15. Effects of systemic lidocaine versus magnesium administration on postoperative functional recovery and chronic pain in patients undergoing breast cancer surgery: A prospective, randomized, double-blind, comparative clinical trial

    PubMed Central

    Kim, Myoung Hwa; Lee, Ki Young; Park, Seho; Kim, Seung Il; Park, Hyung Seok

    2017-01-01

    Introduction We aimed to compare the effects of intraoperative lidocaine and magnesium on postoperative functional recovery and chronic pain after mastectomy due to breast cancer. Systemic lidocaine and magnesium reduce pain hypersensitivity to surgical stimuli; however, their effects after mastectomy have not been evaluated clearly. Methods In this prospective, double-blind, clinical trial, 126 female patients undergoing mastectomy were randomly assigned to lidocaine (L), magnesium (M), and control (C) groups. Lidocaine and magnesium were administered at 2 mg/kg and 20 mg/kg for 15 minutes immediately after induction, followed by infusions of 2 mg/kg/h and 20 mg/kg/h, respectively. The control group received the same volume of saline. Patient characteristics, perioperative parameters, and postoperative recovery profiles, including the Quality of Recovery 40 (QoR-40) survey, pain scales, length of hospital stay, and the short-form McGill pain questionnaire (SF-MPQ) at postoperative 1 month and 3 months were evaluated. Results The global QoR-40 scores on postoperative day 1 were significantly higher in group L than in group C (P = 0.003). Moreover, in sub-scores of the QoR-40 dimensions, emotional state and pain scores were significantly higher in group L than those in groups M and C (P = 0.027 and 0.023, respectively). At postoperative 3 months, SF-MPQ and SF-MPQ-sensitive scores were significantly lower in group L than in group C (P = 0.046 and 0.036, respectively). Conclusions Intraoperative infusion of lidocaine improved the quality of recovery and attenuated the intensity of chronic pain in patients undergoing breast cancer surgery. PMID:28253307

  16. Analgesic efficacy of equimolar 50% nitrous oxide/oxygen gas premix (Kalinox®) as compared with a 5% eutectic mixture of lidocaine/prilocaine (EMLA®) in chronic leg ulcer debridement.

    PubMed

    Traber, Juerg; Held, Ulrike; Signer, Maria; Huebner, Tobias; Arndt, Stefan; Neff, Thomas A

    2016-08-08

    Chronic foot and leg ulcers are a common health problem worldwide. A mainstay of chronic ulcer therapy is sharp mechanical wound debridement requiring potent analgesia. In this prospective, controlled, single-centre, crossover design study, patients were assigned to either the administration of topical analgesia with 5% lidocaine/prilocaine cream or the inhalation of an analgesic 50% N2 O/O2 gas premix. Primary outcome parameter was level of pain at maximum wound depth during debridement as measured by a visual analogue scale. Secondary outcomes included level of pain after debridement, overall duration of treatment session, duration and completeness of debridement, and the patient's subjective perception of analgesic quality during debridement. Pain level increased from 0·60/0·94 (first/second debridement; baseline) to 1·76/2·50 (debridement) with 5% lidocaine/prilocaine and from 1·00/1·35 (baseline) to 3·95/3·29 (debridement) with 50% N2 O/O2 gas premix. Patient satisfaction was 90·48%/94·44% (first/second debridement) with topical 5% lidocaine/prilocaine analgesia and 90·48%/76·47% with the inhalation of 50% N2 O/O2 gas premix. Debridement was completed in a significantly higher percentage of 85·71%/88·89% (first/second debridement) with 5% lidocaine/prilocaine than with 50% N2 O/O2 gas premix (42·86%/58·82%) (odds ratio 6·7; P = 0·001). This study provides sound evidence that analgesia with topically administered 5% lidocaine/prilocaine cream is superior to the use of inhaled 50% N2 O/O2 gas premix in chronic leg ulcer debridement.

  17. Changes in acral blood flux under local application of ropivacaine and lidocaine with and without an adrenaline additive: a double-blind, randomized, placebo-controlled study.

    PubMed

    Häfner, Hans-Martin; Schmid, Ute; Moehrle, Matthias; Strölin, Anke; Breuninger, Helmut

    2008-01-01

    Vascular effects of local anesthetics are especially important in dermatological surgery. In particular, adequate perfusion must be ensured in order to offset surgical manipulations during surgical interventions at the acra. However, the use of adrenaline additives appears fraught with problems when anesthesia affects the terminal vascular system, particularly during interventions at the fingers, toes, penis, outer ears, and tip of the nose. We studied skin blood flux at the fingerpads via laser Doppler flowmetry over the course of 24 hours in a prospective, double-blind, randomized, placebo-controlled study with 20 vascularly healthy test persons following Oberst's-method anesthetic blocks. In each case, 6 ml ropivacaine (7.5 mg/ml) (A), lidocaine 1% without an additive (B), and lidocaine 1% with an adrenaline additive (1:200,000) (C) was used respectively as a verum. Isotonic saline solution was injected as a placebo (D). Measurements were carried out with the aid of a computer simultaneously at D II and D IV on both hands. Administration of (A) led to increased blood flux (+155.2%); of (B) initially to a decrease of 27%; of (C) to a reduction of 55% which was reversible after 40 minutes and of (D) to no change.(A) resulted in sustained vasodilatation which was still demonstrable after 24 h. (B) had notably less vasodilative effect, although comparison with (D) clearly showed that (B) is indeed vasodilative. (C) resulted in only a passing decrease in perfusion; this was no longer measurable when checked after 6 and 24 h. This transient inadequacy of blood flux also appeared after administration of (D). These tests show that adrenaline additive in local anesthesia does not decrease blood flow more than 55% for a period of 16 min. Following these results an adrenaline additive can be safely used for anesthetic blocks at the acra in healthy persons.

  18. Differential effects of infralimbic vs. ventromedial orbital PFC lidocaine infusions in CD-1 mice on defensive responding in the mouse defense test battery and rat exposure test.

    PubMed

    Wall, P M; Blanchard, R J; Yang, M; Blanchard, D C

    2004-09-10

    The ventromedial prefrontal cortex (vmPFC) is extremely sensitive to a variety of stressful situations and threatening events, and has been suggested to be an associative cortical brain system processing the integration of anxiety-related cognitive, affective and motivated behavior in rodents, primates and humans. In addition, recent evidence suggests that (a) anxiety-related affective processing appears to be lateralized to the right hemisphere vmPFC; and (b) there appears to be functional heterogeneity within the rodent vmPFC. The present study evaluated the possibility that distinct sub-areas of the right hemisphere ventral PFC might differentially influence anxiety-like defensive responding in two different predator stress situations following transient inactivation of the ventromedial orbital (vMO) or infralimbic (IL) vmPFC in CD-1 mice. In week 1, IL vmPFC lidocaine infusions reduced anxiety-like defensive responding in mice (enhanced approach and contact) confronted with a hand-held anesthetized rat stimulus in the mouse defense test battery (vMO inactivation exerted minimal effects). In week 2, vMO lidocaine infusions enhanced anxiety-like defensive responding (enhanced avoidance and protected risk assessment) toward a barricaded live rat in the rat exposure test (IL inactivation exerted minimal effects). Although it is unclear whether week 1 mouse defense test battery testing influenced week 2 rat exposure test results, these preliminary data suggest functional differences within the mouse right hemisphere ventral PFC related to cautious evaluation of predator threat. Given the dense unilateral reciprocal connectivity between the IL and vMO subregions of the PFC, both associative ventromedial cortical areas may exert complimentary yet dissociable roles in the processing of threat stimuli. This suggests that while the IL vmPFC may mediate cautious evaluation of threat situations (risk assessment), the vMO PFC may inhibit prepotent avoidance responses to

  19. Preformulation and characterization of a lidocaine hydrochloride and dexamethasone sodium phosphate thermo-reversible and bioadhesive long-acting gel for intraperitoneal administration.

    PubMed

    Arbelaez-Camargo, Diana; Suñé-Negre, Josep Maria; Roig-Carreras, Manel; García-Montoya, Encarna; Pérez-Lozano, Pilar; Miñarro-Carmona, Montserrat; Ticó-Grau, Josep Ramon

    2016-02-10

    The search for new formulations of anaesthetic agents that allow a localized administration and provide a prolonged effect is of great interest in the multimodal management of postoperative pain. The pre-formulation and characterization of a lidocaine and dexamethasone thermosensitive and bioadhesive long-acting gel for intraperitoneal administration was done as a tool in the management of pain in abdominal surgeries. The pre-formulation process was conducted by a systematic variation of the concentration of the different polymers, until setting it, in a suitable concentration that allowed an adequate gelation temperature. The poloxamer 407 (P407) was used as the main polymer; hydroxypropyl methylcellulose (HPMC) as the bioadhesive agent and polyvinyl pyrrolidone (PVP) to adjust the gelation temperature and physicochemical properties. The formulations were characterized by gelation temperature, pH, viscosity at 25°C and 37°C, gelation time, density and osmolality. Gelation temperature was decreased when increasing the concentration of hydroxypropyl methylcellulose and poloxamer 407, this effect was also observed when adding lidocaine hydrochloride and dexamethasone sodium phosphate to the formulations. The gelation temperature did not have statistically significant relation with the PVP concentration (P-value of 0.6797), even though, there is a tendency in the gelation temperature by varying it. Between the developed formulations, the 12.5/3.3/0.4% (P407/HPMC/PVP) formulation presents an appropriate gelation temperature, a suitable viscosity for administration by syringe, an adequate and stable pH and osmolality to prevent tissue damage and a correct gelation time that allowed the formation of a prolonged release implant.

  20. Investigation of Behavior of Forced Degradation of Lidocaine HCl by NMR Spectroscopy and GC-FID Methods: Validation of GC-FID Method for Determination of Related Substance in Pharmaceutical Formulations.

    PubMed

    Kadioglu, Yucel; Atila, Alptug; Serdar Gultekin, Mehmet; Alcan Alp, Nurdan

    2013-01-01

    The forced degradation study of lidocaine HCl was carried out according to the ICH guideline Q1A (R2). The degradation conditions were assessed to be hydrolysis, oxidation, photolysis and dry heat during 24 h, 48 h and 72 h and then the samples were investigated by GC-FID method and nuclear magnetic resonance (NMR) spectroscopy. According to these results, the degradation products were not observed in all reaction conditions during the 72 h period. Only spectral changes in the 1H and 13C-NMR spectrum were observed in hydrogen peroxide and acid degradation. As a result of this degradation, n-oxide was formed. After acid-induced degradation with HCl, the secondary amine salt was formed. Furthermore, trifluoroacetic acid (TFA) was used as the acidic media, and the decomposition products were observed. A simple and reliable gas chromatography method with flame ionization detection (GC-FID) was developed and validated for the determination of lidocaine HCl in pharmaceutical formulations in the form of a cream and injections. The GC-FID method can be used for a routine analysis of lidocaine HCl in pharmaceutical formulations and the proposed method, together with NMR spectroscopy, can be applied in stability studies.

  1. Evaluation of the anaesthetic properties and tolerance of 1:100,000 articaine versus 1:100,000 lidocaine. A comparative study in surgery of the lower third molar

    PubMed Central

    Barona-Dorado, Cristina; Martín-Arés, María; Cortés-Bretón-Brinkman, Jorge; Martínez-González, José M.

    2012-01-01

    Objectives: To evaluate the anaesthetic properties and tolerance of articaine versus lidocaine at equal vasoconstrictor concentration. Study Design: A total of 96 male and female patients who underwent surgical treatment of the lower third molar participated. Patients were randomly assigned to articaine hydrochloride with epinephrine 1:100,000 and lidocaine hydrochloride with epinephrine 1:100,000. The variables analysed were latency period, duration of anaesthetic effect, tolerance and adverse reactions. Results: Both the latency period and the duration of anaesthetic effect were greater for articaine, although the differences were not statistically significant. Latency: mean difference of 2.70 ± 2.12 minutes (95%CI of -1.51 minutes - 6.92 minutes). Duration: mean difference of -33 minutes 5 seconds ± 31 minutes (95% CI -1 hour 35 minutes - 29 minutes). There were 4 adverse events that did not require the patients to be withdrawn from the study. Conclusions: The anaesthetics in this study have very similar properties for use in surgery and have demonstrated a good safety and tolerability profile Key words: Articaine, lidocaine, vasoconstrictor, adverse reactions. PMID:22143691

  2. Development of fast Fourier transform continuous cyclic voltammetry at Au microelectrode in flowing solutions as a novel method for sub-nanomolar monitoring of lidocaine in injection and biological fluids.

    PubMed

    Norouzi, P; Ganjali, M R; Daneshgar, P; Dinarvand, R; Moosavi-Movahedi, A A; Saboury, A A

    2007-05-02

    In this work a novel method for the fast monitoring of lidocaine in flow-injection systems has been developed. The fast Fourier transform continuous cyclic voltammetry (FFTCV) at gold microelectrode in flowing solution system was used for determination of lidocaine in its pharmaceutical formulation. The presented technique was very simple, precise, accurate, time saving and economical, compared with all of the previously reported methods. The recommended technique demonstrated some advantages over other reported methods. Firstly, there was no need for the oxygen removal from the test solution. Secondly, a picomolar detection limit was achieved, and additionally, the method was fast enough for the determination of any such compound, in a wide variety of chromatographic methods. The method was linear across the concentration range of 240-1.1 x 10(5) pg mL(-1) (r=0.996) with a limit of detection and quantitation 117.3 and 240 pg mL(-1), respectively. As a conclusion this system offers the requisite accuracy, sensitivity, precision and selectivity to assay lidocaine in injections.

  3. A Prospective, Randomized, Double-Blind Comparison of 2% Mepivacaine With 1 : 20,000 Levonordefrin Versus 2% Lidocaine With 1 : 100,000 Epinephrine for Maxillary Infiltrations

    PubMed Central

    Lawaty, Ingrid; Drum, Melissa; Reader, Al; Nusstein, John

    2010-01-01

    The purpose of this prospective, randomized, double-blind crossover study was to compare the anesthetic efficacy of 2% mepivacaine with 1 : 20,000 levonordefrin versus 2% lidocaine with 1 : 100,000 epinephrine in maxillary central incisors and first molars. Sixty subjects randomly received, in a double-blind manner, maxillary central incisor and first molar infiltrations of 1.8 mL of 2% mepivacaine with 1 : 20,000 levonordefrin and 1.8 mL of 2% lidocaine with 1 : 100,000 epinephrine at 2 separate appointments spaced at least 1 week apart. The teeth were electric pulp tested in 2-minute cycles for a total of 60 minutes. Anesthetic success (obtaining 2 consecutive 80 readings with the electric pulp tester within 10 minutes) was not significantly different between 2% mepivacaine with 1 : 20,000 levonordefrin and 2% lidocaine with 1 : 100,000 epinephrine for the central incisor and first molar. However, neither anesthetic agent provided an hour of pulpal anesthesia. PMID:21174567

  4. Efficacy and Safety of a Lidocaine Gel in Patients from 6 Months up to 8 Years with Acute Painful Sites in the Oral Cavity: A Randomized, Placebo-Controlled, Double-Blind, Comparative Study

    PubMed Central

    Wolf, Dörte; Otto, Joachim

    2015-01-01

    Lidocaine is a well-accepted topical anaesthetic, also used in minors to treat painful conditions on mucosal membranes. This randomized, double-blind, placebo-controlled study (registered prospectively as EudraCT number 2011-005336-25) was designed to generate efficacy and safety data for a lidocaine gel (2%) in younger children with painful conditions in the oral cavity. One hundred sixty-one children were included in two subgroups: 4–8 years, average age 6.4 years, treated with verum or placebo and 6 months–<4 years, average age 1.8 years, treated only with verum. Pain reduction was measured from the time prior to administration to 10 or 30 minutes after. In addition, adverse events and local tolerability were evaluated. In group I, pain was reduced significantly after treatment with verum compared to placebo at both time points. In group II, the individual pain rating shift showed statistically significant lower pain after treatment. Only seven out of 161 patients reported an adverse event but none were classified as being related to the study medication. The local tolerability was assessed as very good in over 97% of cases. For painful sites in the oral cavity, a 2% lidocaine gel is a meaningful tool for short-term treatment in the paediatric population. PMID:26693229

  5. Investigation of Behavior of Forced Degradation of Lidocaine HCl by NMR Spectroscopy and GC-FID Methods: Validation of GC-FID Method for Determination of Related Substance in Pharmaceutical Formulations

    PubMed Central

    Kadioglu, Yucel; Atila, Alptug; Serdar Gultekin, Mehmet; Alcan Alp, Nurdan

    2013-01-01

    The forced degradation study of lidocaine HCl was carried out according to the ICH guideline Q1A (R2). The degradation conditions were assessed to be hydrolysis, oxidation, photolysis and dry heat during 24 h, 48 h and 72 h and then the samples were investigated by GC-FID method and nuclear magnetic resonance (NMR) spectroscopy. According to these results, the degradation products were not observed in all reaction conditions during the 72 h period. Only spectral changes in the 1H and 13C-NMR spectrum were observed in hydrogen peroxide and acid degradation. As a result of this degradation, n-oxide was formed. After acid-induced degradation with HCl, the secondary amine salt was formed. Furthermore, trifluoroacetic acid (TFA) was used as the acidic media, and the decomposition products were observed. A simple and reliable gas chromatography method with flame ionization detection (GC-FID) was developed and validated for the determination of lidocaine HCl in pharmaceutical formulations in the form of a cream and injections. The GC-FID method can be used for a routine analysis of lidocaine HCl in pharmaceutical formulations and the proposed method, together with NMR spectroscopy, can be applied in stability studies. PMID:24523745

  6. Effect of xylazine, isoxsuprine, and lidocaine on Doppler sonographic uterine and umbilical blood flow measurements in cows during the last month of pregnancy.

    PubMed

    Waldvogel, D; Bleul, U

    2014-04-15

    The maternal portion of the bovine placenta receives blood mainly from the uterine arteries (AUT) and the fetal portion from the umbilical arteries (AUM). Placental perfusion is crucial for fetal development and undergoes adaptive changes during pregnancy according to the fetal requirements. One goal of this study was to investigate changes in Doppler sonographic measurements of blood vessels that supply blood to the placenta in cows during the last 4 weeks of pregnancy. Another goal was to examine how these measurements are affected by three drugs commonly used in cows at the time of parturition. Nine cows underwent Doppler sonographic examination of the AUT ipsilateral and contralateral to the pregnant horn and one AUM three times per week during the last 4 weeks of gestation. This was followed by the randomized administration of one of the three following experimental drugs per day: isoxsuprine (200 mg/cow, iv), xylazine (2 mg/100 kg, iv), and lidocaine for epidural anesthesia (100 mg/cow). Doppler sonographic examination was repeated 30 minutes after medication. Maternal pulse rate increased during the study period (P < 0.001), and the diameter of the contralateral AUT was smaller in the last week before birth than in the two preceding weeks. The resistance index (RI) of the ipsilateral AUT was smaller in the last week than in the first 2 weeks of the study period. Uterine blood flow volume increased after isoxsuprine by 5% and after epidural anesthesia by 6% (both P ≤ 0.05) and decreased after xylazine by 10% (P < 0.001). Isoxsuprine was the only drug that elevated the blood flow volume in the AUM (P ≤ 0.05). Xylazine increased the RI of both AUT (both P < 0.001) and significantly reduced maternal and fetal pulse frequencies, whereas isoxsuprine significantly reduced the RI of both AUT and the AUM and increased maternal and fetal pulse frequencies. The results reported that Doppler sonographic measurements of uterine and AUM change little in the last

  7. Small-Volume Adenosine, Lidocaine, and Mg2+ 4-Hour Infusion Leads to 88% Survival after 6 Days of Experimental Sepsis in the Rat without Antibiotics.

    PubMed

    Griffin, Maddison Jade; Letson, Hayley Louise; Dobson, Geoffrey Phillip

    2016-11-01

    Innovative host-directed drug therapies are urgently required to treat sepsis. We tested the effect of a small-volume 0.9% NaCl adenosine, lidocaine, and Mg(2+) (ALM) bolus and a 4-h intravenous infusion on survivability in the rat model of polymicrobial sepsis over 6 days. ALM treatment led to a significant increase in survivability (88%) compared to that of controls (25%). Four controls died on day 2 to 3, and two died on day 5. Early death was associated with elevated plasma and lung inflammatory markers (interleukin-6 [IL-6], IL-1β, C-reactive protein), reduced white blood cell (WBC) count, hypoxemia, hypercapnia, acidosis, hyperkalemia, and elevated lactate, whereas late death was associated with a massive cytokine storm, a neutrophil-dominated WBC rebound/overshoot, increased lung oxidant injury, edema, and persistent ischemia. On day 6, seven of eight ALM survivors had inflammatory and immunological profiles not significantly different from those of sham-treated animals. We conclude in the rat model of experimental sepsis that small-volume ALM treatment led to higher survivability at 6 days (88%) than that of controls (25%). Early death in controls (day 2 to 3) was associated with significantly elevated plasma levels of IL-1β, IL-6, and C-reactive protein, severe plasma lymphocyte deficiency, reduced neutrophils, and acute lung injury. Late death (day 5) was associated with a massive neutrophil inflammatory storm, increased lung injury, and persistent ischemia. Possible mechanisms of ALM protection are discussed.

  8. Oral mucosal blood flow, plasma epinephrine and haemodynamic responses after injection of lidocaine with epinephrine during midazolam sedation and isoflurane anaesthesia.

    PubMed

    Homma, Y; Ichinohe, T; Kaneko, Y

    1999-04-01

    We have investigated the relationship between oral mucosal blood flow and plasma epinephrine concentration, and the effects of conscious sedation vs general anaesthesia on haemodynamic responses after submucosal epinephrine injection in 14 subjects. The same seven patients were studied both as controls and after sedation. For sedation, midazolam i.v. was used. Another seven patients underwent orthognathic surgery with isoflurane anaesthesia. All subjects received a submucosal injection of epinephrine 0.8 microgram kg-1, given as 2% lidocaine hydrochloride with epinephrine 12.5 micrograms ml-1. Baseline mucosal blood flow and peak increase in plasma epinephrine concentration in the general anaesthesia and sedation groups were approximately 2.0 and 1.5 times, respectively, higher than those in the control group. Mean plasma epinephrine concentration reached a maximum 3 min after administration of epinephrine in all groups. Overall, there was a significant correlation (r = 0.65) between baseline mucosal blood flow and the maximum increase in plasma epinephrine concentration. There were no differences in haemodynamic changes except for heart rate, between the three groups. These results suggest that plasma epinephrine concentration after submucosal injection depends on the initial mucosal blood flow in the injected area. Haemodynamic changes, except heart rate, in the sedation and general anaesthesia groups were similar despite different changes in maximum plasma epinephrine concentration.

  9. Validated RP-HPLC and TLC-Densitometric Methods for Analysis of Ternary Mixture of Cetylpyridinium Chloride, Chlorocresol and Lidocaine in Oral Antiseptic Formulation.

    PubMed

    Abdelwahab, Nada S; Ali, Nouruddin W; Abdelkawy, M; Emam, Aml A

    2016-03-01

    This work was concerned with development, optimization, application and validation of reversed phase high performance liquid chromatography (RP-HPLC) and thin layer chromatography (TLC)-densitometric methods for analysis of cetylpyridinium chloride, chlorocresol and lidocaine in Canyon(®) gel. The first developed RP-HPLC method depended on chromatographic separation on a ZORBAX Eclipse Plus C8 column, with elution with a mobile phase consisting of 0.05% phosphoric acid solution : acetonitrile : methanol (15 : 24 : 61, by volume), pumping the mobile phase at a flow rate of 1.00 mL min(-1), with ultraviolet detection at 220 nm. While in the subsequently developed method, the TLC-densitometric method, complete separation of the studied mixture was achieved using methanol : acetone : acetic acid (7 : 3 : 0.2, by volume) as a mobile phase, aluminum plates precoated with silica gel 60 F254 as a stationary phase and 215 nm as the scanning wavelength. Factors affecting the developed methods were studied and optimized; moreover, methods had been validated as per the International Conference of Harmonization guideline and the results indicated that the suggested methods were reproducible, reliable and applicable for rapid routine analysis. Statistical comparison of the two developed methods with the reported HPLC ones using F- and Student's t tests showed no significant difference.

  10. Comparison of effects of ephedrine, lidocaine and ketamine with placebo on injection pain, hypotension and bradycardia due to propofol injection: a randomized placebo controlled clinical trial.

    PubMed

    Ayatollahi, Vida; Behdad, Shekoufeh; Kargar, Saeed; Yavari, Tayebe

    2012-01-01

    Propofol is a widely used anesthetic drug because of its minor complication and also its fast effect. One of most popular complication in using this drug is pain during injection that is more sever in new generation of its components (lipid-free microemulsion). Other complications of propofol are bradycardia and hypotension. This study compares 3 drugs with placebo in control of these complications of propofol. In this double blinded randomized placebo controlled trial 140 patient who were candidates for elective surgery were divided in 4 groups (35 patients in each groups) and drugs (ephedrine, lidocaine, ketamine and NaCl solution (as placebo) were tried on each group by a blinded technician and responses to drugs were evaluated under supervision of a blinded anesthesiologist. Pain after injection, systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP) and heart rate (HR) were measured 5 times during anesthesia process of each patient. All gathered data were analyzed using t-test and Chi-square under SPSS software. Our data shows that in pain management all tested drugs can decrease pain significantly comparing with placebo (P=0.017). In control of hemodynamic parameters ephedrine could efficiently control SBP, DBP, MAP at the time 1 min after intubation. Based on our study ephedrine can be an appropriate suggestion for control of both pain and hemodynamic changes induced by propofol, although because of inconsistent result in other studies it is recommended to design a systematic review to draw a broader view on this issue.

  11. Case report: computed tomography scan-guided Gasserian ganglion injection of dexamethasone and lidocaine for the treatment of recalcitrant pain associated with herpes simplex type 1 infection of the ophthalmic division of the trigeminal nerve.

    PubMed

    Candido, Kenneth D; Germanovich, Andrew; Ghaly, Ramsis F; Gorelick, Gleb H; Knezevic, Nebojsa Nick

    2011-01-01

    We describe the case of a 17-year-old boy with dermatologic herpes simplex virus-1 outbreaks with incapacitating facial pain requiring multiple hospitalizations. He failed to respond to aggressive treatments including antiviral drugs, opioid analgesics, stellate ganglion, and supraorbital and supratrochlear nerve blocks. The patient elected to undergo dexamethasone and lidocaine Gasserian ganglion block under computed tomography-scan guidance. He had immediate and complete relief of his pain for the first time in almost 2 years. The patient remained pain free during 6-month follow-up visits. This is the first reported use of Gasserian ganglion block for treatment of herpes simplex virus-1 infection of the trigeminal nerve.

  12. Coelomic implantation of satellite transmitters in the bar-tailed godwit (Limosa lapponica) and the bristle-thighed curlew (Numenius tahitiensis) using propofol, bupivacaine, and lidocaine

    USGS Publications Warehouse

    Mulcahy, Daniel M.; Gartrell, Brett D.; Gill, Robert E.; Tibbitts, T. Lee; Ruthrauff, Daniel R.

    2011-01-01

    Intravenous propofol was used as a general anesthetic with a 2∶1 (mg∶mg) adjunctive mixture of lidocaine and bupivacaine as local anesthetics infiltrated into the surgical sites for implantation of satellite transmitters into the right abdominal air sac of 39 female and 4 male bar-tailed godwits (Limosa lapponica baueri and Limosa lapponica menzbeiri) and 11 female and 12 male bristle-thighed curlews (Numenius tahitiensis). The birds were captured on nesting grounds in Alaska, USA, and on overwintering areas in New Zealand and Australia from 2005 through 2008. As it was developed, the mass of the transmitter used changed yearly from a low of 22.4 ± 0.2 g to a high of 27.1 ± 0.2 g and weighed 25.1 ± 0.2 g in the final year. The mean load ratios ranged from 5.2% to 7.7% for godwits and from 5.7% to 7.5% for curlews and exceeded 5% for all years, locations, and genders of both species. The maximum load ratio was 8.3% for a female bar-tailed godwit implanted in Australia in 2008. Three godwits and no curlews died during surgery. Most birds were hyperthermic upon induction but improved during surgery. Two godwits (one in New Zealand and one in Australia) could not stand upon release, likely due to capture myopathy. These birds failed to respond to treatment and were euthanized. The implanted transmitters were used to follow godwits through their southern and northern migrations, and curlews were followed on their southern migration.

  13. Effects of intermittent positive pressure ventilation on cardiopulmonary function in horses anesthetized with total intravenous anesthesia using combination of medetomidine, lidocaine, butorphanol and propofol (MLBP-TIVA).

    PubMed

    Ishizuka, Tomohito; Tamura, Jun; Nagaro, Tsukasa; Sudo, Kanako; Itami, Takaharu; Umar, Mohammed Ahamed; Miyoshi, Kenjirou; Sano, Tadashi; Yamashita, Kazuto

    2014-12-01

    Effects of intermittent positive pressure ventilation (IPPV) on cardiopulmonary function were evaluated in horses anesthetized with total intravenous anesthesia using constant rate infusions of medetomidine (3.5 µg/kg/hr), lidocaine (3 mg/kg/hr), butorphanol (24 µg/kg/hr) and propofol (0.1 mg/kg/min) (MLBP-TIVA). Five horses were anesthetized twice using MLBP-TIVA with or without IPPV at 4-week interval (crossover study). In each occasion, the horses breathed 100% oxygen with spontaneous ventilation (SB-group, n=5) or with IPPV (CV-group, n=5), and changes in cardiopulmonary parameters were observed for 120 min. In the SB-group, cardiovascular parameters were maintained within acceptable ranges (heart rate: 33-35 beats/min, cardiac output: 27-30 l/min, mean arterial blood pressure [MABP]: 114-123 mmHg, mean pulmonary arterial pressure [MPAP]: 28-29 mmHg and mean right atrial pressure [MRAP]: 19-21 mmHg), but severe hypercapnea and insufficient oxygenation were observed (arterial CO(2) pressure [PaCO(2)]: 84-103 mmHg and arterial O(2) pressure [PaO(2)]: 155-172 mmHg). In the CV-group, normocapnea (PaCO(2): 42-50 mmHg) and good oxygenation (PaO(2): 395-419 mmHg) were achieved by the IPPV without apparent cardiovascular depression (heart rate: 29-31 beats/min, cardiac output: 17-21 l /min, MABP: 111-123 mmHg, MPAP: 27-30 mmHg and MRAP: 15-16 mmHg). MLBP-TIVA preserved cardiovascular function even in horses artificially ventilated.

  14. The quaternary lidocaine derivative QX-314 in combination with bupivacaine for long-lasting nerve block: Efficacy, toxicity, and the optimal formulation in rats

    PubMed Central

    Zheng, Qingshan; Yang, Xiaolin; Lv, Rong; Ma, Longxiang; Liu, Jin; Zhu, Tao; Zhang, Wensheng

    2017-01-01

    Objective The quaternary lidocaine derivative (QX-314) in combination with bupivacaine can produce long-lasting nerve blocks in vivo, indicating potential clinical application. The aim of the study was to investigate the efficacy, safety, and the optimal formulation of this combination. Methods QX-314 and bupivacaine at different concentration ratios were injected in the vicinity of the sciatic nerve in rats; bupivacaine and saline served as controls (n = 6~10). Rats were inspected for durations of effective sensory and motor nerve blocks, systemic adverse effects, and histological changes of local tissues. Mathematical models were established to reveal drug-interaction, concentration-effect relationships, and the optimal ratio of QX-314 to bupivacaine. Results 0.2~1.5% QX-314 with 0.03~0.5% bupivacaine produced 5.8~23.8 h of effective nerve block; while 0.5% bupivacaine alone was effective for 4 h. No systemic side effects were observed; local tissue reactions were similar to those caused by 0.5% bupivacaine if QX-314 were used < 1.2%. The weighted modification model was successfully established, which revealed that QX-314 was the main active ingredient while bupivacaine was the synergist. The formulation, 0.9% QX-314 plus 0.5% bupivacaine, resulted in 10.1 ± 0.8 h of effective sensory and motor nerve blocks. Conclusion The combination of QX-314 and bupivacaine facilitated prolonged sciatic nerve block in rats with a satisfactory safety profile, maximizing the duration of nerve block without clinically important systemic and local tissue toxicity. It may emerge as an alternative approach to post-operative pain treatment. PMID:28334014

  15. Effects of Intermittent Positive Pressure Ventilation on Cardiopulmonary Function in Horses Anesthetized with Total Intravenous Anesthesia Using Combination of Medetomidine, Lidocaine, Butorphanol and Propofol (MLBP-TIVA)

    PubMed Central

    ISHIZUKA, Tomohito; TAMURA, Jun; NAGARO, Tsukasa; SUDO, Kanako; ITAMI, Takaharu; UMAR, Mohammed Ahamed; MIYOSHI, Kenjirou; SANO, Tadashi; YAMASHITA, Kazuto

    2014-01-01

    Effects of intermittent positive pressure ventilation (IPPV) on cardiopulmonary function were evaluated in horses anesthetized with total intravenous anesthesia using constant rate infusions of medetomidine (3.5 µg/kg/hr), lidocaine (3 mg/kg/hr), butorphanol (24 µg/kg/hr) and propofol (0.1 mg/kg/min) (MLBP-TIVA). Five horses were anesthetized twice using MLBP-TIVA with or without IPPV at 4-week interval (crossover study). In each occasion, the horses breathed 100% oxygen with spontaneous ventilation (SB-group, n=5) or with IPPV (CV-group, n=5), and changes in cardiopulmonary parameters were observed for 120 min. In the SB-group, cardiovascular parameters were maintained within acceptable ranges (heart rate: 33–35 beats/min, cardiac output: 27–30 l/min, mean arterial blood pressure [MABP]: 114–123 mmHg, mean pulmonary arterial pressure [MPAP]: 28–29 mmHg and mean right atrial pressure [MRAP]: 19–21 mmHg), but severe hypercapnea and insufficient oxygenation were observed (arterial CO2 pressure [PaCO2]: 84–103 mmHg and arterial O2 pressure [PaO2]: 155–172 mmHg). In the CV-group, normocapnea (PaCO2: 42–50 mmHg) and good oxygenation (PaO2: 395–419 mmHg) were achieved by the IPPV without apparent cardiovascular depression (heart rate: 29–31 beats/min, cardiac output: 17–21 l /min, MABP: 111–123 mmHg, MPAP: 27–30 mmHg and MRAP: 15–16 mmHg). MLBP-TIVA preserved cardiovascular function even in horses artificially ventilated. PMID:25649938

  16. Probing the combined effect of flunitrazepam and lidocaine on the stability and organization of bilayer lipid membranes. A differential scanning calorimetry and dynamic light scattering study.

    PubMed

    Caruso, Benjamín; Sánchez, Julieta M; García, Daniel A; de Paula, Eneida; Perillo, María A

    2013-07-01

    Combined effects of flunitrazepam (FNZ) and lidocaine (LDC) were studied on the thermotropic equilibrium of dipalmitoyl phosphatidylcholine (dpPC) bilayers. This adds a thermodynamic dimension to previously reported geometric analysis in the erythrocyte model. LDC decreased the enthalpy and temperature for dpPC pre- and main-transitions (ΔHp, ΔHm, Tp, Tm) and decreased the cooperativity of the main-transition (ΔT(1/2,m)). FNZ decreased ΔHm and, at least up to 59 μM, also decreased ΔHp. In conjunction with LDC, FNZ induced a recovery of ∆T(1/2,m) control values and increased ΔHm even above the control level. The deconvolution of the main-transition peak at high LDC concentrations revealed three components possibly represented by: a self-segregated fraction of pure dpPC, a dpPC-LDC mixture and a phase with a lipid structure of intermediate stability associated with LDC self-aggregation within the lipid phase. Some LDC effects on thermodynamic parameters were reverted at proper LDC/FNZ molar ratios, suggesting that FNZ restricts the maximal availability of the LDC partitioned into the lipid phase. Thus, beyond its complexity, the lipid-LDC mixture can be rationalized as an equilibrium of coexisting phases which gains homogeneity in the presence of FNZ. This work stresses the relevance of nonspecific drug-membrane binding on LDC-FNZ pharmacological interactions and would have pharmaceutical applications in liposomal multidrug-delivery.

  17. A randomized clinical study of the heated lidocaine/tetracaine patch versus subacromial corticosteroid injection for the treatment of pain associated with shoulder impingement syndrome

    PubMed Central

    Radnovich, Richard; Trudeau, Jeremiah; Gammaitoni, Arnold R

    2014-01-01

    Background Treatment for pain due to shoulder impingement syndrome (SIS) typically begins conservatively with nonsteroidal anti-inflammatory drugs and physical therapy and can include subacromial injection of corticosteroids, particularly in patients unresponsive to conservative measures. The heated lidocaine/tetracaine (HLT) patch has been reported to reduce SIS pain in a small case series. Methods This was a prospective, randomized, open-label clinical trial in which adult patients with SIS pain lasting at least 14 days, with an average intensity of ≥4 on a 0–10 scale (0= no pain, 10= worst pain) were randomized to treatment with the HLT patch or a single subacromial injection of triamcinolone acetonide (10 mg). Patients in the HLT patch group applied a single HLT patch to the shoulder for 4 hours twice daily, with a 12-hour interval between treatments during the first 14 days, and could continue to use the patch on an as-needed basis (up to twice daily) during the second 14-day period. No treatment was allowed in the final 14-day period. At baseline and at days 14, 28, and 42, patients rated their pain and pain interference with specific activities (0–10 scale). Results Sixty patients enrolled in the study (average age =51 years, range 18–75, n=21 female). Average pain scores declined from 6.0±1.6 at baseline to 3.5±2.4 at day 42 in the HLT patch group (n=29, P<0.001) and from 5.6±1.2 to 3.2±2.6 in the injection group (n=31, P<0.001). Similar improvements were seen in each group for worst pain; pain interference with general activity, work, or sleep; and range of motion. No significant between-group differences were seen for any pain or pain interference scores at any time point. Conclusion These results suggest that short-term, noninvasive treatment with the HLT patch has similar efficacy to subacromial corticosteroid injections for the treatment of pain associated with SIS. PMID:25525385

  18. Microemulsions as colloidal vehicle systems for dermal drug delivery. Part IV: Investigation of microemulsion systems based on a eutectic mixture of lidocaine and prilocaine as the colloidal phase by dynamic light scattering.

    PubMed

    Shukla, Anuj; Krause, Annett; Neubert, Reinhard H H

    2003-06-01

    Stable oil-in-water (o/w) microemulsions used as vehicles for dermal drug delivery have been developed using lidocaine (lignocaine) and prilocaine in oil form (eutectic mixture), a blend of a high (Tween 80, hydrophilic-lipophilic balance (HLB) = 15.0) and a low (Poloxamer 331, HLB = 1.0) HLB surfactant and propylene glycol-water as hydrophilic phase. These microemulsions were able to solubilize up to 20% eutectic mixture of lidocaine and prilocaine without phase separation. The dispersity of the oil phase was investigated by dynamic light scattering. Small colloidal droplets for stable microemulsions of 5~10 nm were observed. At constant surfactant and hydrophilic phase concentration, increasing the total drug concentration in the microemulsion resulted in an increase in the droplet size of the dispersed, colloidal phase. It was observed that a monolayer of surfactant surrounds the oil (eutectic mixture) core. Colloidal droplets of the microemulsion interact via hard sphere with supplementary attractive interaction. This observed interparticle attractive interaction could explain the observed phase behaviour with respect to change in the basicity of the hydrophilic phase as well as the increase in volume fraction of the dispersed, colloidal phase. It was also observed that the stability and size of this dispersed phase depends on the pH of the composition. Because these microemulsions formed stable, isotropic systems in the range of pH 9.5 to 10.4 with alkali buffer or NaOH solution instead of water as hydrophilic phase, so one can produce microemulsions in this pH area.

  19. An Evaluation of 4% Prilocaine with 1:200,000 Epinephrine and 2% Mepivacaine with 1:20,000 Levonordefrin Compared with 2% Lidocaine with 1:100,000 Epinephrine for Inferior Alveolar Nerve Block

    PubMed Central

    Hinkley, Stewart A.; Reader, Al; Beck, Mike; Meyers, William J.

    1991-01-01

    The purpose of this study was to measure the degree of anesthesia obtained with 4% prilocaine with 1:200,000 epinephrine and 2% mepivacaine with 1:20,000 levonordefrin compared with 2% lidocaine with 1:100,000 epinephrine for inferior alveolar nerve block. Using a repeated measures design, 30 subjects randomly received an inferior alveolar injection using masked cartridges of each solution at three successive appointments. The first molar, first premolar, lateral incisor, and contralateral canine (control) were blindly tested with an Analytic Technology pulp tester at 3-min cycles for 50 min. Anesthetic success was defined as no subject response to the maximum output of the pulp tester (80 reading) within 16 min and maintenance of this reading for the remainder of the testing period. Although subjects felt numb subjectively, anesthetic success as defined here occurred in 46% to 57% of the molars, in 50% to 57% of the premolars, and in 21% to 36% of the lateral incisors. No statistically significant differences in onset, success, failure, or incidence were found among the solutions. We conclude that the three preparations are equivalent for inferior alveolar nerve block of 50-min duration. PMID:1814249

  20. Allergic response to metabisulfite in lidocaine anesthetic solution.

    PubMed Central

    Campbell, J. R.; Maestrello, C. L.; Campbell, R. L.

    2001-01-01

    True allergies to local anesthetics are rare. It is common for practitioners to misdiagnose a serious adverse event to local anesthetics as an allergic reaction. The most likely causes for an allergic response are the preservative, antioxidant, or metabolites and not the anesthetic itself. This case report illustrates the need for practitioners to understand the many potential allergens in local anesthetics and to correctly diagnose patients that are truly allergic to the local anesthetic. Images Figure 1 Figure 2 Figure 3 Figures 4 and 5 PMID:11495401

  1. Amiodarone supplants lidocaine in ACLS and CPR protocols.

    PubMed

    Mizzi, Anna; Tran, Thanh; Mangar, Devanand; Camporesi, Enrico M

    2011-09-01

    Amiodarone is an antiarrhythmic medication used to treat and prevent certain types of serious, life-threatening ventricular arrhythmias. Amiodarone gained slow acceptance outside the specialized field of cardiac antiarrhythmic surgery because the side-effects are significant. Recent adoption of amiodarone in the ACLS (Advanced Cardiac Life Support) protocol has somewhat popularized this class of antiarrhythmics. Its use is slowly expanding in the acute medicine setting of anesthetics. This article summarizes the use of Amiodarone by anesthesiologists in the operating room and during cardiopulmonary resuscitation.

  2. The Effectiveness of Articaine and Lidocaine Single Buccal Infiltration versus Conventional Buccal and Palatal Injection Using Lidocaine during Primary Maxillary Molar Extraction: A Randomized Control Trial

    PubMed Central

    Kolli, Naveen Kumar Reddy; Nirmala, S. V. S. G.; Nuvvula, Sivakumar

    2017-01-01

    Background: Despite the advent of modern injection techniques, palatal injection continues to be a painful experience for children. Aims: To compare the pain experienced during extraction of maxillary primary molars with conventional lignocaine anesthesia versus lignocaine and articaine buccal infiltration in children aged 6–14 years. Materials and Methods: A prospective randomized triple blinded study was conducted with ninety children (n = 90), randomly allocated to receive lignocaine conventional anesthesia (Group I [control group]), and buccal infiltration using articaine (Group II [articaine group]) or lignocaine (Group III [lignocaine group]). A composite score of self-report (faces pain scale-revised), behavioral measure (face legs activity cry consolability scale), and a physiological response (pulse rate) was measured following maxillary primary molar extraction. Statistical Analysis Used: To test the mean difference between two groups, Students’ t-test was used and among the three groups, one-way ANOVA with post hoc test was used. Results: Articaine group had significantly lower pain scores for self-report (P < 000.1) and behavioral measures (P < 000.1) while there was no significant difference (P > 0.05) between articaine and control groups during primary maxillary molar extraction. Conclusion: Maxillary primary molar extraction procedure can be successfully accomplished by bypassing the palatal injection. Articaine buccal infiltration can be considered as an alternative to conventional local anesthesia for the extraction of maxillary primary molars. PMID:28298777

  3. Index to Drug-Specific Information

    MedlinePlus

    ... Levofloxacin Levonorgestrel Levothyroxine sodium Lexapro (escitalopram) Lexiscan (regadenoson) Lidocaine Lidocaine Viscous Linagliptin Lindane Liraglutide Lisdexamfetamine dimesylate Lisinopril ...

  4. [Neutralization of lidocaine-adrenaline. A simple method for less painful application of local anesthesia].

    PubMed

    Momsen, O H; Roman, C M; Mohammed, B A; Andersen, G

    2000-08-14

    The amount of sodium bicarbonate necessary to neutralise commercially available lignocaine-epinephrine (pH 4.7) to physiologically neutral pH (7.4) was established. The analysis showed that neutral pH could be accomplished by adding 1.0 ml sodium bicarbonate (8.4 g/l) to 10 ml lignocaine-epinephrine (1%, 5 microgram/ml). Chemical analysis also established that the neutralised lignocaine-epinephrine was stable for 24 hours after adding sodium bicarbonate. A double-blinded randomised clinical trial with crossover design done on volunteers from hospital staff proved that injection of neutralised lignocaine-epinephrine is less painful than commercially available lignocaine-epinephrine (p < 0.001).

  5. On Beyond Lidocaine: Reconsidering Local Anesthetics in Tumescent Liposuction-A Critical Review.

    PubMed

    Hsia, Henry C

    2016-02-01

    The use of tumescent solution in liposuction is now considered standard of care; however, much debate still exists regarding its ideal components, especially surrounding the inclusion of local anesthetics. This article reviews the discussion regarding the use of local anesthetics in tumescent liposuction and how it may evolve in the future. The need for local anesthetic additives in tumescent liposuction has been questioned, and the use of longer-acting agents discouraged; however, increasing number of reports in recent years have described the increasingly widespread use of tumescent anesthesia where a wetting solution is infiltrated to achieve anesthesia in an operative field for procedures other than liposuction. More high-level evidence, such as randomized controlled clinical trials, will be required; however, it should be possible to develop a useful standardized algorithm that can guide surgeons to optimize patient safety as well as patient experience.

  6. Glossopharyngeal Nerve Block versus Lidocaine Spray to Improve Tolerance in Upper Gastrointestinal Endoscopy

    PubMed Central

    Ortega Ramírez, Moisés; Linares Segovia, Benigno; García Cuevas, Marco Antonio; Sánchez Romero, Jorge Luis; Botello Buenrostro, Illich; Amador Licona, Norma; Guízar Mendoza, Juan Manuel; Guerrero Romero, Jesús Francisco; Vázquez Zárate, Víctor Manuel

    2013-01-01

    Aim of the Study. To compare the effect of glossopharyngeal nerve block with topical anesthesia on the tolerance of patients to upper gastrointestinal endoscopy. Methods. We performed a clinical trial in one hundred patients undergoing upper gastrointestinal endoscopy. Subjects were randomly assigned to one of the following two groups: (1) treatment with bilateral glossopharyngeal nerve block (GFNB) and intravenous midazolam or (2) treatment with topical anesthetic (TASS) and intravenous midazolam. We evaluated sedation, tolerance to the procedure, hemodynamic stability, and adverse symptoms. Results. We studied 46 men and 54 women, from 17 to 78 years of age. The procedure was reported without discomfort in 48 patients (88%) in the GFNB group and 32 (64%) in the TAAS group; 6 patients (12%) in GFNB group and 18 (36%) in TAAS group reported the procedure as little discomfort (χ2 = 3.95, P = 0.04). There was no difference in frequency of nausea (4% in both groups) and retching, 4% versus 8% for GFNB and TASS group, respectively (P = 0.55). Conclusions. The use of glossopharyngeal nerve block provides greater comfort and tolerance to the patient undergoing upper gastrointestinal endoscopy. It also reduces the need for sedation. PMID:23533386

  7. Glossopharyngeal Nerve Block versus Lidocaine Spray to Improve Tolerance in Upper Gastrointestinal Endoscopy.

    PubMed

    Ortega Ramírez, Moisés; Linares Segovia, Benigno; García Cuevas, Marco Antonio; Sánchez Romero, Jorge Luis; Botello Buenrostro, Illich; Amador Licona, Norma; Guízar Mendoza, Juan Manuel; Guerrero Romero, Jesús Francisco; Vázquez Zárate, Víctor Manuel

    2013-01-01

    Aim of the Study. To compare the effect of glossopharyngeal nerve block with topical anesthesia on the tolerance of patients to upper gastrointestinal endoscopy. Methods. We performed a clinical trial in one hundred patients undergoing upper gastrointestinal endoscopy. Subjects were randomly assigned to one of the following two groups: (1) treatment with bilateral glossopharyngeal nerve block (GFNB) and intravenous midazolam or (2) treatment with topical anesthetic (TASS) and intravenous midazolam. We evaluated sedation, tolerance to the procedure, hemodynamic stability, and adverse symptoms. Results. We studied 46 men and 54 women, from 17 to 78 years of age. The procedure was reported without discomfort in 48 patients (88%) in the GFNB group and 32 (64%) in the TAAS group; 6 patients (12%) in GFNB group and 18 (36%) in TAAS group reported the procedure as little discomfort (χ (2) = 3.95, P = 0.04). There was no difference in frequency of nausea (4% in both groups) and retching, 4% versus 8% for GFNB and TASS group, respectively (P = 0.55). Conclusions. The use of glossopharyngeal nerve block provides greater comfort and tolerance to the patient undergoing upper gastrointestinal endoscopy. It also reduces the need for sedation.

  8. Analysis of the Ability of DMSO (Dimethyl Sulfoxide) and Lidocaine to Penetrate Dentin

    DTIC Science & Technology

    1988-01-15

    end of the experiments the cats were euthanitized with 10 ml satur- ated KC1 i.v. Dental pain was induced by perfusing a hyperosmotic (4 M sucrose...the induction of dental pain . Bipolar recording electrodes were placed on the sympathetic chain between the T and T connecting rami to determine if... dental pain 2 3 will evoke reflex activation of sympathetic cardiac efferents. Approximately 5 ml of the stimulating solution was introduced to the

  9. Manipulation of hyperbaric lidocaine using a weak magnetic field: a pilot study.

    PubMed

    Thiele, Robert H; Colquhoun, Douglas A; Gillies, George T; Tiouririne, Mohamed

    2012-06-01

    High spinal block is a potentially fatal complication of spinal anesthesia, with an incidence of 0.6 per 1000. Current prevention strategies include decreasing the dose of local anesthetic drug and altering patient positioning such that the location of hyperbaric anesthetic drugs in the neuraxis can be manipulated by gravity. Incorporation of a ferrofluid into a local anesthetic solution, combined with application of an external magnetic field in an in vitro spine model, allowed control of position of a solution of ferrofluid, dye, and local anesthetic against gravity, suggesting an additional mechanism by which anesthesia providers may prevent high spinal block.

  10. The Minimum Effective Dose of Lidocaine Needed to Block Evoked Potentials in the Sciatic Nerve of the Rat

    DTIC Science & Technology

    1998-10-01

    a higher concentration of sodium (Na+) ions extracellularly. This, along with the semi-permeable cell membrane, creates a resting membrane potential... sodium ions through voltage gated sodium channels located in the cellular membrane of a nerve (Stoelting, 1991). The anesthetics attach to a specific...receptor on the voltage gated sodium channels that respond to nerve impulses. Blockage of this flow of sodium ions will stop the membrane from

  11. SCI with Brain Injury: Bedside to Bench Modeling for Developing Treatment and Rehabilitation Strategies

    DTIC Science & Technology

    2013-10-01

    BISACODYL 5 OMEPRAZOLE 7 OMEPRAZOLE 1 ALBUTEROL 6 ALBUTEROL 2 LIDOCAINE 5 LIDOCAINE 1 ASCORBIC  ACID 4 ASCORBIC  ACID 2 HYDROCODONE/ACETAMINOPHEN 4...Frequency ACETAMINOPHEN 10 ACETAMINOPHEN 7 DOCUSATE 8 DOCUSATE 8 OMEPRAZOLE 8 OMEPRAZOLE 1 SENNA 7 SENNA 4 LIDOCAINE 5 LIDOCAINE 1 ONDANSETRON 5 ONDASETRON 1

  12. SCI with Brain Injury: Bedside-to-Bench Modeling for Developing Treatment and Rehabilitation Strategies

    DTIC Science & Technology

    2012-10-01

    LIDOCAINE 5 LIDOCAINE 1 ONDANSETRON 5 ONDASETRON 1 GABAPENTIN 4 GABAPENTIN 2 ASCORBIC  ACID 4 ASCORBIC ACID 1 BISACODYL 4 BISACODYL 1 TRAZODONE 3... LIDOCAINE 5 LIDOCAINE 1 ASCORBIC  ACID 4 ASCORBIC  ACID 2 HYDROCODONE/ACETAMINOPHEN 4 HYDROCODONE/ACETAMINOPHEN 2 ONDANSETRON 4 ONDASENTRON 1

  13. Effect of a single dose of lidocaine and ketamine on intraoperative opioids requirements in patients undergoing elective gynecological laparotomies under general anesthesia. A randomized, placebo controlled pilot study.

    PubMed

    García-Navia, Jusset Teresa; Tornero López, Javier; Egea-Guerrero, Juan José; Vilches Arenas, Angel; Vázquez Gutiérrez, Tiburcio

    2016-01-01

    Introducción y objetivos del estudio: existe evidencia de que la administracion perioperatoria de ketamina y lidocaina intravenosa reduce el dolor y el consumo de opioides postoperatorio, acorta la estancia hospitalaria y acelera la recuperacion de la funcion intestinal. Sin embargo, no se han estudiado los efectos beneficiosos en el periodo intraoperatorio. El objetivo de este estudio fue evaluar el efecto de una unica dosis de lidocaina y ketamina sobre el consumo intraoperatorio de opioides en pacientes sometidas a cirugia ginecologica electiva bajo anestesia general. Material y métodos: estudio prospectivo, aleatorizado, doble ciego, controlado con placebo en un solo centro. Se incluyeron 33 pacientes (11 en el grupo ketamina, 11 en el grupo lidocaina y 11 en el grupo placebo). Para la analgesia postoperatoria se utilizo una bomba PCA (Analgesia Controlada por el Paciente ) de morfina. Los pacientes fueron asignados al azar a uno de los tres grupos de estudio: 1,5 mg/kg de lidocaina al 2%, 0,5 mg/kg de ketamina al 5% o solucion salina 0.9%. La variable principal del estudio fue el consumo de opioides durante la cirugia. Las variables secundarias fueron: tiempo de educcion de la anestesia, intensidad del dolor, consumo de opioides en las 24 horas posteriores a la cirugia y efectos adversos. Resultados: se observo una disminucion del consumo intraoperatorio de opioides en los grupos ketamina (402,3 } 106,3) y lidocaina (397,7 } 107,5) frente al grupo placebo (561,4 } 97,1); p = 0,001. Se encontro una correlacion positiva entre el consumo intraoperatorio de opioides y el tiempo de despertar (r = 0,864, p.

  14. Behavioral Health Needs Assessment Survey (BHNAS): Overview of Survey Items and Measures

    DTIC Science & Technology

    2013-02-12

    are not opioids (including Celebrex, Vioxx, Bextra, topical lidocaine ) • Prescription opioid/narcotic painkiller (including OxyContin, Percocet...Prescription painkillers that are not opioids (including Celebrex, Vioxx, Bextra, topical lidocaine ). O 5. Prescription opioid/narcotic painkiller

  15. 16 CFR 1700.14 - Substances requiring special packaging.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... breath fresheners. It does not include throat sprays or aerosol breath fresheners. (23) Lidocaine. Products containing more than 5.0 mg of lidocaine in a single package (i.e., retail unit) shall be...

  16. 16 CFR 1700.14 - Substances requiring special packaging.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... breath fresheners. It does not include throat sprays or aerosol breath fresheners. (23) Lidocaine. Products containing more than 5.0 mg of lidocaine in a single package (i.e., retail unit) shall be...

  17. SCI with Brain Injury: Bedside to Bench Modeling for Developing Treatment and Rehabilitation Strategies

    DTIC Science & Technology

    2013-10-01

    DOCUSATE 10 ACETAMINOPHEN 9 ACETAMINOPHEN 7 SENNA 9 SENNA 4 BISACODYL 7 BISACODYL 5 OMEPRAZOLE 7 OMEPRAZOLE 1 ALBUTEROL 6 ALBUTEROL 2 LIDOCAINE 5... LIDOCAINE 1 ASCORBIC ACID 4 ASCORBIC ACID 2 HYDROCODONE/ACETAMINOPHEN 4 HYDROCODONE/ACETAMINOPHEN 2 ONDANSETRON 4 ONDASENTRON 1 ENOXAPARIN 3 ENOXAPARIN 3...7 SENNA 4 LIDOCAINE 5 LIDOCAINE 1 ONDANSETRON 5 ONDASETRON 1 GABAPENTIN 4 GABAPENTIN 2 ASCORBIC ACID 4 ASCORBIC ACID 1 BISACODYL 4 BISACODYL 1

  18. Cimetidine

    MedlinePlus

    ... trimipramine (Surmontil); chlordiazepoxide (Librium); clopidogrel (Plavix), diazepam (Valium); lidocaine (Xylocaine); metronidazole (Flagyl); nifedipine (Adalat, Procardia); phenytoin (Dilantin); ...

  19. The Effect of Smoking on Muscle Adaptation to Exercise

    DTIC Science & Technology

    2010-12-01

    skin was cleaned with betadine and infused with 2% lidocaine (McKesson, San Francisco, CA). A 1.5 cm incision was made and additional lidocaine was...of 2% lidocaine hydrochloride solution, a small (1-3cm) incision was made in the skin and fascia, the biopsy needle is inserted, and about 200 mg...taken from the vastus lateralis muscle. The biopsy will be obtained under local anesthesia ( Lidocaine ) by a licensed physician. ! The procedure is

  20. Neurofibromatosis and the Painful Neuroma

    DTIC Science & Technology

    2010-01-01

    clinical treatment of neuropathic pain and pain from neuroma formation. Systemic administration of lidocaine has also been used to treat neuropathic... pain . We performed an experiment to compare the effect of pregabalin(PGB), morphine, and lidocaine (LDC) on the TNT model. Method: TNT model...of mechanical hyperalgesia (partially dennervated skin). Further, systemic lidocaine can be expected to impact neuroma sensitivity related pain

  1. Drug release from hydroethanolic gels. Effect of drug's lipophilicity (logP), polymer-drug interactions and solvent lipophilicity.

    PubMed

    Sawant, Prashant D; Luu, Dewitt; Ye, Rose; Buchta, Richard

    2010-08-30

    We demonstrate drug release properties from hydroethanolic formulations as a function of the drug's lipophilicity (logP), solvent lipophilicity and drug-polymer interactions, for the first time. A hydrophilic polymer, hydroxypropyl cellulose (HPC), provides the non-Fickian slower release of the lipophilic drug, lidocaine (logP=2.6) and the burst (Fickian) release of hydrophilic drug, lidocaine hydrochloride (logPlidocaine. However, the cationic hydrophobic polymer (Eudragit E100) retained more lidocaine (approximately 50%) topically than other hydrophobic polymers: Eudragit S100 (anionic) and Eudragit RLPO (cationic copolymer with quaternary ammonium group) ( approximately 25% lidocaine retention) which release lidocaine systematically. Thus, minute changes in functional groups of hydrophobic polymers help tune the lidocaine release topically or systemically. An interaction between HPC and lidocaine as determined by FTIR helps the non-Fickian slower lidocaine release from HPC formulations. However, no interactions between lidocaine and hydrophobic Eudragit polymers explain the Fickian burst release of lidocaine from their formulations. A lipophilic solvent, isostearyl alcohol which when replacing ethanol by 30%, slows the release rate and enhances the topical adsorption of lidocaine. Thus, solvent lipophilicity also modulates drug release properties.

  2. 77 FR 42733 - Novartis AG; Analysis of Agreement Containing Consent Orders to Aid Public Comment

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-07-20

    ... lidocaine-prilocaine cream, and generic metronidazole topical gel (``Marketed Divestiture Products'') and... generic calcipotriene topical solution, generic lidocaine-prilocaine cream, generic metronidazole topical... lidocaine-prilocaine cream is used as a local anesthetic to treat intact skin and to relieve pain...

  3. Coating solid dispersions on microneedles via a molten dip coating method: development and in vitro evaluation for transdermal delivery of a water insoluble drug

    PubMed Central

    Ma, Yunzhe; Gill, Harvinder S.

    2014-01-01

    This study demonstrates for the first time the ability to coat solid dispersions on microneedles as a means to deliver water-insoluble drugs through the skin. Polyethylene glycol (PEG) was selected as the hydrophilic matrix, and lidocaine base was selected as the model hydrophobic drug to create the solid dispersion. First, thermal characterization and viscosity measurements of the PEG-lidocaine mixture at different mass fractions were performed. The results show that lidocaine can remain stable at temperatures up to ~130 °C, and that viscosity of the PEG-lidocaine molten solution increases as the mass fraction of lidocaine decreases. Differential scanning calorimetry demonstrated that at lidocaine mass fraction less than or equal to 50%, lidocaine is well dispersed in the PEG-lidocaine mixture. Uniform coatings were obtained on microneedle surfaces. In vitro dissolution studies in porcine skin showed that microneedles coated with PEG-lidocaine dispersions resulted in significantly higher delivery of lidocaine in just 3 min compared to 1 h topical application of 0.15 g EMLA®, a commercial lidocaine-prilocaine cream. In conclusion, the molten coating process we introduce here offers a practical approach to coat water-insoluble drugs on microneedles for transdermal delivery. PMID:25213295

  4. The Effect of a Third Generation Hemostatic Dressing in a Subclavian Artery and Vein Transection Porcine Model

    DTIC Science & Technology

    2014-04-01

    small skin incision. The exposed subclavian vessels were treated with lidocaine , transected and allowed to free bleed for thirty seconds prior to...cavity depth, and cavity volume. The subclavian vessels were then immersed in 30 mL of 2% lidocaine (Phoenix Pharmaceuticals, St. Joseph, MO) for 10...maintained above 60 mmHg. When the stabilization period was completed, excess lidocaine in the cavity was removed and vessels were measured again. The

  5. The Effect of Smoking on Muscle Adaptation to Exercise Stress

    DTIC Science & Technology

    2011-12-01

    lateralis muscles using a Bergstrom 5-6 mm biopsy needle. Skin was first lightly anesthetized with 4 ml of 2% lidocaine hydrochloride solution, a small...Clarkson ! Muscle biopsies will be taken from the vastus lateralis muscle. The biopsy will be obtained under local anesthesia ( Lidocaine ) by a...first Assistant will open the top of the Lidocaine vial and clean with alcohol pad, and hold the vial upside down for physician to withdraw

  6. Medial Prefrontal Cortex and HPA Axis Roles in Generation of PTSD-Like Symptoms in SPS Model

    DTIC Science & Technology

    2012-09-01

    onsecutive weight gain. The PL and IL were temporarily inactivated by infusion of the odium channel blocker, lidocaine HCL (Sigma–Aldrich, St. Louis, O) in...a concentration of 2%. Lidocaine HCl was dissolved in a 0.9% aline solution, which was also used as the vehicle treatment. A icrosyringe pump...5min, then analyzed t a later date. Lidocaine and saline infusions were performed on eparate groups of rats. The order of TMT-induced freezing and OF

  7. SCI with Brain Injury: Bedside-to-Bench Modeling for Developing Treatment and Rehabilitation Strategies

    DTIC Science & Technology

    2012-10-01

    12 VA Frequency SCVMC Frequency ACETAMINOPHEN 10 ACETAMINOPHEN 7 DOCUSATE 8 DOCUSATE 8 OMEPRAZOLE 8 OMEPRAZOLE 1 SENNA 7 SENNA 4 LIDOCAINE 5... LIDOCAINE 1 ONDANSETRON 5 ONDASETRON 1 GABAPENTIN 4 GABAPENTIN 2 ASCORBIC  ACID 4 ASCORBIC ACID 1 BISACODYL 4 BISACODYL 1 TRAZODONE 3 TRAZADONE 5...DOCUSATE 9 DOCUSATE 10 ACETAMINOPHEN 9 ACETAMINOPHEN 7 SENNA 9 SENNA 4 BISACODYL 7 BISACODYL 5 OMEPRAZOLE 7 OMEPRAZOLE 1 ALBUTEROL 6 ALBUTEROL 2 LIDOCAINE 5

  8. An Evaluation of the Effectiveness of a Vibrating Syringe Attachment in Decreasing Intraoral Injection Pain Perception

    DTIC Science & Technology

    2012-06-01

    blindfolded and given headphones prior to all injections. The amount of anesthetic delivered was limited to 0.1 ml of 2% lidocaine with 1: 1 00,000... lidocaine with 1: 1 00,000 epinephrine) into the mucosa. On a third VAS, they marked the overall level of discomfort from the entire anesthetic...use of local anesthetics (e.g., lidocaine ) with epinephrine. • Pregnant females. 17 • Participants who do not consent to the study. Participants

  9. Motor Cortex Stimulation Reverses Maladaptive Plasticity Following Spinal Cord Injury

    DTIC Science & Technology

    2011-09-01

    Additional anesthesia (10 mg/kg intraperitoneal, diluted ketamine 1:10 in saline) was administered whenneeded. Local anesthetic (2% lidocaine )was applied to...behavioral testing to obtain reliable baseline values for efficacy of MCS, the microdialysis probe was used to administer lidocaine (2%), muscimol (200 lM...cannulae in ZI as well as MCS electrodes above M1. Animals received infu- sions of either saline (n = 4) or 2% lidocaine into ZI during MCS and changes in

  10. Effects of Simulated Pathophysiology on the Performance of a Decision Support Medical Monitoring System for Early Detection of Hemodynamic Decompensation in Humans

    DTIC Science & Technology

    2014-10-01

    anesthesia (2% lidocaine ) using aseptic techniques and advanced until an appro- priate CVP waveform was obtained. This catheter was connected to a high...was placed under local anesthesia (2% lidocaine ) using aseptic techniques. Preservative/anticoagulant bags (63 ml anticoag- ulant citrate phosphate...catheter was placed into a brachial artery under local anesthesia (2% lidocaine ) using aseptic techniques and ultrasound guidance. The catheter was

  11. Development of a Standard Swine Hemorrhage Model for Efficacy Assessment of Topical Hemostatic Agents

    DTIC Science & Technology

    2011-07-01

    1. Pictures of preparation of femora l artery injury model in swine: (A) femoral artery vessel was isolated and treated with lidocaine for optimum...Briefly, the femoral artery was isolated and treated with lidocaine for optimum dilation (Fig. I, A). The vascular injury (6-mm punched hole in...effective in any circumstance. Application of lidocaine to dilate the vessel is not clinically relevant; how- ever, it is a necessary step in this

  12. Using the Estimating Supplies Program to Develop Material Solutions for the U.S. Air Force Medical Gynecological Treatment Team (FFGYN)

    DTIC Science & Technology

    2007-12-10

    Debride/Suture/Incision) 100 167 DEFINITIVE CARE EMEDS+25 Interpret Lab Results 75 168 EN ROUTE CARE Warm Fluid Infusion 50 Figure 1. PC 118...AMB100S 6505014554200 LIDOCAINE AND EPINEPHRINE 1:100,000 20 ML VI 6505005986116 LIDOCAINE HYDROCHLORIDE 1.0%/ML 50ML 6515015261726 NEEDLE HYP SAFE W...6505005986116 LIDOCAINE HYDROCHLORIDE 1.0%/ML 50ML 6515007542836 NEEDLE HYPO 20GA 1.438-1.562IN LUER LOCK 100S 6510007863736 PAD ISOPROPYL ALCOHOL

  13. Local Anesthetic Microencapsulation.

    DTIC Science & Technology

    1983-11-04

    tollowing I.M. injection of microencapsulated lidocaine and etidocaine than following solution injections. Local toxicity of these microcapsule injections...Distribution 41 Table 12 Processing Summary of Lidocaine (Base) 43 Microencapsulation Table 13 Lidocaine (Base) Microcapsule Size 44 Distribution...Table 14 Processing Summary of Et’idocaine-HCl 45 Microencapsulation Table 15 Etidocaine-HCl Microcapsule Size 47 Distribution Table 16 Process Summary

  14. Local Anesthetic Microcapsules.

    DTIC Science & Technology

    1981-04-15

    III Chemical Structure of Local Anesthetics 12 Table IV Processing Summary of Lidocaine Microencapsulation 15 Table V Lidocaine Microcapsule Size...Distribution 17 Table VI Processing Summary of Etidocaine Microencapsulation 18 Table VII Etidocaine Microcapsule Size Distribution 19 Table VIII Lidocaine...REPORT I PERIOD COVERED Annual Local Anesthetic Microcapsules 1 July 1980-30 March 1981 6. PERFORMING ORG. REPORT NUMBER 2106-1 7. AUTHOR() S

  15. Co-administration of memantine with epinephrine produces a marked peripheral action in intensifying and prolonging analgesia in response to local skin pinprick in rats.

    PubMed

    Chen, Yu-Wen; Tzeng, Jann-Inn; Pan, He-Jia; Hung, Ching-Hsia; Chen, Yu-Chung; Wang, Jhi-Joung

    2014-06-27

    The purpose of this study was to examine the effect of epinephrine as adjuvant for memantine or lidocaine as an infiltrative anesthetic. Using a rat model of cutaneous trunci muscle reflex (CTMR), we evaluated the effects of adding epinephrine to memantine or lidocaine on infiltrative cutaneous analgesia. Lidocaine, a known local anesthetic, was used as control. We found that epinephrine, memantine, and lidocaine produced a dose-dependent local anesthetic effect as infiltrative cutaneous analgesia. On a 50% effective dose (ED50) basis, the relative potencies were epinephrine [0.012 (0.006-0.020)μmol]>memantine [4.010 (3.311-4.988)μmol]>lidocaine [6.177 (5.333-7.218)μmol] (P<0.05 for each comparison). Mixtures of epinephrine (2.7nmol or 13.7nmol) with drugs (memantine or lidocaine) at ED50 or ED95, respectively, enhanced the potency and prolonged the duration of action on infiltrative cutaneous analgesia. Intraperitoneal injection of co-administration of drugs (memantine or lidocaine) at ED95 with epinephrine (13.7nmol) produced no cutaneous analgesia (data not shown). Epinephrine, memantine, and lidocaine were shown to have local anesthetic effects as infiltrative cutaneous analgesia. Epinephrine increased the duration and potency of memantine and lidocaine as an infiltrative anesthetic.

  16. 21 CFR 862.3200 - Clinical toxicology calibrator.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Toxicology Test...., ethanol, lidocaine, etc.). (See also § 862.2 in this part.) (b) Classification. Class II....

  17. Do not use epinephrine in digital blocks: myth or truth?

    PubMed

    Wilhelmi, B J; Blackwell, S J; Miller, J H; Mancoll, J S; Dardano, T; Tran, A; Phillips, L G

    2001-02-01

    The purpose of this study was to examine the role for epinephrine augmentation of digital block anesthesia by safely prolonging its duration of action and providing a temporary hemostatic effect. After obtaining approval from the review board of the authors' institution, 60 digital block procedures were performed in a prospective randomized double-blinded study. The digital blocks were performed using the dorsal approach. All anesthetics were delivered to treat either posttraumatic injuries or elective conditions. Of the 60 digital block procedures, 31 were randomized to lidocaine with epinephrine and 29 to plain lidocaine. Of the procedures performed using lidocaine with epinephrine, one patient required an additional injection versus five of the patients who were given plain lidocaine (p = 0.098). The need for control of bleeding required digital tourniquet use in 20 of 29 block procedures with plain lidocaine and in 9 of 31 procedures using lidocaine with epinephrine (p < 0.002). Two patients experienced complications after plain lidocaine blocks, while no complications occurred after lidocaine with epinephrine blocks (p = 0.23). By prolonging lidocaine's duration of action, epinephrine may prevent the need for an additional injection and prolong post-procedure pain relief. This study demonstrated that the temporary hemostatic effect of epinephrine decreased the need for, and thus the potential risk of, using a digital tourniquet (p < 0.002). As the temporary vasoconstrictor effect is reversible, the threat of complication from vasoconstrictor-induced ischemia is theoretical.

  18. Local anesthesia in the palate: a comparison of techniques and solutions.

    PubMed Central

    Meechan, J. G.; Day, P. F.; McMillan, A. S.

    2000-01-01

    It was the purpose of the present investigation to determine if there were differences in soft-tissue anesthesia in the palate following infiltration and greater palatine nerve block anesthesia and to compare lidocaine with lidocaine plus epinephrine as palatal soft tissue anesthetics. Two studies using 10 volunteers were performed. In one trial, volunteers received a palatal infiltration opposite the second maxillary bicuspid on one side and a greater palatine nerve block on the other. Response to sharp probing and pain-pressure thresholds were measured on each side over a 1-hour census period. In the second trial, volunteers received 2% plain lidocaine as a palatal infiltration on one side and a similar infiltration of 2% lidocaine with 1:80,000 epinephrine on the other in a double-blind randomized fashion. Response to sharp probing was assessed over a 55-minute period. Data were analyzed using Student's paired t tests. The response to sharp probing and pressure-pain thresholds did not differ between palatal infiltration and greater palatine nerve block over the 1-hour period. Lidocaine with epinephrine provided longer lasting anesthesia than plain lidocaine following palatal infiltration (P < .001). Greater palatine nerve block and palatal infiltration provide similar soft-tissue anesthesia. Lidocaine with epinephrine produces longer-lasting soft-tissue anesthesia than plain lidocaine following palatal infiltration. PMID:11432180

  19. Assessment of Regenerative Capacity in the Dolphin

    DTIC Science & Technology

    2012-06-30

    block ( lidocaine ) in the approximate area where the infusion cannula will be inserted. An infusion cannula with attached syringe is then used to...infuse the intended adipose harvest site with tumescent solution; a solution consisting of lidocaine , epinephrine and saline. A waiting period of

  20. Use of the Abdominal Aortic Tourniquet for Hemorrhage Control

    DTIC Science & Technology

    2013-10-01

    for pain control after completion of ONS experiments. Additional drugs such as dopamine (1-10mcg/kg/hr), lidocaine (50mcg/kg/min) and amiodarone...overlying abductor muscle will be excised. The femoral artery will be bathed in 2% lidocaine until the artery is dilated to greater than 1 cm in

  1. Anesthesia Providers’ Adherence to the Use of Gloves and Eye Protection

    DTIC Science & Technology

    2013-01-31

    needles. The majority of these instances occurred just prior to venipuncture when providers injected Lidocaine intradermally and subsequently recapped...after injection of a subcutaneous wheal of Lidocaine prior to venipuncture. Finally, 100% of the 11 providers observed touched equipment with

  2. The Effect of a Bio-Behavioral Intervention on the Release of Cytokines

    DTIC Science & Technology

    2012-04-04

    intravenous lidocaine demonstrated less increase in levels of pro-inflammatory cytokines to include IL-8 and lesser severity of postoperative pain than...Comparison of the effects of thoracic epidural analgesia and i.v. infusion with lidocaine on cytokine response, postoperative pain and bowel

  3. Tactical Combat Casualty Care 2007: Evolving Concepts and Battlefield Experience

    DTIC Science & Technology

    2007-11-01

    or thoracic) hemorrhage: no IV fluid resuscitation Head wound patient: Hespan at minimal flow to maintain infusion unless there is concurrent...airway obstruction: chin lift or jaw thrust, nasopharyngeal airway, place casualty in recovery position Surgical cricothyroidotomy (with lidocaine ...laryngeal mask airway /ILMA or Combitube or endotracheal intubation or surgical cricothyroidotomy (with lidocaine if conscious) Spinal immobilization is

  4. Disruption of memory reconsolidation impairs storage of other, non-reactivated memory.

    PubMed

    Tzeng, Wen-Yu; Chang, Wan-Ting; Chuang, Jia-Ying; Lin, Kuey-Yin; Cherng, Chianfang G; Yu, Lung

    2012-02-01

    Two hypotheses were tested in this study. First, blockade of neural activity by lidocaine immediately following the retrieval of a memory may impair the reconsolidation and subsequent expression of that memory. Second, a non-retrieved memory would not be affected by this lidocaine treatment. Since the basolateral nucleus of the amygdala (BLA) is involved in emotion-related memory, an intra-BLA lidocaine infusion was used immediately after the retrieval of two emotion-related memories, the step-through passive avoidance response (PA) and cocaine-induced conditioned place preference (CPP). Intra-BLA lidocaine infusion immediately after cocaine-induced CPP retrieval diminished CPP magnitude in retests. However, intra-BLA lidocaine infusion alone did not affect cocaine-induced CPP performance. Intra-BLA lidocaine infusion immediately after PA retrieval decreased PA performance in retests. Omission of PA retrieval procedure, intra-BLA lidocaine infusion did not affect subsequent PA performance. Surprisingly, intra-BLA lidocaine infusion immediately following the retrieval of PA or cocaine-induced CPP diminished both PA and cocaine-induced CPP performance in the retests. Finally, Fos-staining results revealed that a number of BLA neurons were activated by the retrieval of both cocaine-induced CPP and PA. We conclude that inactivation of neural activity in BLA immediately following retrieval of a fear or cocaine-conditioned memory can impair subsequent expression of both memories. More importantly, retrieval of a memory does not seem to be an absolute condition for rapidly changing the memory.

  5. Memantine elicits spinal blockades of motor function, proprioception, and nociception in rats.

    PubMed

    Chen, Yu-Wen; Chiu, Chong-Chi; Liu, Kuo-Sheng; Hung, Ching-Hsia; Wang, Jhi-Joung

    2015-12-01

    Although memantine blocks sodium currents and produces local skin anesthesia, spinal anesthesia with memantine is unknown. The purpose of the study was to evaluate the local anesthetic effect of memantine in spinal anesthesia and its comparison with a widely used local anesthetic lidocaine. After intrathecally injecting the rats with five doses of each drug, the dose-response curves of memantine and lidocaine were constructed. The potencies of the drugs and durations of spinal anesthetic effects on motor function, proprioception, and nociception were compared with those of lidocaine. We showed that memantine produced dose-dependent spinal blockades in motor function, proprioception, and nociception. On a 50% effective dose (ED50 ) basis, the rank of potency was lidocaine greater than memantine (P < 0.05 for the differences). At the equipotent doses (ED25 , ED50 , ED75 ), the block duration produced by memantine was longer than that produced by lidocaine (P < 0.05 for the differences). Memantine, but not lidocaine, displayed more sensory/nociceptive block than motor block. The preclinical data demonstrated that memantine is less potent than lidocaine, whereas memantine produces longer duration of spinal anesthesia than lidocaine. Memantine shows a more sensory-selective action over motor blockade.

  6. Intoxication mortelle après ingestion accidentelle de xylocaine visqueuse à 2% chez une jeune enfant.

    PubMed

    Nisse, P; Lhermitte, M; Dherbecourt, V; Fourier, C; Leclerc, F; Houdret, N; Mathieu-Nolf, M

    2002-01-01

    We report a case of fatal intoxication with 2% viscous lidocaine. A 18 month old infant was admitted after malaise and cardiorespiratory arrest at home. He was resuscitated, then seizures appeared before arrival at the hospital. Treatment was symptomatic, including cardiorespiratory resuscitation and administration of anticonvulsants. Identification of lidocaine and its metabolite monoethylglycinexylidide (MEGX) MEGX was performed after organic extraction by High Performance Liquid Chromatography (HPLC) with Diode Array Detection (DAD); the serum concentrations, determined by Fluorescence Polarisation Immuno Assay (FPIA), were : 1,1 μg / ml for lidocaine and 0,94 μg / ml for MEGX (H+7) and 0,30 μg / ml for the lidocaine (Day+1). Neurotoxic manifestations appear at lower concentrations than cardiotoxic symptoms which are correlated with plasma levels of lidocaine. The toxic symptoms begin with headache, hallucinations, seizure, coma, respiratory arrest and circulatory collapse. The toxic symptoms can persist even after the decrease of lidocaine concentration under therapeutic levels. There is no antidote and acute lidocaine toxicity is managed with supportive therapy (diazepam for seizures, intubation, chronotropic agents). Considering the gravity of these poisonings which remain rare, the 2% viscous lidocaine prescription is forbidden for children under 6 years old.

  7. Acute physiological responses to castration-related pain in piglets: the effect of two local anesthetics with or without meloxicam.

    PubMed

    Bonastre, C; Mitjana, O; Tejedor, M T; Calavia, M; Yuste, A G; Úbeda, J L; Falceto, M V

    2016-09-01

    Methods to reduce castration-related pain in piglets are still issues of concern and interest for authorities and producers. Our objectives were to estimate the effectiveness of two protocols of local anesthesia (lidocaine and the combination of lidocaine+bupivacaine) as well as the use of meloxicam as a postoperative analgesic in alleviating castration-related pain, measured by acute physiological responses. Eight groups (15 piglets/group) were included in the study: (1) castration without anesthesia or analgesia, without meloxicam (TRAD WITHOUT), (2) castration without anesthesia or analgesia, but with meloxicam (TRAD WITH), (3) handling without meloxicam (SHAM WITHOUT), (4) handling with meloxicam (SHAM WITH), (5) castration after local anesthesia with lidocaine but without meloxicam (LIDO WITHOUT), (6) castration after local anesthesia with lidocaine and meloxicam (LIDO WITH), (7) castration after local anesthesia with lidocaine+bupivacaine without meloxicam (LIDO+BUPI WITHOUT), (8) castration after local anesthesia with lidocaine+bupivacaine and meloxicam (LIDO+BUPI WITH). Acute physiological responses measured included skin surface temperature and serum glucose and cortisol concentrations. On days 4 and 11 post-castration BW was recorded and average daily gain was calculated over this period. Furthermore, piglet mortality was recorded over the 11-day post-castration period. Administration of local anesthetic or meloxicam did not prevent the decrease in skin surface temperature associated with castration. Lidocaine reduced the increase in glucose concentration associated with castration. For castrated pigs, the joint use of lidocaine and meloxicam caused a significant decrease in cortisol concentration; the combination of intratesticular lidocaine and bupivacaine did not seem to be more effective than lidocaine alone. No effect of treatments on mortality and growth were detected.

  8. Anesthetics alter the physical and functional properties of the Ca-ATPase in cardiac sarcoplasmic reticulum.

    PubMed Central

    Karon, B S; Geddis, L M; Kutchai, H; Thomas, D D

    1995-01-01

    We have studied the effects of the local anesthetic lidocaine, and the general anesthetic halothane, on the function and oligomeric state of the CA-ATPase in cardiac sarcoplasmic reticulum (SR). Oligomeric changes were detected by time-resolved phosphorescence anisotropy (TPA). Lidocaine inhibited and aggregated the Ca-ATPase in cardiac SR. Micromolar calcium or 0.5 M lithium chloride protected against lidocaine-induced inhibition, indicating that electrostatic interactions are essential to lidocaine inhibition of the Ca-ATPase. The phospholamban (PLB) antibody 2D12, which mimics PLB phosphorylation, had no effect on lidocaine inhibition of the Ca-ATPase in cardiac SR. Inhibition and aggregation of the Ca-ATPase in cardiac SR occurred at lower concentrations of lidocaine than necessary to inhibit and aggregate the Ca-ATPase in skeletal SR, suggesting that the cardiac isoform of the enzyme has a higher affinity for lidocaine. Halothane inhibited and aggregated the Ca-ATPase in cardiac SR. Both inhibition and aggregation of the Ca-ATPase by halothane were much greater in the presence of PLB antibody or when PLB was phosphorylated, indicating a protective effect of PLB on halothane-induced inhibition and aggregation. The effects of halothane on cardiac SR are opposite from the effects of halothane observed in skeletal SR, where halothane activates and dissociates the Ca-ATPase. These results underscore the crucial role of protein-protein interactions on Ca-ATPase regulation and anesthetic perturbation of cardiac SR. PMID:7756557

  9. Effects of reversible inactivation of the medial septum on rat exploratory behavior in the elevated plus-maze using a test-retest paradigm.

    PubMed

    Lamprea, Marisol Rodríguez; Garcia, Andrea Milena Becerra; Morato, Silvio

    2010-06-26

    The effect of intraseptal injections of lidocaine before a first or a second session in the elevated plus-maze, in a test-retest paradigm, was investigated. In addition to gross session analyses, a minute-by-minute analysis of the sessions was used to evaluate both anxiety and memory. Lidocaine injections before the test session produced increases in the frequency of entries, time spent and distance run in the open arms without affecting activity occurring in the closed arms. During the retest session, saline- and lidocaine-treated rats exhibited increased indices of anxiety and lidocaine-treated rats exhibited decreased closed-arm entries. The minute-by-minute analysis showed a faster decrease in anxiety-related behaviors during the test session by saline- than by lidocaine-treated rats and a significant decrease in closed-arm exploration by saline-treated rats, but not by lidocaine-treated ones. Lidocaine injection before the retest session produced increases in the frequency of entries, time spent and distance run in the open arms in the second session when compared with saline-treated rats. Minute-by-minute analysis showed an increase in the time spent in the open arms by lidocaine animals at the beginning of the retest session in comparison to saline animals and a significant decrease in closed-arm exploration by both groups. These results suggest that inactivation of the medial septum by lidocaine affects the expression of unconditioned and conditioned forms of anxiety in the elevated plus-maze and, in a lesser way, the acquisition and retention of spatial information.

  10. Anesthetic efficacy of infiltrations in mandibular anterior teeth.

    PubMed Central

    Yonchak, T.; Reader, A.; Beck, M.; Clark, K.; Meyers, W. J.

    2001-01-01

    The purpose of this prospective, randomized, double-blind study was to measure the degree of anesthesia obtained with a labial infiltration of either 2% lidocaine with 1:50,000 or 2% lidocaine with 1:100,000 epinephrine in mandibular anterior teeth. Another objective was to measure the degree of anesthesia obtained with a lingual infiltration of 2% lidocaine with 1:100,000 epinephrine in mandibular anterior teeth. Through use of a repeated-measures design, 40 subjects randomly received a labial infiltration at the lateral incisor apex of either 1.8 mL of 2% lidocaine with 1:100,000 epinephrine or 1.8 mL of 2% lidocaine with 1:50,000 epinephrine at 2 separate appointments. An additional 40 subjects received a lingual infiltration at the lateral incisor apex of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine. The mandibular anterior teeth were blindly pulp tested at 4-minute cycles for 60 minutes postinjection. No response from the subject to the maximum output (80 reading) of the pulp tester was used as the criterion for pulpal anesthesia. Anesthesia was considered successful when 2 consecutive 80 readings were obtained. For the 3 infiltrations, success rates for the lateral incisor ranged from 43 to 50%. Adjacent teeth had success rates of 27 to 63%. There was no significant difference (P > 0.05) in success between the labial infiltration of 2% lidocaine with 1:100,000 epinephrine and 2% lidocaine with 1:50,000 epinephrine or the lingual infiltration of 2% lidocaine with 1:100,000 epinephrine when compared with the labial infiltration of 2% lidocaine with 1:100,000 epinephrine. Duration of pulpal anesthesia declined steadily for all solutions over the 60 minutes. In conclusion, the success rate of 43-50% and declining duration of pulpal anesthesia over an hour indicates that a labial infiltration of 1.8 mL of either 2% lidocaine with 1:100,000 epinephrine or 1: 50,000 epinephrine or a lingual infiltration of 2% lidocaine with 1:100,000 epinephrine over the

  11. Convection-Enhanced Delivery (CED) in an Animal Model of Malignant Peripheral Nerve Sheath Tumors and Plexiform Neurofibromas

    DTIC Science & Technology

    2011-09-01

    povidone-iodine swabs or gauzes. 70% alcohol swab or gauze is used to remove the remaining povidone-iodine from the skin. ~100μL 1% lidocaine is...site. A few drops of lidocaine are dropped on the nerve. A 34 Gauge fused silica (WPI) cannula is inserted at a sharp angle (~10°) along the nerve...remove the remaining povidone-iodine from the skin. ~100μL 1% lidocaine is injected along the incision line to ensure adequate analgesia. A 15mm dorsal

  12. Modernization of the Air Expeditionary Squadron AMAL 0960

    DTIC Science & Technology

    2012-07-25

    Med 100s Standard health precautions 5276265212 Hand Sanitizer (1 Dz Pump 8 Oz Pump Bottles) Hand sanitation 6505014554200 Lidocaine And Epinephrine...6505014821064 Ketorolac Tromethamine Inj 30mg/Ml 1ml 10s 1 1 PG 6505015249195 Levonorgestrel Tablets 0.075mg 2s 2 2 PG 6505005986116 Lidocaine ...Hydroch Inj 1.0%/Ml 50ml 3 1 BT 6505014554200 Lidocaine &Epinephrine 1:100000 20ml Vi 3 1 VI 6505010666568 Loperamide Hydroch Caps 2mg 100s 2 1 BT

  13. U.S. Air Force Operational Medicine: Using the Enterprise Estimating Supplies Program to Develop Materiel Solutions for the Mobile Aeromedical Staging Facility (FFQM1)

    DTIC Science & Technology

    2012-05-30

    0.12 $10.42 B 6505011947265UM LIDOCAINE HCL 0.4% & D5W INJ 500ML BAG 18S PG 2 5 2.72 0.10 $14.46 6.81 0.24 $36.15 D 6505015332656UM LIDOCAINE HCL...INJ 2% 5ML 10S PG 3 0 0.06 0.01 $1.14 0.00 0.00 $0.00 D 6505005986116 LIDOCAINE HYDROCH INJ 1.0%/ML 50ML BT 3 0 0.75 0.30 $57.66 0.00 0.00 $0.00 D

  14. Efficacy of Opioid-free Anesthesia in Reducing Postoperative Respiratory Depression in Children Undergoing Tonsillectomy

    ClinicalTrials.gov

    2016-12-08

    Anesthesia; General Anesthesia; Analgesics, Opioid; Postoperative Complications; Pathologic Processes; Physiologic Effects of Drugs; Narcotics; Analgesics; Sleep Disordered Breathing; Obstructive Sleep Apnea of Child; Tonsillectomy; Respiratory Depression; Dexmedetomidine; Ketamine; Lidocaine; Gabapentin; Pulse Oximetry

  15. Toxicological Findings of Pilots Involved in Aviation Accidents Operated under 14 CFR Part 135

    DTIC Science & Technology

    2009-08-01

    pilots), dextromethorphan (2 pilots), doxylamine (1 pilot), naphazoline (1 pilot), and theophylline (1 pilot) . Other medications found in these 33...aviation accidents between 1997 and 2007. 6 pseudoephedrine, phenylpropanolamine, dextrometho- rphan, doxylamine , and dextrorphan . Finally, lidocaine

  16. Assessment of Regenerative Capacity in the Dolphin

    DTIC Science & Technology

    2010-10-10

    is allowed to stabilize while respiration and heart- rate monitors are attached. The animal is given a local skin block ( lidocaine ) in the...approximate area where the infusion cannula will be inserted. An infusion cannula with attached syringe is then used to infuse the intended adipose harvest...site with tumescent solution; a solution consisting of lidocaine , epinephrine and saline. A waiting period of between 10 and 20 minutes is then

  17. Medial Prefrontal Cortex and HPA Axis Roles in Generation of PTSD-Like Symptoms in SPS Model

    DTIC Science & Technology

    2011-09-01

    inactivated by infusion of the sodium channel blocker, lidocaine HCL (Sigma- Aldrich, St. Louis, MO) in a concentration of 2 %. Lidocaine HCl was dissolved in...syringes (Hamilton Company, Reno, NV) was used for infusions . Polyethylene tubing connected infusion cannulae (33-gauge, 11 mm; Plastics One, Roanoke...VA) to the syringes and controller. Solutions were infused bilaterally at a rate of 0.2 µL/minute for one minute and infusion cannulae remained in

  18. Journal of Special Operations Medicine. Volume 10, Edition 2, Spring 2010

    DTIC Science & Technology

    2010-01-01

    resuscitation. No coagulopathy was seen with Hextend use so long as the maximum infused volume was 1000cc, as called for by the TCCC Guidelines. A recent article...cricothyroidotomy (with lidocaine if conscious) 3. Breathing a. In a casualty with progressive respiratory distress and known or suspected torso trauma...LMA)/intubating LMA or – Combitube or – Endotracheal intubation or – Surgical cricothyroidotomy (with lidocaine if conscious). c. Spinal immobilization

  19. Journal of Special Operations Medicine. Volume 1, Edition 3, Fall 2001

    DTIC Science & Technology

    2001-01-01

    abscess or indi- rect laryngoscopy with laryngeal mirrors. In painful first and second-degree burns, an application of lidocaine can entirely relieve...hygienic tech- niques, especially in a land ridden with hepatitis. And, too, why suffer too much pain on a holy mission when Lidocaine was readily...Preventing Painful Shins Splints� articles. With the last edition of the JSOM, you found a survey. Thank you to the many who filled it out and

  20. Local Anesthetic Microcapsulation.

    DTIC Science & Technology

    1982-06-14

    viscosities as disparate as R. S. V. 4.~O~6dl/g. ’ Microencapsulation of lidocaine (base) yielded 212-300 micron microcapsules with 50% in vitro drug...release in 6 hours; 150-212 micron microcapsules released 3-0% i7n-2 hours. Etidocaing and bupivacaine vo> 41’. were microencapsulated in a more...Etidocaine Microencapsulation 9 c. Bupivacaine Microencapsulation 12 3. In Vitro Drug Release from Microcapsules 15 a. Lidocaine (base) Release Studies

  1. Research and Development in Preventive Dentistry.

    DTIC Science & Technology

    1979-12-01

    Characterization 16 B. Core Material Preparation 18 C. Microencapsulation 20 D. Characterization of Microcapsules 22 1. Size Distribution 22 2. Assays 22 3... microencapsulated with a biodegradable polymer, poly-L(-)- lactide, using a fluidized bed coating technique. A series of microcapsule batches with different...lbs/hr. Material was less than 15 iim (99%), and most of the lidocaine was in the 1 micron range, * C. MICROENCAPSULATION Lidocaine microcapsules were

  2. Pain reduction in local anesthetic administration through pH buffering.

    PubMed

    Christoph, R A; Buchanan, L; Begalla, K; Schwartz, S

    1988-02-01

    The effects of pH buffering on the pain of administration and efficacy of three local anesthetics (1% lidocaine, 1% lidocaine with 1:100,000 epinephrine, and 1% mepivacaine) were investigated in a randomized, prospective, double-blind study of 25 adult volunteers. Plain and buffered solutions of the three local anesthetics were prepared, and a 0.5 intradermal injection of each was administered. Pain of anesthetic infiltration was rated from zero to ten. The area of anesthetized skin surrounding each injection site was measured at time intervals following each injection. Buffering the local anesthetics significantly reduced the mean quantitative pain estimates compared to the nonbuffered controls: 1) 1% lidocaine compared with buffered 1% lidocaine, 4.9 +/- 0.4 versus 1.1 +/- 0.2 (P less than 10(-6)); 2) 1% lidocaine with epinephrine compared with buffered 1% lidocaine with epinephrine, 5.1 +/- 0.4 versus 1.8 +/- 0.4 (P less than 10(-6)); and 3) 1% mepivacaine compared with buffered 1% mepivacaine, 5.1 +/- 0.4 versus 0.9 +/- 0.2 (P less than 10(-6)). Onset, extent, and duration of skin anesthesia were not statistically altered by pH buffering. The pain of local anesthetic administration can be dramatically reduced by buffering the local anesthetic prior to its infiltration. Anesthetic efficacy is not compromised, and patient acceptance may be significantly increased.

  3. Comparative cardiac effects of three hepatobiliary radiopharmacologicals in the dog: concise communication

    SciTech Connect

    Shani, J.; Rogel, S.; Weininger, J.; Lubin, E.

    1982-04-01

    Three hepatobiliary agents with an acetanilide-imidoacetic-acid moiety resembling that in lidocaine were investigated for their possible effects on contractility and conductivity in the heart and on arterial pressure and aortic blood flow. This was done in the light of lidocaine's numerous cardiac side effects. HIDA, BIDA, and DIPA, each with traces of decayed Tc-99m, were injected i.v. into anesthetized dogs with an A-V block, and their effects on the above parameters were followed until control levels were reestablished. Wheras lidocaine raises the diastolic threshold and prolongs the refractory period, the three agents tested do not prolong myocardial conductivity. Both HIDA and BIDA have an effect similar to that of lidocaine, but DIPA has no effect on the latter two parameters. Moreover, whereas lidocaine depresses myocardial contractility, blood pressure, and blood flow, HIDA has a less prominent effect on these parameters, and neither BIDA nor DIPA has any such effect. It is concluded that even though the effect of HIDA on the heart is milder than that of lidocaine, the effects of both BIDA and DIPA are even less pronounced, and they are less likely to cause cardiac side effects when similar doses are administered during nuclear medicine procedures.

  4. Comparative cardiac effects of three hepatobiliary radiopharmacologicals in the dog: concise communication

    SciTech Connect

    Shani, J.; Sarel, O.; Rogel, S.; Weininger, J.; Lubin, E.

    1982-04-01

    Three hepatobiliary agents with an acetanilide-imidoacetic-acid moiety resembling that in lidocaine were investigated for their possible effects on contractility and conductivity in the heart and on arterial pressure and aortic blood flow. This was done in the light of lidocaine's numerous cardiac side effects. HIDA, BIDA, and DIPA, each with traces of decayed /sup 99m/Tc, were injected i.v. into anesthetized dogs with an A-V block, and their effects on the above parameters were followed until control levels were reestablished. Whereas lidocaine raises the diastolic threshold and prolongs the refractory period, the three agents tested do not prolong myocardial conductivity. Both HIDA and BIDA have an effect similar to that of lidocaine, but DIPA has no effect on the latter two parameters. Moreover, whereas lidocaine depressed myocardial contractility, blood pressure, and blood flow, HIDA has a less prominent effect on these parameters, and neither BIDA nor DIPA has any such effect. It is concluded that even though the effect of HIDA on the heart is milder than that of lidocaine, the effects of both BIDA and DIPA are even less pronounced, and they are less likely to cause cardiac side effects when similar doses are administered during nuclear medicine procedures.

  5. Safety and efficacy of using high-dose topical and nebulized anesthesia to obtain endobronchial cultures.

    PubMed

    Berger, R; McConnell, J W; Phillips, B; Overman, T L

    1989-02-01

    We evaluated the safety and efficacy of high-dose topical and nebulized airway anesthesia in normal volunteers and in patients undergoing diagnostic fiberoptic bronchoscopy. Lidocaine solution (4 percent) was used for gargling, for spraying the palate and oropharynx with an atomizer, and for nebulization with an air-powered nebulizer (mean total dose, 1,682 mg) and 2 percent lidocaine (Xylocaine) jelly for anesthetizing nasal passages. In six normal subjects and in eight patients, lidocaine blood levels were measured at baseline, after gargling, after spraying, after nebulization, and then at 5, 10, 15, 30, and 60 min; 19 normal subjects and ten patients underwent the same anesthesia protocol but had no blood drawn. Fiberoptic bronchoscopy was performed in 21 normal volunteers and in 18 patients and cultures obtained using the protected specimen brush. Additional endobronchial lidocaine (mean 256 mg) was given to the 18 patients after collecting the microbiology specimens. Peak lidocaine blood levels remained below 6 micrograms/ml in all cases. Cough and discomfort during bronchoscopic examination was absent or minimal in 17 of 21 normal subjects (80 percent) and in 14 of 18 patients (77 percent) and was severe in only one instance (5 percent). There were no related complications. Using only topical and nebulized anesthesia is safe and effective for performing fiberoptic bronchoscopy, especially when bacterial cultures are to be obtained and endobronchial instillation of lidocaine must be avoided.

  6. Effect of low-molecular-weight beta-cyclodextrin polymer on release of drugs from mucoadhesive buccal film dosage forms.

    PubMed

    Arakawa, Yotaro; Kawakami, Shigeru; Yamashita, Fumiyoshi; Hashida, Mitsuru

    2005-09-01

    We investigated the effect of low-molecular-weight beta-cyclodextrin (beta-CyD) polymer on in vitro release of two drugs with different lipophilicities (i.e., lidocaine and ketoprofen) from mucoadhesive buccal film dosage forms. When beta-CyD polymer was added to hydroxypropylcellulose (HPC) or polyvinylalcohol (PVA) film dosage forms, the release of lidocaine into artificial saliva (pH 5.7) was reduced by 40% of the control. In contrast, the release of ketoprofen from the polymer film was enhanced by addition of beta-CyD polymer to the vehicle. When lidocaine and ketoprofen was incubated with beta-CyD polymer in the artificial saliva, concentration of free lidocaine molecules decreased in a beta-CyD polymer concentration-dependent manner. The association constant with beta-CyD polymer was 6.9+/-0.6 and 520+/-90 M(-1) for lidocaine and ketoprofen, respectively. Retarded release of the hydrophilic lidocaine by beta-CyD polymer might be due to the decrease in thermodynamic activity by inclusion complex formation, whereas enhanced release of the lipophilic ketoprofen by the beta-CyD polymer might be due to prevention of recrystallization occurring after contacting the film with aqueous solution. Thus, effects of low-molecular-weight beta-CyD polymer to the drug release rate from film dosage forms would vary according to the strength of interaction with and the solubility of active ingredient.

  7. Onset and duration of anesthesia for local anesthetic combinations commonly used in forefoot surgery; surprise results with sequential blocks.

    PubMed

    Blazer, Marie Mantini; Petrozzi, Rocco; Harris, Samantha Y; Greer, Hillary; Goldfarb, Jacqueline; Biernacki, Tomasz; Kawalec, Jill S

    2015-06-01

    Local anesthetic nerve blocks are frequently used for postoperative analgesia and to the best of our knowledge no studies have evaluated the effects of injecting bupivacaine into an area previously injected with lidocaine. Sensation was tested in three groups of subjects receiving local anesthetic digital blocks. Group A received bupivacaine 0.25% plain. Group B received a 1:1 mixture of lidocaine 1% plain and bupivacaine 0.25%. Group C received an initial block of lidocaine 1% plain sequentially followed by bupivacaine 0.25% 1h later. Bupivacaine exhibited a delayed onset and the longest duration when compared to the other two groups. The group receiving the 1:1 mixture showed a rapid onset that resembled that of lidocaine and a shortened duration that did not resemble bupivacaine. The group receiving the sequential injections showed that even after a 1h interval following the lidocaine infiltration, there was a deleterious effect on duration of action of the bupivacaine. Using bupivacaine as a post-surgical block in the presence of residual lidocaine from a preoperative block is not warranted as once again, the extended duration of bupivacaine is mitigated. Bupivacaine alone as an initial operative block affords clinically acceptable onset of anesthesia while also providing extended duration of action.

  8. [Local anesthesia in the children undergoing the fibroendoscopic study of the nasal cavity, nasopharynx, and larynx: are topical anesthetics needed?].

    PubMed

    Soldatsky, Yu L; Denisova, O A; Mazur, E M

    2015-01-01

    This prospective randomized study with double blind control was designed to evaluate the effectiveness of various anesthetic techniques employed prior to fibroendoscopy of the nose, nasopharynx, and larynx of the children. The study included 160 children at the age varying from 3 to 14 (mean 7.4±2.96) years randomly allocated to four statistically comparable groups matched for age and sex. The following preparations were used to treat the children prior to fibroendoscopy: physiological solution (group 1), a 0.05% xylometazoline solution (group 2), a 10% lidocaine solution (group 3), and a mixture of 0.05% xylometazoline and 10% lidocaine solutions (group 4). The evaluation of the tolerance to the pretreatment of the nasal cavity with lidocaine and lidocaine plus xylometazoline (groups 3 and 4) showed that it was significantly (p<0.05) worse than in groups 1 and 2. The subjective tolerance to fibroendoscopy as reported by the patients was on the average similar in the children of all four groups (p>0.05). The doctors found the tolerance of fibroendoscopy to be the worst following pretreatment with the physiological solution (group 1) and the best after pretreatment with a mixture of lidocaine and xylometazoline (group 4) (p=0.03). The children comprising groups 2 and 3 were not significantly different in terms of the tolerance to fibroendoscopy (p>0.05). It is concluded that the pretreatment of the nasal cavity of the children with a 10% lidocaine solution before fibroendoscopy has no advantage over the pretreatment with a 0.05% xylometazoline solution; at the same time, insuflation of lidocaine as an anesthetic induces more pronounced negative emotions compared with the application of 0.05% xylometazoline.

  9. Drug-coated microneedles for rapid and painless local anesthesia.

    PubMed

    Baek, Sung-Hyun; Shin, Ju-Hyung; Kim, Yeu-Chun

    2017-03-01

    This study showed that drug-coated PLLA (Poly (L-lactide)) microneedle arrays can induce rapid and painless local anesthesia. Microneedle arrays were fabricated using a micro-molding technique, and the needle tips were coated with 290.6 ± 45.9 μg of lidocaine, the most widely used local anesthetic worldwide. A dip-coating device was newly designed for the coating step using an optimized coating formulation. Lidocaine coated on the arrays was released rapidly into PBS within 2 min, and its stability in storage lasted 3 weeks at 4, 25, and 37°C. Furthermore, the microneedle arrays showed consistent in vitro skin penetration and delivered 200.8 ± 43.9, 224.2 ± 39.3, and 244.1 ± 19.6 μg of lidocaine into the skin 1, 2, and 5 min after application with a high delivery efficiency of 69, 77, and 84%. Compared to a commercially available topical anesthetic EMLA® cream, a 22.0, 13.6, and 14.0-fold higher amount of lidocaine was delivered into the skin. Note, in vitro skin permeation of Lidocaine was also notably enhanced by a 2-min-application of the lidocaine-coated microneedle arrays. Altogether, these results suggest that the biocompatible lidocaine-coated PLLA microneedle arrays could provide significantly rapid local anesthesia in a painless manner without any of the issues from topical applications or hypodermic injections of local anesthetics.

  10. Mechanisms of atrial fibrillation termination by rapidly unbinding Na+ channel blockers: insights from mathematical models and experimental correlates.

    PubMed

    Comtois, Philippe; Sakabe, Masao; Vigmond, Edward J; Munoz, Mauricio; Texier, Anne; Shiroshita-Takeshita, Akiko; Nattel, Stanley

    2008-10-01

    Atrial fibrillation (AF) is the most common sustained clinical arrhythmia and is a problem of growing proportions. Recent studies have increased interest in fast-unbinding Na(+) channel blockers like vernakalant (RSD1235) and ranolazine for AF therapy, but the mechanism of efficacy is poorly understood. To study how fast-unbinding I(Na) blockers affect AF, we developed realistic mathematical models of state-dependent Na(+) channel block, using a lidocaine model as a prototype, and studied the effects on simulated cholinergic AF in two- and three-dimensional atrial substrates. We then compared the results with in vivo effects of lidocaine on vagotonic AF in dogs. Lidocaine action was modeled with the Hondeghem-Katzung modulated-receptor theory and maximum affinity for activated Na(+) channels. Lidocaine produced frequency-dependent Na(+) channel blocking and conduction slowing effects and terminated AF in both two- and three-dimensional models with concentration-dependent efficacy (maximum approximately 89% at 60 microM). AF termination was not related to increases in wavelength, which tended to decrease with the drug, but rather to decreased source Na(+) current in the face of large ACh-sensitive K(+) current-related sinks, leading to the destabilization of primary generator rotors and a great reduction in wavebreak, which caused primary rotor annihilations in the absence of secondary rotors to resume generator activity. Lidocaine also reduced the variability and maximum values of the dominant frequency distribution during AF. Qualitatively similar results were obtained in vivo for lidocaine effects on vagal AF in dogs, with an efficacy of 86% at 2 mg/kg iv, as well as with simulations using the guarded-receptor model of lidocaine action. These results provide new insights into the mechanisms by which rapidly unbinding class I antiarrhythmic agents, a class including several novel compounds of considerable promise, terminate AF.

  11. Pain and efficacy of local anesthetics for central venous access

    PubMed Central

    Culp, William C; Yousaf, Mohammed; Lowry, Benjamin; McCowan, Timothy C; Culp, William C

    2008-01-01

    Purpose To compare pain during injection and efficacy of analgesia of local anesthetics during central venous line placement. Methods Sixty-two patients were studied in a randomized, double-blinded prospective fashion. Patients received 1% lidocaine (L), buffered 1% lidocaine (LB), or 2% chloroprocaine (CP) injected around the internal jugular vein for procedural analgesia for central venous access. Patients reported pain via a standard linear visual analog scale, with 0 representing no pain and 10 being the worst pain imaginable. Results Overall patient perception of pain was better with CP and L than LB with mean scores of CP 2.4, L 2.6, LB 4.2. Pain with injection mean scores were CP 2.1, L 2.5, LB 3.2. Pain with catheter placement scores were CP 2.5, L 1.7, LB 3.4. Operator assessment of overall pain values were CP 1.9, L 2.2, LB 3.4. LB consistently scored the worst, though compared with CP, this only reached statistical significance in overall patient pain and pain at catheter insertion compared with L. Conclusion Though chloroprocaine scored better than lidocaine in 3 of 4 parameters, this trend did not achieve statistical significance. Adding sodium bicarbonate to lidocaine isn’t justified in routine practice, nor is routine replacement of lidocaine with chloroprocaine. PMID:22915859

  12. Amygdala modulation of multiple memory systems: hippocampus and caudate-putamen.

    PubMed

    Packard, M G; Teather, L A

    1998-03-01

    A series of five experiments examined the differential mnemonic roles of the hippocampus and caudate-putamen and the modulatory influence of the amygdala on hippocampal and caudate-putamen memory processes. Findings indicate that (a) posttraining intrahippocampal injections of amphetamine selectively enhance memory in a hidden platform water maze task, (b) posttraining intracaudate injections of amphetamine selectively enhance memory in a visible platform water maze task, (c) posttraining intra-amygdala injections of amphetamine enhance memory in both water maze tasks, (d) preretention intrahippocampal lidocaine injections block expression of the memory enhancing effects of posttraining intrahippocampal amphetamine injections in the hidden platform task, (e) preretention intracaudate lidocaine injections block expression of the memory enhancing effects of posttraining intracaudate amphetamine injections in the visible platform task, (f) preretention intra-amygdala lidocaine injections do not block the memory enhancing effect of posttraining intra-amygdala amphetamine injections on either task, (g) in the hidden platform task, posttraining intrahippocampal, but not intracaudate, lidocaine injections block the memory enhancing effects of posttraining intra-amygdala amphetamine, (h) in the visible