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Sample records for local anesthetic concentration

  1. Methylparaben concentration in commercial Brazilian local anesthetics solutions

    PubMed Central

    da SILVA, Gustavo Henrique Rodriguez; BOTTOLI, Carla Beatriz Grespan; GROPPO, Francisco Carlos; VOLPATO, Maria Cristina; RANALI, José; RAMACCIATO, Juliana Cama; MOTTA, Rogério Heládio Lopes

    2012-01-01

    Objective To detect the presence and concentration of methylparaben in cartridges of commercial Brazilian local anesthetics. Material and methods Twelve commercial brands (4 in glass and 8 in plastic cartridges) of local anesthetic solutions for use in dentistry were purchased from the Brazilian market and analyzed. Different lots of the commercial brands were obtained in different Brazilian cities (Piracicaba, Campinas and São Paulo). Separation was performed using high performance liquid chromatography (HPLC) with UV-Vis detector. The mobile phase used was acetonitrile:water (75:25 - v/v), pH 4.5, adjusted with acetic acid at a flow rate of 1.0 ml.min-1. Results When detected in the solutions, the methylparaben concentration ranged from 0.01% (m/v) to 0.16% (m/v). One glass and all plastic cartridges presented methylparaben. Conclusion 1. Methylparaben concentration varied among solutions from different manufacturers, and it was not indicated in the drug package inserts; 2. Since the presence of methylparaben in dental anesthetics is not regulated by the Brazilian National Health Surveillance Agency (ANVISA) and this substance could cause allergic reactions, it is important to alert dentists about its possible presence. PMID:23032206

  2. The relationship between pH and concentrations of antioxidants and vasoconstrictors in local anesthetic solutions.

    PubMed Central

    Hondrum, S. O.; Ezell, J. H.

    1996-01-01

    pH affects the efficacy of local anesthetics by determining the percentage of the lipid-soluble base form of the anesthetic available for diffusion and penetration of the nerve sheath. The purpose of this study was to determine the relationship between pH and the concentrations of antioxidant and vasoconstrictor in dental local anesthetic solutions over real-time and after accelerated aging. Several batches of lidocaine and mepivacaine with vasoconstrictors were tested. Results showed that, immediately upon receipt from the manufacturers, three batches were below the USP pH limit (pH 3.3), and two batches contained less than the minimum limit of vasoconstrictors (90%). Real-time tests on batches that were within normal limits revealed that solutions were stable past 4 yr. Accelerated aging tests revealed a strong correlation between a decrease in pH and loss of antioxidants and vasoconstrictors. In conclusion, a quality batch of local anesthetic should remain efficacious long past the manufacturer's stated shelf life; a batch that is less than optimal, or one that is exposed to environmental stresses, will degrade rapidly, and efficacy may be affected by decreases in pH and loss of vasoconstrictor. pH may be an inexpensive, readily available screening test for efficacy of local anesthetics. PMID:10323112

  3. 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

  4. Continuous Femoral Nerve Blocks: Decreasing Local Anesthetic Concentration to Minimize Quadriceps Femoris Weakness

    PubMed Central

    Bauer, Maria; Wang, Lu; Onibonoje, Olusegun K.; Parrett, Chad; Sessler, Daniel I.; Mounir-Soliman, Loran; Zaky, Sherif; Krebs, Viktor; Buller, Leonard T.; Donohue, Michael C.; Stevens-Lapsley, Jennifer E.; Ilfeld, Brian M.

    2012-01-01

    Background Whether decreasing the local anesthetic concentration during a continuous femoral nerve block results in less quadriceps weakness remains unknown. Methods Preoperatively, bilateral femoral perineural catheters were inserted in patients undergoing bilateral knee arthroplasty (n = 36) at a single clinical center. Postoperatively, right-sided catheters were randomly assigned to receive perineural ropivacaine of either 0.1% (basal 12 mL/h; bolus 4 mL) or 0.4% (basal 3 mL/h; bolus 1 mL), with the left catheter receiving the alternative concentration/rate in an observer- and subject-masked fashion. The primary endpoint was the maximum voluntary isometric contraction of the quadriceps femoris muscles the morning of postoperative day 2. Equivalence of treatments would be concluded if the 95% confidence interval for the difference fell within the interval of −20% to 20%. Secondary endpoints included active knee extension, passive knee flexion, tolerance to cutaneous electrical current applied over the distal quadriceps tendon, dynamic pain scores, opioid requirements, and ropivacaine consumption. Results Quadriceps maximum voluntary isometric contraction for limbs receiving 0.1% ropivacaine was a mean (SD) of 13 (8) N·m, versus 12 (8) N·m for limbs receiving 0.4% [intra-subject difference of 3 (40) percentage points; 95% CI −10 to 17; p = 0.63]. Because the 95% confidence interval fell within prespecified tolerances, we conclude that the effect of the two concentrations were equivalent. Similarly, there were no statistically significant differences in secondary endpoints. Conclusions For continuous femoral nerve blocks, we found no evidence that local anesthetic concentration and volume influence block characteristics, suggesting that local anesthetic dose (mass) is the primary determinant of perineural infusion effects. PMID:22293719

  5. Local anesthetic update.

    PubMed Central

    MacKenzie, T. A.; Young, E. R.

    1993-01-01

    The development of new local anesthetics has not been an area of particularly active research for a number of years. However, as the use of regional anesthesia has expanded, additional anesthetic requirements and techniques have stimulated the search for newer drugs and ways of modifying existing ones. This article reviews some of the more recent developments in this field. PMID:8185087

  6. The effect of low concentrations versus high concentrations of local anesthetics for labour analgesia on obstetric and anesthetic outcomes: a meta-analysis.

    PubMed

    Sultan, Pervez; Murphy, Caitriona; Halpern, Stephen; Carvalho, Brendan

    2013-09-01

    The influence that different concentrations of labour epidural local anesthetic have on assisted vaginal delivery (AVD) and many obstetric outcomes and side effects is uncertain. The purpose of this meta-analysis was to determine whether local anesthetics utilized at low concentrations (LCs) during labour are associated with a decreased incidence of AVD when compared with high concentrations (HCs). We searched PubMed, Ovid EMBASE, Ovid MEDLINE, CINAHL, Scopus, clinicaltrials.gov, and Cochrane databases for randomized controlled trials of labouring patients that compared LCs (defined as ≤ 0.1% epidural bupivacaine or ≤ 0.17% ropivacaine) of epidural local anesthetic with HCs for maintenance of analgesia. The primary outcome was AVD and secondary outcomes included Cesarean delivery, duration of labour, analgesia, side effects (nausea and vomiting, motor block, hypotension, pruritus, and urinary retention), and neonatal outcomes. The odds ratios (OR) or weighted mean differences (WMD) and 95% confidence intervals (CI) were calculated using random effects modelling. An OR < 1 or a WMD < 0 favoured LCs. Eleven studies met our criteria (eight bupivacaine and three ropivacaine studies), providing 1,145 patients in the LCs group and 852 patients in the HCs group for analysis of the primary outcome. Low concentrations were associated with a reduction in the incidence of AVD (OR = 0.70; 95% CI 0.56 to 0.86; P < 0.001). There was no difference in the incidence of Cesarean delivery (OR 1.05; 95% CI 0.82 to 1.33; P = 0.7). The LCs group had less motor block (OR 3.9; 95% CI 1.59 to 9.55; P = 0.003), greater ambulation (OR 2.8; 95% CI 1.1 to 7.14; P = 0.03), less urinary retention (OR 0.42; 95% CI 0.23 to 0.73; P = 0.002), and a shorter second stage of labour (WMD -14.03; 95% CI -27.52 to -0.55; P = 0.04) compared with the HCs group. There were no differences between groups in pain scores, maternal nausea and vomiting, hypotension, fetal heart rate abnormalities, five

  7. 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

  8. Local anesthetics induce human renal cell apoptosis.

    PubMed

    Lee, H Thomas; Xu, Hua; Siegel, Cory D; Krichevsky, Igor E

    2003-01-01

    Renal cell apoptosis contributes significantly to the pathogenesis of acute renal failure. Local anesthetics induce apoptosis in neuronal and lymphocytic cell lines. We examined the effects of chronic (48 h) local anesthetic treatment (lidocaine, bupivacaine and tetracaine) on human proximal tubular (HK-2) cells. Apoptosis induction was assessed by detecting poly(ADP)-ribose polymerase fragmentation, caspase activation, terminal deoxynucleotidyl transferase biotin-dUTP nick end labeling (TUNEL) staining, DNA laddering and by cellular morphology. Cell death was quantified by measuring neutral red dye uptake and lactate dehydrogenase released into the cell culture medium. All 3 local anesthetics caused concentration-dependent cell death, induced HK-2 cell apoptosis and potentiated TNF-alpha induced apoptosis. Local anesthetics induced HK-2 cell apoptosis by activation of caspases 3, 6, 7, 8 and 9. ZVAD-fmk, a pan-caspase inhibitor, blocked the local anesthetic induced HK-2 cell apoptosis. Local anesthetics also inhibited the activities of anti-apoptotic kinases protein kinase B (Akt) and extracellular signal regulated mitrogen-activated protein kinase. Local anesthetic's pro-apoptotic effects are independent of sodium channel inhibition as tetrodotoxin, a selective voltage-gated sodium channel blocker, failed to mimic local anesthetic-mediated induction or potentiation of HK-2 cell apoptosis. We conclude that local anesthetics induce human renal cell apoptotic signaling by caspase activation and via inhibition of pro-survival signaling pathways.

  9. Local anesthetics: pharmacology and toxicity.

    PubMed

    Moore, Paul A; Hersh, Elliot V

    2010-10-01

    The development of safe and effective local anesthetic agents has possibly been the most important advancement in dental science to occur in the last century. The agents currently available in dentistry are extremely safe and fulfill most of the characteristics of an ideal local anesthetic. These local anesthetic agents can be administered with minimal tissue irritation and with little likelihood of inducing allergic reactions. A variety of agents are available that provide rapid onset and adequate duration of surgical anesthesia. This introductory article provides a brief update of the clinical pharmacology of local anesthetic agents and formulations used in dentistry at present. Copyright © 2010 Elsevier Inc. All rights reserved.

  10. Local Anesthetic-Induced Neurotoxicity

    PubMed Central

    Verlinde, Mark; Hollmann, Markus W.; Stevens, Markus F.; Hermanns, Henning; Werdehausen, Robert; Lirk, Philipp

    2016-01-01

    This review summarizes current knowledge concerning incidence, risk factors, and mechanisms of perioperative nerve injury, with focus on local anesthetic-induced neurotoxicity. Perioperative nerve injury is a complex phenomenon and can be caused by a number of clinical factors. Anesthetic risk factors for perioperative nerve injury include regional block technique, patient risk factors, and local anesthetic-induced neurotoxicity. Surgery can lead to nerve damage by use of tourniquets or by direct mechanical stress on nerves, such as traction, transection, compression, contusion, ischemia, and stretching. Current literature suggests that the majority of perioperative nerve injuries are unrelated to regional anesthesia. Besides the blockade of sodium channels which is responsible for the anesthetic effect, systemic local anesthetics can have a positive influence on the inflammatory response and the hemostatic system in the perioperative period. However, next to these beneficial effects, local anesthetics exhibit time and dose-dependent toxicity to a variety of tissues, including nerves. There is equivocal experimental evidence that the toxicity varies among local anesthetics. Even though the precise order of events during local anesthetic-induced neurotoxicity is not clear, possible cellular mechanisms have been identified. These include the intrinsic caspase-pathway, PI3K-pathway, and MAPK-pathways. Further research will need to determine whether these pathways are non-specifically activated by local anesthetics, or whether there is a single common precipitating factor. PMID:26959012

  11. [Transdermal Local Anesthetics].

    PubMed

    Hanaoka, Kazuo; Arita, Hideko; Nagase, Masaki; Suzuki, Takashi; Ogawa, Sestsuro

    2015-11-01

    Taking EMLA cream and Penles tape 18 mg as examples, this article describes the conditions for skin penetration of topical anesthetics, with their onset time of action, duration of effect and a precautions for their use. EMLA cream is a unique cream for topical anesthesia which is the eutectic mixture of lidocaine and propitocaine to increase skin penetration. The safety study demonstrated that blood concentrations of active ingredients of EMLA cream were below toxic levels. EMLA cream, with confirmed high skin penetrability and safety, should be used for pain reduction of various treatments for many diseases. Here in Japan, EMLA cream has indications not only for pain reduction of skin laser therapy but also for reduction of needle puncture pain. This means the use of topical anesthesia would be expanded to wider ranges of treatments.

  12. Allergy to local anesthetics: Reality or myth?

    PubMed

    Malinovsky, Jean-Marc; Chiriac, Anca M; Tacquard, Charles; Mertes, Paul Michel; Demoly, Pascal

    2016-09-01

    The incidence of allergic reactions to local anesthetics is low. Most cases involve a psychogenic reaction rather than an allergic reaction. Additives and preservatives added to local anesthetics may cause allergic reactions. Vascular resorption of epinephrine-containing local anesthetics may produce cardiovascular signs similar to an allergic reaction. Diagnosis of allergy to local anesthetics must be established by skin testing and provocative challenge.

  13. Choices of local anesthetics for ocular surgery.

    PubMed

    Cass, Gary D

    2006-06-01

    This article will help clinicians to be aware of their choices of local anesthetic solutions before they make their ocular anesthetic plan based on the specific requirements of the patient, the surgical procedure, and the properties of the local anesthetic. Choices of local anesthetic solutions and additives for both topical anesthesia and conduction blockade are discussed.

  14. 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

  15. Clinical Concentrations of Local Anesthetics Bupivacaine and Lidocaine Differentially Inhibit Human Kir2.x Inward Rectifier K+ Channels.

    PubMed

    Nakahira, Kei; Oshita, Kensuke; Itoh, Masayuki; Takano, Makoto; Sakaguchi, Yoshiro; Ishihara, Keiko

    2016-04-01

    Inward rectifier K channels of the Kir2.x subfamily are widely expressed in neuronal tissues, controlling neuronal excitability. Previous studies reported that local anesthetics (LAs) do not affect Kir2 channels. However, the effects have not been studied at large concentrations used in regional anesthesia. This study used the patch-clamp technique to examine the effects of bupivacaine and lidocaine on Kir2.1, Kir2.2, and Kir2.3 channels expressed in human embryonic kidney 293 cells. When applied extracellularly in whole-cell recordings, both LAs inhibited Kir2.x currents in a voltage-independent manner. Inhibition with bupivacaine was slow and irreversible, whereas that with lidocaine was fast and reversible. Kir2.3 displayed a greater sensitivity to bupivacaine than Kir2.1 and Kir2.2 (50% inhibitory concentrations at approximately 5 minutes, 0.6 vs 8-10 mM), whereas their sensitivities to lidocaine were similar (50% inhibitory concentrations, 1.5-2.7 mM). Increases in the charged/neutral ratio of the LAs at an acidic extracellular pH attenuated their inhibitory effects, and a permanently charged lidocaine derivative QX-314 exhibited no effects when applied extracellularly. Inside-out experiments demonstrated that inhibition of Kir2.1 with cytoplasmic lidocaine and QX-314 was rapid and reversible, whereas that induced by bupivacaine was slow and irreversible. Furthermore, dose-inhibition relations for the charged form of bupivacaine and lidocaine obtained at different cytoplasmic pHs could be approximated by a single relation for each LA. The results indicate that both LAs at clinical concentrations equilibrated rapidly with the intracellular milieu, differentially inhibiting Kir2.x channel function from the cytoplasmic side.

  16. Local anesthetics adsorbed onto infusion balloon.

    PubMed

    Mizogami, Maki; Tsuchiya, Hironori; Takakura, Ko

    2004-09-01

    We compared the adsorption of different local anesthetics onto infusion balloons and studied one of the possible mechanisms for adsorption. After injection of lidocaine, bupivacaine, ropivacaine, and mepivacaine solutions (1 mM each; pH 7.4) into balloons of 100-mL volume, their concentrations in effluents flowing out at 4 mL/h were determined over time by high-performance liquid chromatography. All were adsorbed in a structure-dependent manner, and the concentration decreased by 6%-14% within 5 min. Bupivacaine was most strongly adsorbed, followed by lidocaine, ropivacaine, and mepivacaine. QX-314, a quaternary ammonium derivative of lidocaine, was only weakly adsorbed compared with the parent compound lidocaine. The extent of adsorption of local anesthetics was related to their hydrophobicity (evaluated by reversed-phase chromatography) and was much more at pH 7.4 than at pH 6.0. A hydrophobic interaction with balloon materials appears to be responsible for the adsorption of local anesthetics. When infusion balloons are used for the continuous administration of local anesthetics, attention should be paid to the possibility that their actual concentrations in effluents are smaller than those present when they are initially prepared.

  17. Dentistry's wonder drugs: local anesthetics and vasoconstrictors.

    PubMed

    Wahl, Michael J; Brown, Ronald S

    2010-01-01

    This article reviews recent developments concerning local anesthetics, including the amount of pain resulting from injection, which drugs achieve anesthesia most effectively, proper dosing for anesthetizing children and adults, the maximum recommended doses of lidocaine 2% with epinephrine for cardiac patients, and which drugs can be used for patients taking monoamine oxidase (MAO) inhibitors, tricyclic antidepressants, or nonselective beta blockers. Dentists should be familiar with all aspects of local anesthetics, especially anesthetic toxicity and maximum recommended doses.

  18. Strabismus complications from local anesthetics.

    PubMed

    Guyton, David L

    2008-01-01

    Strabismus developing after retrobulbar or peribulbar anesthesia for both anterior and posterior segment eye surgery may be due to myotoxicity to an extraocular muscle from the local anesthetic agent. Initial paresis often causes diplopia immediately after surgery, but later progressive segmental fibrosis occurs, and/or hypertrophy of the muscle, producing diplopia in the opposite direction from the direction of the initial diplopia. The inferior rectus muscle is most commonly affected. Usually a large recession on an adjustable suture of the involved muscle(s) yields good alignment. Using topical anesthesia or sub-Tenon's anesthesia can avoid this complication.

  19. Local anesthetics for facial plastic procedures.

    PubMed

    Ahlstrom, Karen K; Frodel, John L

    2002-02-01

    The use of local anesthetic in facial plastic surgical procedures is well established as an effective and safe mode of anesthesia delivery. Local infiltration of anesthesia may be used alone for minor surgical procedures, or it may be used with general anesthesia or intravenous sedation and analgesia for more complex, lengthy procedures. When considered independently, the use of local anesthetic agents has undeniable limitations. Local anesthetics can cause toxicity and side effects. Injection of local anesthetics for subcutaneous infiltration frequently is painful until sensory anesthesia occurs. Local anesthetics have limited efficacy with respect to the intensity and duration of sensory blockade that can be achieved. In some situations, use of local anesthesia with the maintenance of an awake patient also may be undesirable for the surgeon and impractical for the patient. Despite these shortcomings, local anesthetics are fundamentally ideal for use in facial plastic surgery.

  20. Selection factors for local anesthetic agents.

    PubMed

    Budenz, Alan W

    2008-10-01

    The decision to inject local anesthetic agents to achieve profound anesthesia is dependent upon many factors, particularly the depth and duration of anesthesia required, and the possible need for hemostasis. To maximize the safety of local anesthetic injections, it is necessary to weigh the risks against the benefits for each patient, for each anesthetic agent, for use of a vasoconstrictor, and for the delivery technique for the selected agent.

  1. Managing patients with local anesthetic complications using alternative methods.

    PubMed

    Lu, Dominic P

    2002-01-01

    This article discusses various alternative methods of treating the patient who encounters problems with local anesthetics. Those alternative methods include: acupuncture, hypnosis, sedation, general anesthesia, and antihistamines as a substitute for local anesthetics with more of a focus in using antihistamines as an effective local anesthetic agent. Although not frequently encountered in the clinical setting, allergic reactions to local anesthetics do occur. Various surveys indicate the number of deaths attributed to local anesthesia range from 1:1,500,000 to 1:4,000,000, with oral surgery offices having higher mortality rates than general dentistry offices. This occurs despite clinicians' attention to patient medical histories, aspiration of the local anesthetic syringe during injections, and minimizing the dosage of local anesthetic solutions. Generally speaking, local anesthetics can be divided into two groups: ester of benzoic and aminobenzoic derivatives (cocaine, benzocaine, procaine, tetracaine, butacaine, etc.) or amide-derivatives of xylidine and toluidine groups (lidocaine, mepivacaine, prilocaine a.k.a. Citanest, etc.). Adverse effects include allergic or toxic reactions, as well as negative effects of any vasoconstrictors contained within the local anesthetic solution. This article will concentrate on how to successfully manage patients who have previously encountered allergic reactions.

  2. Lipid Emulsion for Local Anesthetic Systemic Toxicity

    PubMed Central

    Ciechanowicz, Sarah; Patil, Vinod

    2012-01-01

    The accidental overdose of local anesthetics may prove fatal. The commonly used amide local anesthetics have varying adverse effects on the myocardium, and beyond a certain dose all are capable of causing death. Local anesthetics are the most frequently used drugs amongst anesthetists and although uncommon, local anaesthetic systemic toxicity accounts for a high proportion of mortality, with local anaesthetic-induced cardiac arrest particularly resistant to standard resuscitation methods. Over the last decade, there has been convincing evidence of intravenous lipid emulsions as a rescue in local anesthetic-cardiotoxicity, and anesthetic organisations, over the globe have developed guidelines on the use of this drug. Despite this, awareness amongst practitioners appears to be lacking. All who use local anesthetics in their practice should have an appreciation of patients at high risk of toxicity, early symptoms and signs of toxicity, preventative measures when using local anesthetics, and the initial management of systemic toxicity with intravenous lipid emulsion. In this paper we intend to discuss the pharmacology and pathophysiology of local anesthetics and toxicity, and the rationale for lipid emulsion therapy. PMID:21969824

  3. Local Anesthetics: A Century of Progress

    PubMed Central

    Yagiela, John A.

    1985-01-01

    One century after the clinical introduction of cocaine, local anesthesia remains the most important method of pain control in dentistry. Many local anesthetics have been marketed since 1884, and it is likely that attempts to produce drugs that enhance anesthetic efficacy, reduce systemic and local toxicity, and increase nociceptive selectivity, will continue. In addition, new methods of drug administration have been and will be developed to achieve these goals. Of fundamental importance to such improvements are investigations into the pharmacology of drugs with local anesthetic activity and anatomical and physiologic studies pertaining to the reasons why local anesthetics sometimes fail to achieve desired results. This paper reviews recent advances in our understanding of these drugs and their clinical use. ImagesFig. 1 PMID:2408504

  4. Effect of Local and General Anesthetics on Interfacial Water

    PubMed Central

    2016-01-01

    Background Water undergoes structural change as it interfaces with hydrophilic surfaces, including the many hydrophilic surfaces within the cell. This interfacial water has become known as “Exclusion Zone (EZ) water” or “fourth-phase water” [1]. Methods We tested the hypothesis that anesthetics diminish the amount of EZ water, and that this change may correlate with functional changes in anesthesia. By using the local anesthetics Lidocaine and Bupivacaine as well as a general inhalational anesthetic, Isoflurane, we tracked the EZ size as these anesthetics were introduced. Results All three anesthetics diminished EZ size in a concentration-dependent manner at concentrations of 0.18 mM and greater for Bupivacaine, 0.85 mM and greater for Lidocaine, and 0.2% for Isoflurane. At extremely low (micromolar) concentrations, however, all three anesthetics increased EZ size. Conclusions The sharp increase of EZ size associated with micromolar anesthetic concentrations follows a similar pattern to induction of general anesthesia, from the excitation stage (Stage II) to the depression and overdose stages of surgical anesthesia (Stages III and IV). The results are consistent with the hypothesis that anesthetics may act on water, a fundamental organizational component common to all cells. PMID:27054588

  5. Local anesthetics: dentistry's most important drugs.

    PubMed

    Malamed, S F

    1994-12-01

    One hundred and fifty years ago, Horace Wells opened the door to local anesthetics. Since then, many advances have been made in pain control. The development of dentistry's most important drugs is highlighted here.

  6. An update on local anesthetics in dentistry.

    PubMed

    Haas, Daniel A

    2002-10-01

    Local anesthetics are the most commonly used drugs in dentistry. This article provides a brief update on the pharmacology, adverse effects and clinical applications of these drugs, as well as the role of vasoconstrictors.

  7. Diphenhydramine as an Alternative Local Anesthetic Agent

    PubMed Central

    Pavlidakey, Peter G.; Brodell, Erin E.

    2009-01-01

    Patients who present with a history of “allergy” to local anesthetics are common in clinical practice. Injectable 1% diphenhydramine is a safe, inexpensive, and effective local anesthetic for simple dermatological procedures in patients who report “caine” allergies. Utilizing this agent permits the dermatologist to operate at the time of the initial visit and schedule a referral to the allergist for definitive sensitivity testing at the patient’s convenience. PMID:20725573

  8. Local Anesthetics: Review of Pharmacological Considerations

    PubMed Central

    Becker, Daniel E; Reed, Kenneth L

    2012-01-01

    Local anesthetics have an impressive history of efficacy and safety in medical and dental practice. Their use is so routine, and adverse effects are so infrequent, that providers may understandably overlook many of their pharmacotherapeutic principles. The purpose of this continuing education article is to provide a review and update of essential pharmacology for the various local anesthetic formulations in current use. Technical considerations will be addressed in a subsequent article. PMID:22822998

  9. SYSTEMIC TOXIC REACTIONS TO LOCAL ANESTHETICS

    PubMed Central

    Moore, Daniel C.; Green, John

    1956-01-01

    The topical use of anesthetic agents involves an element of risk. Systemic toxic reactions are rare, but they do occur and may result in death. When a reaction occurs from a topical application, it usually progresses rapidly to respiratory and cardiovascular collapse, and thus therapy must be instituted with more haste to avoid deaths. Fatal systemic toxic reactions from topically administered anesthetic drugs are, in effect, usually not due to well informed use of the drug but to misuse owing to less than complete understanding of absorption. Emphasis is placed on the causes, prophylaxis and treatment of severe systemic toxic reactions which follow the topical application of local anesthetic drugs. If systemic toxic reactions resulting from a safe dose of a local anesthetic agent are correctly treated, there will usually follow an uneventful recovery rather than a catastrophe. PMID:13343009

  10. Knowledge about local anesthetics in odontology students.

    PubMed

    Guzmán Alvarez, Rodrigo; Campos Sepúlveda, Alfonso Efraín; Martínez González, Adrian Alejandro

    2009-01-01

    The purpose of the study was to identify the level of knowledge of local anesthetics frequently used in the surgical clinic by third and fourth year dental students in daily practice. The importance of pharmacology in dental practice in underscored by potential drug toxicity. The study was performed with 244 third and fourth grade career dental students (CDS). Eleven items regarding the knowledge over local anesthetics at the clinic; i.e., the appropriate doses, possible toxic effects and side effects were examined. The reference questionnaire which is in a validation process, is a way to evaluate student knowledge about most drugs used in odontology practice such as: NSAIDs, antibiotics and local anesthetics. The results were found to be unsatisfactory with a high percentage of students failing (less than six of eleven items correct). We conclude that determination of practice knowledge is an essential step in informing the institution about cognitive deficiencies identified in order to plan learning solutions.

  11. Buffered local anesthetics and epinephrine degradation.

    PubMed

    Murakami, C S; Odland, P B; Ross, B K

    1994-03-01

    Lidocaine with epinephrine is currently the most common local anesthetic agent used for facial soft tissue surgery. This combination is generally safe and effective in providing complete anesthesia and adequate hemostasis. Because epinephrine is unstable at physiologic pH, the commercial preparation is formulated with a low pH (3.5-5.5). Unfortunately, this acidic pH causes significant pain during infiltration. To reduce pain, clinicians sometimes buffer acidic local anesthetic agents with sodium bicarbonate. However, little is known about the stability of epinephrine when the pH of epinephrine is clinically altered. Using high pressure liquid chromatography (HPLC), epinephrine levels were measured after the addition of sodium bicarbonate. Our results indicate a significant amount of epinephrine degradation occurs in some of these specimens. Recommendations regarding the use of buffered local anesthetic agents are made.

  12. Long-acting local anesthetics in dentistry.

    PubMed Central

    Sisk, A. L.

    1992-01-01

    Long-acting local anesthetics have proved to be effective for the suppression of both intraoperative and postoperative pain. They are useful for lengthy dental treatments and for prevention of severe pain following many types of surgical procedures. Although the currently available long-acting local anesthetics for dentistry have minimal side effects in the doses usually employed, there are potential problems. Bupivacaine, for example, can cause significant cardiac depressant and dysrhythmogenic responses. Etidocaine has less pronounced effects on the cardiovascular system, but its use may be associated with inadequate control of intraoperative bleeding. A new long-acting local anesthetic, ropivacaine, appears to offer advantages over either of the currently used long-acting agents. PMID:1308373

  13. Long-acting local anesthetics in dentistry.

    PubMed

    Sisk, A L

    1992-01-01

    Long-acting local anesthetics have proved to be effective for the suppression of both intraoperative and postoperative pain. They are useful for lengthy dental treatments and for prevention of severe pain following many types of surgical procedures. Although the currently available long-acting local anesthetics for dentistry have minimal side effects in the doses usually employed, there are potential problems. Bupivacaine, for example, can cause significant cardiac depressant and dysrhythmogenic responses. Etidocaine has less pronounced effects on the cardiovascular system, but its use may be associated with inadequate control of intraoperative bleeding. A new long-acting local anesthetic, ropivacaine, appears to offer advantages over either of the currently used long-acting agents.

  14. Effects of Epidural Labor Analgesia With Low Concentrations of Local Anesthetics on Obstetric Outcomes: A Systematic Review and Meta-analysis of Randomized Controlled Trials.

    PubMed

    Wang, Ting-Ting; Sun, Shen; Huang, Shao-Qiang

    2017-05-01

    Low concentrations of local anesthetics (LCLAs) are increasingly popular for epidural labor analgesia. The effects of epidural analgesia with low concentrations of anesthetics on the duration of the second stage of labor and the instrumental birth rate, however, remain controversial. A systematic review was conducted to compare the effects of epidural analgesia with LCLAs with those of nonepidural analgesia on obstetric outcomes. The databases of PubMed, Embase, and the Cochrane controlled trials register were independently searched by 2 researchers, and randomized controlled trials that compared epidural labor analgesia utilizing LCLAs with nonepidural analgesia were retrieved. The primary outcomes were the duration of the second stage of labor and the instrumental birth rate; secondary outcomes included the cesarean delivery rate, the spontaneous vaginal delivery rate, and the duration of the first stage of labor. Ten studies (1809 women) were included. There was no significant difference between groups in the duration of the second stage of labor (mean difference = 5.71 minutes, 95% confidence interval [CI], -6.14 to 17.83; P = .36) or the instrumental birth rate (risk ratio [RR] = 1.52, 95% CI, 0.97-2.4; P = .07). There was no significant difference between groups in the cesarean delivery rate (RR = 0.8, 95% CI, 0.6-1.05; P = .11), the spontaneous vaginal delivery rate (RR = 0.98, 95% CI, 0.91-1.06; P = .62), or the duration of the first stage of labor (mean difference = 17.34 minutes, 95% CI, -5.89 to 40.56; P = .14). Compared with nonepidural analgesia, epidural analgesia with LCLAs is not associated with a prolonged duration of the second stage of labor or an increased instrumental birth rate. The results of this meta-analysis are based on small trials of low quality. These conclusions require confirmation by large-sample and high-quality trials in the future.

  15. Effect of local anesthetics on serotonin1A receptor function.

    PubMed

    Rao, Bhagyashree D; Shrivastava, Sandeep; Chattopadhyay, Amitabha

    2016-12-01

    The fundamental mechanism behind the action of local anesthetics is still not clearly understood. Phenylethanol (PEtOH) is a constituent of essential oils with a pleasant odor and can act as a local anesthetic. In this work, we have explored the effect of PEtOH on the function of the hippocampal serotonin1A receptor, a representative neurotransmitter receptor belonging to the G protein-coupled receptor (GPCR) family. Our results show that PEtOH induces reduction in ligand binding to the serotonin1A receptor due to lowering of binding affinity, along with a concomitant decrease in the degree of G-protein coupling. Analysis of membrane order using the environment-sensitive fluorescent probe DPH revealed decrease in membrane order with increasing PEtOH concentration, as evident from reduction in rotational correlation time of the probe. Analysis of results obtained shows that the action of local anesthetics could be attributed to the combined effects of specific interaction of the receptor with anesthetics and alteration of membrane properties (such as membrane order). These results assume relevance in the perspective of anesthetic action and could be helpful to achieve a better understanding of the possible role of anesthetics in the function of membrane receptors.

  16. [The use of vasoconstrictor agents in low concentration as additives to local anesthetics in ambulatory maxillofacial interventions].

    PubMed

    Pässler, L; Benkert, P

    1979-01-01

    The authors studied in several test series the suitability of adrenaline and noradrenaline as vasoconstrictor additives to 2% Xylocitin, in a concentration of 1:100,000. At this concentration, noradrenaline proved well suited in tooth extractions. The vasoconstrictor effect of adrenaline is sufficient in all maxillofacial interventions on an outpatient basis.

  17. [Effect of physiologic concentrations of local anesthetics of the procaine series on the structural and functional state of cerebral synaptosome membranes].

    PubMed

    Aksentsev, S L; Okun', I M; Rakovich, A A; Miliutin, A A; Konev, S V

    1978-01-01

    Studies are presented of the effect of procaine group anesthetics on rat brain synaptosome stability to dodecyl sulfate and on catalytic properties of the membrane bound alkaline phosphatase. The dose curves of detergent stability are characterized by two maxima, one at 3.10(-4) M for tetracaine, 2.10(-6) M for lidocaine and 5.10(-5) M for procaine; the other being at 10(-3) M for all anesthetics. The curves of Vmax and KM versus procaine concentration to exhibit the minimum at 5.10(-7) M and maximum at 3,2.10(-6) M. Procaine at 5.10(-7) M increases enthalpy and enthropy of membraneous alkaline phosphatase. It is suggested that interactions between anesthetics and centers of high affinity lead to synaptosome structural rearrangements, which affect the properties of membraneous enzymes.

  18. Serum Ropivacaine Concentrations and Systemic Local Anesthetic Toxicity in Trauma Patients Receiving Long-Term Continuous Peripheral Nerve Block Catheters

    DTIC Science & Technology

    2010-02-01

    concentrations were calculated from the following 2 methods: 1. Using peak area ratio of ropivacaine/ bupivacaine of samples versus peak area ratio of...ropivacaine/ bupivacaine of standards (0–3000 ng/mL) using the following formula: RopS (PA of Rop)/(PA of Bup)S /(PA of Rop)/(PA of Bup)STD Bup...1/mL serum used) where Rop ropivacaine, Bup bupivacaine , PA peak area, S sample, and STD standard. 2. Samples of ropivacaine concentrations

  19. Age, minimum alveolar anesthetic concentration, and minimum alveolar anesthetic concentration-awake.

    PubMed

    Eger, E I

    2001-10-01

    Two defining effects of inhaled anesthetics (immobility in the face of noxious stimulation, and absence of memory) correlate with the end-tidal concentrations of the anesthetics. Such defining effects are characterized as MAC (the concentration producing immobility in 50% of patients subjected to a noxious stimulus) and MAC-Awake (the concentration suppressing appropriate response to command in 50% of patients; memory is usually lost at MAC-Awake). If the concentrations are monitored and corrected for the effects of age and temperature, the concentrations may be displayed as multiples of MAC for a standard age, usually 40 yr. This article provides an algorithm that might be used to produce such a display, including provision of an estimate of the effect of nitrous oxide. Two defining effects of inhaled anesthetics (immobility in the face of noxious stimulation, and absence of memory) correlate with the end-tidal concentrations of the anesthetics. Thus, these defining effects may be monitored and the results displayed if the concentrations are known and corrected for the effects of age and temperature.

  20. Effect of local anesthetic concentration, dose and volume on the duration of single-injection ultrasound-guided axillary brachial plexus block with mepivacaine: a randomized controlled trial.

    PubMed

    Fenten, Maaike G E; Schoenmakers, Karin P W; Heesterbeek, Petra J C; Scheffer, Gert Jan; Stienstra, Rudolf

    2015-09-30

    In what way volume, concentration and dose affect block duration is controversial. The purpose of the present study is to investigate the effect of dose, volume and concentration of mepivacaine on the duration of sensory and motor blockade in ultrasound-guided single shot axillary brachial plexus blockade. In this parallel group randomized trial conducted in the Sint Maartenskliniek Nijmegen, 45 adult patients undergoing minor orthopaedic forearm, wrist or hand surgery were randomized to 3 groups. Group A: 20 mL mepivacaine 1.5 %, Group B: 30 mL mepivacaine 1 % and Group C: 30 mL mepivacaine 1.5 %. Randomization was computer-generated, with allocation concealment by opaque sequentially numbered sealed envelopes. Patients and observers were blinded to group allocation. duration of sensory block. Forty-five patients were randomized, four patients were excluded and replaced, and 15 patients in each group were included in the analysis. Mean (95 % CI) sensory and motor block duration was 256 (230-282) and 254 (226-282) minutes in Group A, 226 (209-243) and 220 (200-240) minutes in Group B and 270 (249-291) and 264 (244-284) minutes in Group C. Duration of sensory and motor block duration differed significantly between groups (p = 0.012 and p = 0.016 respectively). Post-hoc analysis showed a significantly reduced sensory and motor block duration in Group B when compared to Group C of 44 min. No local anesthetic systemic toxicity was reported. When using mepivacaine for axillary brachial plexus block, a higher dose and concentration was associated with a longer duration of sensory and motor blockade, but not a higher volume. The Netherlands National Trial Register NTR3648 . Registered October 3, 2012.

  1. Crystallization of Local Anesthetics When Mixed With Corticosteroid Solutions

    PubMed Central

    Hwang, Hyeoncheol; Park, Jihong; Lee, Won Kyung; Lee, Woo Hyung; Leigh, Ja-Ho; Lee, Jin Joo; Chung, Sun G.; Lim, Chaiyoung; Park, Sang Jun

    2016-01-01

    Objective To evaluate at which pH level various local anesthetics precipitate, and to confirm which combination of corticosteroid and local anesthetic crystallizes. Methods Each of ropivacaine-HCl, bupivacaine-HCl, and lidocaine-HCl was mixed with 4 different concentrations of NaOH solutions. Also, each of the three local anesthetics was mixed with the same volume of 3 corticosteroid solutions (triamcinolone acetonide, dexamethasone sodium phosphate, and betamethasone sodium phosphate). Precipitation of the local anesthetics (or not) was observed, by the naked eye and by microscope. The pH of each solution and the size of the precipitated crystal were measured. Results Alkalinized with NaOH to a certain value of pH, local anesthetics precipitated (ropivacaine pH 6.9, bupivacaine pH 7.7, and lidocaine pH 12.9). Precipitation was observed as a cloudy appearance by the naked eye and as the aggregation of small particles (<10 µm) by microscope. The amount of particles and aggregation increased with increased pH. Mixed with betamethasone sodium phosphate, ropivacaine was precipitated in the form of numerous large crystals (>300 µm, pH 7.5). Ropivacaine with dexamethasone sodium phosphate also precipitated, but it was only observable by microscope (a few crystals of 10–100 µm, pH 7.0). Bupivacaine with betamethasone sodium phosphate formed precipitates of non-aggregated smaller particles (<10 µm, pH 7.7). Lidocaine mixed with corticosteroids did not precipitate. Conclusion Ropivacaine and bupivacaine can precipitate by alkalinization at a physiological pH, and therefore also produce crystals at a physiological pH when they are mixed with betamethasone sodium phosphate. Thus, the potential risk should be noted for their use in interventions, such as epidural steroid injections. PMID:26949665

  2. Enhanced local anesthetic action of mepivacaine from the bioadhesive gels.

    PubMed

    Cho, Cheong-Weon; Choi, Jun-Shik; Shin, Sang-Chul

    2011-01-01

    Mepivacaine, an amide-type local anesthetic, has been used to relieve local pain. Among the many drug delivery systems, transdermal drug delivery has some advantages, as it provides controlled drug delivery for an extended period of time. To develop new gel formulations that have suitable bioadhesion, the bioadhesive force of hydroxypropyl methylcellulose (HPMC) was assessed using an auto-peeling tester. The effect of drug concentration on drug release from 2% HPMC gel was studied using synthetic cellulose membrane at 37±0.5°C. The drug concentrations tested were 0.5, 1, 1.5, 2, and 2.5%. The effect of temperature on drug release from the 2% drug gel was evaluated at 27, 32, 37 and 42°C. To increase the skin permeation of mepivacaine from HPMC gel, enhancers such as saturated and unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants were incorporated into the mepivacaine-HPMC gels. The enhancing effect of the enhancer on drug permeation was then examined in the modified Keshary-Chien cell. For the efficacy study, the anesthetic action of the formulated mepivacaine gel containing enhancer and vasoconstrictor was evaluated with the tail-flick analgesimeter. Among the various kinds of HPMC, HPMC-K100M gel showed the highest viscosity and bioadhesive force. As the viscosity of the HPMC gels increased, the bioadhesive forces increased. Increasing the drug concentration or temperature increased the drug release rate. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancement of permeation. Based on the area under the efficacy curve of the rat tail flick test curve, mepivacaine gel containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed prolonged and increased local anesthetic action compared to the control. For bioadhesive mepivacaine gels with enhanced local anesthetic action, mepivacaine gels containing penetration enhancer and vasoconstrictor could be developed with the

  3. Membrane interactivity of charged local anesthetic derivative and stereoselectivity in membrane interaction of local anesthetic enantiomers

    PubMed Central

    Tsuchiya, Hironori; Mizogami, Maki

    2008-01-01

    With respect to the membrane lipid theory as a molecular mechanism for local anesthetics, two critical subjects, the negligible effects of charged drugs when applied extracellularly and the stereoselective effects of enantiomers, were verified by paying particular attention to membrane components, phospholipids with the anionic property, and cholesterol with several chiral carbons. The membrane interactivities of structurally-different anesthetics were determined by their induced fluidity changes of liposomal membranes. Lidocaine (3.0 μmol/mL) fluidized phosphatidylcholine membranes, but not its quaternary derivative QX-314 (3.0 μmol/mL). Similarly to the mother molecule lidocaine, however, QX-314 fluidized phosphatidylserine-containing nerve cell model membranes and acidic phospholipids-constituting membranes depending on the acidity of membrane lipids. Positively charged local anesthetics are able to act on lipid bilayers by ion-pairing with anionic (acidic) phospholipids. Bupivacaine (0.75 mol/mL) and ropivacaine (0.75 and 1.0 μmol/mL) fluidized nerve cell model membranes with the potency being S(−)-enantiomer < racemate < R(+)-enantiomer (P < 0.01, vs antipode and racemate) and cardiac cell model membranes with the potency being S(−)-ropivacaine < S(−)-bupivacaine < R(+)-bupivacaine (P < 0.01). However, their membrane effects were not different when removing cholesterol from the model membranes. Stereoselectivity is producible by cholesterol which increases the chirality of lipid bilayers and enables to discriminate anesthetic enantiomers. The membrane lipid interaction should be reevaluated as the mode of action of local anesthetics. PMID:22915858

  4. Membrane interactivity of charged local anesthetic derivative and stereoselectivity in membrane interaction of local anesthetic enantiomers.

    PubMed

    Tsuchiya, Hironori; Mizogami, Maki

    2008-01-01

    With respect to the membrane lipid theory as a molecular mechanism for local anesthetics, two critical subjects, the negligible effects of charged drugs when applied extracellularly and the stereoselective effects of enantiomers, were verified by paying particular attention to membrane components, phospholipids with the anionic property, and cholesterol with several chiral carbons. The membrane interactivities of structurally-different anesthetics were determined by their induced fluidity changes of liposomal membranes. Lidocaine (3.0 μmol/mL) fluidized phosphatidylcholine membranes, but not its quaternary derivative QX-314 (3.0 μmol/mL). Similarly to the mother molecule lidocaine, however, QX-314 fluidized phosphatidylserine-containing nerve cell model membranes and acidic phospholipids-constituting membranes depending on the acidity of membrane lipids. Positively charged local anesthetics are able to act on lipid bilayers by ion-pairing with anionic (acidic) phospholipids. Bupivacaine (0.75 mol/mL) and ropivacaine (0.75 and 1.0 μmol/mL) fluidized nerve cell model membranes with the potency being S(-)-enantiomer < racemate < R(+)-enantiomer (P < 0.01, vs antipode and racemate) and cardiac cell model membranes with the potency being S(-)-ropivacaine < S(-)-bupivacaine < R(+)-bupivacaine (P < 0.01). However, their membrane effects were not different when removing cholesterol from the model membranes. Stereoselectivity is producible by cholesterol which increases the chirality of lipid bilayers and enables to discriminate anesthetic enantiomers. The membrane lipid interaction should be reevaluated as the mode of action of local anesthetics.

  5. Inhaled anesthetics have hyperalgesic effects at 0.1 minimum alveolar anesthetic concentration.

    PubMed

    Zhang, Y; Eger, E I; Dutton, R C; Sonner, J M

    2000-08-01

    We investigated the hyperalgesic (antianalgesic) effect of the inhaled anesthetics isoflurane, halothane, nitrous oxide, and diethyl ether, or the nonimmobilizer 1, 2-dichlorohexafluorocyclobutane at subanesthetic partial pressures (or, for the nonimmobilizer, subanesthetic partial pressures predicted from lipid solubility) in rats. Hyperalgesia was assessed as a decrease in the time to withdrawal of a rat hind paw exposed to heat. All four anesthetics, including nitrous oxide and diethyl ether, produced hyperalgesia at low partial pressures, with a maximal effect at 0.1 minimum alveolar anesthetic concentration (MAC) required to prevent response to movement in 50% of animals, and analgesia (an increased time to withdrawal of the hind paw) at 0. 4 to 0.8 MAC. The nonimmobilizer had neither analgesic nor hyperalgesia effects. We propose that inhaled anesthetics with a higher MAC-Awake (the MAC-fraction that suppresses appropriate responsiveness to command), such as nitrous oxide and diethyl ether, can be used as analgesics because patients are conscious at higher anesthetic partial pressures, including those which have analgesic effects, whereas anesthetics with a lower MAC-Awake do not produce analgesic effects at concentrations that permit consciousness. The inhaled anesthetics isoflurane, halothane, nitrous oxide, and diethyl ether produce antianalgesia at subanesthetic concentrations, with a maximal effect at approximately one-tenth the concentration required for anesthesia. This effect may enhance perception of pain when such small concentrations are reached during recovery from anesthesia.

  6. Neurotoxic effects of local anesthetics on the mouse neuroblastoma NB2a cell line.

    PubMed

    Mete, M; Aydemir, I; Tuglu, I M; Selcuki, M

    2015-04-01

    Local anesthetics are used clinically for peripheral nerve blocks, epidural anesthesia, spinal anesthesia and pain management; large concentrations, continuous application and long exposure time can cause neurotoxicity. The mechanism of neurotoxicity caused by local anesthetics is unclear. Neurite outgrowth and apoptosis can be used to evaluate neurotoxic effects. Mouse neuroblastoma cells were induced to differentiate and generate neurites in the presence of local anesthetics. The culture medium was removed and replaced with serum-free medium plus 20 μl combinations of epidermal growth factor and fibroblast growth factor containing tetracaine, prilocaine, lidocaine or procaine at concentrations of 1, 10, 25, or 100 μl prior to neurite measurement. Cell viability, iNOS, eNOS and apoptosis were evaluated. Local anesthetics produced toxic effects by neurite inhibition at low concentrations and by apoptosis at high concentrations. There was an inverse relation between local anesthetic concentrations and cell viability. Comparison of different local anesthetics showed toxicity, as assessed by cell viability and apoptotic potency, in the following order: tetracaine > prilocaine > lidocaine > procaine. Procaine was the least neurotoxic local anesthetic and because it is short-acting, may be preferred for pain prevention during short procedures.

  7. In Vivo Quantitation of Local Anesthetic Suppression of Leukocyte Adherence

    PubMed Central

    Giddon, D. B.; Lindhe, J.

    1972-01-01

    Using intravital microscopy, topically applied amide-type local anesthetics suppressed the adherence of leukocytes to the venular endothelium within surgical defects in the hamster cheek pouch. The response was reversible with physiologic saline and was localized to venules within the defect. Quantitation in terms of the percent of initially adhering leukocytes remaining in place on the venule wall at each minute following application of lidocaine and physiologic saline, respectively, revealed the suppression to be reliably related to the concentration, viz: 20.0 >10.0 >5.0 >0.0 mg ml of commercially available Xylocaine® (lidocaine) HCl. ImagesFig 1Fig 1 PMID:5049429

  8. Survey of local anesthetic use by Ontario dentists.

    PubMed

    Gaffen, Andrew S; Haas, Daniel A

    2009-11-01

    Local anesthetics are believed to be the most frequently used drugs in clinical dentistry, and although they are generally regarded as safe, some adverse reactions can be expected and do occur. The purpose of this study was to obtain, by means of a mail survey, information on the types and amounts of local anesthetics used by Ontario dentists during 2007. A survey requesting data on the annual use of injectable local anesthetics was mailed to all 8,058 dentists licensed by the Royal College of Dental Surgeons of Ontario in 2007. The effective response rate to the single mailing was 17.3% (1,395 respondents). By extrapolation, the estimated use of local anesthetics by all Ontario dentists during 2007 was determined to be about 13 million cartridges, which represents an average of 1,613 cartridges per dentist per year. Lidocaine with epinephrine 1:100,000 was the most commonly used formulation with 37.31% of total anesthetic use, followed by articaine with 1:200,000 epinephrine (27.04%) and articaine with 1:100,000 epinephrine (17.16%). Overall, local anesthetics combined with a vasoconstrictor accounted for more than 90% of total anesthetic use. A minority of survey respondents (15.68%) indicated that their pattern of anesthetic use had changed significantly in the past few years. Patterns of use were similar for early and late survey respondents. These data provide a current account of the use of local anesthetics by Ontario dentists.

  9. Local anesthetics: significance of hydrogen bonding in mechanism of action.

    PubMed

    Sax, M; Pletcher, J

    1969-12-19

    The action of local anesthetics is considered in terms of their ability to function as the donor in a hydrogen bond. The formation of a hydrogen-bonded complex between the drug and an acceptor group on the neural membrane is suggested as a feature in the action of local anesthetics.

  10. 21 CFR 346.10 - Local anesthetic active ingredients.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 5 2011-04-01 2011-04-01 false Local anesthetic active ingredients. 346.10 Section 346.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...

  11. 21 CFR 346.10 - Local anesthetic active ingredients.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 5 2013-04-01 2013-04-01 false Local anesthetic active ingredients. 346.10 Section 346.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...

  12. 21 CFR 346.10 - Local anesthetic active ingredients.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Local anesthetic active ingredients. 346.10 Section 346.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...

  13. 21 CFR 346.10 - Local anesthetic active ingredients.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 5 2012-04-01 2012-04-01 false Local anesthetic active ingredients. 346.10 Section 346.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...

  14. 21 CFR 346.10 - Local anesthetic active ingredients.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 5 2014-04-01 2014-04-01 false Local anesthetic active ingredients. 346.10 Section 346.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 346.10 Local anesthetic active ingredients. The active ingredient of the product consists of any of...

  15. Dual effect of local anesthetics on the function of excitable rod outer segment disk membrane

    SciTech Connect

    Mashimo, T.; Abe, K.; Yoshiya, I.

    1986-04-01

    The effects of local anesthetics and a divalent cation, Ca2+, on the function of rhodopsin were estimated from the measurements of light-induced proton uptake. The light-induced proton uptake by rhodopsin in the rod outer segment disk membrane was enhanced at lower pH (4) but depressed at higher pHs (6 to 8) by the tertiary amine local anesthetics lidocaine, bupivacaine, tetracaine, and dibucaine. The order of local anesthetic-induced depression of the proton uptake followed that of their clinical anesthetic potencies. The depression of the proton uptake versus the concentration of the uncharged form of local anesthetic nearly describes the same curve for small and large dose of added anesthetic. Furthermore, a neutral local anesthetic, benzocaine, depressed the proton uptake at all pHs between 4 and 7. These results indicate that the depression of the proton uptake is due to the effect of only the uncharged form. It is hypothesized that the uncharged form of local anesthetics interacts hydrophobically with the rhodopsin in the disk membrane. The dual effect of local anesthetics on the proton uptake, on the other hand, suggests that the activation of the function of rhodopsin may be caused by the charged form. There was no significant change in the light-induced proton uptake by rhodopsin when 1 mM of Ca2+ was introduced into the disk membrane at varying pHs in the absence or presence of local anesthetics. This fact indicates that Ca2+ ion does not influence the diprotonating process of metarhodopsin; neither does it interfere with the local anesthetic-induced changes in the rhodopsin molecule.

  16. Pain management via local anesthetics and responsive hydrogels

    PubMed Central

    Bagshaw, Kyle R; Hanenbaum, Curt L; Carbone, Erica J; Lo, Kevin WH; Laurencin, Cato T; Walker, Joseph; Nair, Lakshmi S

    2015-01-01

    Acute and chronic pain control is a significant clinical challenge that has been largely unmet. Local anesthetics are widely used for the control of post-operative pain and in the therapy of acute and chronic pain. While a variety of approaches are currently used to prolong the duration of action of local anesthetics, an optimal strategy to achieve neural blockage for several hours to days with minimal toxicity has yet to be identified. Several drug delivery systems such as liposomes, microparticles and nanoparticles have been investigated as local anesthetic delivery vehicles to achieve prolonged anesthesia. Recently, injectable responsive hydrogels raise significant interest for the localized delivery of anesthetic molecules. This paper discusses the potential of injectable hydrogels to prolong the action of local anesthetics. PMID:25690085

  17. Identifying and Managing Local Anesthetic Allergy in Dermatologic Surgery.

    PubMed

    Fathi, Ramin; Serota, Marc; Brown, Mariah

    2016-02-01

    Local anesthetic (LA) allergy is a concern for dermatologic surgeons given the large number of procedures performed yearly with LAs. Many patients also have anxiety about past or potential anesthesia allergy. This article will review the symptoms of IgE-mediated allergic reactions, the prevalence of IgE-mediated LA allergy, discuss common mimics of LA, and propose a practical approach for diagnostic and therapeutic options for LA allergy for the dermatologic surgeon in practice. A literature search of Pubmed using keywords "lidocaine," "local anesthetic," "hypersensitivity," and "allergy" was performed. Amide anesthetics result in the most reports of true local anesthetic immediate hypersensitivity. True IgE-mediated anaphylaxis to local anesthesia is very rare. Dermatologic surgeons should be aware of the symptoms of anesthetic allergy and its mimickers, as well as how to manage allergic reactions in their clinical practice.

  18. Development of prilocaine gels for enhanced local anesthetic action.

    PubMed

    Kang, Chung; Shin, Sang-Chul

    2012-07-01

    Prilocaine, one of local anesthetics, has been used for regional pain relief. When applied as an ointments or creams, it is hard to expect their effects to last for long time, because they are easily removed by wetting, movement and contacting. For more comfortable and better application, we developed a prilocaine gel system using a bioadhesive polymer, carboxymethyl cellulose (CMC). For suitable bioadhesion, the bioadhesive force of various polymers was tested using an auto-peeling tester. The bioadhesive force of various types of CMC such as 100MC, 150MC and 300MC, was 0.0264, 0.0461 and 0.0824 N, at 1.5% concentration, respectively. The CMC-300MC gels showed the most suitable bioadhesive forces. The effect of drug concentration on drug release was studied from the prepared 1.5% CMC gels using a synthetic cellulose membrane at 37 ± 0.5°C. As the concentration of drug increased, the drug release increased. The effects of temperature on drug release from the 1.0% prilocaine gels were evaluated at 27, 32, 37 and 42°C. As the temperature of the drug gels increased, drug release increased. The enhancing effects of penetration enhancers such as pyrrolidones, non-ionic surfactants, fatty acids and propylene glycol derivatives were studied. Among the enhancers used, polyoxyethylene 2-oleyl ether was superior. The anesthetic effects were studied by a tail flick analgesic meter. In the rat tailflick test, 1.0% prilocaine gels containing polyoxyethylene 2-oleyl ether showed the most prolonged local analgesic effects. The results support the view that prilocaine gels with enhanced local anesthetic action could be developed using CMC bioadhesive polymer.

  19. Minimize that "pinch and burn": tips and tricks to reduce injection pain with local anesthetics.

    PubMed

    Park, Kelly K

    2015-06-01

    Local anesthetics are commonly utilized in the practice of dermatology. Minimizing local anesthetic injection pain can be beneficial to both physicians and patients. Easily implemented techniques that reduce injection pain of intralesional local anesthetics are reviewed.

  20. Local anesthetics structure-dependently interact with anionic phospholipid membranes to modify the fluidity.

    PubMed

    Tsuchiya, Hironori; Ueno, Takahiro; Mizogami, Maki; Takakura, Ko

    2010-01-05

    While bupivacaine is more cardiotoxic than other local anesthetics, the mechanistic background for different toxic effects remains unclear. Several cardiotoxic compounds act on lipid bilayers to change the physicochemical properties of membranes. We comparatively studied the interaction of local anesthetics with lipid membranous systems which might be related to their structure-selective cardiotoxicity. Amide local anesthetics (10-300 microM) were reacted with unilamellar vesicles which were prepared with different phospholipids and cholesterol of varying lipid compositions. They were compared on the potencies to modify membrane fluidity by measuring fluorescence polarization. Local anesthetics interacted with liposomal membranes to increase the fluidity. Increasing anionic phospholipids in membranes enhanced the membrane-fluidizing effects of local anesthetics with the potency being cardiolipin>phosphatidic acid>phosphatidylglycerol>phosphatidylserine. Cardiolipin was most effective on bupivacaine, followed by ropivacaine. Local anesthetics interacted differently with biomimetic membranes consisting of 10mol% cardiolipin, 50mol% other phospholipids and 40mol% cholesterol with the potency being bupivacaine>ropivacaine>lidocaine>prilocaine, which agreed with the rank order of cardiotoxicity. Bupivacaine significantly fluidized 2.5-12.5mol% cardiolipin-containing membranes at cardiotoxicologically relevant concentrations. Bupivacaine is considered to affect lipid bilayers by interacting electrostatically with negatively charged cardiolipin head groups and hydrophobically with phospholipid acyl chains. The structure-dependent interaction with lipid membranes containing cardiolipin, which is preferentially localized in cardiomyocyte mitochondrial membranes, may be a mechanistic clue to explain the structure-selective cardiotoxicity of local anesthetics.

  1. Increased chondrocyte death after steroid and local anesthetic combination.

    PubMed

    Farkas, Boglárka; Kvell, Krisztián; Czömpöly, Tamás; Illés, Tamás; Bárdos, Tamás

    2010-11-01

    Hyaline articular cartilage has limited repair and regeneration capacity. Intraarticular administration of glucocorticoid and local anesthetic injections play an important role in the therapy of osteoarthritis. Glucocorticoids and anesthetics reportedly enhance apoptosis in chondrocytes, but effects of the combined use of glucocorticoids and local anesthetics are unknown. We asked whether glucocorticoid and local anesthetic agents combined had any synergistic effects on chondrocyte apoptosis. Cell viability and apoptosis/necrosis assessment of human articular chondrocytes were performed in vitro (chondrocyte cell cultures) and ex vivo (osteochondral specimens) using flow cytometry and TUNEL analysis, respectively. Glucocorticoids and local anesthetics induce apoptosis in chondrocytes at various rates. When used in combination, the percentage of dead chondrocytes was increased in in vitro chondrocyte cell cultures and osteochondral ex vivo specimens. We observed a time-dependent decrease in chondrocyte viability after concurrent steroid and local anesthetic exposure. The combination of glucocorticoids and local anesthetics has an adverse effect on articular chondrocytes, and it raises a question regarding whether concomitant administration should be used in treating osteoarthritis.

  2. Local anesthetics: dentistry's most important drugs, clinical update 2006.

    PubMed

    Malamed, Stanley F

    2006-12-01

    Local anesthetics are the safest most effective drugs in medicine for the control and management of pain. They also represent the most important drugs in dentistry. Today, dentistry has a spectrum of local anesthetics that permit pain control to be tailored to the specific needs of the patient: short-, intermediate-, and long-acting drugs. Bupivacaine has become a standard part of the armamentarium for postsurgical pain control while articaine has become the second-most used local anesthetic in the United States since its introduction in 2000. Despite an increase in anecdotal reports of paresthesia since articaine's introduction there is yet, no supporting scientific evidence.

  3. Local Anesthetic Inhibits Hyperpolarization-Activated Cationic Currents

    PubMed Central

    Meng, Qing-tao; Xia, Zhong-yuan; Liu, Jin; Bayliss, Douglas A.

    2011-01-01

    Systemic administration of local anesthetics has beneficial perioperative properties and an anesthetic-sparing and antiarrhythmic effect, although the detailed mechanisms of these actions remain unclear. In the present study, we investigated the effects of a local anesthetic, lidocaine, on hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels that contribute to the pacemaker currents in rhythmically oscillating cells of the heart and brain. Voltage-clamp recordings were used to examine the properties of cloned HCN subunit currents expressed in Xenopus laevis oocytes and human embryonic kidney (HEK) 293 cells under control condition and lidocaine administration. Lidocaine inhibited HCN1, HCN2, HCN1-HCN2, and HCN4 channel currents at 100 μM in both oocytes and/or HEK 293 cells; it caused a decrease in both tonic and maximal current (∼30–50% inhibition) and slowed current activation kinetics for all subunits. In addition, lidocaine evoked a hyperpolarizing shift in half-activation voltage (ΔV1/2 of ∼−10 to −14 mV), but only for HCN1 and HCN1-HCN2 channels. By fitting concentration-response data to logistic functions, we estimated half-maximal (EC50) concentrations of lidocaine of ∼30 to 40 μM for the shift in V1/2 observed with HCN1 and HCN1-HCN2; for inhibition of current amplitude, calculated EC50 values were ∼50 to 70 μM for HCN1, HCN2, and HCN1-HCN2 channels. A lidocaine metabolite, monoethylglycinexylidide (100 μM), had similar inhibitory actions on HCN channels. These results indicate that lidocaine potently inhibits HCN channel subunits in dose-dependent manner over a concentration range relevant for systemic application. The ability of local anesthetics to modulate Ih in central neurons may contribute to central nervous system depression, whereas effects on If in cardiac pacemaker cells may contribute to the antiarrhythmic and/or cardiovascular toxic action. PMID:21303986

  4. Neurotoxicity Questions Regarding Common Peripheral Nerve Block Adjuvants in Combination with Local Anesthetics

    PubMed Central

    Knight, Joshua B.; Schott, Nicholas J.; Kentor, Michael L.; Williams, Brian A.

    2015-01-01

    Purpose of Review Outline the analgesic role of perineural adjuvants for local anesthetic nerve block injections, and evaluate current knowledge regarding whether adjuvants modulate the neurocytologic properties of local anesthetics. Recent Findings Perineural adjuvant medications such as dexmedetomidine, clonidine, buprenorphine, dexamethasone, and midazolam play unique analgesic roles. The dosing of these medications to prevent neurotoxicity is characterized in various cellular and in vivo models. Much of this mitigation may be via reducing the dose of local anesthetic used while achieving equal or superior analgesia. Dose-concentration animal models have shown no evidence of deleterious effects. Clinical observations regarding blocks with combined bupivacaine-clonidine-buprenorphine-dexamethasone have shown beneficial effects on block duration and rebound pain without long-term evidence of neurotoxicity. In vitro and in vivo studies of perineural clonidine and dexmedetomidine show attenuation of perineural inflammatory responses generated by local anesthetics. Summary Dexmedetomidine added as a peripheral nerve blockade adjuvant improves block duration without neurotoxic properties. The combined adjuvants clonidine, buprenorphine, and dexamethasone do not appear to alter local anesthetic neurotoxicity. Midazolam significantly increases local anesthetic neurotoxicity in vitro, but when combined with clonidine-buprenorphine-dexamethasone (sans local anesthetic) produces no in vitro or in vivo neurotoxicity. Further larger-species animal testing and human trials will be required to reinforce the clinical applicability of these findings. PMID:26207854

  5. Liposomes for entrapping local anesthetics: a liposome electrokinetic chromatographic study.

    PubMed

    Lokajová, Jana; Laine, Jaana; Puukilainen, Esa; Ritala, Mikko; Holopainen, Juha M; Wiedmer, Susanne K

    2010-05-01

    Bupivacaine is a lipophilic, long-acting, amide class local anesthetic commonly used in clinical practice to provide local anesthesia during surgical procedures. Several cases of accidental overdose with cardiac arrest and death have been reported since bupivacaine was introduced to human use. Recent case reports have suggested that Intralipid (Fresenius Kabi) is an effective therapy for cardiac toxicity from high systemic concentrations of, e.g. bupivacaine, even though the mechanism behind the interaction is not fully clear yet. Our long-term aim is to develop a sensitive, efficient, and non-harmful lipid-based formulation to specifically trap harmful substances in vivo. In this study, the in vitro interaction of local anesthetics (bupivacaine, prilocaine, and lidocaine) with Intralipid or lipid vesicles containing phosphatidylglycerol, phosphatidylcholine, cardiolipin, cholesterol, and N-palmitoyl-D-erythro-sphingosine (ceramide) was determined by liposome electrokinetic chromatography. The interactions were evaluated by calculating the retention factors and distribution constants. Atomic force microscopy measurements were carried out to confirm that the interaction mechanism was solely due to interactions between the analytes and the moving pseudostationary phase and not by interactions with a stationary lipid phase adsorbed to the fused-silica wall. The heterogeneity of the liposomes was also studied by atomic force microscopy. The liposome electrokinetic chromatography results demonstrate that there is higher interaction between the drugs and negatively charged liposome dispersion than with the commercial Intralipid dispersion.

  6. Application of nanogel systems in the administration of local anesthetics

    PubMed Central

    Tan, Jeremy PK; Tan, Maureen BH; Tam, Michael KC

    2010-01-01

    Nanogels are robust nanoparticles that could be used to deliver active drug compounds in controlled drug delivery applications. This review discusses the design, synthesis, loading, and release of local anesthetics using polymeric nanoparticles produced via various types of polymerization techniques. The strategy of using layer-by-layer approach to control the burst release of procaine hydrochloride (PrHy; a local anesthetic drug of the amino ester group) is described and discussed. PMID:22915875

  7. Pharmacology of local anesthetics used in oral surgery.

    PubMed

    Giovannitti, Joseph A; Rosenberg, Morton B; Phero, James C

    2013-08-01

    This article provides a comprehensive review of the pharmacology of local anesthetics as a class, and provides details of the individual drugs available in dental cartridges. Maximum recommended doses of local anesthetics and vasoconstrictors are presented for healthy adult and pediatric patients, and for patients with cardiovascular system impairments. Various complications and reasons for failure of local anesthesia effectiveness are discussed, and current and future trends in local anesthesia are presented to provide an overview of current research in local anesthesia. Copyright © 2013 Elsevier Inc. All rights reserved.

  8. The effect of adenosine triphosphate on sevoflurane requirements for minimum alveolar anesthetic concentration and minimum alveolar anesthetic concentration-awake.

    PubMed

    Suzuki, A; Katoh, T; Ikeda, K

    1998-01-01

    We evaluated the effects of i.v. adenosine triphosphate (ATP) on sevoflurane minimum alveolar anesthetic concentration (MAC) and MAC-Awake. The study group included healthy patients 20-60 yr of age. The study groups for MAC-Awake determination included 49 patients who were scheduled for elective surgery. The study groups for MAC determination included 53 patients scheduled for elective surgery involving a skin incision. These patients were randomly assigned to two groups, an ATP group and a control group. The ATP group received 100 micrograms.kg-1.min-1 ATP i.v., and the control group received no medication. The ATP group and the control group were compared with regard to MAC-Awake (anesthetic concentration achieving 50% probability of eye opening in response to a verbal command) and MAC (anesthetic concentration achieving 50% probability of no movement in response to skin incision). The MAC-Awake was 0.7% +/- 0.1% in the control group (mean +/- SD) and 0.7% +/- 0.1% in the ATP group. MAC was 1.9% +/- 0.1% in the control group and 2.1% +/- 0.2% in the ATP group. The differences in MAC and MAC-Awake between the two groups were not statistically significant. We conclude that ATP infusion (100 micrograms.kg-1.min-1) has no effect on sevoflurane MAC and MAC-Awake. We found that an i.v. adenosine triphosphate infusion (100 micrograms.kg-1.min-1) has no effect on sevoflurane minimum alveolar anesthetic concentration (anesthetic concentration achieving 50% probability of no movement in response to skin incision) and minimum alveolar anesthetic concentration-Awake (anesthetic concentration achieving 50% probability of eye opening in response to a verbal command) in humans.

  9. Water solvent and local anesthetics: A computational study

    NASA Astrophysics Data System (ADS)

    Bernardi, R. C.; Gomes, D. E. B.; Pascutti, P. G.; Ito, A. S.; Taft, C. A.; Ota, A. T.

    There are various experimental studies regarding the toxicity and the time of action of local anesthetics, which contain general insights about their pharmacological and physicochemical properties. Although a detailed microscopic analysis of the local anesthetics would contribute to understanding these properties, there are relatively few theoretical studies about these molecules. In this article, we present the results from calculations performed for three local anesthetics: tetracaine, procaine, and lidocaine, both in their charged and uncharged forms, in aqueous environment. We have used the density functional theory and molecular dynamics simulations to study the structural characteristics of these compounds. The radial distribution function g(r) was used to examine the structure of water molecules surrounding different regions of the local anesthetics. We demonstrated the nonhomogeneous character of the anesthetics with respect to their affinity to water solvent molecules as well as the modifications in their affinity to water caused by changes in their charge state. We also observed that the biological potency of the anesthetics is more related to the behavior of specific groups within the molecule, which are responsible for the interaction with the lipid phase of membranes, rather than the general properties of the molecule as a whole.

  10. Recognition of local anesthetics by alphabeta+ T cells.

    PubMed

    Zanni, M P; von Greyerz, S; Hari, Y; Schnyder, B; Pichler, W J

    1999-02-01

    Patients with drug allergy show a specific immune response to drugs. Chemically nonreactive drugs like, for example, local anesthetics are directly recognized by alphabeta+ T cells in an HLA-DR restricted way, as neither drug metabolism nor protein processing is required for T cell stimulation. In this study we identified some of the structural requirements that determine cross-reactivity of T cells to local anesthetics, with the aim to improve the molecular basis for the selection of alternatives in individuals sensitized to a certain local anesthetic and to better understand presentation and T cell recognition of these drugs. Fifty-five clones (52 lidocaine specific, three mepivacaine specific from two allergic donors) were analyzed. Stimulatory compounds induced a down-regulation of the T cell receptor, demonstrating that these non-peptide antigens are recognized by the T cell receptor itself. A consistent cross-reactivity between lidocaine and mepivacaine was found, as all except one lidocaine specific clone proliferated to both drugs tested. Sixteen chemically related local anesthetics (including ester local anesthetics, OH- and desalkylated metabolites) were used to identify structural requirements for T cell recognition. Each of the four clones examined in detail was uniquely sensitive to changes in the structures of the local anesthetic: clone SFT24, i.e., did not recognize any of the tested OH- or desalkylated metabolites, while the clone OFB2 proliferated to all OH-metabolites and other differently modified molecules. The broadly reactive clone OFB2 allowed us to propose a model, suggesting that the structure of the amine side chain of local anesthetics is essential for recognition by the T cell receptor.

  11. Local anesthetic use in the pregnant and postpartum patient.

    PubMed

    Fayans, Edgar P; Stuart, Hunter R; Carsten, David; Ly, Quen; Kim, Hanna

    2010-10-01

    The use of systemically absorbed drugs in the gravid and in the lactating patient is of concern to the dentist. This article reviews concerns for the health and safety of the mother, developing fetus, and neonate involving local anesthetics. The available literature on the use of local anesthetics for dentistry in the pregnant and postpartum patient is also reviewed. In addition, the physiology of the pregnant and postpartum woman is discussed because this is essential to understanding potential interplay with local anesthesia and the stress of a dental appointment.

  12. Pain control via opioid analgesic-local anesthetic loaded IPNs.

    PubMed

    Keskin, Dilek Sendil; Wise, Donald L; Hasirci, Vasif

    2004-01-01

    Relief of chronic pain is an important clinical problem requiring special care and approaches. The present study was designed for the construction of a controlled release system for local application of analgesics (hydromorphone (HM), morphine (M), and codeine (C)) and a local anesthetic, bupivacaine (BP). An interpenetrating network (IPN) drug release system was prepared by using a biocompatible, biodegradable copolyester, poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) and another biocompatible but synthetic, nondegradable polymer, poly (2- hydroxyethyl methacrylate), (PHEMA). In situ release kinetics of the IPN system was first order for BP but could not be fitted to any known equation for the other drugs. Complete release from the IPNs occurred within a considerably short time (24 h for 80 % of the drugs) most probably due to the significant hydrophilicity of PHEMA. In order to slow down the release rate these IPNs were coated with PHBV. Release from these coated IPNs (cIPN) resulted in rates that could be described by Higuchi's equations. In vivo measurement of antinociceptive efficacy was carried out in rats with tail flick and paw-withdrawal tests after inducing chronic pain created by sciatic nerve ligation at the right side. Control groups received placebo implants. In vivo studies showed potent, prolonged (2-3 days) antinociception at the site of injury (right paw) for strong opioids (HM and M) and about 2 days for the weak opioid (C) and local anesthetic (BP). In all cases the release rate was found to be as important as the antinociceptive potency. The weakest opioid analgesic of those evaluated (C) had a higher first day antinociception than its stronger counterpart M, probably due to its higher initial concentration that was expected from its faster release rate in the in situ experiments.

  13. Local anesthetics differentially inhibit sympathetic neuron-mediated and C fiber-mediated synovial neurogenic plasma extravasation.

    PubMed

    Pietruck, Christian; Grond, Stefan; Xie, Guo-Xi; Palmer, Pamela P

    2003-05-01

    Local anesthetics are used for local irrigation after many types of operations. However, recent evidence of toxic effects of local anesthetics at large concentrations during continuous administration suggests an advantage of using decreased local anesthetic concentrations for irrigation solutions. In this study, we determined whether smaller concentrations of local anesthetics may maintain an antiinflammatory and, therefore, analgesic effect without the risk of possible toxicity. Lidocaine and bupivacaine were studied for their ability to inhibit both components of neurogenic inflammation-C fiber-mediated and sympathetic postganglionic neuron (SPGN)-mediated inflammation-in the rat knee joint. Intraarticular lidocaine 0.02% reduced 5-hydroxytryptamine (5-HT)-induced (SPGN-mediated) plasma extravasation (PE) by 35%, and further decreases were obtained by perfusing larger concentrations of lidocaine. Intraarticular bupivacaine 0.025% inhibited 5-HT-induced PE by 60%, and a 95% inhibition was obtained with bupivacaine 0.05%. Larger local anesthetic concentrations were necessary to inhibit C fiber-mediated PE than those required to inhibit SPGN-mediated PE. Lidocaine 0.4% was required to reduce mustard oil-induced PE by 60%. Lidocaine 2% inhibited mustard oil-induced PE to baseline levels. Bupivacaine 0.1% was required for an 80% reduction of PE. Bupivacaine 0.25% inhibited mustard oil-induced PE to baseline levels. Our results demonstrate differential effects of local anesthetics on SPGN- and C fiber-mediated PE but confirm the concept of using smaller concentrations of local anesthetics to achieve inhibition of postoperative inflammation. Local anesthetic wound irrigation is often used to treat postoperative surgical pain. Large concentrations of local anesthetics are usually used, and these concentrations may have possible neurotoxic and myotoxic effects. Our results demonstrate antiinflammatory effects of lidocaine and bupivacaine at concentrations smaller than

  14. pH adjustment schedule for the amide local anesthetics.

    PubMed

    Ikuta, P T; Raza, S M; Durrani, Z; Vasireddy, A R; Winnie, A P; Masters, R W

    1989-01-01

    Several studies have indicated that the addition of sodium bicarbonate to solutions of local anesthetics to raise the pH closer to the pKa shortens the latency, increases the intensity, and prolongs the duration of the resultant neural blockade. However, the addition of too much bicarbonate will cause precipitation, and this may result in the injection of particulate free base along with the solution. The present study was carried out to determine the maximal amount of sodium bicarbonate that can be added to each of the amide local anesthetics without the formation of a precipitate, and, thus, to construct a pH adjustment schedule to simplify the alkalinization of local anesthetics in clinical practice.

  15. Adverse reactions triggered by dental local anesthetics: a clinical survey.

    PubMed Central

    Kaufman, E.; Goharian, S.; Katz, Y.

    2000-01-01

    One hundred and seventy-nine patients completed a questionnaire focusing on adverse reactions to dental local anesthetics as manifested by 16 signs and symptoms. Twenty-six percent of the participants reported having at least 1 adverse reaction. It was found that most of the adverse reactions occurred within the first 2 hours following the injection of local anesthetics. Pallor, palpitations, diaphoresis, and dizziness were the most common adverse reactions reported in the study. The results pointed to a significant relationship between anxiety, gender, injection technique, and procedure with a higher incidence of adverse reactions. PMID:11432179

  16. Transient perioperative brainstem paralysis secondary to a local anesthetic.

    PubMed

    Joannides, Alexis J; Santarius, Thomas; Fernandes, Helen M; Laing, Rodney J C; Trivedi, Rikin A

    2012-07-01

    Local anesthesia is widely used, in isolation or in conjunction with general anesthesia. The authors describe 2 adolescent patients presenting with absent brainstem reflexes and delayed awakening following elective foramen magnum decompression for Chiari Type I malformation. In both cases, neurological deficits were closely associated with the administration of a levobupivacaine field block following wound closure. In the absence of any structural or biochemical abnormalities, and with spontaneous recovery approximating the anesthetic half-life, the authors' observations are consistent with transient brainstem paralysis caused by perioperative local anesthetic infiltration.

  17. Changes in Publication-Based Academic Interest in Local Anesthetics Over the Past 50 Years.

    PubMed

    Vlassakov, Kamen V; Kissin, Igor

    2016-07-01

    To present the history of changes in academic interest in local anesthetics quantitatively. The changes in publication-based academic interest in local anesthetics were assessed using information from the database of PubMed. The assessment was mostly based on the following indices: general popularity index (GPI), representing the proportion of articles on a drug relative to all articles in the field of regional anesthesia, and specific popularity index (SPI), representing the proportion of articles on a drug relative to all articles in one of the four forms of regional anesthesia: local anesthesia, spinal anesthesia, epidural anesthesia, and peripheral nerve blocks. The most important general feature of the changes in publication-based academic interest in local anesthetics for the past 50 years was the concentration of this interest on a very limited number of drugs. By 2010-2014, only three anesthetics demonstrated the GPI value above 4.0: bupivacaine (10.1), lidocaine (10.0), and ropivacaine (4.6). All other local anesthetics had GPI declining mostly to less than 1.0 (2010-2014). The rate of change in publication-based academic interest was very slow in both its increase and decline. The most profound change in publication-based academic interests was caused by the introduction of bupivacaine. During a 20-year period (from 1965-1969 to 1985-1989), bupivacaine's GPI increased from 1.3 to 12.9. A slowly developing concentration of publication-based academic interest on a very limited number of local anesthetics was the dominant feature related to this class of anesthetic agents. Copyright © 2016 Anesthesia History Association. Published by Elsevier Inc. All rights reserved.

  18. Local, Controlled Delivery of Local Anesthetics In Vivo from Polymer - Xerogel Composites.

    PubMed

    Qu, Haibo; Costache, Marius C; Inan, Saadet; Cowan, Alan; Devore, David; Ducheyne, Paul

    2016-03-01

    Polymer-xerogel composite materials have been introduced to better optimize local anesthetics release kinetics for the pain management. In a previous study, it was shown that by adjusting various compositional and nano-structural properties of both inorganic xerogels and polymers, zero-order release kinetics over 7 days can be achieved in vitro. In this study, in vitro release properties are confirmed in vivo using a model that tests for actual functionality of the released local anesthetics. Composite materials made with tyrosine-polyethylene glycol(PEG)-derived poly(ether carbonate) copolymers and silica-based sol-gel (xerogel) were synthesized. The in vivo release from the composite controlled release materials was demonstrated by local anesthetics delivery in a rat incisional pain model. The tactile allodynia resulting from incision was significantly attenuated in rats receiving drug-containing composites compared with the control and sham groups for the duration during which natural healing had not yet taken place. The concentration of drug (bupivacaine) in blood is dose dependent and maintained stable up to 120 h post-surgery, the longest time point measured. These in vivo studies show that polymer-xerogel composite materials with controlled release properties represent a promising class of controlled release materials for pain management.

  19. The interaction of local anesthetics with lipid membranes.

    PubMed

    Zapata-Morin, Patricio A; Sierra-Valdez, F J; Ruiz-Suárez, J C

    2014-09-01

    Molecular Dynamic Simulations are performed to evaluate the interaction of lidocaine, procaine and tetracaine with a lipid membrane. The main interest is to evaluate the structural changes produced by these local anesthetics in the bilayers. Penetration trajectories, interaction energies, entropy changes and an order parameter are calculated to quantify the destabilization of the lipid configurations. We show that such structural parameters give important information to understand how anesthetic agents influence the structure of plasma membranes. Graphic processing units (GPUs) are used in our simulations. Copyright © 2014 Elsevier Inc. All rights reserved.

  20. Adjuvants to local anesthetics: Current understanding and future trends

    PubMed Central

    Swain, Amlan; Nag, Deb Sanjay; Sahu, Seelora; Samaddar, Devi Prasad

    2017-01-01

    Although beneficial in acute and chronic pain management, the use of local anaesthetics is limited by its duration of action and the dose dependent adverse effects on the cardiac and central nervous system. Adjuvants or additives are often used with local anaesthetics for its synergistic effect by prolonging the duration of sensory-motor block and limiting the cumulative dose requirement of local anaesthetics. The armamentarium of local anesthetic adjuvants have evolved over time from classical opioids to a wide array of drugs spanning several groups and varying mechanisms of action. A large array of opioids ranging from morphine, fentanyl and sufentanyl to hydromorphone, buprenorphine and tramadol has been used with varying success. However, their use has been limited by their adverse effect like respiratory depression, nausea, vomiting and pruritus, especially with its neuraxial use. Epinephrine potentiates the local anesthetics by its antinociceptive properties mediated by alpha-2 adrenoreceptor activation along with its vasoconstrictive properties limiting the systemic absorption of local anesthetics. Alpha 2 adrenoreceptor antagonists like clonidine and dexmedetomidine are one of the most widely used class of local anesthetic adjuvants. Other drugs like steroids (dexamethasone), anti-inflammatory agents (parecoxib and lornoxicam), midazolam, ketamine, magnesium sulfate and neostigmine have also been used with mixed success. The concern regarding the safety profile of these adjuvants is due to its potential neurotoxicity and neurological complications which necessitate further research in this direction. Current research is directed towards a search for agents and techniques which would prolong local anaesthetic action without its deleterious effects. This includes novel approaches like use of charged molecules to produce local anaesthetic action (tonicaine and n butyl tetracaine), new age delivery mechanisms for prolonged bioavailability (liposomal

  1. Adjuvants to local anesthetics: Current understanding and future trends.

    PubMed

    Swain, Amlan; Nag, Deb Sanjay; Sahu, Seelora; Samaddar, Devi Prasad

    2017-08-16

    Although beneficial in acute and chronic pain management, the use of local anaesthetics is limited by its duration of action and the dose dependent adverse effects on the cardiac and central nervous system. Adjuvants or additives are often used with local anaesthetics for its synergistic effect by prolonging the duration of sensory-motor block and limiting the cumulative dose requirement of local anaesthetics. The armamentarium of local anesthetic adjuvants have evolved over time from classical opioids to a wide array of drugs spanning several groups and varying mechanisms of action. A large array of opioids ranging from morphine, fentanyl and sufentanyl to hydromorphone, buprenorphine and tramadol has been used with varying success. However, their use has been limited by their adverse effect like respiratory depression, nausea, vomiting and pruritus, especially with its neuraxial use. Epinephrine potentiates the local anesthetics by its antinociceptive properties mediated by alpha-2 adrenoreceptor activation along with its vasoconstrictive properties limiting the systemic absorption of local anesthetics. Alpha 2 adrenoreceptor antagonists like clonidine and dexmedetomidine are one of the most widely used class of local anesthetic adjuvants. Other drugs like steroids (dexamethasone), anti-inflammatory agents (parecoxib and lornoxicam), midazolam, ketamine, magnesium sulfate and neostigmine have also been used with mixed success. The concern regarding the safety profile of these adjuvants is due to its potential neurotoxicity and neurological complications which necessitate further research in this direction. Current research is directed towards a search for agents and techniques which would prolong local anaesthetic action without its deleterious effects. This includes novel approaches like use of charged molecules to produce local anaesthetic action (tonicaine and n butyl tetracaine), new age delivery mechanisms for prolonged bioavailability (liposomal

  2. Distribution of local anesthetics between aqueous and liposome phases.

    PubMed

    Ruokonen, Suvi-Katriina; Duša, Filip; Rantamäki, Antti H; Robciuc, Alexandra; Holma, Paula; Holopainen, Juha M; Abdel-Rehim, Mohamed; Wiedmer, Susanne K

    2017-01-06

    Liposomes were used as biomimetic models in capillary electrokinetic chromatography (EKC) for the determination of distribution constants (KD) of certain local anesthetics and a commonly used preservative. Synthetic liposomes comprised phosphatidylcholine and phosphatidylglycerol phospholipids with and without cholesterol. In addition, ghost liposomes made from red blood cell (RBC) lipid extracts were used as pseudostationary phase to acquire information on how the liposome composition affects the interactions between anesthetics and liposomes. These results were compared with theoretical distribution coefficients at pH 7.4. In addition to 25°C, the distribution constants were determined at 37 and 42°C to simulate physiological conditions. Moreover, the usability of five electroosmotic flow markers in liposome (LEKC) and micellar EKC (MEKC) was studied. LEKC was proven to be a convenient and fast technique for obtaining data about the distribution constants of local anesthetics between liposome and aqueous phase. RBC liposomes can be utilized for more representative model of cellular membranes, and the results indicate that the distribution constants of the anesthetics are greatly dependent on the used liposome composition and the amount of cholesterol, while the effect of temperature on the distribution constants is less significant.

  3. Electronic dental anesthesia in a patient with suspected allergy to local anesthetics: report of case.

    PubMed

    Malamed, S F; Quinn, C L

    1988-01-01

    A 56-year-old patient with alleged allergy to local anesthetics required restorative dental treatment. Electronic dental anesthesia was used successfully, in lieu of injectable local anesthetics, to manage intraoperative pain associated with the restoration of vital mandibular teeth.

  4. The action of local anesthetics on myelin structure and nerve conduction in toad sciatic nerve.

    PubMed

    Mateu, L; Morán, O; Padrón, R; Borgo, M; Vonasek, E; Márquez, G; Luzzati, V

    1997-06-01

    X-ray scattering and electrophysiological experiments were performed on toad sciatic nerves in the presence of local anesthetics. In vitro experiments were performed on dissected nerves superfused with Ringer's solutions containing procaine, lidocaine, tetracaine, or dibucaine. In vivo experiments were performed on nerves dissected from animals anesthesized by targeted injections of tetracaine-containing solutions. In all cases the anesthetics were found to have the same effects on the x-ray scattering spectra: the intensity ratio of the even-order to the odd-order reflections increases and the lattice parameter increases. These changes are reversible upon removal of the anesthetic. The magnitude of the structural changes varies with the duration of the superfusion and with the nature and concentration of the anesthetic molecule. A striking quantitative correlation was observed between the structural effects and the potency of the anesthetic. Electron density profiles, which hardly showed any structural alteration of the unit membrane, clearly indicated that the anesthetics have the effect of moving the pairs of membranes apart by increasing the thickness of the cytoplasmic space. Electrophysiological measurements performed on the very samples used in the x-ray scattering experiments showed that the amplitude of the compound action potential is affected earlier than the structure of myelin (as revealed by the x-ray scattering experiments), whereas conduction velocity closely follows the structural alterations.

  5. Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol: Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects

    PubMed Central

    2013-01-01

    Despite a long history in medical and dental application, the molecular mechanism and precise site of action are still arguable for local anesthetics. Their effects are considered to be induced by acting on functional proteins, on membrane lipids, or on both. Local anesthetics primarily interact with sodium channels embedded in cell membranes to reduce the excitability of nerve cells and cardiomyocytes or produce a malfunction of the cardiovascular system. However, the membrane protein-interacting theory cannot explain all of the pharmacological and toxicological features of local anesthetics. The administered drug molecules must diffuse through the lipid barriers of nerve sheaths and penetrate into or across the lipid bilayers of cell membranes to reach the acting site on transmembrane proteins. Amphiphilic local anesthetics interact hydrophobically and electrostatically with lipid bilayers and modify their physicochemical property, with the direct inhibition of membrane functions, and with the resultant alteration of the membrane lipid environments surrounding transmembrane proteins and the subsequent protein conformational change, leading to the inhibition of channel functions. We review recent studies on the interaction of local anesthetics with biomembranes consisting of phospholipids and cholesterol. Understanding the membrane interactivity of local anesthetics would provide novel insights into their anesthetic and cardiotoxic effects. PMID:24174934

  6. Intraperitoneal Local Anesthetic in Pediatric Surgery: A Systematic Review.

    PubMed

    Hamill, James K; Rahiri, Jamie-Lee; Liley, Andrew; Hill, Andrew G

    2016-12-01

    Introduction Systematic reviews report intraperitoneal local anesthetic (IPLA) effective in adults but until now no review has addressed IPLA in children. The objective of this review was to answer the question, does IPLA compared with control reduce pain after pediatric abdominal surgery. Materials and Methods Data sources: MEDLINE, EMBASE, Cochrane databases, trials registries, ProQuest, Web of Science, Google Scholar, and Open Gray.

  7. Interactions of some local anesthetics and alcohols with membranes.

    PubMed

    Frangopol, P T.; Mihăilescu, D

    2001-09-01

    A review of the results obtained by our group in the last decade regarding the interactions of procaine, lidocaine, dibucaine and tetracaine with membranes is presented in the context of the literature data. The action upon membranes, in first approximation monomolecular film of stearic acid spread at the air/water interface used as a membrane model, the modification of biomembrane structure and function using diffraction methods, lipid phase transition, fluidity of lipids and proteins, membrane expansion and platelet aggregation were studied. The thermodynamic knowledge of membrane-alcohol interactions improved by using highly sensitive calorimetric techniques are briefly reported. One of the main conclusions is that the physical state of a monolayer model membrane was the result of competitive interactions between film-film and film-substrate interactions. It was taken into account that local anesthetics, such as lidocaine, carbisocaine, mesocaine, showed changes in the bilayer structure, reflected in macroscopic mechanical properties. This restructuring of the lipid bilayer has a significant influence on the operation of functional subunits, e.g. ionic channels formed by gramicidin. The results support the concept of non-specific interactions of local anesthetics with lipid bilayers. The theoretical modeling of the interactions of local anesthetics is closely compared with experimental data. Our new theory of relaxation for these interactions is using a non-archimedean formalism based on a process resulting from superpositions of different component processes which take place at different scales of time.

  8. 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.

  9. Intralipid therapy for inadvertent peripheral nervous system blockade resulting from local anesthetic overdose.

    PubMed

    Kamel, Ihab; Trehan, Gaurav; Barnette, Rodger

    2015-01-01

    Although local anesthetics have an acceptable safety profile, significant morbidity and mortality have been associated with their use. Inadvertent intravascular injection of local anesthetics and/or the use of excessive doses have been the most frequent causes of local anesthetic systemic toxicity (LAST). Furthermore, excessive doses of local anesthetics injected locally into the tissues may lead to inadvertent peripheral nerve infiltration and blockade. Successful treatment of LAST with intralipid has been reported. We describe a case of local anesthetic overdose that resulted in LAST and in unintentional blockade of peripheral nerves of the lower extremity; both effects completely resolved with administration of intralipid.

  10. Local anesthetics inhibit uterine activity in vitro. Possible application on preterm labor prevention and treatment.

    PubMed

    Fauza, Dario O; Kohane, Daniel S; Beeuwkes, Elizabeth B; Clayton, Nicholas; Maher, Timothy J

    2003-01-01

    Analysis of the effects of local anesthetics upon the gravid uterus. Isolated strips of pregnant-rat myometrium were placed within tissue baths. Muscular activity was then recorded by a force transducer, at cumulative concentrations of either procaine, lidocaine, or ropivacaine. The effects of myometrial activity were non-monotonic. At lower concentrations, an increase in contraction frequency was noted, concomitant with a depression in amplitude. As the concentrations increased, both amplitude and frequency were depressed until, eventually, activity was abolished. Local anesthetics administered in situ consistently inhibit or completely arrest overall myometrial activity. These agents may prove clinically useful in preterm labor management, if administered locally to the myometrium via suitable slow release drug delivery systems, warranting further trials in vivo. Copyright 2003 S. Karger AG, Basel

  11. Influence of local anesthetics on molecular organization in phosphatidylethanolamine membranes

    SciTech Connect

    Kelusky, E.C.; Smith, I.C.

    1984-09-01

    The influence of the local anesthetics tetracaine (TTC) and procaine (PRC) on bilayers of specifically deuterated phosphatidylethanolamines (PE) has been studied by /sup 2/H and /sup 31/P NMR. Dimyristoylphosphatidylethanolamines (DMPE), deuterated at positions 2, 4, and 14 of the sn-2 chain, position 2 of the sn-1 chain, and in the ethanolamine headgroup, were mixed 1:1 with a semisynthetic egg PE and the effect of measured quantities of TTC and PRC on the /sup 2/H quadrupole splittings, spin-lattice relaxation times, and /sup 31/P chemical shift anisotropy were observed. Experiments were performed at pH 5.5, when the anesthetics are primarily charged, and at pH 9.5, when they are uncharged. Tetracaine was observed to disorder the hydrocarbon region of the bilayer and to induce a conformational change in the PE headgroup. Conversely, procaine had little or no effect on the hydrocarbon region and induced only a small change in the headgroup. These conformational changes and disordering effects, when adjusted for anesthetic partitioning, are essentially independent of the charge on the anesthetic. However, at pH 5.5 and low TTC/PE molar ratios (less than 0.1), the /sup 2/H NMR spectra showed two lipid environments--one corresponding to free PE and the other to PE in contact with TTC. Continued addition of TTC resulted in the eventual disappearance of the free PE signal and the corresponding growth of the signal from PE in contact with TTC. At pH 9.5, when TTC is uncharged, only one signal is observed. In mixtures of PE and phosphatidylserine, a conformational change in the headgroup was noted which was similar to that seen in the pure PE; however, there was no evidence for slow lateral diffusion of the anesthetics.

  12. Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose.

    PubMed

    Galenko-Yaroshevskii, A P; Varlashkina, I A; Takhchidi, Kh P; Malyugin, B E; Dukhanin, A S

    2007-05-01

    Conformation and kinetic characteristics of the interactions of local anesthetics lidocaine (xycaine), tetracaine (dicaine), bupivacaine, and new RU-1117 compound with proven anesthetic activity with Visiton (1% hydroxypropylmethylcellulose in phosphate buffer) were studied. It was found that complex formation between the local anesthetics and hydroxypropylmethylcellulose is a time-dependent reversible process. The equilibrium is attained within 2.5-8.0 h and depends on the chemical nature of local anesthetic.

  13. The predictive value of skin testing in the diagnosis of local anesthetic allergy.

    PubMed

    McClimon, Brad; Rank, Matthew; Li, James

    2011-01-01

    Local anesthetics are commonly used medications and can result in adverse reactions. The diagnostic workup of local anesthetic reactions remains controversial. This study was designed to determine the effectiveness of skin testing for local anesthetic allergy evaluation. A retrospective chart review was performed on patients undergoing local anesthetic skin testing. Patients were included if they underwent prick and intradermal skin testing followed by incremental subcutaneous challenge. Charts were further systematically reviewed to evaluate response to local anesthetics in the clinical setting after open subcutaneous challenge. One hundred seventy-eight patients underwent 227 local anesthetic skin tests. Two hundred twenty (97%) of the skin tests were negative. Of the negative skin tests results, 214 (97%) had negative challenge or probable non-IgE-mediated events during challenge. Three patients with six negative skin tests had a local reaction during the open subcutaneous challenge. Seven skin tests on five patients met the criteria for a positive skin test with local anesthetics. One patient had an equivocal local skin reaction with subcutaneous challenge without systemic effects. Three patients had a negative subcutaneous challenge and one patient did not undergo a challenge. Ninety-eight percent of patients receiving local anesthetics in the clinical setting after open subcutaneous challenge tolerated the medications. The negative predictive value of the local anesthetic skin test was 97% with few positive skin tests. Positive local anesthetic skin tests are uncommon and the local anesthetic skin tests have an excellent negative predictive value. Additional study with skin test-only protocols is warranted.

  14. The efficacy of eutectic mixture of local anesthetics as a topical anesthetic agent used for dental procedures: A brief review.

    PubMed

    Daneshkazemi, Alireza; Abrisham, Seyyed Mohammad; Daneshkazemi, Pedram; Davoudi, Amin

    2016-01-01

    Dental pain management is one of the most critical aspects of modern dentistry which might affect patient's quality of life. Several methods are suggested to provide a painless situation for patients. Desensitization of the oral site using topical anesthetics is one of those methods. The improvements of topical anesthetic agents are probably one of the most important advances in dental science in the past 100 years. Most of them are safe and can be applied on oral mucosa with minimal irritation and allergic reactions. At present, these agents are various with different potent and indications. Eutectic mixture of local anesthetics (EMLA) (lidocaine + prilocaine) is a commercial anesthetic agent which has got acceptance among dental clinicians. This article provides a brief review about the efficacy of EMLA as a topical anesthetic agent when used during dental procedures.

  15. The efficacy of eutectic mixture of local anesthetics as a topical anesthetic agent used for dental procedures: A brief review

    PubMed Central

    Daneshkazemi, Alireza; Abrisham, Seyyed Mohammad; Daneshkazemi, Pedram; Davoudi, Amin

    2016-01-01

    Dental pain management is one of the most critical aspects of modern dentistry which might affect patient's quality of life. Several methods are suggested to provide a painless situation for patients. Desensitization of the oral site using topical anesthetics is one of those methods. The improvements of topical anesthetic agents are probably one of the most important advances in dental science in the past 100 years. Most of them are safe and can be applied on oral mucosa with minimal irritation and allergic reactions. At present, these agents are various with different potent and indications. Eutectic mixture of local anesthetics (EMLA) (lidocaine + prilocaine) is a commercial anesthetic agent which has got acceptance among dental clinicians. This article provides a brief review about the efficacy of EMLA as a topical anesthetic agent when used during dental procedures. PMID:27746520

  16. Lipid Emulsions Enhance the Norepinephrine-Mediated Reversal of Local Anesthetic-Induced Vasodilation at Toxic Doses

    PubMed Central

    Lee, Soo Hee; Sung, Hui-Jin; Ok, Seong-Ho; Yu, Jongsun; Choi, Mun-Jeoung; Lim, Jin Soo

    2013-01-01

    Purpose Intravenous lipid emulsions have been used to treat the systemic toxicity of local anesthetics. The goal of this in vitro study was to examine the effects of lipid emulsions on the norepinephrine-mediated reversal of vasodilation induced by high doses of levobupivacaine, ropivacaine, and mepivacaine in isolated endothelium-denuded rat aorta, and to determine whether such effects are associated with the lipid solubility of local anesthetics. Materials and Methods The effects of lipid emulsions (0.30, 0.49, 1.40, and 2.61%) on norepinephrine concentration-responses in high-dose local anesthetic (6×10-4 M levobupivacaine, 2×10-3 M ropivacaine, and 7×10-3 M mepivacaine)-induced vasodilation of isolated aorta precontracted with 60 mM KCl were assessed. The effects of lipid emulsions on local anesthetic- and diltiazem-induced vasodilation in isolated aorta precontracted with phenylephrine were also assessed. Results Lipid emulsions (0.30%) enhanced norepinephrine-induced contraction in levobupivacaine-induced vasodilation, whereas 1.40 and 2.61% lipid emulsions enhanced norepinephrine-induced contraction in both ropivacaine- and mepivacaine-induced vasodilation, respectively. Lipid emulsions (0.20, 0.49 and 1.40%) inhibited vasodilation induced by levobupivacaine and ropivacaine, whereas 1.40 and 2.61% lipid emulsions slightly attenuated mepivacaine (3×10-3 M)-induced vasodilation. In addition, lipid emulsions attenuated diltiazem-induced vasodilation. Lipid emulsions enhanced norepinephrine-induced contraction in endothelium-denuded aorta without pretreatment with local anesthetics. Conclusion Taken together, these results suggest that lipid emulsions enhance the norepinephrine-mediated reversal of local anesthetic-induced vasodilation at toxic anesthetic doses and inhibit local anesthetic-induced vasodilation in a manner correlated with the lipid solubility of a particular local anesthetic. PMID:24142661

  17. Lipid emulsions enhance the norepinephrine-mediated reversal of local anesthetic-induced vasodilation at toxic doses.

    PubMed

    Lee, Soo Hee; Sung, Hui-Jin; Ok, Seong-Ho; Yu, Jongsun; Choi, Mun-Jeoung; Lim, Jin Soo; Sohn, Ju-Tae

    2013-11-01

    Intravenous lipid emulsions have been used to treat the systemic toxicity of local anesthetics. The goal of this in vitro study was to examine the effects of lipid emulsions on the norepinephrine-mediated reversal of vasodilation induced by high doses of levobupivacaine, ropivacaine, and mepivacaine in isolated endothelium-denuded rat aorta, and to determine whether such effects are associated with the lipid solubility of local anesthetics. The effects of lipid emulsions (0.30, 0.49, 1.40, and 2.61%) on norepinephrine concentration-responses in high-dose local anesthetic (6×10(-4) M levobupivacaine, 2×10(-3) M ropivacaine, and 7×10(-3) M mepivacaine)-induced vasodilation of isolated aorta precontracted with 60 mM KCl were assessed. The effects of lipid emulsions on local anesthetic- and diltiazem-induced vasodilation in isolated aorta precontracted with phenylephrine were also assessed. Lipid emulsions (0.30%) enhanced norepinephrine-induced contraction in levobupivacaine-induced vasodilation, whereas 1.40 and 2.61% lipid emulsions enhanced norepinephrine-induced contraction in both ropivacaine- and mepivacaine-induced vasodilation, respectively. Lipid emulsions (0.20, 0.49 and 1.40%) inhibited vasodilation induced by levobupivacaine and ropivacaine, whereas 1.40 and 2.61% lipid emulsions slightly attenuated mepivacaine (3×10(-3) M)-induced vasodilation. In addition, lipid emulsions attenuated diltiazem-induced vasodilation. Lipid emulsions enhanced norepinephrine-induced contraction in endothelium-denuded aorta without pretreatment with local anesthetics. Taken together, these results suggest that lipid emulsions enhance the norepinephrine-mediated reversal of local anesthetic-induced vasodilation at toxic anesthetic doses and inhibit local anesthetic-induced vasodilation in a manner correlated with the lipid solubility of a particular local anesthetic.

  18. Clinical concentrations of chemically diverse general anesthetics minimally affect lipid bilayer properties

    PubMed Central

    Herold, Karl F.; Sanford, R. Lea; Lee, William; Andersen, Olaf S.; Hemmings, Hugh C.

    2017-01-01

    General anesthetics have revolutionized medicine by facilitating invasive procedures, and have thus become essential drugs. However, detailed understanding of their molecular mechanisms remains elusive. A mechanism proposed over a century ago involving unspecified interactions with the lipid bilayer known as the unitary lipid-based hypothesis of anesthetic action, has been challenged by evidence for direct anesthetic interactions with a range of proteins, including transmembrane ion channels. Anesthetic concentrations in the membrane are high (10–100 mM), however, and there is no experimental evidence ruling out a role for the lipid bilayer in their ion channel effects. A recent hypothesis proposes that anesthetic-induced changes in ion channel function result from changes in bilayer lateral pressure that arise from partitioning of anesthetics into the bilayer. We examined the effects of a broad range of chemically diverse general anesthetics and related nonanesthetics on lipid bilayer properties using an established fluorescence assay that senses drug-induced changes in lipid bilayer properties. None of the compounds tested altered bilayer properties sufficiently to produce meaningful changes in ion channel function at clinically relevant concentrations. Even supra-anesthetic concentrations caused minimal bilayer effects, although much higher (toxic) concentrations of certain anesthetic agents did alter lipid bilayer properties. We conclude that general anesthetics have minimal effects on bilayer properties at clinically relevant concentrations, indicating that anesthetic effects on ion channel function are not bilayer-mediated but rather involve direct protein interactions. PMID:28265069

  19. Local Anesthetics and Antipsychotic Phenothiazines Interact Nonspecifically with Membranes and Inhibit Hexose Transporters in Yeast

    PubMed Central

    Uesono, Yukifumi; Toh-e, Akio; Kikuchi, Yoshiko; Araki, Tomoyuki; Hachiya, Takushi; Watanabe, Chihiro K.; Noguchi, Ko; Terashima, Ichiro

    2016-01-01

    Action mechanisms of anesthetics remain unclear because of difficulty in explaining how structurally different anesthetics cause similar effects. In Saccharomyces cerevisiae, local anesthetics and antipsychotic phenothiazines induced responses similar to those caused by glucose starvation, and they eventually inhibited cell growth. These drugs inhibited glucose uptake, but additional glucose conferred resistance to their effects; hence, the primary action of the drugs is to cause glucose starvation. In hxt0 strains with all hexose transporter (HXT) genes deleted, a strain harboring a single copy of HXT1 (HXT1s) was more sensitive to tetracaine than a strain harboring multiple copies (HXT1m), which indicates that quantitative reduction of HXT1 increases tetracaine sensitivity. However, additional glucose rather than the overexpression of HXT1/2 conferred tetracaine resistance to wild-type yeast; therefore, Hxts that actively transport hexoses apparently confer tetracaine resistance. Additional glucose alleviated sensitivity to local anesthetics and phenothiazines in the HXT1m strain but not the HXT1s strain; thus, the glucose-induced effects required a certain amount of Hxt1. At low concentrations, fluorescent phenothiazines were distributed in various membranes. At higher concentrations, they destroyed the membranes and thereby delocalized Hxt1-GFP from the plasma membrane, similar to local anesthetics. These results suggest that the aforementioned drugs affect various membrane targets via nonspecific interactions with membranes. However, the drugs preferentially inhibit the function of abundant Hxts, resulting in glucose starvation. When Hxts are scarce, this preference is lost, thereby mitigating the alleviation by additional glucose. These results provide a mechanism that explains how different compounds induce similar effects based on lipid theory. PMID:26757771

  20. Local anesthetic toxicity and lipid resuscitation in pregnancy.

    PubMed

    Bern, Sarah; Weinberg, Guy

    2011-06-01

    Lipid emulsion has emerged as an effective treatment of local anesthetic-induced cardiac arrest, but its therapeutic application for the obstetric patient requires definition at present. This review discusses clinical reports, relevant laboratory studies, and future directions for the development of an optimal protocol for lipid resuscitation in pregnancy. Several mechanisms have been postulated to account for the apparent enhanced sensitivity to local anesthetic systemic toxicity during pregnancy. One case report of lipid resuscitation in the pregnant patient demonstrates favorable outcomes and supports the safety of lipid therapy. Current guidelines and case reports propose that a large bolus of lipid at the earliest signs of toxicity may prevent cardiovascular collapse. As the obstetric demographic becomes older and more obese, new technologies and strategies can assist in controlling maternal death and major morbidity secondary to anesthesia complications. Lipid resuscitation appears to be an effective treatment for toxicity induced by lipophilic medications and may be useful in treating systemic toxicity in the pregnant patient. Obstetric care providers should be aware of lipid resuscitation and consider its use as described by American Society of Regional Anesthesia and Pain Medicine guidelines.

  1. Preventive Analgesia by Local Anesthetics: The Reduction of Postoperative Pain by Peripheral Nerve Blocks and Intravenous Drugs

    PubMed Central

    Barreveld, Antje; Witte, Jürgen; Chahal, Harkirat; Durieux, Marcel E.; Strichartz, Gary

    2012-01-01

    The use of local anesthetics to reduce acute postoperative pain has a long history, but recent reports have not been systematically reviewed. In addition, the need to include only those clinical studies that meet minimum standards for randomization and blinding must be adhered to. In this review we have applied stringent clinical study design standards to identify publications on the use of perioperative local anesthetics. We first examined several types of peripheral nerve blocks, covering a variety of surgical procedures, and second, for effects of intentionally administered IV local anesthetic (lidocaine) for suppression of postoperative pain. Thirdly, we have examined publications in which vascular concentrations of local anesthetics were measured at different times after peripheral nerve block procedures, noting the incidence when those levels reached ones achieved during intentional IV administration. Importantly, the very large number of studies using neuraxial blockade techniques (epidural, spinal) has not been included in this review but will be dealt with separately in a later review. The overall results showed a strongly positive effect of local anesthetics, by either route, for suppressing postoperative pain scores and analgesic (opiate) consumption. In only a few situations were the effects equivocal. Enhanced effectiveness with the addition of adjuvants was not uniformly apparent. The differential benefits between drug delivery before, during, or immediately after a surgical procedure are not obvious, and a general conclusion is that the significant antihyperalgesic effects occur when the local anesthetic is present during the acute postoperative period, and its presence during surgery is not essential for this action. PMID:23408672

  2. Peripheral nerve catheters and local anesthetic infiltration in perioperative analgesia.

    PubMed

    Merritt, Christopher K; Mariano, Edward R; Kaye, Alan David; Lissauer, Jonathan; Mancuso, Kenneth; Prabhakar, Amit; Urman, Richard D

    2014-03-01

    Peripheral nerve catheters (PNCs) and local infiltration analgesia (LIA) represent valuable options for controlling perioperative pain. PNCs have been increasingly utilized to provide both surgical anesthesia and prolonged postoperative analgesia for a wide variety of procedures. PNCs can be more technically challenging to place than typical single-injection nerve blocks (SINB), and familiarity with the indications, contraindications, relevant anatomy, and appropriate technical skills is a prerequisite for the placement of any PNC. PNCs include risks of peripheral nerve injury, damage to adjacent anatomic structures, local anesthetic toxicity, intravascular injection, risks associated with motor block, risks of unnoticed injury to the insensate limb, and risks of sedation associated with PNC placement. In addition to these common risks, there are specific risks unique to each PNC insertion site. LIA strategies have emerged that seek to provide the benefit of targeted local anesthesia while minimizing collateral motor block and increasing the applicability of durable local anesthesia beyond the extremities. LIA involves the injection and/or infusion of a local anesthetic near the site of surgical incision to provide targeted analgesia. A wide variety of techniques have been described, including single-injection intraoperative wound infiltration, indwelling wound infusion catheters, and the recent high-volume LIA technique associated with joint replacement surgery. The efficacy of these techniques varies depending on specific procedures and anatomic locations. The recent incorporation of ultra-long-acting liposomal bupivacaine preparations has the potential to dramatically increase the utility of single-injection LIA. LIA represents a promising yet under-investigated method of postoperative pain control.

  3. Continuous spinal anesthesia with high dose of local anesthetics.

    PubMed

    Imbelloni, Luiz Eduardo; Neto, Savino Gasparini; Ganem, Eliana Marisa

    2010-01-01

    Better control of the level, intensity, and duration of spinal analgesia represents the greatest advantages of continuous spinal anesthesia. With the advent of intermediate catheters (over-the-needle catheter) and its low incidence of headaches and neurological symptoms, the technique has been gaining credibility. The objective of this paper is to report the possible safety of the new catheter with a large dose of hyperbaric 0.5% bupivacaine with 1.6% glucose associated with hyperbaric 2% lidocaine with 1.6% glucose. Male patient, 78 years old, 85 kg, 168 cm, physical status ASA III, with hypertension, coronary artery disease, and chronic renal failure. The patient was candidate for surgery for huge bilateral inguinal and umbilical hernias, being submitted to preoperative pneumoperitoneum for one week to stretch abdominal cavity. After venoclysis with an 18G catheter, he was monitored with cardioscope, non-invasive blood pressure, and pulse oximetry; he was sedated with 1 mg of midazolam and 100 μg of fentanyl intravenously, and placed in left lateral decubitus. He underwent continuous spinal anesthesia by a median puncture in L₃-L₄ with a set with a 27G cut-bevel needle and 22G catheter. The total dose of anesthetic used was 25mg of 0.5% bupivacaine (hyperbaric, with 1.6% glucose), 160 mg of 2% lidocaine (hyperbaric, with 1.6% glucose), and morphine (100 μg). The patient was followed-up until the 30th postoperative day without neurological complaints. Recently, the poor distribution of the local anesthetic through the microcatheter was attributed as the cause of cauda equina syndrome. This case report showed that, with the administration of high doses of hyperbaric anesthetics through the new catheter, poor distribution or risk of cauda equina syndrome were not observed. Copyright © 2010 Elsevier Editora Ltda. All rights reserved.

  4. Preparation and evaluation of bioadhesive dibucaine gels for enhanced local anesthetic action.

    PubMed

    Kang, Chung; Shin, Sang-Chul

    2010-08-01

    In relieving local pains, dibucaine, one of ester type local anesthetics, has been used. In case of their application such as ointments and creams, it is difficult to expect their effects for a required period of time, because they are easily removed by wetting, movement and contacting. To develop suitable bioadhesive gels, the bioadhesive force of hydroxypropyl cellulose (HPC) was tested using auto-peeling tester. The effect of drug concentration on drug release was studied from the prepared 2% HPC-HF gels using synthetic cellulose membrane at 37 +/- 0.5 degrees C. We investigated the enhancing effects on drug permeation into skins, using some kind of enhancers such as the glycols, the non-ionic surfactants, the fatty acids, and the propylene glycol derivatives. Anesthetic effects of dibucaine gels containing polyoxyethylene 2-oleyl ether were measured by tail flick analgesic meter. The bioadhesive force of various types of HPC such as GF, MF, and HF, was 0.0131, 0.0501, and 0.1346 N, at 2% HPC concentration, respectively. The HPC-HF gels showed the highest bioadhesive force. As the concentration of HPC-HF increased, the drug release increased. As the temperature increased, the drug release increased. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest enhancing effects. According to the rat tail flick test, 1% drug gels containing polyoxyethylene 2-oleyl ether showed the prolonged local anesthetic effects. In conclusion, the dibucaine gel containing penetration enhancer and vasoconstrictor showing enhanced local anesthetic action could be developed by using the bioadhesive polymer, HPC.

  5. Local Anesthetics Inhibit the Growth of Human Hepatocellular Carcinoma Cells.

    PubMed

    Le Gac, Grégoire; Angenard, Gaëlle; Clément, Bruno; Laviolle, Bruno; Coulouarn, Cédric; Beloeil, Hélène

    2017-08-29

    Hepatocellular carcinoma (HCC) is an aggressive cancer with limited therapeutic options. Retrospective studies have shown that the administration of local anesthetics (LAs) during cancer surgery could reduce cancer recurrence. Besides, experimental studies reported that LAs could inhibit the growth of cancer cells. Thus, the purpose of this study was to investigate the effects of LAs on human HCC cells. The effects of 2 LAs (lidocaine and ropivacaine) (10 to 10 M) were studied after an incubation of 48 hours on 2 HCC cell lines, namely HuH7 and HepaRG. Cell viability, cell cycle analysis, and apoptosis and senescence tests were performed together with unsupervised genome-wide expression profiling and quantitative real-time polymerase chain reaction for relevant genes. We showed that LAs decreased viability and proliferation of HuH7 cells (from 92% [P < .001] at 5 × 10 M to 40% [P = .02] at 10 M with ropivacaine and from 87% [P < .001] to 37% [P = .02] with lidocaine) and HepaRG progenitor cells (from 58% at 5 × 10 M [P < .001] to 29% at 10 M [P = .04] with lidocaine and 59% [P < .001] with ropivacaine 5 × 10 M) in concentration-dependent manner. LAs have no effect on well-differentiated HepaRG. Ropivacaine decreased the mRNA level of key cell cycle regulators, namely cyclin A2, cyclin B1, cyclin B2, and cyclin-dependent kinase 1, and the expression of the nuclear marker of cell proliferation MKI67. Lidocaine had no specific effect on cell cycle but increased by 10× the mRNA level of adenomatous polyposis coli (P < .01), which acts as an antagonist of the Wnt/β-catenin pathway. Both LAs increased apoptosis in Huh7 and HepaRG progenitor cells (P < .01). The data demonstrate that LAs induced profound modifications in gene expression profiles of tumor cells, including modulations in the expression of cell cycle-related genes that result in a cytostatic effect and induction of apoptosis.

  6. From micro- to nanostructured implantable device for local anesthetic delivery.

    PubMed

    Zorzetto, Laura; Brambilla, Paola; Marcello, Elena; Bloise, Nora; De Gregori, Manuela; Cobianchi, Lorenzo; Peloso, Andrea; Allegri, Massimo; Visai, Livia; Petrini, Paola

    2016-01-01

    Local anesthetics block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibers, and find application in the management of acute and chronic pain. Despite the key role they play in modern medicine, their cardio and neurotoxicity (together with their short half-life) stress the need for developing implantable devices for tailored local drug release, with the aim of counterbalancing their side effects and prolonging their pharmacological activity. This review discusses the evolution of the physical forms of local anesthetic delivery systems during the past decades. Depending on the use of different biocompatible materials (degradable polyesters, thermosensitive hydrogels, and liposomes and hydrogels from natural polymers) and manufacturing processes, these systems can be classified as films or micro- or nanostructured devices. We analyze and summarize the production techniques according to this classification, focusing on their relative advantages and disadvantages. The most relevant trend reported in this work highlights the effort of moving from microstructured to nanostructured systems, with the aim of reaching a scale comparable to the biological environment. Improved intracellular penetration compared to microstructured systems, indeed, provides specific drug absorption into the targeted tissue and can lead to an enhancement of its bioavailability and retention time. Nanostructured systems are realized by the modification of existing manufacturing processes (interfacial deposition and nanoprecipitation for degradable polyester particles and high- or low-temperature homogenization for liposomes) or development of novel strategies (electrospun matrices and nanogels). The high surface-to-volume ratio that characterizes nanostructured devices often leads to a burst drug release. This drawback needs to be addressed to fully exploit the advantage of the interaction between the target tissues and the drug: possible strategies

  7. From micro- to nanostructured implantable device for local anesthetic delivery

    PubMed Central

    Zorzetto, Laura; Brambilla, Paola; Marcello, Elena; Bloise, Nora; De Gregori, Manuela; Cobianchi, Lorenzo; Peloso, Andrea; Allegri, Massimo; Visai, Livia; Petrini, Paola

    2016-01-01

    Local anesthetics block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibers, and find application in the management of acute and chronic pain. Despite the key role they play in modern medicine, their cardio and neurotoxicity (together with their short half-life) stress the need for developing implantable devices for tailored local drug release, with the aim of counterbalancing their side effects and prolonging their pharmacological activity. This review discusses the evolution of the physical forms of local anesthetic delivery systems during the past decades. Depending on the use of different biocompatible materials (degradable polyesters, thermosensitive hydrogels, and liposomes and hydrogels from natural polymers) and manufacturing processes, these systems can be classified as films or micro- or nanostructured devices. We analyze and summarize the production techniques according to this classification, focusing on their relative advantages and disadvantages. The most relevant trend reported in this work highlights the effort of moving from microstructured to nanostructured systems, with the aim of reaching a scale comparable to the biological environment. Improved intracellular penetration compared to microstructured systems, indeed, provides specific drug absorption into the targeted tissue and can lead to an enhancement of its bioavailability and retention time. Nanostructured systems are realized by the modification of existing manufacturing processes (interfacial deposition and nanoprecipitation for degradable polyester particles and high- or low-temperature homogenization for liposomes) or development of novel strategies (electrospun matrices and nanogels). The high surface-to-volume ratio that characterizes nanostructured devices often leads to a burst drug release. This drawback needs to be addressed to fully exploit the advantage of the interaction between the target tissues and the drug: possible strategies

  8. Efficacy of articaine: a new amide local anesthetic.

    PubMed

    Malamed, S F; Gagnon, S; Leblanc, D

    2000-05-01

    The authors compared the safety and efficacy of 4 percent articaine with epinephrine 1:100,000 with 2 percent lidocaine with epinephrine 1:100,000. In three identical randomized, double-blind, multicenter trials, subjects 4 to 80 years of age received either 4 percent articaine with epinephrine 1:100,000 or 2 percent lidocaine with epinephrine 1:100,000 for simple or complex dental procedures. In each trial, the authors randomized the subjects in a 2:1 ratio to receive articaine or lidocaine. Efficacy was determined by both subject and investigator using a visual analog scale, or VAS. The authors used the Kruskal-Wallis test to analyze the data. A total of 882 subjects received articaine, and 443 received lidocaine. The authors found no statistical differences between the groups (P = .05). They also compared drug volumes for both articaine and lidocaine groups (2.5 milliliters +/- 0.07 standard error of mean, or SEM, vs. 2.6 mL +/- 0.09 SEM for simple procedures and 4.2 mL +/- 0.15 SEM vs. 4.5 mL +/- 0.21 SEM for complex procedures). The procedures' durations were comparable for both the articaine and lidocaine groups. The authors found no statistical difference between the two treatment groups (P = .05) with respect to subject or investigator pain ratings using the VAS; the mean pain scores determined by both patients and investigators for all groups tested were less than 1.0. The authors found that 4 percent articaine with epinephrine 1:100,000 was well-tolerated in 882 subjects. It also provided clinically effective pain relief during most dental procedures and had a time to onset and duration of anesthesia appropriate for clinical use and comparable to those observed for other commercially available local anesthetics. Pain control is a major component of patient comfort and safety. Local anesthetics form the backbone of pain control techniques in dentistry. Four percent articaine with epinephrine is an amide local anesthetic that will meet the clinical

  9. Loss of anatomical landmarks with eutectic mixture of local anesthetic cream for neonatal male circumcision.

    PubMed

    Plank, Rebeca M; Kubiak, David W; Abdullahi, Rasak Bamidele; Ndubuka, Nnamdi; Nkgau, Maggie M; Dapaah-Siakwan, Fredrick; Powis, Kathleen M; Lockman, Shahin

    2013-02-01

    We report two cases of newborns who developed marked local edema after application of a eutectic mixture of local anesthetic (EMLA) topical anesthetic cream for neonatal male circumcision (NMC). Although local edema and erythema are known potential side effects of EMLA cream, a common anesthetic used for NMC, the loss of landmarks precluding safe NMC has not previously been reported, and is described here. Although we cannot recommend an alternate local anesthetic for neonates with this reaction to EMLA, based on a review of the published data we think that serious systemic adverse events related to EMLA are extremely rare.

  10. Development of Bioadhesive Transdermal Bupivacaine Gels for Enhanced Local Anesthetic Action

    PubMed Central

    Cho, Cheong-Weon; Kim, Deok-Bae; Shin, Sang-Chul

    2012-01-01

    Topical drug dosage forms such as ointments and creams can be easily removed through wetting, movement and contact. The new bioadhesive formulations with enhanced local anesthetic effects are needed for topical administration. The adhesive capacity of hydroxypropyl methylcellulose (HPMC) was determined by measuring the maximum detachment force and the adhesion work with an auto peeling tester. The release of drug from a HPMC gel was studied according to the drug concentration. Permeation study through the rat skin was performed at 37°C using phosphate buffer solution (pH = 7.4) as a receptor medium. To increase the skin permeation of bupivacaine from the HPMC gels, penetration enhancer such as the saturated and unsaturated fatty acids, the pyrrolidones, the propylene glycol derivatives, the glycerides, and the non-ionic surfactants were incorporated in the bupivacaine-HPMC gels. The local anesthetic effect of the formulated gel preparation was examined using a tail-flick analgesimeter. As the concentration of HPMC increased, the bioadhesive force and viscosity were increased. The rate of drug release was increased with increasing the drug concentration. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the most enhancing effects on drug permeation through the skin. In the rat tail flick test, the area under the efficacy curve of bupivacaine gel containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed a 2.36-fold increase in anesthetic activity compared to control gel without any additives. The bupivacaine gels containing both penetration enhancer and vasoconstrictor showed enhancement and prolonged efficacy compared to the control gel. To enhance the local anesthetic effects of bupivacaine, the transdermal bupivacaine gel formulation containing penetration enhancer and vasoconstrictor could be developed. PMID:24250466

  11. 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.

  12. A local scavenging system to remove waste anesthetic gases during general anesthesia.

    PubMed

    Li, Shou-Huang; Li, Shou-Nan; Shih, Hui-Ya; Chiou, Shin-Fu; Yi, Hann-De

    2004-06-01

    A local scavenging system was constructed and tested in both the operating room and the laboratory to remove the waste anesthetic gases so as to lower the exposure risk of the anesthetic personnel. A local scavenging system was developed to suck away the waste anesthetic gases (e.g., N2O and sevoflurane) escaping from the mouth and nostrils of a patient. The local scavenging system used was composed of an inlet funnel (with a diameter of 20 cm), a flexible connecting tubing, a high efficiency particulate air (HEPA) filter and a vacuum pump. To help evaluate the performance of the local scavenging system, a tracer gas (SF6) of a fixed concentration (= 200 ppm) and flow rate (= 5 l/min) was introduced around the nostrils of the patient during anesthesia. The concentrations of the gases (SF6, N2O and SEV) drawn away by the scavenging system were then determined by an extractive Fourier transform infrared (FTIR) spectrometer and those spreading around the breathing zone of the anesthesiologist were obtained by the other FTIR. In the laboratory tests, the relationship between the scavenging efficiency and the inlet funnel position was obtained using the aforementioned SF6-FTIR techniques. With the application of this local scavenging system, during three surgical operations, the average personnel exposure concentrations of N2O and sevoflurane (SEV) as measured were 8.7 and 0.06 ppm, respectively. Both measured concentrations were lower than the TWA values recommended by the US-NIOSH for N2O (= 25 ppm) and SEV (= 2 ppm). Based on the tracer gas (SF6) results, it was found that the average scavenging efficiency was equal to 87%, which was lower than the laboratory testing results of 95%. The (scavenging) efficiency difference between the laboratory and on-site tests could be due to the movement and action of the anesthesiologist during anesthesia. To optimize the performance of the local scavenging device, the inlet (funnel) should be placed close to the breathing region

  13. [Intravenous regional anesthesia with long-acting local anesthetics. An update].

    PubMed

    Atanassoff, P G; Lobato, A; Aguilar, J L

    2014-02-01

    Intravenous regional anesthesia is a widely used technique for brief surgical interventions, primarily on the upper limbs and less frequently, on the lower limbs. It began being used at the beginning of the 20th century, when Bier injected procaine as a local anesthetic. The technique to accomplish anesthesia has not changed much since then, although different drugs, particularly long-acting local anesthetics, such as ropivacaine and levobupivacaine in low concentrations, were introduced. Additionally, drugs like opioids, muscle relaxants, paracetamol, neostigmine, magnesium, ketamine, clonidine, and ketorolac, have all been investigated as adjuncts to intravenous regional anesthesia, and were found to be fairly useful in terms of an increased onset of operative anesthesia and longer lasting perioperative analgesia. The present article provides an overview of current knowledge with emphasis on long-acting local anesthetic drugs. Copyright © 2013 Sociedad Española de Anestesiología, Reanimación y Terapéutica del Dolor. Published by Elsevier España. All rights reserved.

  14. The Sodium Channel as a Target for Local Anesthetic Drugs

    PubMed Central

    Fozzard, Harry A.; Sheets, Michael F.; Hanck, Dorothy A.

    2011-01-01

    Na channels are the source of excitatory currents for the nervous system and muscle. They are the target for a class of drugs called local anesthetics (LA), which have been used for local and regional anesthesia and for excitatory problems such as epilepsy and cardiac arrhythmia. These drugs are prototypes for new analgesic drugs. The drug-binding site has been localized to the inner pore of the channel, where drugs interact mainly with a phenylalanine in domain IV S6. Drug affinity is both voltage- and use-dependent. Voltage-dependency is the result of changes in the conformation of the inner pore during channel activation and opening, allowing high energy interaction of drugs with the phenylalanine. LA drugs also reduce the gating current of Na channels, which represents the movement of charged residues in the voltage sensors. Specifically, drug binding to phenylalanine locks the domain III S4 in its outward (activated) position, and slows recovery of the domain IV S4. Although strongly affecting gating, LA drugs almost certainly also block by steric occlusion of the pore. Molecular definition of the binding and blocking interactions may help in new drug development. PMID:22053156

  15. Extended duration local anesthetic agent in a rat paw model.

    PubMed

    Ickowicz, D E; Golovanevski, L; Domb, A J; Weiniger, C F

    2014-07-01

    Encapsulated local anesthetics extend postoperative analgesic effect following site-directed nerve injection; potentially reducing postoperative complications. Our study aim was to investigate efficacy of our improved extended duration formulation - 15% bupivacaine in poly(DL-lactic acid co castor oil) 3:7 synthesized by ring opening polymerization. In vitro, around 70% of bupivacaine was released from the p(DLLA-CO) 3:7 after 10 days. A single injection of the optimal formulation of 15% bupivacaine-polymer or plain (0.5%) bupivacaine (control), was injected via a 22G needle beside the sciatic nerve of Sprague-Dawley rats under anesthesia; followed (in some animals) by a 1cm longitudinal incision through the skin and fascia of the paw area. Behavioral tests for sensory and motor block assessment were done using Hargreave's hot plate score, von Frey filaments and rearing count. The 15% bupivacaine formulation significantly prolonged sensory block duration up to at least 48 h. Following surgery, motor block was observed for 48 h following administration of bupivacaine-polymer formulation and rearing was reduced (returning to baseline after 48 h). No significant differences in mechanical nociceptive response were observed. The optimized bupivacaine-polymer formulation prolonged duration of local anesthesia effect in our animal model up to at least 48 h.

  16. Evolving Role of Local Anesthetics in Managing Postsurgical Analgesia.

    PubMed

    Golembiewski, Julie; Dasta, Joseph

    2015-06-01

    Opioid analgesics, the cornerstone of effective postsurgical pain management, may be associated with risk of opioid-related adverse drug events (ADEs) that may complicate the postsurgical experience. Perioperative multimodal analgesic regimens have the potential to improve postsurgical pain control and may permit use of lower analgesic doses and reduce the incidence of opioid-related ADEs. Utility of traditional local anesthetic formulations to provide analgesia over the entire postsurgical period is limited by their short duration of action. Liposome bupivacaine, a liposomal formulation of bupivacaine indicated for single-dose administration into the surgical site to produce postsurgical analgesia, was evaluated in multiple surgical models as part of multimodal analgesic regimens and was found in clinical trials to provide postsurgical analgesia for up to 72 hours. Here, we provide an overview of the available multimodal analgesic options and recent recommendations for optimal postsurgical pain management. A review of the literature was conducted, and results from recent clinical trials are included. The use of a multimodal analgesic regimen, including liposome bupivacaine, can extend the time to first postsurgical opioid use, may reduce postsurgical opioid consumption, and reduce hospital length of stay and costs compared with an opioid-only analgesic regimen. Use of multimodal analgesic regimens is a practical way to achieve good postsurgical analgesia while minimizing reliance on opioids and associated adverse events. Taken as a whole, evidence from the clinical studies of liposome bupivacaine suggests this local anesthetic formulation may be a useful component of multimodal analgesic regimens for managing postsurgical pain in select patients, with the potential to reduce opioid use and opioid-related ADEs in the postsurgical setting. As with bupivacaine, appropriate use of liposome bupivacaine to optimize clinical effects, economic implications, and patient

  17. Comparative study on anesthetic potency of dental local anesthetics assessed by the jaw-opening reflex in rabbits.

    PubMed Central

    Miyoshi, T.; Aida, H.; Kaneko, Y.

    2000-01-01

    The potency of 4 local anesthetics to dental pulp was compared. Drugs were 4% articaine with 12 microgram/mL epinephrine (A12), 4% articaine with 6 microgram/mL epinephrine (A6), 2% lidocaine with 12.5 microgram/mL epinephrine (L), and 3% propitocaine with 0.03 IU/mL felypressin (P). Local anesthetics were injected into the dental root of the mandibular incisor. Electromyogram (EMG) of the digastric muscle was measured during the jaw-opening reflex induced by electrical stimulation. The disappearance of the EMG wave was judged as positive evidence of anesthesia. The determination of ED50 of the anesthetic was made by probit analysis. The ED50 of the A12 was minimal in all the tested anesthetics throughout the entire course. The potency in the A6 was 2.8 times that of the L. The potency of the A12 at the 15-minute measurement was 3.8 times that of the A6. The ED50 of the P was higher compared with those of the other 3 groups. It was concluded that articaine showed quicker onset than lidocaine and propitocaine and that there was a need to increase the dosage to attain a quick onset or to extend the duration. PMID:11881694

  18. Infrared image monitoring of local anesthetic poisoning in rats.

    PubMed

    Carstens, Angelo Manoel G; Tambara, Elizabeth Milla; Colman, Daniel; Carstens, Márcio G; Matias, Jorge Eduardo Fouto

    To evaluate the thermographic predictive value of local anesthetic poisoning in rats that indicates the early recognition of thermal signs of intoxication and enable the immediate start of advanced life support. Wistar rats underwent intraperitoneal injection of saline and ropivacaine; they were allocated into pairs, and experiments performed at baseline and experimental times. For thermography, central and peripheral compartment were analyzed, checking the maximum and average differences of temperatures between groups. Thermographic and clinical observations were performed for each experiment, and the times in which the signs of intoxication occurred were recorded. In the thermal analysis, the thermograms corresponding to the times of interest were sought and relevant data sheets extracted for statistical analysis. Basal and experimental: the display of the thermal images at times was possible. It was possible to calculate the heat transfer rate in all cases. At baseline it was possible to see the physiology of microcirculation, characterized by thermal distribution in the craniocaudal direction. It was possible to visualize the pathophysiological changes or thermal dysautonomias caused by intoxication before clinical signs occur, characterized by areas of hyper-radiation, translating autonomic nervous system pathophysiological disorders. In animals poisoned by ropivacaine, there was no statistically significant difference in heat transfer rate at the experimental time. The maximum temperature, medium temperature, and heat transfer rate were different from the statistical point of view between groups at the experimental time, thus confirming the systemic thermographic predictive value. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  19. [Infrared image monitoring of local anesthetic poisoning in rats].

    PubMed

    Carstens, Angelo Manoel G; Tambara, Elizabeth Milla; Colman, Daniel; Carstens, Márcio G; Matias, Jorge Eduardo Fouto

    To evaluate the thermographic predictive value of local anesthetic poisoning in rats that indicates the early recognition of thermal signs of intoxication and enable the immediate start of advanced life support. Wistar rats underwent intraperitoneal injection of saline and ropivacaine; they were allocated into pairs, and experiments performed at baseline and experimental times. For thermography, central and peripheral compartment were analyzed, checking the maximum and average differences of temperatures between groups. Thermographic and clinical observations were performed for each experiment, and the times in which the signs of intoxication occurred were recorded. In the thermal analysis, the thermograms corresponding to the times of interest were sought and relevant data sheets extracted for statistical analysis. Basal and experimental: the display of the thermal images at times was possible. It was possible to calculate the heat transfer rate in all cases. At baseline it was possible to see the physiology of microcirculation, characterized by thermal distribution in the craniocaudal direction. It was possible to visualize the pathophysiological changes or thermal dysautonomias caused by intoxication before clinical signs occur, characterized by areas of hyper-radiation, translating Autonomic Nervous System pathophysiological disorders. In animals poisoned by ropivacaine, there was no statistically significant difference in heat transfer rate at the experimental time. The maximum temperature, medium temperature, and heat transfer rate were different from the statistical point of view between groups at the experimental time, thus confirming the systemic thermographic predictive value. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  20. 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

  1. 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.

  2. Local anesthetics, pulpal blood flow and C. Edmund Kells.

    PubMed

    Gutmann, James L

    2011-01-01

    Historically there was an attempt by many dental practitioners to implicate anesthetic solutions in the death of the dental pulp. However, their implications may or may not have been valid, as damage to the dental pulp may have resulted from excessive and deleterious restorative procedures on teeth that were anesthetized. Unfortunately little was known about the anesthetic solutions at that time, their composition, which included vasoconstrictors, and their potential to alter pulpal blood flow. This paper will explore both the historical perspectives and concerns regarding the impact of anesthetic solutions on the dental pulp through the eyes of Dr. C. Edmund Kells, along with the contemporary perspectives and realities through the eyes of science, sound research data and clinical practice.

  3. Inhibition of the transthylakoid gradient of electrochemical proton potential by the local anesthetic dibucaine.

    PubMed

    Laasch, H; Schumann, J; Günther, G

    1991-03-01

    The effects of the local anesthetic dibucaine on coupling between electron transport and ATP synthesis-hydrolysis by the coupling-factor complex (CF0CF1 ATPase) were investigated in thylakoid membranes from Spinacia oleracea L. cv. Monatol. Evidence is presented that inhibition of ATP synthesis was produced by a specific uncoupling mechanism which was based on dibucaine-membrane surface interactions rather than on the interaction of dibucaine with the ATPase complex. Dibucaine reduced the osmotic space of thylakoid vesicles. At low pH of the medium it stimulated ATP hydrolysis beyond the rates obtained with optimum concentrations of 'classical' uncouplers. After addition of dibucaine, there was displacement of membrane-bound Mg(2+) and strong thylakoid stacking in the presence of only low Mg(2+) concentrations. Inhibition of ATP synthesis and transmembrane pH gradient increased with medium pH. Hydrolysis of ATP by isolated CF1 and the CF0CF1 complex was only slightly affected by dibucaine. The data are discussed assuming the involvement of localized proton channels on the membrane surface in protonic coupling of electron transport and ATP synthesis. A hypothesis for the mechanisms of action of local anesthetics at the thylakoid membrane is presented.

  4. Comparison of use of an infrared anesthetic gas monitor and refractometry for measurement of anesthetic agent concentrations.

    PubMed

    Ambrisko, Tamas D; Klide, Alan M

    2011-10-01

    To assess agreement between anesthetic agent concentrations measured by use of an infrared anesthetic gas monitor (IAGM) and refractometry. SAMPLE-4 IAGMs of the same type and 1 refractometer. Mixtures of oxygen and isoflurane, sevoflurane, desflurane, or N(2)O were used. Agent volume percent was measured simultaneously with 4 IAGMs and a refractometer at the common gas outlet. Measurements obtained with each of the 4 IAGMs were compared with the corresponding refractometer measurements via the Bland-Altman method. Similarly, Bland-Altman plots were also created with either IAGM or refractometer measurements and desflurane vaporizer dial settings. Bias ± 2 SD for comparisons of IAGM and refractometer measurements was as follows: isoflurane, -0.03 ± 0.18 volume percent; sevoflurane, -0.19 ± 0.23 volume percent; desflurane, 0.43 ± 1.22 volume percent; and N(2)O, -0.21 ± 1.88 volume percent. Bland-Altman plots comparing IAGM and refractometer measurements revealed nonlinear relationships for sevoflurane, desflurane, and N(2)O. Desflurane measurements were notably affected; bias ± limits of agreement (2 SD) were small (0.1 ± 0.22 volume percent) at < 12 volume percent, but both bias and limits of agreement increased at higher concentrations. Because IAGM measurements did not but refractometer measurements did agree with the desflurane vaporizer dial settings, infrared measurement technology was a suspected cause of the nonlinear relationships. Given that the assumption of linearity is a cornerstone of anesthetic monitor calibration, this assumption should be confirmed before anesthetic monitors are used in experiments.

  5. Stereostructure-based differences in the interactions of cardiotoxic local anesthetics with cholesterol-containing biomimetic membranes.

    PubMed

    Tsuchiya, Hironori; Ueno, Takahiro; Mizogami, Maki

    2011-06-01

    Amide-type pipecoloxylidide local anesthetics, bupivacaine, and ropivacaine, show cardiotoxic effects with the potency depending on stereostructures. Cardiotoxic drugs not only bind to cardiomyocyte membrane channels to block them but also modify the physicochemical property of membrane lipid bilayers in which channels are embedded. The opposite configurations allow enantiomers to be discriminated by their enantiospecific interactions with another chiral molecule in membranes. We compared the interactions of local anesthetic stereoisomers with biomimetic membranes consisting of chiral lipid components, the differences of which might be indicative of the drug design for reducing cardiotoxicity. Fluorescent probe-labeled biomimetic membranes were prepared with cardiolipin and cholesterol of varying compositions and different phospholipids. Local anesthetics were reacted with the membrane preparations at a cardiotoxically relevant concentration of 200 μM. The potencies to interact with biomimetic membranes and change their fluidity were compared by measuring fluorescence polarization. All local anesthetics acted on lipid bilayers to increase membrane fluidity. Chiral cardiolipin was ineffective in discriminating S(-)-enantiomers from their antipodes. On the other hand, cholesterol produced the enantiospecific membrane interactions of bupivacaine and ropivacaine with increasing its composition in membranes. In 40 mol% and more cholesterol-containing membranes, the membrane-interacting potency was S(-)-bupivacaine

  6. New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles.

    PubMed

    Beiranvand, Siavash; Eatemadi, Ali; Karimi, Arash

    2016-12-01

    Lipid nanoparticles (liposomes) were first described in 1965, and several work have led to development of important technical advances like triggered release liposomes and drug-loaded liposomes. These advances have led to numerous clinical trials in such diverse areas such as the delivery of anti-cancer, antifungal, and antibiotic drugs; the delivery of gene medicines; and most importantly the delivery of anesthesia drugs. Quite a number of liposomes are on the market, and many more are still in developmental stage. Lipid nanoparticles are the first nano-medicine delivery system to be advanced from laboratory concept to clinical application with high considerable clinical acceptance. Drug delivery systems for local anesthetics (LAs) have caught the interest of many researchers because there are many biomedical advantages connected to their application. There have been several formulation techniques to systemically deliver LA that include encapsulation in liposomes and complexation in cyclodextrins, nanoparticles, and to a little extent gold nanoparticles. The proposed formulations help to decrease the LA concentration utilized, increase its permeability, and most importantly increase the localization of the LA for a long period of time thereby leading to increase in the duration of the LA effect and finally to reduce any local and systemic toxicity. In this review, we will highlight on new updates pertaining to drug delivery of local anesthetics in particular bupivacaine using lipid nanoparticles.

  7. New Updates Pertaining to Drug Delivery of Local Anesthetics in Particular Bupivacaine Using Lipid Nanoparticles

    NASA Astrophysics Data System (ADS)

    Beiranvand, Siavash; Eatemadi, Ali; Karimi, Arash

    2016-06-01

    Lipid nanoparticles (liposomes) were first described in 1965, and several work have led to development of important technical advances like triggered release liposomes and drug-loaded liposomes. These advances have led to numerous clinical trials in such diverse areas such as the delivery of anti-cancer, antifungal, and antibiotic drugs; the delivery of gene medicines; and most importantly the delivery of anesthesia drugs. Quite a number of liposomes are on the market, and many more are still in developmental stage. Lipid nanoparticles are the first nano-medicine delivery system to be advanced from laboratory concept to clinical application with high considerable clinical acceptance. Drug delivery systems for local anesthetics (LAs) have caught the interest of many researchers because there are many biomedical advantages connected to their application. There have been several formulation techniques to systemically deliver LA that include encapsulation in liposomes and complexation in cyclodextrins, nanoparticles, and to a little extent gold nanoparticles. The proposed formulations help to decrease the LA concentration utilized, increase its permeability, and most importantly increase the localization of the LA for a long period of time thereby leading to increase in the duration of the LA effect and finally to reduce any local and systemic toxicity. In this review, we will highlight on new updates pertaining to drug delivery of local anesthetics in particular bupivacaine using lipid nanoparticles.

  8. Additives to local anesthetics for peripheral nerve blocks or local anesthesia: a review of the literature.

    PubMed

    Opperer, Mathias; Gerner, Peter; Memtsoudis, Stavros G

    2015-01-01

    A multitude of studies have focused on individual additives to local anesthetics and their effect on quality, onset, duration, spread and selectivity, as well as the potential toxic effects of their use. This review aims to give a broad overview of the current evidence in this developing field, based on beneficial and adverse effects of these drugs. We discuss the limitations of the available data and hope to convey implications and future perspectives for clinicians and researchers alike.

  9. Obtaining written informed consent for the administration of local anesthetic in dentistry.

    PubMed

    Orr, Daniel L; Curtis, William J

    2005-11-01

    The purpose of this study was to examine the frequency with which dentists obtain written informed consent for the administration of local anesthetic in dentistry. The authors administered an informal survey to 252 dentists. Most respondents who practiced a dental specialty or limited their practice to anesthesiology for dentistry obtained written informed consent for the administration of local anesthetic. Most general practitioners did not. Written informed consent appears to be obtained more often by dental specialists and dentists limiting their practices to anesthesiology for dentistry than by general practitioners. All dentists may want to consider obtaining written informed consent for the administration of local anesthetic.

  10. How Local Anesthetics affect the structural and dynamical properties of bio-membranes

    NASA Astrophysics Data System (ADS)

    Yi, Zheng; Nagao, Michihiro; Bossev, Dobrin

    2009-03-01

    To address the question of how local anesthetics influences the structural and dynamical properties of bio-membranes, neutron-spin echo spectroscopy (NSE) has been performed on 1,2-Dimyristoyl-sn-Glycero-3-Phosphocholine (DMPC) unilamellar vesicles (ULV) with different concentrations of Lidocaine in D2O to study the influence of Lidocaine on the bending elasticity of DMPC ULV bilayers in fluid crystal (L&_slash;alpha) phase and the ripple gel (P&_slash;beta') phase; The measurement of small-angle neutron scattering (SANS) has been performed to determine the bilayer thickness as a function of the concentration of Lidocaine. In the existence of molecules of Lidocaine the bending elasticity of DMPC bilayers was increased 30&%slash; -100&%slash; in L&_slash;alpha phase. The NSE data confirmed that fluid crystal/ripple gel transition temperature of DMPC bilayers was depressed by the addition of local anesthetics, which has also been examined via differential scanning calorimetry (DSC).

  11. Local anesthetic effects of cocaethylene and isopropylcocaine on rat peripheral nerves.

    PubMed

    Tokuno, Hajime A; Bradberry, Charles W; Everill, Brian; Agulian, Samuel K; Wilkes, Steven; Baldwin, Ronald M; Tamagnan, Gilles D; Kocsis, Jeffery D

    2004-01-23

    Cocaethylene is a naturally occurring cocaine derivative that has been used as a tool in both clinical studies of cocaine reward and as a potential model compound for agonist substitution therapy in cocaine dependence. It is equipotent to cocaine at inhibiting dopamine uptake in-vitro and in-vivo. Because it has been reported that local anesthetic properties may influence the reinforcing effects of dopamine uptake inhibitors, we investigated the local anesthetic properties of cocaethylene as well as isopropylcocaine, another potential pharmacological tool in studies of cocaine reward and agonist substitution therapy. We compared the efficacy of nerve impulse blockade by lidocaine, cocaine, cocaethylene and isopropylcocaine using rat sciatic nerves and dorsal roots (DRs). Nerves were placed in a modified sucrose gap chamber and repetitively stimulated at high frequency. The amplitude of compound action potentials (CAPs) at the beginning and end of each stimulus train was measured before and after exposure to each compound. All compounds produced concentration-dependent and use-dependent decrements in CAP amplitude, but cocaethylene and isopropylcocaine at medium to high concentration (0.375-1.875 mM) showed a more prolonged block after washout relative to cocaine or lidocaine. Patch clamp studies on dorsal root ganglion (DRG) neurons indicated a use-dependent blockade of sodium channels. These studies provide a more complete understanding of the pharmaocology of potential agonist treatment candidates, and suggest a mechanism whereby cocaethylene produces a decreased euphoria in humans compared to cocaine.

  12. PROPOFOL AS AN IMMERSION ANESTHETIC AND IN A MINIMUM ANESTHETIC CONCENTRATION (MAC) REDUCTION MODEL IN GOLDFISH (CARASSIUS AURATUS).

    PubMed

    Balko, Julie A; Wilson, Sarah K; Lewbart, Gregory A; Gaines, Brian R; Posner, Lysa P

    2017-03-01

    Propofol is a novel immersion anesthetic in goldfish ( Carassius auratus ). Objectives were to characterize propofol as an anesthetic and assess its suitability in a minimum anesthetic concentration (MAC) reduction model. Using a crossover design, eight goldfish were submerged in 1, 5, or 10 mg/L propofol. Data included induction time, recovery time, heart rate, opercular rate, and response to supramaximal stimulation. Baseline MAC (Dixon's up-and-down method) was determined, and 15 fish were anesthetized with propofol on 4 consecutive days with MAC determination on the fifth day, weekly, for 1 mo. Using a crossover design, MAC of propofol (n = 15) was determined 1 hr following administration of i.m. butorphanol 0.05, 0.5, and 1 mg/kg, dexmedetomidine 0.01, 0.02, and 0.04 mg/kg, ketoprofen 0.5, 1, and 2 mg/kg, morphine 5, 10, and 15 mg/kg, or saline 1 ml/kg. Comparisons were performed with Wilcoxon signed-rank tests (P < 0.05) and Tango's score confidence interval. Propofol at 1 mg/L did not produce anesthesia. Induction time with 10 mg/L (112, 84-166 s) was faster than 5 mg/L (233, 150-289 s; P = 0.0078). Heart and opercular rates for 5 and 10 mg/L were 36 (24-72) beats/min, 58 (44-68) operculations/min and 39 (20-48) beats/min, 57 (48-80) operculations/min, respectively. Recovery time was 249 (143-396) s and 299 (117-886) s with 5 and 10 mg/L, respectively. Response to supramaximal stimulation was not significantly different with 5 mg/L (1/8) compared with 10 mg/L (0/8). Baseline and weekly MAC following daily exposure was 8.4 and 9.0, 8.1, 8.1, and 8.7 mg/L, respectively. MAC reduction was no more than 8% following any drug or dosage. Propofol at 5 and 10 mg/L produced anesthesia, and anesthetic needs were similar following repeated exposure. Propofol was not suitable to test MAC reduction in goldfish in this study.

  13. [The action of Carpule-delivered local anesthetics and their combinations with vasoconstrictors].

    PubMed

    Anisimova, E N; Zorian, E V; Shugaĭlov, I A

    1998-01-01

    Analysis of published data on the effects of drugs used in dentistry for local analgesia and of the authors' findings will help the dentists properly select adequate analgesia with due consideration for the extent of intervention and patient's condition. Study of carpulated local amide anesthetics lidocaine, mepivacaine, and articaine revealed the relationship between the efficacy of anesthesia and its effects on cardiovascular system, on the one hand, and the anesthetic proper, presence of a vasoconstrictor, and type of anesthesia, on the other.

  14. Epinephrine: Systemic Effects and Varying Concentrations in Local Anesthesia

    PubMed Central

    Cassidy, James P.; Phero, James C.; Grau, William H.

    1986-01-01

    The range of vasoconstrictors available for use with local anesthetics in dentistry has been reviewed with emphasis on epinephrine and its physiological effects. All of the vasoconstrictors reviewed provide satisfactory results in dental anesthetic solutions when administered in appropriate concentrations and volumes. Possible drug interactions of concern to dentists include the use of vasoconstrictors with inhalational anesthetics, tricyclic antidepressants, beta blockers and, possibly, phenothiazines. Data reviewed indicates that the amounts of epinephrine used in dentistry can result in significant elevations in circulating levels of ephinephrine and concomitant physiologic changes. Evidence reviewed suggests that 1:200,000 epinephrine concentration results in optional duration and depth of local anesthesia. With the potential for adverse effects from epinephrine concentrations that are needlessly increased, it appears that in most clinical situations a 1:200,000 concentration of epinephrine can be used in an efficacious manner. PMID:3544965

  15. Hypersensitivity dermatitis following suction-assisted lipectomy: a complication of local anesthetic.

    PubMed

    Fine, P G; Dingman, D L

    1988-06-01

    We report a case of severe dermatitis involving the abdomen and thighs following suction-assisted lipectomy of these areas wherein local anesthetic containing the preservative methylparaben was used for infiltrative anesthesia. This use of local anesthetics with epinephrine can be of value in the performance of suction-assisted lipectomy to reduce blood loss, serve as an adjunct to other intraoperative anesthetic techniques, and for postoperative analgesia. Local anesthetic solutions commonly contain additives, which serve as antioxidants and antimicrobials. The most common of these preservatives is methylparaben, which can cause delayed hypersensitivity reactions. These reactions may be neither recognized nor clinically significant in small areas of infection, whereas in large body surface infiltrative procedures, such as suction-assisted lipectomy, these reactions may be of considerable consequence. This article reviews the pathophysiology and treatment of these reactions and gives recommendations for avoiding them.

  16. Inhibition of Kv7/M Channel Currents by the Local Anesthetic Chloroprocaine.

    PubMed

    Zhang, Fan; Cheng, Yanxin; Li, Hong; Jia, Qingzhong; Zhang, Hailin; Zhao, Senming

    2015-01-01

    Chloroprocaine is a local ester anesthetic, producing excellent sensory block in clinical use. The Kv7/M potassium channel plays an important role in the control of neuronal excitability. In this study, we investigated the effects of the local anesthetic chloroprocaine on Kv7/M channels as well as the effect of retigabine on chloroprocaine-induced seizures. A perforated whole-cell patch technique was used to record Kv7 currents from HEK293 cells and M-type currents from rat dorsal root ganglion (DRG) neurons. Chloroprocaine produced a number of effects on Kv7.2/Kv7.3 currents, including a lowering of current amplitudes, a rightward shift in the voltage-dependent activation curves, and a slowing of channel activation. Chloroprocaine had a more selective inhibitory effect on the homomeric Kv7.3 and heteromeric Kv7.2/Kv7.3 channels than on the homomeric Kv7.2 channel. Chloroprocaine also inhibited native M channel currents and induced a depolarization of the DRG neuron membrane potential. Taken together, the findings indicate that chloroprocaine concentration dependently inhibited Kv7/M channel currents. © 2015 S. Karger AG, Basel.

  17. Hypnosis control based on the minimum concentration of anesthetic drug for maintaining appropriate hypnosis.

    PubMed

    Furutani, Eiko; Nishigaki, Yuki; Kanda, Chiaki; Takeda, Toshihiro; Shirakami, Gotaro

    2013-01-01

    This paper proposes a novel hypnosis control method using Auditory Evoked Potential Index (aepEX) as a hypnosis index. In order to avoid side effects of an anesthetic drug, it is desirable to reduce the amount of an anesthetic drug during surgery. For this purpose many studies of hypnosis control systems have been done. Most of them use Bispectral Index (BIS), another hypnosis index, but it has problems of dependence on anesthetic drugs and nonsmooth change near some particular values. On the other hand, aepEX has an ability of clear distinction between patient consciousness and unconsciousness and independence of anesthetic drugs. The control method proposed in this paper consists of two elements: estimating the minimum effect-site concentration for maintaining appropriate hypnosis and adjusting infusion rate of an anesthetic drug, propofol, using model predictive control. The minimum effect-site concentration is estimated utilizing the property of aepEX pharmacodynamics. The infusion rate of propofol is adjusted so that effect-site concentration of propofol may be kept near and always above the minimum effect-site concentration. Simulation results of hypnosis control using the proposed method show that the minimum concentration can be estimated appropriately and that the proposed control method can maintain hypnosis adequately and reduce the total infusion amount of propofol.

  18. Synthesis and antispasmodic activity of lidocaine derivatives endowed with reduced local anesthetic action.

    PubMed

    Costa, Jorge C S; Neves, Josiane S; de Souza, Marcus V N; Siqueira, Rodrigo A; Romeiro, Nelilma C; Boechat, Nubia; e Silva, Patrícia M R; Martins, Marco A

    2008-02-01

    The present structure-activity relationship (SAR) study focused on chemical modifications of the structure of the local anesthetic lidocaine, and indicated analogues having reduced anesthetic potency, but with superior potency relative to the prototype in preventing anaphylactic or histamine-evoked ileum contraction. From the SAR analysis, 2-(diethylamino)-N-(trifluoromethyl-phenyl) and 2-(diethylamino)-N-(dimethyl-phenyl) acetamides were selected as the most promising compounds. New insights into the applicability of non-anesthetic lidocaine derivatives as templates in drug discovery for allergic syndromes are provided.

  19. Assessment of the densities of local anesthetics and their combination with adjuvants: an experimental study.

    PubMed

    Imbelloni, Luiz Eduardo; Moreira, Adriano Dias; Gaspar, Flávia Cunha; Gouveia, Marildo A; Cordeiro, José Antônio

    2009-01-01

    The relative density of a local anesthetic in relation to that of the cerebrospinal fluid (CSF) at 37 degrees C is one of the most important physical properties that affect the level of analgesia obtained after the subarachnoid administration of the drug. The objective of this study was to determine the density of local anesthetic solutions, with and without glucose, and the combination of the local anesthetic with adjuvants at 20 degrees C, 25 degrees C, and 37 degrees C. The density (g.mL(-1)) was determined by using a DMA 450 densimeter with a sensitivity of +/- 0.00001 g.mL(-1). The densities, and variations, according to the temperature were obtained for all local anesthetics and their combination with opioids at 20 degrees C, 25 degrees C, and 37 degrees C. The solution is hyperbaric if its density exceeds 1.00099, hypobaric when its density is lower than 1.00019, and isobaric when its density is greater than 1.00019 and lower than 1.00099. The densities of both local anesthetics and adjuvants decrease with the increase in temperature. At 37 degrees C, all glucose-containing solutions are hyperbaric. In the absence of glucose, all solutions are hypobaric. At 37 degrees C, morphine, fentanyl, sufentanil, and clonidine are hypobaric. The densities of local anesthetics and adjuvants decrease with the increase in temperature and increase when glucose is added. The knowledge of the relative density helps select the most adequate local anesthetic to be administered in the subarachnoid space.

  20. Computer simulations of local anesthetic mechanisms: Quantum chemical investigation of procaine

    SciTech Connect

    Smith, Jeremy C; Bondar, A.N.; Suhai, Sandor; Frangopol, P.T.

    2007-02-01

    A description at the atomic level of detail of the interaction between local anesthetics, lipid membranes and membrane proteins, is essential for understanding the mechanism of local anesthesia. The importance of performing computer simulations to decipher the mechanism of local anesthesia is discussed here in the context of the current status of understanding of the local anesthetics action. As a first step towards accurate simulations of the interaction between local anesthetics, proteins, lipid and water molecules, here we use quantum mechanical methods to assess the charge distribution and structural properties of procaine in the presence and in the absence of water molecules. The calculations indicate that, in the absence of hydrogen-bonding water molecules, protonated procaine strongly prefers a compact structure enabled by intramolecular hydrogen bonding. In the presence of water molecules the torsional energy pro?le of procaine is modified, and hydrogen bonding to water molecules is favored relative to intra-molecular hydrogen bonding.

  1. Uses and Doses of Local Anesthetics in Fish, Amphibians, and Reptiles.

    PubMed

    Chatigny, Frederic; Kamunde, Collins; Creighton, Catherine M; Stevens, E Don

    2017-05-01

    Local anesthetics are an integral part of routine pain management in mammals, yet their use is relatively limited in fish, amphibians and reptiles. These animals frequently undergo potentially painful surgical procedures and therefore could possibly benefit from those drugs. Some recommendations are currently available in the literature concerning analgesic use in these animals. However the pharmacological properties, safety and often efficacy of local anesthetic drugs have not been investigated yet in fish, amphibians, or reptiles. This review compiled current information concerning the use of those agents in fish, reptiles and amphibians to help clinicians make an informed decision as to which dose and drug to use. The resulting literature search showed that the literature concerning use of local analgesics in fish and amphibians is very limited while the literature for reptiles is more extensive. We found few experimental studies evaluating the efficacy of local anesthetics. Further studies would provide additional information for developing guidelines to improve the welfare of fish, amphibians and reptiles.

  2. Effect of intraperitoneal local anesthetic on pain characteristics after laparoscopic cholecystectomy

    PubMed Central

    Choi, Geun Joo; Kang, Hyun; Baek, Chong Wha; Jung, Yong Hun; Kim, Dong Rim

    2015-01-01

    AIM: To systematically evaluate the effect of intraperitoneal local anesthetic on pain characteristics after laparoscopic cholecystectomy (LC). METHODS: We searched MEDLINE, EMBASE, and the Cochrane Library. Randomized controlled trials in English that compared the effect of intraperitoneal administration of local anesthetics on pain with that of placebo or nothing after elective LC under general anesthesia were included. The primary outcome variables analyzed were the combined scores of abdominal, visceral, parietal, and shoulder pain after LC at multiple time points. We also extracted pain scores at resting and dynamic states. RESULTS: We included 39 studies of 3045 patients in total. The administration of intraperitoneal local anesthetic reduced pain intensity in a resting state after laparoscopic cholecystectomy: abdominal [standardized mean difference (SMD) = -0.741; 95%CI: -1.001 to -0.48, P < 0.001]; visceral (SMD = -0.249; 95%CI: -0.493 to -0.006, P = 0.774); and shoulder (SMD = -0.273; 95%CI: -0.464 to -0.082, P = 0.097). Application of intraperitoneal local anesthetic significantly reduced the incidence of shoulder pain (RR = 0.437; 95%CI: 0.299 to 0.639, P < 0.001). There was no favorable effect on resting parietal or dynamic abdominal pain. CONCLUSION: Intraperitoneal local anesthetic as an analgesic adjuvant in patients undergoing laparoscopic cholecystectomy exhibited beneficial effects on postoperative abdominal, visceral, and shoulder pain in a resting state. PMID:26715824

  3. Differential mechanism of the effects of ester-type local anesthetics on sarcoplasmic reticulum Ca-ATPase.

    PubMed

    Sánchez, G A; Di Croce, D E; de la Cal, C; Richard, S B; Takara, D

    2013-12-01

    The effect of the local anesthetics procaine and tetracaine on sarcoplasmic reticulum membranes isolated from two masticatory muscles, masseter and medial pterygoid, was tested and compared to fast-twitch muscles. The effects of the anesthetics on Ca-ATPase activity, calcium binding, uptake, and phosphorylation of the enzyme by inorganic phosphate (Pi) were tested with radioisotopic methods. Calcium binding to the Ca-ATPase was non-competitively inhibited, and the enzymatic activity decreased in a concentration-dependent manner. The inhibition of the activity depended on pH, calcium concentration, the presence of the calcium ionophore calcimycin, and the membrane protein concentration. Unlike fast-twitch membranes, the pre-exposure of the masseter and medial pterygoid membranes to the anesthetics enhanced the enzymatic activity in the absence of calcimycin, supporting their permeabilizing effect. Procaine and tetracaine also interfered with the calcium transport capability, decreasing the maximal uptake without modification of the calcium affinity for the ATPase. Besides, the anesthetics inhibited the phosphorylation of the enzyme by Pi in a competitive manner. Tetracaine revealed a higher inhibitory potency on Ca-ATPase compared to procaine, and the inhibitory concentrations were lower than usual clinical doses. It is concluded that procaine and tetracaine not only affect key steps of the Ca-ATPase enzymatic cycle but also exert an indirect effect on membrane permeability to calcium and suggest that the consequent myoplasmic calcium increase induced by the anesthetics might account for myotoxic effects, such as sustained contraction and eventual rigidity of both fast-twitch and masticatory muscles.

  4. Local anesthetics inhibit tissue factor expression in activated monocytes via inhibition of tissue factor mRNA synthesis.

    PubMed

    Kim, Ji-Eun; Kim, Ki Jun; Ahn, Wonsik; Han, Kyou-Sup; Kim, Hyun Kyung

    2011-01-01

    Local anesthetics have been reported to have anticoagulant properties, but the mechanisms responsible for this action are poorly understood. Here, we evaluated the in vitro effects of 3 local anesthetics--lidocaine, ropivacaine, and bupivacaine--on the tissue factor expression by monocytes. Monocytes from peripheral blood were stimulated with lipopolysaccharide (LPS) in the presence or absence of local anesthetics. All 3 local anesthetics inhibited the expression of tissue factor antigen and tissue factor activity in LPS-stimulated monocytes in a dose- and time-dependent manner and reduced tissue factor messenger RNA (mRNA) expression in endothelial cells and a monocytic cell line. None of the 3 drugs induced apoptosis or affected the viability of monocytes. Our findings that local anesthetics inhibited the tissue factor induction in activated monocytes by inhibiting tissue factor mRNA level may demonstrate the feasibility of using local anesthetics in hypercoagulable and inflammatory conditions.

  5. History of T-cain: a local anesthetic developed and manufactured in Japan.

    PubMed

    Tobe, Masaru; Saito, Shigeru

    2015-10-01

    In many anesthesia textbooks written in English, lidocaine, tetracaine, bupivacaine, ropivacaine, and chloroprocaine are listed as useful local anesthetics for spinal anesthesia. In contrast, T-cain is not included in these lists, even though it has been reported to be suitable for spinal anesthesia in Japan. T-cain was developed as a local anesthetic in the early 1940s by Teikoku Kagaku Sangyo Inc. in Itami, Japan, by replacing a methyl group on tetracaine (Pantocaine(®)) with an ethyl group. T-cain was clinically approved for topical use in Japan in November 1949, and a mixture of dibucaine and T-cain (Neo-Percamin S(®)) was approved for spinal use in May 1950. Simply because of a lack of foreign marketing strategy, T-cain has never attracted global attention as a local anesthetic. However, in Japan, T-cain has been used topically or intrathecally (as Neo-Percamin S(®)) for more than 60 years. Other than the side effects generally known for all local anesthetics, serious side effects have not been reported for T-cain. In fact, several articles have reported that T-cain decreases the neurotoxicity of dibucaine. In this historical review, the characteristics of T-cain and its rise to become a major spinal anesthetic in Japan are discussed.

  6. Tracking local anesthetic effects using a novel perceptual reference approach

    PubMed Central

    Ettlin, Dominik A.; Lukic, Nenad; Abazi, Jetmir; Widmayer, Sonja

    2016-01-01

    Drug effects of loco-regional anesthetics are commonly measured by unidimensional pain rating scales. These scales require subjects to transform their perceptual correlates of stimulus intensities onto a visual, verbal, or numerical construct that uses a unitless cognitive reference frame. The conceptual understanding and execution of this magnitude estimation task may vary among individuals and populations. To circumvent inherent shortcomings of conventional experimental pain scales, this study used a novel perceptual reference approach to track subjective sensory perceptions during onset of an analgesic nerve block. In 34 male subjects, nociceptive electric stimuli of 1-ms duration were repetitively applied to left (target) and right (reference) mandibular canines every 5 s for 600 s, with a side latency of 1 ms. Stimulus strength to the target canine was programmed to evoke a tolerable pain intensity perception and remained constant at this level throughout the experiment. A dose of 0.6 ml of articaine 4% was submucosally injected at the left mental foramen. Subjects then reported drug effects by adjusting the stimulus strength (in milliamperes) to the reference tooth, so that the perceived intensity in the reference tooth was equi-intense to the target tooth. Pain and stimulus perception offsets were indicated by subjects. Thus, the current approach for matching the sensory experience in one anatomic location after regional anesthesia allows detailed tracking of evolving perceptual changes in another location. This novel perceptual reference approach facilitates direct and accurate quantification of analgesic effects with high temporal resolution. We propose using this method for future experimental investigations of analgesic/anesthetic drug efficacy. PMID:26792885

  7. [The effect of anesthetic concentration on burst-suppression of the EEG in rats].

    PubMed

    Zhang, Dandan; Jia, Xiaofeng; Ding, Haiyan

    2012-04-01

    The term "burst-suppression" is used to describe the electroencephalogram (EEG) pattern characterized by theta or delta waves, at times intermixed with faster waves, and intervening periods of relative quiescence. Burst-suppression pattern can reflect the seriously suppressed brain activity under deep anesthesia. To investigate the relationship between burst-suppression features and anesthetic concentration, we adopted four straightforward indexes, i. e., burst-suppression ratio (BSR), burst frequency, burst amplitude and suppression amplitude, and used them to analyze the EEG recordings in ten isoflurane-anesthetized rats. It was found that all the four burst-suppression indexes changed along with anesthetic concentration, that BSR and burst amplitude increased with higher concentration of isoflurane while burst frequency and suppression amplitude decreased, and that BSR was the most sensitive and consistent measurement to indicate isoflurane concentration so it constituted a valuable tool for timely evaluation of burst-suppression feature under deep anesthesia. The result also showed that the composition of carrier gas (i. e. pure oxygen vs. mixed oxygen) did not influence the effect of anesthesia significantly; and the four indexes of burst-suppression features could keep relatively stable within 60 min under the isoflurane concentration of 2%. The present study provides quantitative information of burst-suppression features under different anesthetic depth and may help to develop a clinically satisfied system that could quantify the characteristics of EEG and rigorously evaluate the cerebral state of patients.

  8. Recognition of local anesthetic maldistribution in axillary brachial plexus block guided by ultrasound and nerve stimulation.

    PubMed

    Veneziano, Giorgio C; Rao, Vidya K; Orebaugh, Steven L

    2012-03-01

    Nerve stimulation may occur despite the presence of a fascial barrier between the needle tip and the nerve, which may prevent appropriate flow or distribution of local anesthetic solution. During an axillary nerve block, ultrasound (US) guidance was used to identify the median nerve. Insertion of a needle with US and nerve stimulator guidance resulted in the appearance of the needle tip in contact with the nerve. However, as local anesthetic injection was begun, it was clear that the injectate was accumulating superficial to the investing fascia of the neurovascular bundle. No injectate was seen below the fascia. With US guidance, the needle was repositioned at a greater depth. Repeat injection of local anesthetic clearly flowed around the nerve. Copyright © 2012 Elsevier Inc. All rights reserved.

  9. 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.

  10. Infant spinal anesthesia: Do girls need a larger dose of local anesthetic?

    PubMed

    Frawley, Geoff; Huque, Md Hamidul

    2017-10-01

    Gender differences in absorption, distribution, and metabolism of a number of anesthetic agents have been identified in adults. Clinically, adult studies suggest women demonstrate slower onset of opioid analgesic effects, lower spinal and epidural dose requirements, and greater sensitivity to neuromuscular blocking agents. Sex-related differences in the pharmacokinetics and pharmacodynamics of local anesthetics in neonates and infants, however, have not been well documented. As a result, it is not known whether modification of the dose of local anesthetic for awake spinal anesthesia in infants is required. Our aim was to determine whether the ED50 and ED95 of local anesthetics used for infant spinal anesthesia are different between sexes. This was a retrospective analysis of data previously collected during dose-response studies of levobupivacaine and ropivacaine spinal anesthetics. The doses were reanalyzed using generalized linear regression analysis to determine whether there is a discernible difference in dose requirements between male and female infants. One hundred and twenty infant spinal anesthetics were reviewed. For levobupivacaine, the ED50 (95% CI) was 0.49 (0.33-0.65) mg vs 0.69 (0.49-0.88), whereas the ED95 (95% CI) was 1.07 (0.73-1.41) vs 0.93 (0.64-1.22) for girls and boys, respectively. For ropivacaine spinal anesthesia, the ED50 (95% CI) was 0.64 (0.35-0.92) mg vs 0.30 (-0.32-0.92), whereas the ED95 (95% CI) was 1.30 (0.73-1.87) vs 1.66 (0.55-2.76) for girls and boys, respectively. There is no evidence that sex differences occur at the ED50 dose range or at the clinically relevant ED95 dose. Modification of spinal anesthetic dose is not required for infant girls. © 2017 John Wiley & Sons Ltd.

  11. New procedure to synthesize silver nanoparticles and their interaction with local anesthetics.

    PubMed

    Mocanu, Aurora; Pasca, Roxana Diana; Tomoaia, Gheorghe; Garbo, Corina; Frangopol, Petre T; Horovitz, Ossi; Tomoaia-Cotisel, Maria

    2013-01-01

    Silver nanoparticles (AgNPs) were prepared in aqueous colloid dispersions by the reduction of Ag(+) with glucose in alkaline medium. Tetraethyl orthosilicate and L-asparagine were added as stabilizers of NPs. The AgNPs were characterized, and their interaction with three local anesthetics (procaine, dibucaine, or tetracaine) was investigated. Optical spectra show the characteristic absorption band of AgNPs, due to surface plasmon resonance. Modifications in the position and shape of this band reflect the self-assembly of metal NPs mediated by anesthetic molecules and the progress in time of the aggregation process. Zeta-potential measuring was applied in order to characterize the electrostatic stability of the NPs. The size and shape of the AgNPs, as well as the features of the assemblies formed by their association in the presence of anesthetics, were evidenced by transmission electron microscopy images. Atomic force microscopy images showed the characteristics of the films of AgNPs deposited on glass support. The effect of the anesthetics could be described in terms of electrostatic forces between the negatively charged AgNPs and the anesthetic molecules, existing also in their cationic form at the working pH. But also hydrophobic and hydrogen bonding interactions between the coated nanoparticles and anesthetics molecular species should be considered.

  12. Local anesthetics induce apoptosis in human thyroid cancer cells through the mitogen-activated protein kinase pathway.

    PubMed

    Chang, Yuan-Ching; Hsu, Yi-Chiung; Liu, Chien-Liang; Huang, Shih-Yuan; Hu, Meng-Chun; Cheng, Shih-Ping

    2014-01-01

    Local anesthetics are frequently used in fine-needle aspiration of thyroid lesions and locoregional control of persistent or recurrent thyroid cancer. Recent evidence suggests that local anesthetics have a broad spectrum of effects including inhibition of cell proliferation and induction of apoptosis in neuronal and other types of cells. In this study, we demonstrated that treatment with lidocaine and bupivacaine resulted in decreased cell viability and colony formation of both 8505C and K1 cells in a dose-dependent manner. Lidocaine and bupivacaine induced apoptosis, and necrosis in high concentrations, as determined by flow cytometry. Lidocaine and bupivacaine caused disruption of mitochondrial membrane potential and release of cytochrome c, accompanied by activation of caspase 3 and 7, PARP cleavage, and induction of a higher ratio of Bax/Bcl-2. Based on microarray and pathway analysis, apoptosis is the prominent transcriptional change common to lidocaine and bupivacaine treatment. Furthermore, lidocaine and bupivacaine attenuated extracellular signal-regulated kinase 1/2 (ERK1/2) activity and induced activation of p38 mitogen-activated protein kinase (MAPK) and c-jun N-terminal kinase. Pharmacological inhibitors of MAPK/ERK kinase and p38 MAPK suppressed caspase 3 activation and PARP cleavage. Taken together, our results for the first time demonstrate the cytotoxic effects of local anesthetics on thyroid cancer cells and implicate the MAPK pathways as an important mechanism. Our findings have potential clinical relevance in that the use of local anesthetics may confer previously unrecognized benefits in the management of patients with thyroid cancer.

  13. Difficult Airway Management Caused by Local Anesthetic Allergy During Emergent Cesarean Delivery: A Case Report.

    PubMed

    Maxey-Jones, Courtney L; Palmerton, Alec; Farmer, Jocelyn R; Bateman, Brian T

    2017-08-01

    Difficult airway management in the gravid patient is a well-described phenomenon. We present a case of emergent cesarean delivery complicated by a "cannot intubate, cannot ventilate" scenario that was later determined to be secondary to an allergic, IgE-mediated reaction to epidurally administered local anesthetic.

  14. Hypersensitive reactions to local dental anesthetics and patient information: critical review of a drug leaflet

    PubMed Central

    Simonet, Daniel

    2011-01-01

    This paper discusses the case of a patient who experienced adverse reactions to a local anesthetic. It reviews symptoms of adverse reactions, possible causes, patient management, and alternative anesthesia modes. The second part of the paper discusses the product leaflet information and the associated legal issues. PMID:22915891

  15. Delayed-Onset Digital Ischemia After Local Anesthetic With Epinephrine Injection Requiring Phentolamine Reversal.

    PubMed

    Zhu, Andy F; Hood, Brandon R; Morris, Mark S; Ozer, Kagan

    2017-06-01

    The use of low-dose epinephrine in hand surgery has made it possible to perform a wide range of surgical procedures in the office setting. Low-dose epinephrine use is safe, and its vasoconstrictive effects are reversible with phentolamine. In this report, we present late-onset finger ischemia beginning 3 hours after an ipsilateral carpal tunnel and A1 pulley release of the middle finger anesthetized with local anesthetic and low-dose epinephrine (1:100,000). Finger ischemia lasted 14 hours until rescued with phentolamine injection. Copyright © 2017 American Society for Surgery of the Hand. Published by Elsevier Inc. All rights reserved.

  16. [Rapid simultaneous assay of the principalamide-type local anesthetics by gas-liquid chromatography].

    PubMed

    Desch, G; Cavadore, D; Jullien, Y; Mercier, L; Descomps, B; de Rodez, M

    1981-01-01

    This method can assay simultaneously, using 300 microliters of plasma, of the three principle local anesthetic agents used by peridural injection for post-operative anesthesia and analgesia: xylocaïne, etidocaïne, bupivacaïne. The assay method consists of three steps: (a) the addition of an internal calibrating agent (mepivacaïne). (b) defecation using trichlorocetic acid. (c) alcalinization of the supernatent (pH 11), extraction with dichloromethane and concentration at room temperature of the organic phase. (d) chromotography using an SE 30 or OV 17 impregnated column. The method is sensitive between 0.37 mumoles per l-1 (0.1 microgram . ml-1) and the coefficient for the mean deviation is 10.9% for concentration between 0.37 mumoles 1-1 and 75 mumole1-1 (0.1 microgram . ml-1 and 20 micrograms . ml-1). The correspondence of the figures recorded in this large concentration range without any change in the technique means that the kinetics of the plasma concentrations before and after peridural injection can be followed. The results obtained by gas liquid chromatography for the assay of lidocaïne were compared in 115 different plasma samples with concentrations obtained by an immuno enzymatic method ("EMIT") fitted to a centrifuge analyser. The correlation coefficient between the two methods was: (r = 0.95 with y = 0.09 x +0.25 microgram . ml-1 implying the absence of any interference and the specificity of the two methods. The columns also separate in 20 minutes the two main metabolites of lidocaïne: monoethylglycinexylidide (M.E.G.X.) and glycinexylidide (G.X.). These results demonstrate that continuous peridural injection of lidocaïne produces a high plasma concentration without any clinical toxic phenomena.

  17. [Pregnancy and lactation period: Which local anesthetics and analgesics].

    PubMed

    Fatori Popovic, Sandra; Lübbers, Heinz-Theo; von Mandach, Ursula

    2016-01-01

    The aim of this paper is to show relevant aspects of dental treatment in pregnancy. Common medication used in dental offices should be highlighted in special regard to the pregnant patient during dental treatment. The reader should gain more security in the election of the proper drugs for local anesthesia and oral analgesics. Local anaesthetics such as articain with adrenalin in a dilution of 1 : 200 000 can be used for dental treatment at any time. Paracetamol should be used as first line oral analgesic. Elective dental procedures should be postponed after delivery and after lactation period.

  18. [Pregnancy and lactation period: Which local anesthetics and analgesics?].

    PubMed

    Fatori Popovic, Sandra; Lübbers, Heinz-Theo; von Mandach, Ursula

    2016-01-01

    The aim of this paper is to show relevant aspects of dental treatment in pregnancy. Common medication used in dental offices should be highlighted in special regard to the pregnant patient during dental treatment. The reader should gain more security in the election of the proper drugs for local anesthesia and oral analgesics. Local anaesthetics such as articain with adrenalin in a dilution of 1 : 200 000 can be used for dental treatment at any time. Paracetamol should be used as first line oral analgesic. Elective dental procedures should be postponed after delivery and after lactation period.

  19. Geriatric abdominal surgery under local anesthetic: a case report.

    PubMed

    Calhoon, E L

    1991-06-01

    Abdominal surgery in a fragile elderly patient is often a dilemma, especially in the rural hospital setting where complex anesthesiology services are not available. We have done thyroidectomies and umbilical and inguinal hernias under local anesthesia, and report the following case where the technique was extended to a critically ill geriatric patient with a strangulated hernia.

  20. Tumescent local anesthetic technique for inguinal hernia repairs

    PubMed Central

    Chyung, Ju Won; Kwon, Yujin; Cho, Dong Hui; Lee, Kyung Bok; Park, Sang Soo; Yoon, Jin; Jang, Yong Seog

    2014-01-01

    Purpose We evaluated the adequacy and feasibility of a tumescent solution containing lidocaine and bupivacaine for inguinal hernia repairs. Methods The medical records of 146 consecutive inguinal hernia patients with 157 hernia repairs using the tumescent local anesthesia technique performed by a single surgeon between September 2009 and December 2013 were retrospectively reviewed. Results The mean operation time (±standard deviation) and hospital stay were 64.5 ± 17.6 minutes and 2.7 ± 1.5 days. The postoperative complication rate was 17.8%. There were four cases of recurrences (2.5%) at a mean follow-up of 24 ± 14 months. Conclusion Our results suggest that local anesthesia with the tumescent technique is an effective and safe modality for inguinal hernia repairs. PMID:25485241

  1. Anesthetic effectiveness of the supplemental intraligamentary injection, administered with a computer-controlled local anesthetic delivery system, in patients with irreversible pulpitis.

    PubMed

    Nusstein, John; Claffey, Elizabeth; Reader, Al; Beck, Mike; Weaver, Joel

    2005-05-01

    The purpose of this study was to determine the anesthetic effectiveness of the supplemental intraligamentary injection, administered with a computer-controlled local anesthetic delivery system, in mandibular posterior teeth diagnosed with irreversible pulpitis when the conventional inferior alveolar nerve block failed. Fifty-four emergency patients, diagnosed with irreversible pulpitis of a mandibular posterior tooth, received an inferior alveolar nerve block and had moderate to severe pain upon endodontic access. A computer-controlled local anesthetic delivery system was then used to administer intraligamentary injections of 1.4 ml of 2% lidocaine with 1:100,000 epinephrine. Success of the intraligamentary injection was defined as none or mild pain upon endodontic access or initial instrumentation. The results demonstrated that anesthetic success was obtained in 56% (30 of 54) of the patients. We concluded that when the inferior alveolar nerve block failed to provide profound pulpal anesthesia in mandibular posterior teeth of patients presenting with irreversible pulpitis, the intraligamentary injection administered with a computer-controlled local anesthetic delivery system was successful approximately 56% of the time.

  2. The Effect of Local Anesthetic on Pro-inflammatory Macrophage Modulation by Mesenchymal Stromal Cells

    PubMed Central

    Gray, Andrea; Marrero-Berrios, Ileana; Weinberg, Jonathan; Manchikalapati, Devasena; SchianodiCola, Joseph; Schloss, Rene S.; Yarmush, Joel

    2016-01-01

    Administering local anesthetics (LAs) peri- and post-operatively aims to prevent or mitigate pain in surgical procedures and after tissue injury in cases of osteoarthritis (OA) and other degenerative diseases. Innovative tissue protective and reparative therapeutic interventions such as mesenchymal stromal cells (MSCs) are likely to be exposed to co-administered drugs such as LAs. Therefore, it is important to determine how this exposure affects the therapeutic functions of MSCs and other cells in their target microenvironment. In these studies, we measured the effect of LAs, lidocaine and bupivacaine, on macrophage viability and pro-inflammatory secretion. We also examined their effect on modulation of the macrophage pro-inflammatory phenotype in an in vitro co-culture system with MSCs, by quantifying macrophage tumor necrosis factor (TNF)-α secretion and MSC prostaglandin E2 (PGE2) production. Our studies indicate that both LAs directly attenuated macrophage TNF-α secretion, without significantly affecting viability, in a concentration- and potency-dependent manner. LA-mediated attenuation of macrophage TNF-α was sustained in co-culture with MSCs, but MSCs did not further enhance this anti-inflammatory effect. Concentration- and potency-dependent reductions in macrophage TNF-α were concurrent with decreased PGE2 levels in the co-cultures further indicating MSC-independent macrophage attenuation. MSC functional recovery from LA exposure was assessed by pre-treating MSCs with LAs prior to co-culture with macrophages. Both MSC attenuation of TNF-α and PGE2 secretion were impaired by pre-exposure to the more potent bupivacaine and high dose of lidocaine in a concentration-dependent manner. Therefore, LAs can affect anti-inflammatory function by both directly attenuating macrophage inflammation and MSC secretion and possibly by altering the local microenvironment which can secondarily reduce MSC function. Furthermore, the LA effect on MSC function may persist

  3. The effect of local anesthetic on pro-inflammatory macrophage modulation by mesenchymal stromal cells.

    PubMed

    Gray, Andrea; Marrero-Berrios, Ileana; Weinberg, Jonathan; Manchikalapati, Devasena; SchianodiCola, Joseph; Schloss, Rene S; Yarmush, Joel

    2016-04-01

    Administering local anesthetics (LAs) peri- and post-operatively aims to prevent or mitigate pain in surgical procedures and after tissue injury in cases of osteoarthritis (OA) and other degenerative diseases. Innovative tissue protective and reparative therapeutic interventions such as mesenchymal stromal cells (MSCs) are likely to be exposed to co-administered drugs such as LAs. Therefore, it is important to determine how this exposure affects the therapeutic functions of MSCs and other cells in their target microenvironment. In these studies, we measured the effect of LAs, lidocaine and bupivacaine, on macrophage viability and pro-inflammatory secretion. We also examined their effect on modulation of the macrophage pro-inflammatory phenotype in an in vitro co-culture system with MSCs, by quantifying macrophage tumor necrosis factor (TNF)-α secretion and MSC prostaglandin E2 (PGE2) production. Our studies indicate that both LAs directly attenuated macrophage TNF-α secretion, without significantly affecting viability, in a concentration- and potency-dependent manner. LA-mediated attenuation of macrophage TNF-α was sustained in co-culture with MSCs, but MSCs did not further enhance this anti-inflammatory effect. Concentration- and potency-dependent reductions in macrophage TNF-α were concurrent with decreased PGE2 levels in the co-cultures further indicating MSC-independent macrophage attenuation. MSC functional recovery from LA exposure was assessed by pre-treating MSCs with LAs prior to co-culture with macrophages. Both MSC attenuation of TNF-α and PGE2 secretion were impaired by pre-exposure to the more potent bupivacaine and high dose of lidocaine in a concentration-dependent manner. Therefore, LAs can affect anti-inflammatory function by both directly attenuating macrophage inflammation and MSC secretion and possibly by altering the local microenvironment which can secondarily reduce MSC function. Furthermore, the LA effect on MSC function may persist

  4. The Wide-Awake Approach to Dupuytren’s Disease: Fasciectomy under Local Anesthetic with Epinephrine

    PubMed Central

    Higgins, Amanda; Conrad, Joanie; Bell, Mike; Lalonde, Don

    2009-01-01

    The Wide-Awake Approach to Dupuytren's contracture involves fasciectomy under local anesthetic with epinephrine and no tourniquet. The goal of this study is to show that the Wide-Awake Approach produces equivalent outcomes to fasciectomy under general anesthetic with a tourniquet, with fewer risks to the patient. A multicenter retrospective review was conducted on 111 patients with fasciectomies under local or general anesthetic between 2001 and 2007. Data on patient demographics, comorbidities, cost, as well as range of motion was collected and evaluated using Microsoft Excel and SAS. Of 148 fingers, 102 were treated under local and 46 under general anesthetic. The average postoperative Total Active Motion (TAM) for general anesthetic patients was 199.0 ± 29.6 (D5), 223.9 ± 29.3 (D4), 234.6 ± 14.6 (D3), and 246.7 ± 14.4 (D2). The average postoperative TAM for local anesthetic patients was 168.3 ± 62.2 (D5), 195.9 ± 67.5 (D4), 173.0 ± 72.6 (D3), and 177.5 ± 31.8 (D2). There were no significant differences between any of these individual groups (p = 0.09, 0.26, 0.12, and 0.20, respectively); however, when pooled, the overall TAM was significantly greater in the general anesthesia group (222.0 ± 29.7 vs. 186.0 ± 63.0, p = 0.002.). Complication rates and types were similar with both techniques. The Wide-Awake Approach to Dupuytren’s contracture avoids general anesthetic risks and has cost benefits to healthcare providers. Although it yields similar range of motion outcomes to fasciectomy performed under general anesthesia, total active motion may be better with fasciectomy done under general anesthesia. PMID:19902309

  5. Effect of local anesthetics with and without vasoconstrictor agent in patients with ventricular arrhythmias.

    PubMed

    Cáceres, Maria Teresa Fernández; Ludovice, Ana Cristina P P; Brito, Fabio Sândoli de; Darrieux, Francisco Carlos; Neves, Ricardo Simões; Scanavacca, Mauricio Ibrahim; Sosa, Eduardo A; Hachul, Denise Tessariol

    2008-09-01

    The routine use of local anesthetics associated to vasoconstrictors for the dental treatment of patients with cardiopathies is still controversial, due to the risk of adverse cardiovascular effects. To evaluate and compare the hemodynamic effects of the use of local anesthetics with a non-adrenergic vasoconstrictor in patients with ventricular arrhythmia, when compared to the use of anesthetics without vasoconstrictor. A prospective randomized study evaluated 33 patients with positive serology for Chagas' disease and 32 patients with coronary artery disease that presented complex ventricular arrhythmia at Holter monitoring (>10 EV/h and NSVT), of which 21 were females, aged 54.73 + 7.94 years, submitted to routine dental treatment with pterygomandibular anesthesia. These patients were divided in two groups: group I received prilocaine 3% associated with felypressin 0.03 IU/ml and group II received lidocaine 2% without vasoconstrictor. The number and complexity of extrasystoles were analyzed, as well as the heart rate and systemic arterial pressure of the patients on the day before, one hour before, during the procedure and one hour after the dental procedure. No hemodynamic alterations or increase in the number and complexity of the ventricular arrhythmia related to the anesthetic used in the dental procedure were observed in either group. The results suggest that prilocaine 3% associated to a felypressin 0.03 IU/ml can be safely used in patients with Chagas' disease or coronariopathy with complex ventricular arrhythmia.

  6. Oropharyngeal oxygen and volatile anesthetic agent concentration during the use of laryngeal mask airway in children.

    PubMed

    Hakim, Mumin; Krishna, Senthil G; Syed, Ahsan; Lind, Meredith; Elmaraghy, Charles; Tobias, Joseph D

    2016-01-01

    The laryngeal mask airway is increasingly used as an airway adjunct during general anesthesia. Although placement is generally simpler than an endotracheal tube, complete sealing of the airway may not occur, resulting in contamination of the oropharynx with anesthetic gases. Oropharyngeal oxygen enrichment may be one of the contributing factors predisposing to an airway fire during adenotonsillectomy. The current study prospectively assesses the oropharyngeal oxygen and volatile anesthetic agent concentration during laryngeal mask airway use in infants and children. Following the induction of general anesthesia and placement of a laryngeal mask airway, the oropharyngeal gas sample was obtained by placing a 14-gauge catheter attached to the gas sampling tube into the oropharynx above the laryngeal mask airway. The oropharyngeal concentration of the oxygen and the anesthetic agent were recorded for five breaths during both spontaneous ventilation (SV) and positive pressure ventilation (PPV). The study included 238 patients. The oropharyngeal concentration of sevoflurane was >50% of the inspired sevoflurane concentration during SV in 10 of 238 (4.2%) patients and during PPV in 135 of 238 (56.7%) patients. Similarly, during SV and PPV, the oropharyngeal oxygen concentration was >21% in 30 of 238 (12.6%) patients and in 188 of 238 (79%) patients, respectively. Significantly, we also noticed that the oropharyngeal oxygen concentration exceeded 50% in 5 of 238 (2.1%) patients during SV and in 139 of 238 patients (58.4%) patients during PPV. With the use of a laryngeal mask airway and the administration of 100% oxygen, there was significant contamination of the oropharynx during both PPV and SV. The oropharyngeal concentration of oxygen was high enough to support combustion in a significant number of patients. The use of a laryngeal mask airway does not ensure sealing of the airway and may be one risk factor for an airway fire during adenotonsillectomy. © 2015 John Wiley

  7. Postoperative seroma formation after abdominoplasty with placement of continuous infusion local anesthetic pain pump

    PubMed Central

    Smith, Melissa M; Lin, Michael P; Hovsepian, Raffi V; Wood, David; Nguyen, Trung; Evans, Gregory RD; Wirth, Garrett A

    2009-01-01

    The most common complication after abdominoplasty is seroma formation. The incidence of seroma formation in abdominal procedures as a whole, including abdominoplasty, panniculectomy and transverse rectus abdominis myocutaneous flap abdominal donor sites, ranges from 1% to 38%. A recent concern among surgeons is the possibility of a causal relationship between the use of continuous infusion devices such as local anesthetic pain pumps and the development of seromas. A case of postoperative, persistent, recurrent seroma formation after abdominoplasty with the use of continuous infusion local anesthetic pain pump is presented. After several attempts at aspiration and drain catheter placement, only open surgical excision of the seroma cavity was found to be definitively effective in treating the development of seroma. PMID:21119843

  8. Isoflurane waste anesthetic gas concentrations associated with the open-drop method.

    PubMed

    Taylor, Douglas K; Mook, Deborah M

    2009-01-01

    The open-drop technique is used frequently for anesthetic delivery to small rodents. Operator exposure to waste anesthetic gas (WAG) is a potential occupational hazard if this method is used without WAG scavenging. This study was conducted to determine whether administration of isoflurane by the open-drop technique without exposure controls generates significant WAG concentrations. We placed 0.1, 0.2, or 0.3 ml of liquid isoflurane into screw-top 500 or 1000 ml glass jars. WAG concentration was measured at the opening of the container and 20 and 40 cm from the opening, a distance at which users likely would operate, at 1, 2, or 3 min WAG was measured by using a portable infrared gas analyzer. Mean WAG concentrations at the vessel opening were as high as 662 +/- 168 ppm with a 500 ml jar and 122 +/- 87 ppm with a 1000 ml jar. At operator levels, WAG concentrations were always at or near 0 ppm. For measurements made at the vessel opening, time was the only factor that significantly affected WAG concentration when using the 500 ml jar. Neither time nor liquid volume were significant factors when using 1000 ml jar. At all liquid volumes and time points, the WAG concentration associated with using the 500 ml container was marginally to significantly greater than that for the 1000 ml jar.

  9. Triple rubber band ligation for hemorrhoids: prospective, randomized trial of use of local anesthetic injection.

    PubMed

    Law, W L; Chu, K W

    1999-03-01

    Rubber band ligation is a common office procedure for hemorrhoids. Triple rubber band ligation in a single session has been shown to be a safe and economical way of treating hemorrhoids. However, postligation discomfort after triple rubber band ligation is not uncommon. The aim of this study was to evaluate the effectiveness of local anesthetic injection to the banded hemorrhoidal tissue in reducing postligation discomfort. Patients attending an outpatient clinic for symptomatic hemorrhoids suitable for triple rubber band ligation were randomly assigned to two groups. In the treatment group rubber band ligation was performed at three columns of hemorrhoids, and 1 to 2 ml of 2 percent lignocaine was injected into the banded hemorrhoidal tissue. In the control group triple rubber band ligation was performed in a similar manner, but local anesthetic was not given. Patients were followed up by telephone at the second week and in the clinic after six weeks. From April to August 1996, 101 patients entered the trial and were treated with triple rubber band ligation. Sixty-two patients were randomly assigned to the local anesthetic injection group and 39 to the control group. Overall good to excellent results occurred in 89 percent of patients, and there was no difference between the two groups. Postligation pain occurred in 26 and 20 percent of patients in the treatment and control groups, respectively (P > 0.05). Postligation tenesmus occurred in 32 and 41 percent of patients in the treatment and control groups, respectively (P > 0.05). No patients suffered from septic complications or bleeding that required transfusion. Triple rubber band ligation in a single session is a safe, economical, and effective way of treating symptomatic hemorrhoids. Postligation pain and tenesmus occurred in 24 and 37 percent, respectively. Discomfort was usually tolerable. Local anesthetic injection to the banded hemorrhoidal tissue did not help to reduce postligation discomfort.

  10. Hysteroscopic local anesthetic intrauterine cornual block in office endometrial ablation: a randomized controlled trial.

    PubMed

    Kumar, Vinod; Tryposkiadis, Konstantinos; Gupta, Janesh Kumar

    2016-02-01

    To evaluate the efficacy of a hysteroscopic local anesthetic intrauterine cornual block (ICOB) on pain experienced during office endometrial ablation (EA) in addition to a traditional direct local anesthetic cervical block (DCB). Prospective, randomized, double-blind, placebo-controlled trial. University teaching hospital. Women with heavy menstrual bleeding scheduled for an office endometrial ablation. Before office EA, DCB plus hysteroscopic ICOB just medial to each tubal ostium using local anesthetic mixture made up of 1 mL 3% mepivacaine plus 1 mL 0.5% bupivacaine versus control group receiving DBC plus ICOB with 2 mL of placebo (saline). pain reported during procedure via visual analogue scale (VAS) from 0 to 10; secondary outcomes: postoperative pain, rescue analgesic requirement, and duration of hospital stay. Most characteristics were similar across groups. The mean VAS score during the procedure was statistically significantly lower by 1.44 (95% confidence interval, -2.65 to -0.21) in the active group compared with the placebo group. There were no statistically significant differences between the two groups in the postprocedural mean VAS scores, rescue analgesic requirement, or duration of hospital stay. Used in addition to DCB, ICOB reduces the pain experienced during office EA compared with DCB alone. NCT01808898. Copyright © 2016 American Society for Reproductive Medicine. Published by Elsevier Inc. All rights reserved.

  11. Efficacy of epidural local anesthetic and dexamethasone in providing postoperative analgesia: A meta-analysis

    PubMed Central

    Jebaraj, B; Khanna, P; Baidya, DK; Maitra, S

    2016-01-01

    Background: Dexamethasone is a potent anti-inflammatory, analgesic, and antiemetic drug. Individual randomized controlled trials found a possible benefit of epidural dexamethasone. The purpose of this meta-analysis is to estimate the benefit of epidural dexamethasone on postoperative pain and opioid consumption and to formulate a recommendation for evidence-based practice. Materials and Methods: Prospective, randomized controlled trials comparing the analgesic efficacy of epidural local anesthetic and dexamethasone combination, with local anesthetic alone for postoperative pain management after abdominal surgery, were planned to be included in this meta-analysis. PubMed, PubMed Central, Scopus, and Central Register of Clinical Trials of the Cochrane Collaboration (CENTRAL) databases were searched for eligible controlled trials using the following search words: “Epidural”, “dexamethasone”, and “postoperative pain”, until February 20, 2015. Results: Data from five randomized control trials have been included in this meta-analysis. Epidural dexamethasone significantly decreased postoperative morphine consumption (mean difference −7.89 mg; 95% confidence interval [CI]: −11.66 to −3.71) and number of patients required postoperative rescue analgesic boluses (risk ratio: 0.51; 95% CI: 0.41-0.63). Conclusion: The present data shows that the addition of dexamethasone to local anesthetic in epidural is beneficial for postoperative pain management. PMID:27375389

  12. Ice Reduces Needle-Stick Pain Associated With Local Anesthetic Injection

    PubMed Central

    Mahshidfar, Babak; Cheraghi Shevi, Salimeh; Abbasi, Mohsen; Kasnavieh, Mohammad Hosseini; Rezai, Mahdi; Zavereh, Mina; Mosaddegh, Reza

    2016-01-01

    Background Local anesthetic injections are widely used in the emergency department for different purposes. Pain management for such injections is of great importance to both patients and the healthcare system. Objectives Our study aimed to determine the effectiveness and safety of cryotherapy in patients receiving local anesthetic injections. Methods Subjects who presented with superficial lacerations were randomly assigned to 2 groups, the first group received ice packing prior to injection and the second did not. The pain severity, length and depth of the laceration, and the other necessary information before and after the pain-reducing intervention were measured, documented, and compared at the end of the study. Pain scores were measured using a numerical rating scale before and after the procedure, and the differences were compared using a t-test. Results Ninety subjects were enrolled in the study, 45 in each group. There were no statistical differences between the 2 groups in terms of baseline preoperative and operative characteristics (P > 0.05). The pain scores in the cryotherapy group were significantly lower before and after the procedure (P < 0.001). There was no statistically significant difference between the 2 groups for wound infection (P = 0.783). Conclusions Cooling the injection site prior to local anesthetic injection is an effective and inexpensive method to reduce the pain and discomfort caused by the injection. PMID:27847696

  13. [Axillary local anesthetic spread after the thoracic interfacial ultrasound block - A cadaveric and radiological evaluation].

    PubMed

    Torre, Patricia Alfaro de la; Jones, Jerry Wayne; Álvarez, Servando López; Garcia, Paula Diéguez; Miguel, Francisco Javier Garcia de; Rubio, Eva Maria Monzon; Boeris, Federico Carol; Sacramento, Monir Kabiri; Duany, Osmany; Pérez, Mario Fajardo; Gordon, Borja de la Quintana

    2017-09-01

    Oral opioid analgesics have been used for management of peri- and postoperative analgesia in patients undergoing axillary dissection. The axillary region is a difficult zone to block and does not have a specific regional anesthesia technique published that offers its adequate blockade. After institutional review board approval, anatomic and radiological studies were conducted to determine the deposition and spread of methylene blue and local anesthetic injected respectively into the axilla via the thoracic inter-fascial plane. Magnetic Resonance Imaging studies were then conducted in 15 of 34 patients scheduled for unilateral breast surgery that entailed any of the following: axillary clearance, sentinel node biopsy, axillary node biopsy, or supernumerary breasts, to ascertain the deposition and time course of spread of solution within the thoracic interfascial plane in vivo. Radiological and cadaveric studies showed that the injection of local anesthetic and methylene blue via the thoracic inter-fascial plane, using ultrasound guide technique, results in reliable deposition into the axilla. In patients, the injection of the local anesthetic produced a reliable axillary sensory block. This finding was supported by Magnetic Resonance Imaging studies that showed hyper-intense signals in the axillary region. These findings define the anatomic characteristics of the thoracic interfascial plane nerve block in the axillary region, and underline the clinical potential of this novel nerve block. Copyright © 2016 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  14. Amide-Type Local Anesthetics and Human Mesenchymal Stem Cells: Clinical Implications for Stem Cell Therapy

    PubMed Central

    Lyons, Nicolette F.; Reischling, Patrick D.; Centeno, Christopher J.

    2014-01-01

    In the realm of regenerative medicine, human mesenchymal stem cells (hMSCs) are gaining attention as a cell source for the repair and regeneration of tissues spanning an array of medical disciplines. In orthopedics, hMSCs are often delivered in a site-specific manner at the area of interest and may require the concurrent application of local anesthetics (LAs). To address the implications of using hMSCs in combination with anesthetics for intra-articular applications, we investigated the effect that clinically relevant doses of amide-type LAs have on the viability of bone marrow-derived hMSCs and began to characterize the mechanism of LA-induced hMSC death. In our study, culture-expanded hMSCs from three donors were exposed to the amide-type LAs ropivacaine, lidocaine, bupivacaine, and mepivacaine. To replicate the physiological dilution of LAs once injected into the synovial capsule, each anesthetic was reduced to 12.5%, 25%, and 50% of the stock solution and incubated with each hMSC line for 40 minutes, 120 minutes, 360 minutes, and 24 hours. At each time point, cell viability assays were performed. We found that extended treatment with LAs for 24 hours had a significant impact on both hMSC viability and adhesion. In addition, hMSC treatment with three of the four anesthetics resulted in cell death via apoptosis following brief exposures. Ultimately, we concluded that amide-type LAs induce hMSC apoptosis in a time- and dose-dependent manner that may threaten clinical outcomes, following a similar trend that has been established between these particular anesthetics and articular chondrocytes both in vitro and in vivo. PMID:24436443

  15. Amide-type local anesthetics and human mesenchymal stem cells: clinical implications for stem cell therapy.

    PubMed

    Dregalla, Ryan C; Lyons, Nicolette F; Reischling, Patrick D; Centeno, Christopher J

    2014-03-01

    In the realm of regenerative medicine, human mesenchymal stem cells (hMSCs) are gaining attention as a cell source for the repair and regeneration of tissues spanning an array of medical disciplines. In orthopedics, hMSCs are often delivered in a site-specific manner at the area of interest and may require the concurrent application of local anesthetics (LAs). To address the implications of using hMSCs in combination with anesthetics for intra-articular applications, we investigated the effect that clinically relevant doses of amide-type LAs have on the viability of bone marrow-derived hMSCs and began to characterize the mechanism of LA-induced hMSC death. In our study, culture-expanded hMSCs from three donors were exposed to the amide-type LAs ropivacaine, lidocaine, bupivacaine, and mepivacaine. To replicate the physiological dilution of LAs once injected into the synovial capsule, each anesthetic was reduced to 12.5%, 25%, and 50% of the stock solution and incubated with each hMSC line for 40 minutes, 120 minutes, 360 minutes, and 24 hours. At each time point, cell viability assays were performed. We found that extended treatment with LAs for 24 hours had a significant impact on both hMSC viability and adhesion. In addition, hMSC treatment with three of the four anesthetics resulted in cell death via apoptosis following brief exposures. Ultimately, we concluded that amide-type LAs induce hMSC apoptosis in a time- and dose-dependent manner that may threaten clinical outcomes, following a similar trend that has been established between these particular anesthetics and articular chondrocytes both in vitro and in vivo.

  16. Effect of flumazenil on sevoflurane requirements for minimum alveolar anesthetic concentration-awake and recovery status.

    PubMed

    Liang, Peng; Zhou, Cheng; Li, Kai-Yu; Guo, Li-Juan; Liu, Bin; Liu, Jin

    2014-01-01

    It is controversial that whether the GABA receptors contribute to the hypnotic action of volatile anesthetics. This study was to detect the effect of GABA receptors on the hypnotic action of volatile anesthetics by evaluation of the effect of intravenous flumazenil on sevoflurane minimum alveolar anesthetic concentration-awake (MAC-Awake) and emergence mental status. This study included two steps. Firstly, 49 healthy patients, aged 20-40 years scheduled for elective surgeries, were randomly assigned to two groups, a flumazenil group (n=24) and a saline group (n=25). The flumazenil group received 0.006 mg/Kg IV, and the control group received the same volume of saline 20 min before induction. The flumazenil group and the control group were compared with regard to MAC-Awake (anesthetic concentration achieving 50% probability of eye opening in response to a verbal command). We used the mask inhalation to measure the MAC-Awake by up-and-down method. The second steps, 60 patients undergoing lower abdomen surgeries were randomly divided into two groups, a experimental group (n=30) and a saline group (n=30). All patients were anesthetized with sevoflurane/sulfentanil. The experimental group received flumazenil at 0.006 mg/Kg IV, and the control group received the same volume of saline at the end of surgery. We recorded the time to awake and extubation. After extubation, the patients' recovery status was scored with the Mini-Mental state examination (MMSE) system in post anesthesia care unit (PACU). The MAC-Awake was 0.65% in the control group and 0.82% in the flumazenil group (p=0.34). After extubation, the recovery time and time to extubation showed no difference between the flumazenil group and the saline group (p>0.05). But the 10 min and 15 min MMSE scores after extubation were better in the flumazenil group than those in the saline group (p<0.05). There was no difference for MMSE scores after 30 min between two groups. We found that an IV flumazenil (0.006 mg/Kg) has

  17. Cytotoxicity of local anesthetics and nonionic contrast agents on bovine intervertebral disc cells cultured in a three-dimensional culture system.

    PubMed

    Chee, Ana V; Ren, Jing; Lenart, Brett A; Chen, Er-Yun; Zhang, Yejia; An, Howard S

    2014-03-01

    Carragee et al. reported an accelerated progression of lumbar intervertebral disc (IVD) degeneration after discography in a human trial. Local anesthetics and contrast agents have exhibited toxicity to cardiac, renal, and neuronal cells. We hypothesize that local anesthetics or contrast agents commonly injected into the disc space during discography may result in cytotoxicity in vitro. In this study, we compared the cytotoxicity of these agents, alone or in combination, using nucleus pulposus (NP) and annulus fibrosus (AF) cells in a three-dimensional (3D) culture system. The purpose of this study was to examine the effects of local anesthetics and contrast agents on IVD cells to help guide their usage in future clinical practices. Ours was an in vitro study to assess the cytotoxicity of local anesthetics and contrast agents commonly used in discography, using bovine NP and AF cells cultured in a 3D system. Bovine NP and AF cells were isolated and encapsulated in alginate beads and cultured in media completed with serum and ascorbic acid. Beads were transferred to a 24-well plate and treated with local anesthetics, nonionic contrast agents, or with saline as a control for 2, 6, and 16 hours. Three different concentrations of local anesthetics, lidocaine and bupivacaine, were tested: 0.25%, 0.125%, and 0.0625%. Two different dilutions (1:2 or 1:4) of nonionic contras agents, iohexol and iopamidol, were tested. In a parallel study, beads were incubated with a combination of local anesthetics at equipotent concentrations and contrast agents for 6 hours. Cells were then examined with the LIVE/DEAD cell assay. Live cells (fluorescing green) and dead cells (fluorescing red) were visualized using fluorescent microscopy. The percentage of live cells after treatment was determined. More cell death was observed when NP and AF cells were incubated with anesthetics than contrast agents at the concentrations tested. When tested at equipotent concentrations, 0

  18. Charged local anesthetics block ionic conduction in the sheep cardiac sarcoplasmic reticulum calcium release channel.

    PubMed Central

    Tinker, A; Williams, A J

    1993-01-01

    We have examined the effect of the charged local anesthetics QX314, QX222, and Procaine on monovalent cation conduction in the Ca2+ release channel of the sheep cardiac sarcoplasmic reticulum. All three blockers only affect cation conductance when present at the cytoplasmic face of the channel. QX222 and Procaine act as voltage-dependent blockers. With 500 Hz filtering, this is manifest as a relatively smooth reduction in single-channel current amplitude most prominent at positive holding potentials. Quantitative analysis gives an effective valence of approximately 0.9 for both ions and Kb(0)s of 9.2 and 15.8 mM for QX222 and Procaine, respectively. Analysis of the concentration dependence of block suggests that QX222 is binding to a single site with a Km of 491 microM at a holding potential of 60 mV. The use of amplitude distribution analysis, with the data filtered at 1 to 2 kHz, reveals that the voltage and concentration dependence of QX222 block occurs largely because of changes in the blocker on rate. The addition of QX314 has a different effect, leading to the production of a substate with an amplitude of approximately one-third that of the control. The substate's occurrence is dependent on holding potential and QX314 concentration. Quantitative analysis reveals that the effect is highly voltage dependent, with a valence of approximately 1.5 caused by approximately equal changes in the on and off rates. Kinetic analysis of the concentration dependence of the substate occurrence reveals positive cooperativity with at least two QX314s binding to the conduction pathway, and this is largely accounted for by changes in the on rate. A paradoxical increase in the off rate at high positive holding potentials and with increasing QX314 concentration at 80 mV suggests the existence of a further QX314-dependent reaction that is both voltage and concentration dependent. The substate block is interpreted physically as a form of partial occlusion in the vestibule of the

  19. Effect of a new local anesthetic buffering device on pain reduction during nerve block injections.

    PubMed

    Comerci, Andrew W; Maller, Steven C; Townsend, Richard D; Teepe, John D; Vandewalle, Kraig S

    2015-01-01

    The purpose of this double-blind, split-mouth, randomized human clinical study was to evaluate the effectiveness of a new sodium bicarbonate local anesthetic buffering device (Onset) in reducing pain associated with dental injections. Twenty patients were given bilateral inferior alveolar (IA) and long buccal (LB) nerve block injections and asked to quantify the pain experienced during injection on a visual analog scale (0, no pain; 10, worst possible pain). One side of the mouth received standard-of-care injections of 2% lidocaine with 1:100,000 epinephrine. On the opposite side, after the buffering device was used to mix the components within the anesthetic carpule, patients received injections of 2% lidocaine with 1:100,000 epinephrine buffered 9:1 with 8.4% sodium bicarbonate. The mean pain scores were 2.7 (SD, 1.3) for buffered and 2.7 (SD, 1.9) for unbuffered IA injections. The mean pain scores were 2.0 (SD, 1.4) for buffered and 2.7 (SD, 1.8) for unbuffered LB injections. The data were analyzed with a paired t test (α = 0.05), and no statistically significant difference was found between groups for IA (P = 0.94) or LB (P = 0.17) nerve block injections. In this study of patients receiving common dental nerve block injections, local anesthetic buffering technology did not significantly lessen pain compared to that experienced during a standard unbuffered injection.

  20. Behavioral response and pain perception to computer controlled local anesthetic delivery system and cartridge syringe.

    PubMed

    Yogesh Kumar, T D; John, J Baby; Asokan, Sharath; Geetha Priya, P R; Punithavathy, R; Praburajan, V

    2015-01-01

    The present study evaluated and compared the pain perception, behavioral response, physiological parameters, and the role of topical anesthetic administration during local anesthetic administration with cartridge syringe and computer controlled local anesthetic delivery system (CCLAD). A randomized controlled crossover study was carried out with 120 children aged 7-11 years. They were randomly divided into Group A: Receiving injection with CCLAD during first visit; Group B: Receiving injection with cartridge syringe during first visit. They were further subdivided into three subgroups based on the topical application used: (a) 20% benzocaine; (b) pressure with cotton applicator; (c) no topical application. Pulse rate and blood pressure were recorded before and during injection procedure. Objective evaluation of disruptive behavior and subjective evaluation of pain were done using face legs activity cry consolability scale and modified facial image scale, respectively. The washout period between the two visits was 1-week. Injections with CCLAD produced significantly lesser pain response, disruptive behavior (P < 0.001), and pulse rate (P < 0.05) when compared to cartridge syringe injections. Application of benzocaine produced lesser pain response and disruptive behavior when compared to the other two subgroups, although the result was not significant. Usage of techniques which enhance behavioral response in children like injections with CCLAD can be considered as a possible step toward achieving a pain-free pediatric dental practice.

  1. A clinical trial of long-acting local anesthetics for periodontal surgery.

    PubMed Central

    Crout, R. J.; Koraido, G.; Moore, P. A.

    1990-01-01

    The efficacy of long-acting local anesthetics for anesthesia during periodontal surgery and for analgesia during the immediate postoperative period was evaluated. The rationale for using long-acting local anesthetics such as etidocaine and bupivacaine is that they can provide surgical anesthesia and, because of their long duration, prevent discomfort that may occur for 4-6 hours postoperatively. Two clinical trials were performed. The first enrolled patients requiring bilateral periodontal surgery. Using a matched pair design and double-blind randomized study conditions, 2% lidocaine 1/100,000 epinephrine was compared with 1.5% etidocaine 1/200,000 epinephrine for periodontal surgery. The time until complete recovery and the time until pain onset were found to be longer for the etidocaine surgeries. Postoperative pain appeared more severe, and the need for oral analgesics was greater for the lidocaine surgeries. Surgeons' rating of surgical bleeding was significantly greater for the etidocaine procedures. When matched bilateral surgeries were not available, a second double-blind randomized parallel trial was performed that compared 1.5% etidocaine 1/200,000 epinephrine to 0.5% bupivacaine 1/200,000 epinephrine. No significant differences were seen in the quality of anesthesia, degree of bleeding, or postoperative pain between these two long-acting anesthetics. PMID:2096742

  2. An echocardiographic study of interactions between pindolol and epinephrine contained in a local anesthetic solution.

    PubMed Central

    Sugimura, M.; Hirota, Y.; Shibutani, T.; Niwa, H.; Hori, T.; Kim, Y.; Matsuura, H.

    1995-01-01

    An increasing number of dental patients are taking beta-adrenergic blockers for the treatment of hypertension or angina pectoris. If epinephrine-containing local anesthetics are administered to such patients, interactions between epinephrine and the beta-blocking agent may induce cardiovascular complications. We assessed in volunteers the effects of intraoral injection with 2% lidocaine containing 1:80,000 epinephrine (L-E) on cardiac function after pretreatment with the beta-blocking agent pindolol. M-Mode echocardiography was used for the assessment. The injection of L-E after administration of pindolol did not alter cardiac preload, whereas it reduced the stroke volume, due to an increase in afterload and a decrease in myocardial contractility. Reductions in stroke volume and heart rate led to a decrease in cardiac output. Because total peripheral vascular resistance increased markedly, blood pressure was elevated despite the reduced cardiac output. These results suggest that cardiac function of dental patients on beta-blocker therapy can be adversely affected by epinephrine-containing local anesthetics. Therefore, when such an anesthetic solution has to be used in patients on beta-blocker therapy, careful systemic monitoring is needed. PMID:8934951

  3. Dexmedetomidine as an adjuvant to local anesthetics in brachial plexus blocks

    PubMed Central

    Ping, Yongmei; Ye, Qigang; Wang, Wenwei; Ye, Pingke; You, Zhibin

    2017-01-01

    Abstract Background: Brachial plexus block (BPB) for upper extremity surgery provides superior analgesia, but this advantage is limited by the pharmacological duration of local anesthetics. Dexmedetomidine (DEX) as a local anesthetics adjuvant for BPB has been utilized to prolong the duration of the nerve block in some randomized controlled trials (RCTs) but is far from unanimous in the efficacy and safety of the perineural route. Hence, an updated meta-analysis was conducted to assess the efficacy and safety of DEX as local anesthetic adjuvants on BPB. Methods: A search in electronic databases was conducted to collect the RCTs that investigated the impact of adding DEX to local anesthetics for BPB. Sensory block duration, motor block duration, onset time of sensory and motor block, time to first analgesic request, the common adverse effects were analyzed. Results: Eighteen trails (1014 patients) were included with 515 patients receiving perineural DEX. The addition of DEX prolonged the duration of sensory block (WMD 257 minutes, 95%CI 191.79–322.24, P < 0.001), motor block (WMD 242 minutes, 95%CI 174.94–309.34, P < 0.001), and analgesia (WMD 26 6 minutes, 95%CI 190.75–342.81, P < 0.001). Perineural DEX also increased the risk of bradycardia (OR=8.25, 95%CI 3.95–17.24, P < 0.001), hypotension (OR = 5.62, 95%CI 1.52–20.79, P < 0.01), and somnolence (OR = 19.67, 95%CI 3.94–98.09, P < 0.001). There was a lack of evidence that perineural DEX increased the risk of other adverse events. Conclusions: DEX is a potential anesthetic adjuvant that can facilitate better anesthesia and analgesia when administered in BPB. However, it also increased the risk of bradycardia, hypotension, and somnolence. Further research should focus on the efficacy and safety of the preneural administration of DEX. PMID:28121930

  4. Effect of flumazenil on sevoflurane requirements for minimum alveolar anesthetic concentration-awake and recovery status

    PubMed Central

    Liang, Peng; Zhou, Cheng; Li, Kai-Yu; Guo, Li-Juan; Liu, Bin; Liu, Jin

    2014-01-01

    Objective: It is controversial that whether the GABA receptors contribute to the hypnotic action of volatile anesthetics. This study was to detect the effect of GABA receptors on the hypnotic action of volatile anesthetics by evaluation of the effect of intravenous flumazenil on sevoflurane minimum alveolar anesthetic concentration–awake (MAC-Awake) and emergence mental status. Methods: This study included two steps. Firstly, 49 healthy patients, aged 20-40 years scheduled for elective surgeries, were randomly assigned to two groups, a flumazenil group (n=24) and a saline group (n=25). The flumazenil group received 0.006 mg/Kg IV, and the control group received the same volume of saline 20 min before induction. The flumazenil group and the control group were compared with regard to MAC-Awake (anesthetic concentration achieving 50% probability of eye opening in response to a verbal command). We used the mask inhalation to measure the MAC-Awake by up-and-down method. The second steps, 60 patients undergoing lower abdomen surgeries were randomly divided into two groups, a experimental group (n=30) and a saline group (n=30). All patients were anesthetized with sevoflurane/sulfentanil. The experimental group received flumazenil at 0.006 mg/Kg IV, and the control group received the same volume of saline at the end of surgery. We recorded the time to awake and extubation. After extubation, the patients’ recovery status was scored with the Mini-Mental state examination (MMSE) system in post anesthesia care unit (PACU). Results: The MAC-Awake was 0.65% in the control group and 0.82% in the flumazenil group (p=0.34). After extubation, the recovery time and time to extubation showed no difference between the flumazenil group and the saline group (p>0.05). But the 10 min and 15 min MMSE scores after extubation were better in the flumazenil group than those in the saline group (p<0.05). There was no difference for MMSE scores after 30 min between two groups. Conclusion: We

  5. Minimally Painful Local Anesthetic Injection for Cleft Lip/Nasal Repair in Grown Patients

    PubMed Central

    Price, Christopher; Wong, Alison L.; Chokotho, Tilinde

    2014-01-01

    Introduction: There has been a recent interest in injecting large body and face areas with local anesthetic in a minimally painful manner. The method includes adherence to minimal pain injection details as well feedback from the patient who counts the number of times he feels pain during the injection process. This article describes the successes and limitations of this technique as applied to primary cleft lip/nasal repair in grown patients. Methods: Thirty-two primary cleft lip patients were injected with local anesthesia by 3 surgeons and then underwent surgical correction of their deformity. At the beginning of the injection of the local anesthetic, patients were instructed to clearly inform the injector each and every time they felt pain during the entire injection process. Results: The average patient felt pain only 1.6 times during the injection process. This included the first sting of the first 27-gauge needle poke. The only pain that 51% of the patients felt was that first poke of the first needle; 24% of the patients only felt pain twice during the whole injection process. The worst pain score occurred in a patient who felt pain 6 times during the injection process. Ninety-one percent of the patients felt no pain at all after the injection of the local anesthetic and did not require a top-up. Conclusion: It is possible to successfully and reliably inject local anesthesia in a minimally painful manner for cleft lip and nasal repair in the fully grown cleft patient. PMID:25289364

  6. State-dependent block of Na+ channels by articaine via the local anesthetic receptor.

    PubMed

    Wang, Ging Kuo; Calderon, Joanna; Jaw, Shiow-Jiin; Wang, Sho-Ya

    2009-05-01

    Articaine is widely used as a local anesthetic (LA) in dentistry, but little is known regarding its blocking actions on Na+ channels. We therefore examined the state-dependent block of articaine first in rat skeletal muscle rNav1.4 Na+ channels expressed in Hek293t cells. Articaine exhibited a weak block of resting rNav1.4 Na+ channels at -140 mV with a 50% inhibitory concentration (IC(50)) of 378 +/- 26 microM (n = 5). The affinity was higher for inactivated Na+ channels measured at -70 mV with an IC50 value of 40.6 +/- 2.7 microM (n = 5). The open-channel block by articaine was measured using inactivation-deficient rNav1.4 Na+ channels with an IC50 value of 15.8 +/- 1.5 microM (n = 5). Receptor mapping demonstrated that articaine interacted strongly with a D4S6 phenylalanine residue, which is known to form a part of the LA receptor. Thus the block of rNav1.4 Na+ channels by articaine is via the conserved LA receptor in a highly state-dependent manner, with a ranking order of open (23.9x) > inactivated (9.3x) > resting (1x) state. Finally, the open-channel block by articaine was likewise measured in inactivation-deficient hNav1.7 and rNav1.8 Na+ channels, with IC(50) values of 8.8 +/- 0.1 and 22.0 +/- 0.5 microM, respectively (n = 5), indicating that the high-affinity open-channel block by articaine is indeed preserved in neuronal Na+ channel isoforms.

  7. Block of Inactivation-deficient Na+ Channels by Local Anesthetics in Stably Transfected Mammalian Cells

    PubMed Central

    Wang, Sho-Ya; Mitchell, Jane; Moczydlowski, Edward; Wang, Ging Kuo

    2004-01-01

    According to the classic modulated receptor hypothesis, local anesthetics (LAs) such as benzocaine and lidocaine bind preferentially to fast-inactivated Na+ channels with higher affinities. However, an alternative view suggests that activation of Na+ channels plays a crucial role in promoting high-affinity LA binding and that fast inactivation per se is not a prerequisite for LA preferential binding. We investigated the role of activation in LA action in inactivation-deficient rat muscle Na+ channels (rNav1.4-L435W/L437C/A438W) expressed in stably transfected Hek293 cells. The 50% inhibitory concentrations (IC50) for the open-channel block at +30 mV by lidocaine and benzocaine were 20.9 ± 3.3 μM (n = 5) and 81.7 ± 10.6 μM (n = 5), respectively; both were comparable to inactivated-channel affinities. In comparison, IC50 values for resting-channel block at −140 mV were >12-fold higher than those for open-channel block. With 300 μM benzocaine, rapid time-dependent block (τ ≈ 0.8 ms) of inactivation-deficient Na+ currents occurred at +30 mV, but such a rapid time-dependent block was not evident at −30 mV. The peak current at −30 mV, however, was reduced more severely than that at +30 mV. This phenomenon suggested that the LA block of intermediate closed states took place notably when channel activation was slow. Such closed-channel block also readily accounted for the LA-induced hyperpolarizing shift in the conventional steady-state inactivation measurement. Our data together illustrate that the Na+ channel activation pathway, including most, if not all, transient intermediate closed states and the final open state, promotes high-affinity LA binding. PMID:15545401

  8. Effect of needle design on pain from dental local anesthetic injections.

    PubMed

    McPherson, Joanna Saenz; Dixon, Sara A; Townsend, Richard; Vandewalle, Kraig S

    2015-01-01

    The purpose of this randomized, double-blind clinical study was to evaluate the effectiveness of a larger-bore compared with a standard-bore dental local anesthetic needle of the same gauge in reducing pain during inferior alveolar (IA) and long buccal (LB) nerve block injections. Twenty active duty military or Department of Defense beneficiaries undergoing dental treatment were anesthetized using a split-mouth design with 4 anesthetic dental injections. Both sides of the mouth received IA nerve block and LB nerve injections, one using the 27-gauge large-bore Septoject XL needle and other using a 27-gauge standard-bore Septoject needle. Patients rated the pain experienced with each method using a visual analogue scale (VAS). The IA injection mean VAS score and standard deviation were 38.9 ± 22.7 mm and 37.1 ± 22.4 mm, respectively, for the larger and standard-bore needles. The LB injection mean VAS score and standard deviation were 33.5 ± 22.8 mm and 35.1 ± 19.6 mm, respectively, for the larger and standard-bore needles. The data were analyzed with a paired t test (α = .05). No significant difference was found between the IA (P = .70) or LB injections (P = .73). The use of a larger-bore 27-gauge needle did not reduce pain on injection compared with the standard-bore 27-gauge needle.

  9. Mechanism of local anesthetic effect. Involvement of F0 in the inhibition of mitochondrial ATP synthase by phenothiazines.

    PubMed

    Dabbeni-Sala, F; Palatini, P

    1990-02-02

    The mechanism whereby tertiary amine local anesthetics affect the activity of membrane proteins was investigated by studying the interaction of phenothiazines with mitochondrial ATP synthase. These drugs caused inhibition of the activity of the membrane-bound enzyme at concentrations that do not perturb the phospholipid bilayer. The inhibitory effect appeared consequent to interaction with multiple sites located on both the F1 and the F0 components of the enzyme complex, since: (a) Dixon plots were parabolic; (b) the membrane-bound enzyme was more sensitive to the drug effect than the isolated F1 component; (c) conditions that decreased oligomycin sensitivity also decreased the sensitivity to phenothiazines; (d) irreversible binding of photochemically activated phenothiazines to the ATP synthase complex, followed by detachment of the F1 moiety and reconstitution with purified F1 resulted in an inhibited enzyme complex. These data are interpreted as indicating that tertiary amine local anesthetics affect the activity of membrane proteins by interacting with hydrophobic sites located on both their integral and peripheral domains.

  10. Local anesthetic lidocaine inhibits TRPM7 current and TRPM7-mediated zinc toxicity.

    PubMed

    Leng, Tian-Dong; Lin, Jun; Sun, Hua-Wei; Zeng, Zhao; O'Bryant, Zaven; Inoue, Koichi; Xiong, Zhi-Gang

    2015-01-01

    Previous study demonstrated that overstimulation of TRPM7 substantially contributes to zinc-mediated neuronal toxicity. Inhibition of TRPM7 activity and TRPM7-mediated intracellular Zn(2+) accumulation may represent a promising strategy in the treatment of stroke. To investigate whether local anesthetics lidocaine could inhibit TRPM7 channel and TRPM7-mediated zinc toxicity. Whole-cell patch-clamp technique was used to investigate the effect of local anesthetics on TRPM7 currents in cultured mouse cortical neurons and TRPM7-overexpressed HEK293 cells. Fluorescent Zn(2+) imaging technique was used to study the effect of lidocaine on TRPM7-mediated intracellular Zn(2+) accumulation. TRPM7-mediated zinc toxicity in neurons was used to evaluate the neuroprotective effect of lidocaine. (1) Lidocaine dose dependently inhibits TRPM7-like currents, with an IC50 of 11.55 and 11.06 mM in cultured mouse cortical neurons and TRPM7-overexpressed HEK293 cells, respectively; (2) Lidocaine inhibits TRPM7 currents in a use/frequency-dependent manner; (3) Lidocaine inhibits TRPM7-mediated intracellular Zn(2+) accumulation in both cortical neurons and TRPM7-overexpressed HEK293 cells; (4) TRPM7-mediated Zn(2+) toxicity is ameliorated by lidocaine in cortical neurons; (5) QX-314 has a similar inhibitory effect as lidocaine on TRPM7 currents when applied extracellularly; (6) Procaine also shows potent inhibitory effect on the TRPM7 currents in cortical neurons. Our data provide the first evidence that local anesthetic lidocaine inhibits TRPM7 channel and TRPM7-mediated zinc toxicity. © 2014 John Wiley & Sons Ltd.

  11. Reduction of environmental temperature mitigates local anesthetic cytotoxicity in bovine articular chondrocytes.

    PubMed

    Onur, Tarik; Dang, Alexis

    2014-09-01

    The purpose of this study was to assess whether reducing environmental temperature will lead to increased chondrocyte viability following injury from a single-dose of local anesthetic treatment. Bovine articular chondrocytes from weight bearing portions of femoral condyles were harvested and cultured. 96-well plates were seeded with 15,000 chondrocytes per well. Chondrocytes were treated with one of the following conditions: ITS Media, 1x PBS, 2% lidocaine, 0.5% bupivacaine, or 0.5% ropivacaine. Each plate was then incubated at 37°C, 23°C, or 4°C for one hour and then returned to media at 37°C. Chondrocyte viability was assessed 24 hours after treatment. Chondrocyte viability is presented as a ratio of the fluorescence of the treatment group over the average of the media group at that temperature (ratio ± SEM). At 37°C, lidocaine (0.35 ± 0.04) and bupivacaine (0.30 ± 0.05) treated chondrocytes show low cell viability when compared to the media (1.00 ± 0.03) control group (p < 0.001). Lidocaine treated chondrocytes were significantly more viable at 23°C (0.84 ± 0.08) and 4°C (0.86±0.085) than at 37°C (p < 0.001). Bupivacaine treated chondrocytes were significantly more viable at 4°C (0.660 ± 0.073) than at 37°C or 23°C (0.330 ± 0.069) (p < 0.001 and p = 0.002 respectively). Reducing the temperature from 37°C to 23°C during treatment with lidocaine increases chondrocyte viability following injury. Chondrocytes treated with bupivacaine can be rescued by reducing the temperature to 4°C. Key pointsConfirm that local anesthetics, specifically bupivacaine and lidocaine, are toxic to chondrocytes in monolayerChondrocyte viability significantly improved for chondrocytes treated with bupivacaine when the environment was cooled to 23°C.Chondrocyte viability significantly improved for chondrocytes treated with bupivacaine or lidocaine when the environment was cooled to 4°CIt is the recommendation of the authors that physicians should be wary of the

  12. [Investigation, identification and dosage of local anesthetics and antihistaminics in cosmetic products].

    PubMed

    Barbato, F; La Rotonda, M I; Morrica, P; Santagada, V

    1990-08-01

    A rapid and accurate reversed-phase HPLC method for separation and simultaneous quantitation of some local anesthetics, antihistamines and preservatives in skin cosmetics is described. The investigated compounds (procaine, lidocaine, mepivacaine, bupivacaine, benzocaine, brompheniramine, benzoic acid, methyl, ethyl and propyl p-hydroxybenzoate, o-phenylphenol) are extracted by ultrasonic treatment in methanol from cosmetic form. Methanol-aqueous orthophosphoric acid (pH 2.8) containing 0.9% dibutylamine has been used as eluent. The influence of different percentages of methanol on chromatographic behaviour has been studied using both isocratic conditions and gradient elution program. The gradient program allows a rapid resolution and quantitation also for acidic preservatives.

  13. Evaluating complications during intraoral administration of local anesthetics in a rural, portable special needs dental clinic.

    PubMed

    Boynes, Sean; Riley, Amah; Milbee, Sarah

    2014-01-01

    The aim of this study was to identify and quantify complications with local anesthetic administration on consecutive patients seen for dental care in a portable dental clinic providing care to patients with special needs. This prospective study includes data on the patients seen by the portable dental team. A standardized form is used to determine complications and associated information for 172 dental visits in which local anesthetic is administered. After statistical analysis of 172 consecutive cases, the overall complication rate is 8.1%. All of the complications are considered to be mild or moderate; there are no reports of severe events. The complications encountered most frequently are associated with self-inflicted soft tissue injury or inadequate anesthesia. Comprehensive care with local anesthesia delivered by a portable dental clinic has a low risk of complication. The administration of an inferior alveolar nerve block or body-mass status appears to affect the incidence of complications. © 2013 Special Care Dentistry Association and Wiley Periodicals, Inc.

  14. Intraosseous injection as an adjunct to conventional local anesthetic techniques: A clinical study

    PubMed Central

    Idris, Mohamed; Sakkir, Nasil; Naik, Kishore Gopalakrishna; Jayaram, Nandakishore Kunijal

    2014-01-01

    Background: The achievement of successful local anesthesia is a continual challenge in dentistry. Adjunctive local anesthetic techniques and their armamentaria, such as intraosseous injection (the Stabident system and the X-tip system) have been proposed to be advantageous in cases where the conventional local anesthetic techniques have failed. Aim: A clinical study was undertaken using intraosseous injection system by name X-tip to evaluate its effectiveness in cases where inferior alveolar nerve block has failed to provide pulpal anesthesia. Materials and Methods: Sixty adult patients selected were to undergo endodontic treatment for a mandibular molar tooth. Inferior alveolar nerve block was given using 4% articaine with 1:100,000 epinephrine. Twenty-four patients (40%) had pain even after administration of IAN block; intraosseous injection was administered using 4% articaine containing 1:100,000 epinephrine, using the X-tip system. The success of X-tip intraosseous injection was defined as none or mild pain (Heft-Parker visual analog scale ratings ≤ 54 mm) on endodontic access or initial instrumentation. Results: Intraosseous injection technique was successful in 21 out of 24 patients (87.5%), except three patients who had pain even after supplemental X-tip injection. Conclusion: Within the limits of this study, we can conclude that supplemental intraosseous injection using 4% articaine with 1:100,000 epinephrine has a statistically significant influence in achieving pulpal anesthesia in patients with irreversible pulpitis. PMID:25298642

  15. Reversed-phase liquid chromatographic retention and membrane activity relationships of local anesthetics.

    PubMed

    Tsuchiya, Hironori; Mizogami, Maki; Takakura, Ko

    2005-05-06

    The chromatographic retention and membrane activity relationships of local anesthetics were studied to address the possible mechanisms for structure specificity and inflammation-associated decrease of their effects. Five representative drugs (3 mM for each) were reacted with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine liposomes in 25 mM potassium phosphate buffer (pH 5.9-7.9, containing 100 mM NaCl and 0.1 mM EDTA) for 10 min at 37 degrees C and the membrane fluidity changes were analyzed by measuring fluorescence polarization with 1,6-diphenyl-1,3,5-hexatriene. Their capacity factors were determined on octadecyl-, octyl- and phenyl-bonded silica columns with a mobile phase consisting of 25 mM potassium phosphate buffer (pH 5.9-7.9, containing 100 mM NaCl and 0.1 mM EDTA)-methanol (30:70, v/v) at a flow rate of 1.0 ml/min and at a column temperature of 37 degrees C and diode-array detection. Mepivacaine, prilocaine, lidocaine, ropivacaine and bupivacaine fluidized membranes in increasing order of intensity, which agreed with their clinical potency. The relative degree of membrane fluidization correlated with that of retention on an octadecyl stationary phase more significantly than the other phases. Both membrane-fluidizing effects and capacity factors decreased by lowering the reaction and mobile phase pH, being consistent with the hypothesis that anesthetic potency is reduced in inflammation because of tissue acidity. Reversed-phase liquid chromatography appears to be useful for estimating the structure-specific and pH-dependent membrane-fluidizing effects of local anesthetics.

  16. Articaine hydrochloride: a study of the safety of a new amide local anesthetic.

    PubMed

    Malamed, S F; Gagnon, S; Leblanc, D

    2001-02-01

    Articaine is an amide local anesthetic introduced clinically in Germany in 1976 and subsequently throughout Europe, Canada and, in 2000, the United States. The authors report on three identical single-dose, randomized, double-blind, parallel-group, active-controlled multicenter studies that were conducted to compare the safety and efficacy of articaine (4 percent with epinephrine 1:100,000) with that of lidocaine (2 percent with epinephrine 1:100,000). A total of 1,325 subjects participated in these studies, 882 of whom received articaine 4 percent with epinephrine 1:100,000 and 443 of whom received lidocaine 2 percent with epinephrine 1:100,000. The overall incidence of adverse events in the combined studies was 22 percent for the articaine group and 20 percent for the lidocaine group. The most frequently reported adverse events in the articaine group, excluding postprocedural dental pain, were headache (4 percent), facial edema, infection, gingivitis and paresthesia (1 percent each). The incidence of these events was similar to that reported for subjects who received lidocaine. The adverse events most frequently reported as related to articaine use were paresthesia (0.9 percent), hypesthesia (0.7 percent), headache (0.55 percent), infection (0.45 percent), and rash and pain (0.3 percent each). Articaine is a well-tolerated, safe and effective local anesthetic for use in clinical dentistry.

  17. Ultrasound visibility of spinal structures and local anesthetic spread in children undergoing caudal block.

    PubMed

    Shin, Seokyung; Kim, Ji Young; Kim, Won Oak; Kim, Seung Hyun; Kil, Hae Keum

    2014-11-01

    This study assessed ultrasound visibility of spinal structures in children and observed the extent of local anesthetic spread within the epidural space during caudal block. Spinal structures were evaluated with ultrasound from the sacral area to the thoracic area in 80 children, and drug spread levels were observed after caudal injection of 0.5, 1.0, 1.25 and 1.5 mL/kg local anesthetic. The conus medullaris, dural sac and dura mater were easily identified with ultrasound in most children. However, ligamentum flavum visibility declined with increasing vertebral level and markedly decreased at the thoracic level in children older than 7 mo or heavier than 8.5 kg. Drug spread was higher with increasing volume (p < 0.001) and in children ≤12 mo more than children >12 mo (p < 0.001); drug spread was significantly correlated with age (R(2) = 0.534). Spread levels assessed with ultrasound were roughly two to three segments lower than those in previous radiologic studies. Copyright © 2014 World Federation for Ultrasound in Medicine & Biology. Published by Elsevier Inc. All rights reserved.

  18. Lipid emulsion improves survival in animal models of local anesthetic toxicity: a meta-analysis.

    PubMed

    Fettiplace, Michael R; McCabe, Daniel J

    2017-08-01

    The Lipid Emulsion Therapy workgroup, organized by the American Academy of Clinical Toxicology, recently conducted a systematic review, which subjectively evaluated lipid emulsion as a treatment for local anesthetic toxicity. We re-extracted data and conducted a meta-analysis of survival in animal models. We extracted survival data from 26 publications and conducted a random-effect meta-analysis based on odds ratio weighted by inverse variance. We assessed the benefit of lipid emulsion as an independent variable in resuscitative models (16 studies). We measured Cochran's Q for heterogeneity and I(2) to determine variance contributed by heterogeneity. Finally, we conducted a funnel plot analysis and Egger's test to assess for publication bias in studies. Lipid emulsion reduced the odds of death in resuscitative models (OR =0.24; 95%CI: 0.1-0.56, p = .0012). Heterogeneity analysis indicated a homogenous distribution. Funnel plot analysis did not indicate publication bias in experimental models. Meta-analysis of animal data supports the use of lipid emulsion (in combination with other resuscitative measures) for the treatment of local anesthetic toxicity, specifically from bupivacaine. Our conclusion differed from the original review. Analysis of outliers reinforced the need for good life support measures (securement of airway and chest compressions) along with prompt treatment with lipid.

  19. Analysis of clinical records of dental patients attending Jordan University Hospital: Documentation of drug prescriptions and local anesthetic injections

    PubMed Central

    Dar-Odeh, Najla; Ryalat, Soukaina; Shayyab, Mohammad; Abu-Hammad, Osama

    2008-01-01

    Objectives: The aim of this study was to analyze clinical records of dental patients attending the Dental Department at the University of Jordan Hospital: a teaching hospital in Jordan. Analysis aimed at determining whether dental specialists properly documented the drug prescriptions and local anesthetic injections given to their patients. Methods: Dental records of the Dental Department at the Jordan University Hospital were reviewed during the period from April 3rd until April 26th 2007 along with the issued prescriptions during that period. Results: A total of 1000 records were reviewed with a total of 53 prescriptions issued during that period. Thirty records documented the prescription by stating the category of the prescribed drug. Only 13 records stated the generic or the trade names of the prescribed drugs. Of these, 5 records contained the full elements of a prescription. As for local anesthetic injections, the term “LA used” was found in 22 records while the names and quantities of the local anesthetics used were documented in only 13 records. Only 5 records documented the full elements of a local anesthetic injection. Conclusion: The essential data of drug prescriptions and local anesthetic injections were poorly documented by the investigated group of dental specialists. It is recommended that the administration of the hospital and the dental department implement clear and firm guidelines for dental practitioners in particular to do the required documentation procedure. PMID:19209291

  20. Which one is more effective for analgesia in infratentorial craniotomy? The scalp block or local anesthetic infiltration.

    PubMed

    Akcil, Eren Fatma; Dilmen, Ozlem Korkmaz; Vehid, Hayriye; Ibısoglu, Lutfiye Serap; Tunali, Yusuf

    2017-03-01

    The most painful stages of craniotomy are the placement of the pin head holder and the skin incision. The primary aim of the present study is to compare the effects of the scalp block and the local anesthetic infiltration with bupivacaine 0.5% on the hemodynamic response during the pin head holder application and the skin incision in infratentorial craniotomies. The secondary aims are the effects on pain scores and morphine consumption during the postoperative 24h. This prospective, randomized and placebo controlled study included forty seven patients (ASA I, II and III). The scalp block was performed in the Group S, the local anesthetic infiltration was performed in the Group I and the control group (Group C) only received remifentanil as an analgesic during the intraoperative period. The hemodynamic response to the pin head holder application and the skin incision, as well as postoperative pain intensity, cumulative morphine consumption and opioid related side effects were compared. The scalp block reduced the hemodynamic response to the pin head holder application and the skin incision in infratentorial craniotomies. The local anesthetic infiltration reduced the hemodynamic response to the skin incision. As well as both scalp block and local anesthetic infiltration reduced the cumulative morphine consumption in postoperative 24h. Moreover, the pain intensity was lower after scalp block in the early postoperative period. The scalp block may provide better analgesia in infratentorial craniotomies than local anesthetic infiltration. Copyright © 2017 Elsevier B.V. All rights reserved.

  1. Effects of tertiary amine local anesthetics on the assembly and disassembly of brain microtubules in vitro.

    PubMed

    Genna, J M; Coffe, G; Pudles, J

    1980-09-01

    From kinetic and electron microscopy studies on the effects of procaine, tetracaine and dibucaine on the polymerization and depolymerization of the microtubules isolated from pig and rat brains the following results were obtained. 1. Procaine or tetracaine, at the concentration range of 0.5--20 mM and of 0.5--5 mM respectively, increases the rate of tubulin polymerization (24 degrees C or 37 degrees C) and of microtubule depolymerization (4 degrees C) as a linear function of the concentration of the anesthetics, while identical amounts of microtubules are formed. In the absence of microtubule-associated proteins the polymerization of tubulin is not induced by 10 mM procaine, furthermore, the critical concentration of microtubule proteins necessary for assembly into microtubules is not affected at this concentration level of the anesthetic. This suggests that procaine affects not the nucleation, but rather the elongation process. 2. Dibucaine, from 0.5 mM to 3 mM increases the lag time of the polymerization reaction, while from 0.5 mM to 2 mM it linearly decreases both tubulin polymerization (24 degrees C) and microtubule depolymerization (4 degrees C) rates. Dibucaine, up to mM concentration, does not affect the extent of tubulin polymerization; however, above this concentration it induces the formation of amorphous aggregates. 3. Procaine or tetracaine enhances the depolymerizing effect of calcium on microtubules. The half-maximal values for the depolymerizing effect of calcium were 0.96, 0.71 and 0.51 mM for the control, in the presence of 10 mM procaine and 5 mM tetracaine respectively.

  2. Local anesthetic effects of cocaine and several extracts of the coca leaf (E. coca).

    PubMed

    Bedford, J A; Turner, C E; Elsohly, H N

    1984-05-01

    Cocaine and a number of different fractions of a crude ethanol extract of the coca leaf (E. coca) were subjected to a local anesthetic screen using rat tail withdrawal from electric shock. Following an intradermal injection of 0.1 ml of a 2.0% (w.v) solution of cocaine HCl, an immediate response was observed. Two of the coca fractions also produced some local anesthesia. An alkaloidal fraction, containing an equivalent amount of cocaine, produced a maximum effect that was approximately 20% less than that observed with cocaine. The only other fraction producing any effect, a water soluble cocaine-free fraction, showed a maximum response that was approximately 30% of that observed with cocaine.

  3. [Comparative effects of vitamin C on the effects of local anesthetics ropivacaine, bupivacaine, and lidocaine on human chondrocytes].

    PubMed

    Tian, Jun; Li, Yan

    2016-01-01

    Intra-articular injections of local anesthetics are commonly used to enhance post-operative analgesia following orthopedic surgery as arthroscopic surgeries. Nevertheless, recent reports of severe complications due to the use of intra-articular local anesthetic have raised concerns. The study aims to assess use of vitamin C in reducing adverse effects of the most commonly employed anesthetics - ropivacaine, bupivacaine and lidocaine - on human chondrocytes. The chondrocyte viability following exposure to 0.5% bupivacaine or 0.75% ropivacaine or 1.0% lidocaine and/or vitamin C at doses 125, 250 and 500μM was determined by Live/Dead assay and annexin V staining. Expression levels of caspases 3 and 9 were assessed using antibodies by Western blotting. Flow cytometry was performed to analyze the generation of reactive oxygen species. On exposure to the local anesthetics, chondrotoxicity was found in the order ropivacainelocal anesthetics ropivacaine, bupivacaine and lidocaine. Copyright © 2015 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  4. Comparative effects of vitamin C on the effects of local anesthetics ropivacaine, bupivacaine, and lidocaine on human chondrocytes.

    PubMed

    Tian, Jun; Li, Yan

    2016-01-01

    Intra-articular injections of local anesthetics are commonly used to enhance post-operative analgesia following orthopedic surgery as arthroscopic surgeries. Nevertheless, recent reports of severe complications due to the use of intra-articular local anesthetic have raised concerns. The study aims to assess use of vitamin C in reducing adverse effects of the most commonly employed anesthetics - ropivacaine, bupivacaine and lidocaine - on human chondrocytes. The chondrocyte viability following exposure to 0.5% bupivacaine or 0.75% ropivacaine or 1.0% lidocaine and/or vitamin C at doses 125, 250 and 500 μM was determined by LIVE/DEAD assay and annexin V staining. Expression levels of caspases 3 and 9 were assessed using antibodies by Western blotting. Flow cytometry was performed to analyze the generation of reactive oxygen species. On exposure to the local anesthetics, chondrotoxicity was found in the order ropivacainelocal anesthetics ropivacaine, bupivacaine and lidocaine. Copyright © 2015 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  5. 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.

  6. Inhalational and local anesthetics reduce tactile and thermal responses in mimosa pudica.

    PubMed

    Milne, A; Beamish, T

    1999-03-01

    In reaction to a variety of stimuli, the sensitive plant mimosa pudica closes its leaflets and drops its stems. The objective was to investigate the effects of anaesthetics on the reaction of mimosa pudica to a variety of stimuli. The ability of the plants leaflets to close (n=4, Q5min.) was tested after exposure to halothane 4% and 6L x min(-1) O2, or 6L x min(-1) O2. Lidocaine 2% or vehicle were administered through the roots, cut stems, or sprayed on the leaves (n=4). The test consisted of stimulating the leaves, by burning their tips (lidocaine experiments) or touching them with a metal rod (halothane); the closing of the leaflets, or the lack thereof was then observed. After 15 min exposure to halothane, the mimosas had slow and incomplete reactions to tactile stimulation. Following 20 min exposure, the plants had no visible reaction to touch, a stimulus which would normally cause the collapse of the entire leaf. After one minute, mimosa leaves sprayed with lidocaine had no reaction to a lit match being touched to the tips of the leaves, contrary to the control in which the leaves collapsed completely. After exposure to lidocaine 2% through the roots and cut stems, the mimosa's reactivity gradually decreased; after four hours the leaves were insensitive or had slow reaction to tactile stimuli. Inhalational and local anesthetics inhibited motor mechanisms of the mimosa plant. This may be a model to elucidate the mechanisms of action of anesthetics.

  7. Simultaneous determination of four local anesthetics by CE with ECL and study on interaction between procainamide and human serum albumin.

    PubMed

    Duan, Hong-Bing; Cao, Jun-Tao; Yang, Jiu-Jun; Wang, Hui; Liu, Yan-Ming

    2016-07-01

    A new method of capillary electrophoresis (CE) coupled with tris(2, 2'-bipyridyl) ruthenium(II) electrochemiluminescence (ECL) detection has been developed to detect four local anesthetics procainamide (PAH), tetracaine (TCH), proparacaine (PCH) and cinchocaine (CIN) simultaneously. An europium (III)-doped prussian blue analogue film (Eu-PB) modified platinum electrode was prepared and applied to improve the detection sensitivity. The parameters including additives, concentration and pH of the running buffer, separation voltage and detection potential that affect CE separation and ECL detection were optimized in detail. The four local anesthetics were baseline separated and detected within 10min under the optimized conditions. The detection limits (LOD) of PAH, TCH, PCH and CIN are 5.5×10(-8), 9.6×10(-8), 2.5×10(-8) and 3.5×10(-8)molL(-1) (S/N=3), respectively. RSDs of the migration time for four analytes range from 1.2% to 2.5% within intraday and from 2.4% to 4.9% in interday, RSDs of the peak area for four analytes are from 1.7% to 3.3% within intraday and from 2.2% to 5.6% in interday, respectively. The limits of quantitation (LOQ) (S/N=10) for PAH, TCH, PCH and CIN in human urine sample are 5.9×10(-7), 9.2×10(-7), 8.3×10(-7) and 5.0×10(-7)molL(-1), separately. The recoveries (n=3) of four analytes in human urine are from 87.6% to 107.7% with less than 5.9% in RSDs. The developed method was used to determine four local anesthetics in human urine samples and investigate the interaction between PAH and human serum albumin (HSA). The number of binding sites and the binding constant of PAH with HSA were calculated to be 1.03 and 2.4×10(4)Lmol(-1), respectively.

  8. Minimum anesthetic concentration and cardiovascular dose-response relationship of isoflurane in cinereous vultures (Aegypius monachus).

    PubMed

    Kim, Young K; Lee, Scott S; Suh, Euy H; Lee, Lyon; Lee, Hee C; Lee, Hyo J; Yeon, Seong C

    2011-09-01

    This study aimed to determine the minimum anesthetic concentration (MAC) and dose-related cardiovascular effects of isoflurane during controlled ventilation in cinereous vultures (Aegypius monachus). The MAC was determined for 10 cinereous vultures as the midpoint between the end-tidal isoflurane concentration that allows gross purposeful movement and that which prevents the movement in response to clamping a pedal digit. Immediately after the MAC was determined, the cardiovascular effects of isoflurane at 1.0, 1.5, and 2.0 times the MAC were investigated in seven of the 10 birds. The MAC of isoflurane for 10 cinereous vultures during controlled ventilation was 1.06 +/- 0.07% (mean +/- SD). When the isoflurane concentration was increased to 1.5 and 2.0 times the MAC, there was significant dose-dependent decrease in the arterial blood pressure. However, the heart rate did not change over a range of 1.0 to 2.0 times the MAC.

  9. [New anesthetics].

    PubMed

    Malamed, S F

    2000-01-01

    Since the introduction of cocaine local analgesia in 1886, and the subsequent development of procaine (1904) and other closely related ester-type compounds, dentistry has prided itself on being as close to 'painless' as possible. In the late 1940s the newest group of the local anesthetic compounds, the amides, was introduced. The initial amide local analgesic, lignocaine (Xylocaine), revolutionised pain control in dentistry worldwide. In succeeding years other amide-type local anesthetics, mepivacaine, prilocaine, bupivacaine and etidocaine, were introduced. They gave the dental practitioner a local anesthetic armamentarium which provided pulpal analgesia for periods of from 20 minutes (mepivacaine) to as long as three hours (bupivacaine and etidocaine with adrenaline). In addition these popular drugs proved to be more rapid-acting than the older ester-type drug and, at least from the perspective of allergenicity, more safe. In 1976, in Germany, the newest amide local analgesic, carticaine HCl was introduced into dentistry. Articaine (the generic name was changed) possesses properties similar to lignocaine but has additional properties which made the drug quite attractive to the general dental practitioner. In 1986 articaine was introduced in North America (Canada) where it has become the most used local anesthetic, supplanting lignocaine. Articaine has been approved for use in the United Kingdom. In this introductory discussion we review the development of articaine and discuss its place in the dental local analgesic armamentarium.

  10. Local anesthetic failure associated with inflammation: verification of the acidosis mechanism and the hypothetic participation of inflammatory peroxynitrite

    PubMed Central

    Ueno, Takahiro; Tsuchiya, Hironori; Mizogami, Maki; Takakura, Ko

    2008-01-01

    The presence of inflammation decreases local anesthetic efficacy, especially in dental anesthesia. Although inflammatory acidosis is most frequently cited as the cause of such clinical phenomena, this has not been experimentally proved. We verified the acidosis mechanism by studying the drug and membrane lipid interaction under acidic conditions together with proposing an alternative hypothesis. Liposomes and nerve cell model membranes consisting of phospholipids and cholesterol were treated at different pH with lidocaine, prilocaine and bupivacaine (0.05%–0.2%, w/v). Their membrane-interactive potencies were compared by the induced-changes in membrane fluidity. Local anesthetics fluidized phosphatidylcholine membranes with the potency being significantly lower at pH 6.4 than at pH 7.4 (p < 0.01), supporting the acidosis theory. However, they greatly fluidized nerve cell model membranes even at pH 6.4 corresponding to inflamed tissues, challenging the conventional mechanism. Local anesthetics acted on phosphatidylserine liposomes, as well as nerve cell model membranes, at pH 6.4 with almost the same potency as that at pH 7.4, but not on phosphatidylcholine, phosphatidylethanolamine and sphingomyelin liposomes. Since the positively charged anesthetic molecules are able to interact with nerve cell membranes by ion-paring with anionic components like phosphatidylserine, tissue acidosis is not essentially responsible for the local anesthetic failure associated with inflammation. The effects of local anesthetics on nerve cell model membranes were inhibited by treating with peroxynitrite (50 μM), suggesting that inflammatory cells producing peroxynitrite may affect local anesthesia. PMID:22096346

  11. Pregnancy outcome after in utero exposure to local anesthetics as part of dental treatment: A prospective comparative cohort study.

    PubMed

    Hagai, Aharon; Diav-Citrin, Orna; Shechtman, Svetlana; Ornoy, Asher

    2015-08-01

    Dental treatment and use of local anesthetics during pregnancy generally are considered harmless because of lack of evidence of adverse pregnancy effects. Data on the safety of dental treatment and local anesthetics during pregnancy are scant. Dental care is often a reason for concern both among women and their health care providers. The primary objective of this study was to evaluate the rate of major anomalies after exposure to local anesthetics as part of dental care during pregnancy. The authors performed a prospective, comparative observational study at the Israeli Teratology Information Services between 1999 and 2005. The authors followed 210 pregnancies exposed to dental local anesthetics (112 [53%] in the first trimester) and compared them with 794 pregnancies not exposed to teratogens. The rate of major anomalies was not significantly different between the groups (4.8% versus 3.3%, P = .300). There was no difference in the rate of miscarriages, gestational age at delivery, or birth weight. The most common types of dental treatment were endodontic treatment (43%), tooth extraction (31%), and tooth restoration (21%). Most women (63%) were not exposed to additional medications. Approximately one-half (51%) of the women were not exposed to dental radiography, and 44% were exposed to radiation, mostly bite-wing radiography. This study's results suggest that use of dental local anesthetics, as well as dental treatment during pregnancy, do not represent a major teratogenic risk. There seems to be no reason to prevent pregnant women from receiving dental treatment and local anesthetics during pregnancy. Copyright © 2015 American Dental Association. Published by Elsevier Inc. All rights reserved.

  12. Dissociation of the vacuolar and macroautophagic cytopathology from the cytotoxicity induced by the lipophilic local anesthetic bupivacaine.

    PubMed

    Morissette, Guillaume; Bawolak, Marie-Thérèse; Marceau, François

    2011-07-01

    Local anesthetics, like many other cationic drugs, induce a vacuolar and macroautophagic cytopathology that has been observed in vivo and in various cell types; some also induce cytotoxicity of mitochondrial origin (apoptosis and necrosis) and it is not known whether the 2 types of toxicity overlap or interact. We compared bupivacaine with a more hydrophilic agent, lidocaine, for morphological, functional, and toxicological responses in a previously exploited nonneuronal system, primary smooth muscle cells. Bupivacaine induced little vacuolization (≥2.5 mmol/L, 4 h), but elicited autophagic accumulation (≥0.5 mmol/L, 4 h) and was massively cytotoxic at 2.5-5 mmol/L (4-24 h), the latter effect being unabated by the V-ATPase inhibitor bafilomycin A1. Lidocaine exerted little cytotoxicity at and below 5 mmol/L for 24 h, but intensely induced the V-ATPase-dependent vacuolar and autophagic cytopathology. Bupivacaine was more potent than lidocaine in disrupting mitochondrial potential, as judged by Mitotracker staining (significant proportions of cells affected in the 1-5 and 5-10 mmol/L concentration ranges, respectively). The addition of mitochondrial-inactivating toxins antimycin A and oligomycin to lidocaine (2.5 mmol/L) reproduced the profile of bupivacaine action (low intensity of vacuolization and retained autophagic accumulation). The high potency of bupivacaine as a mitochondrial toxicant eclipses the benign vacuolar and autophagic response seen with more hydrophilic local anesthetics.

  13. [Therapy of articular and periarticular pain with local anesthetics (neural therapy of Huneke). Long and short term results].

    PubMed

    Barbagli, P; Bollettin, R

    1998-01-01

    Assessment of the outcomes on the articular and periarticular pain of the knee, by a reflexotherapy with local anesthetics, denominated also neuraltherapy. Retrospective observational study with 3 years' follow-up. An Ambulatory Center for Pain Management. All the patients (N = 115) with knee pain treated with neuraltherapy in the period 1982-31 August 1996 (retired patients 2, mean age 68 +/- 15.2 years in the remaining). The employed reflexotherapy, denominated also neuraltherapy by Huneke, uses a local anesthetic (prevalently lidocaine) in 0.5-1% concentration and small quantity (0.5-1 ml for point) on tender/trigger and/or acupuncture points, as well as in anatomical structures like articulations, nerves, arteries or veins. The number of sessions has been of 7.03 +/- 3.3. Outcomes are evaluated in terms of percentage subjective improvement of the pain at the end of the therapy and at 1-3-6 months, 1-2-3 years, and then divided in 5 groups (no improvement-fair-good-very good-excellent). At the end of the therapy the improven cases were the 91.2%, the 83.7% at 1 month, the 64.6% at 3 months, the 41.3% at 6 months, the 22.5% at 1 year, the 12.1% at 2 years and the 7.9% at 3 years. These outcomes suggest a good effectiveness of this treatment in the painful diseases of the knee, but further randomised double-blind trials are necessary.

  14. 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

  15. A mixed (long- and medium-chain) triglyceride lipid emulsion extracts local anesthetic from human serum in vitro more effectively than a long-chain emulsion.

    PubMed

    Ruan, Weiming; French, Deborah; Wong, Alicia; Drasner, Kenneth; Wu, Alan H B

    2012-02-01

    Lipid emulsion infusion reverses cardiac toxicity of local anesthetics. The predominant effect is likely creation of a "lipid sink." This in vitro study determined the extent to which Intralipid® (Fresenius Kabi, Uppsala, Sweden) and Lipofundin® (B. Braun Melsungen AG, Melsungen, Germany) sequester anesthetics from serum, and whether it varies with pH. Bupivacaine, ropivacaine, and mepivacaine were added to human drug-free serum (pH 7.4) at 10 μg/ml. The lipid emulsions were added, and the mixture shaken and incubated at 37°C. Lipid was removed by ultracentrifugation and drug remaining in the serum measured. Additional experiments were performed using 100 μg/ml bupivacaine and at pH 6.9. Lipofundin® extracted all three anesthetics to a greater extent than Intralipid® (34.7% vs..22.3% for bupivacaine, 25.8% vs..16.5% for ropivacaine, and 7.3% vs..4.7% for mepivacaine). By increasing either concentration of bupivacaine or lipid, there was an increase in drug extraction from serum. Adjusting the pH to 6.9 had no statistically significant effect on the percentage of bupivacaine sequestered. Bupivacaine, ropivacaine, and mepivacaine were sequestered to an extent consistent with their octanol:water partition constants (logP). In contrast with previous studies of extraction of lipids from buffer solutions, an emulsion containing 50% each of medium- and long-chain triglycerides extracted local anesthetics to a greater extent from human serum than one containing exclusively long-chain triglycerides, calling into question recent advanced cardiac life support guidelines for resuscitation from anesthetic toxicity that specify use of a long-chain triglyceride. The current data also do not support recent recommendations to delay administration until pH is normalized.

  16. Computer simulation of local anesthetic effects using a mathematical model of myelinated nerve.

    PubMed

    Condouris, G A; Goebel, R H; Brady, T

    1976-03-01

    A mathematical model of myelinated axon was programmed for digital computer solution of the consequences of the conduction characteristics when the model membrane was affected by local anesthetics simulated by alteration of the ionic conductance parameter. The effects of tetrodotoxin on impulse conduction were studied in detail by means of a systematic reduction in sodium conductance in 1 to 10 nodes of Ranvier. Rhis technique simulates the method used experimentally and clinically to achieve a conduction block with the circumscribed application of local anesthetics to segments of nerve axons or nerve trunks. The analysis of the tetrodotoxin "dose-response" relationships revealed the fact that the model myelinated axon could support three types of conduction when depressed by this drug. One type of conduction of a subnormal impulse at the nodes of Ranvier; a second is characterized by a form of decremental conduction in which the rate of decrement of the nodal impulse is linear with distance. The third type is a second form of decremental conduction which is exponential in configuration and is seen when the g(Na) at the nodes of Ranvier is reduced to less than 27% of normal. Parallel experiments were performed to simulate the effects of lidocaine and some significant differences were observed. Analysis of the action potentials within the internodel region suggests that, although immune to drug action in the model, the internodal segment affects the generation of action potentials at the nodes. A commentary is presented on the limitations of the model as it reflects known pharmacologic relationships in real myelinated axons.

  17. Can determining the minimum alveolar anesthetic concentration of volatile anesthetic be used as an objective tool to assess antinociception in animals?

    PubMed

    Docquier, Marie-Agnes; Lavand'homme, Patricia; Ledermann, Christian; Collet, Valérie; De Kock, Marc

    2003-10-01

    We intended to evaluate the reliability of the minimum anesthetic alveolar concentration (MAC)-sparing effect as an objective measure of the antinociceptive properties of a drug. For this purpose, we tested different variables and analyzed the significance of the results obtained. In a first set of experiments, we studied rats under mechanical ventilation and sevoflurane anesthesia. Outcome variables such as gross purposeful movements consecutive to tail clamping, paw withdrawal consecutive to increasing pressure, and cardio-circulatory reactivity (MACBAR) after these stimuli were recorded. In a second set of experiment, sevoflurane-anesthetized rats under spontaneous breathing conditions were used. Thermal stimuli were compared with pressure. The MAC-sparing effect of several doses of sufentanil and clonidine was evaluated in both anesthetized and awake rodents. When considering the stimulus applied, larger concentrations of sevoflurane were required to suppress reactivity after tail clamp than after paw pressure or radiant heat (1.81 +/- 0.28 versus 1.45 +/- 0.22 and 1.53 +/- 0.26; P < 0.05). For the two first stimuli, no significant differences were noted between the concentrations that suppress motor or cardio-circulatory reactions. All doses of sufentanil tested significantly reduced (P < 0.05) the different MAC values except the smallest one (0.005 micro g x kg(-1) x min(-1)) that significantly increased MACBAR in ventilated animals and both MAC and MACBAR in spontaneously breathing rodents (P < 0.05). Clonidine, at its optimal dose (10 micro g/kg), significantly reduced both MAC and MACBAR to the same degree. In awake animals submitted to radiant heat or pressure challenge, none of the clonidine doses nor sufentanil doses (0.005 and 0.07) were active. In conclusion, the MAC-sparing effect provides several reliable and quantifiable variables that allow comparison between different analgesic substances. However, the observations made are not simply the result

  18. [Application of computer-controlled local anesthetic delivery system in children].

    PubMed

    Zhao, Xin; Liu, Hongling; Qin, Man

    2011-08-01

    To compare the reaction of children receiving computer-controlled local anesthetic delivery system (CCLADS) and a conventional syringe, and evaluate the efficacy of anesthesia and the reaction after treatment. 30 children aged 4 to 9 years old, whose bilateral primary molars in the same jaw present similar lesions with similar treatment were included in the study. These bilateral primary molars were treated under local anesthesia in 2 separate visits with random use of either the CCLADS or conventional syringe. For the first visit, the first group received CCLADS anesthesia, in which buccal infiltration anesthesia was performed for maxillary primary molars, and periodontal ligament anesthesia was performed for mandibular primary molars. The second group received conventional anesthesia, in which buccal infiltration anesthesia was performed for both maxillary and mandibular primary molars. For the second visit, two groups used alternative anesthestic method. Pain behavior was observed and scored by modified-children's hospital of eastern ontario pain scale (MCHEOPS). Pain perception was rated using facial image scale (FIS). The MCHEOPS and FIS scores in 1 min injection of children with CCLADS were lower than children with conventional syringe (P<0.05). No difference was found in the FIS score in treatment between two injectors (P>0.05). In local anesthesia, CCLADS can reduce the injection pain caused by conventional syringe to a certain extent.

  19. Cytotoxicity of local anesthetics to rats' articular cartilage: an experimental study.

    PubMed

    Beyzadeoğlu, Tahsin; Torun Köse, Gamze; Ekinci, Işın D; Bekler, Halil; Yilmaz, Cemil

    2012-01-01

    The aim of this study was to evaluate the effects of both in vivo and in vitro bupivacaine, levobupivacaine and tramadol on articular cartilage and chondrocytes in experimental rat models. Thirty mature Sprague Dawley rats weighing 230-300 g were randomized into 3 groups. Bupivacaine (Group 1), levobupivacaine (Group 2) and tramadol (Group 3) were injected into the right knee joints and a physiological 0.9% saline into the left. From each group, 5 rats were executed 48 hours following drug administration after 5 and 10 days. The specimens were fixed, decalcified and stained with hematoxylin & eosin and toluidine blue. All samples were histopathologically evaluated according to the recommendation of ICRS' osteoarthritis and cartilage histopathology grading and staging system. Articular cartilage cells of the rats were cultured and seeded into cell culture flasks. Cartilage cell seeded samples (104 cells/ml) were incubated in three different anesthetic agents (0.5%); bupivacaine, levobupivacaine, and tramadol, respectively. CellTiter 96(®) Non-Radioactive Cell Proliferation (MTS) assay was used to determine the cell density on the samples. Statistically significant higher OARSI grades and OA stage and scores were detected when comparing the group injected with levobupivacaine and executed after 10 days with the levobupivacaine injected group killed after 48 hours (p<0.01 [p=0.008]). Although, statistical analysis could not be done due to insufficient number of samples in the in vitro part of the experiment, it can be concluded that tramadol is cytotoxic to rat chondrocyte in vitro after 30 min of exposure. Additionally, cell numbers in both the bupivacaine and levobupivacaine treated wells showed decrease throughout 15, 30 and 60 minute exposures. Although chondrotoxicity of bupivacaine was less harmful than levobupivacaine and tramadol, these findings suggest that local anesthetics may negatively affect articular cartilage and chondrocytes.

  20. 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.

  1. Microbiological stability of solutions containing local anesthetics and opioids in closed infusion systems used for epidural analgesia.

    PubMed

    Böttcher, K; Meissner, W; Edel, B; Hartmann, M

    2011-10-01

    Nine solutions containing opiod analgesics and local anesthetics as typically use in epidural catheters were tested for antimicrobial stability. Administration via a pefusor syringe requires several refill processes. It was shown that repetitive refilling of the syringes did not result in any microbiological contamination.

  2. Synthesis of Two Local Anesthetics from Toluene: An Organic Multistep Synthesis in a Project-Oriented Laboratory Course

    ERIC Educational Resources Information Center

    Demare, Patricia; Regla, Ignacio

    2012-01-01

    This article describes one of the projects in the advanced undergraduate organic chemistry laboratory course concerning the synthesis of two local anesthetic drugs, prilocaine and benzocaine, with a common three-step sequence starting from toluene. Students undertake, in a several-week independent project, the multistep synthesis of a…

  3. Synthesis of Two Local Anesthetics from Toluene: An Organic Multistep Synthesis in a Project-Oriented Laboratory Course

    ERIC Educational Resources Information Center

    Demare, Patricia; Regla, Ignacio

    2012-01-01

    This article describes one of the projects in the advanced undergraduate organic chemistry laboratory course concerning the synthesis of two local anesthetic drugs, prilocaine and benzocaine, with a common three-step sequence starting from toluene. Students undertake, in a several-week independent project, the multistep synthesis of a…

  4. Potentiation of local anesthetic activity of neosaxitoxin with bupivacaine or epinephrine: development of a long-acting pain blocker.

    PubMed

    Rodriguez-Navarro, Alberto J; Lagos, Marcelo; Figueroa, Cristian; Garcia, Carlos; Recabal, Pedro; Silva, Pamela; Iglesias, Veronica; Lagos, Nestor

    2009-11-01

    Local anesthetics effectively block and relieve pain, but with a relatively short duration of action, limiting its analgesic effectiveness. Therefore, a long-acting local anesthetic would improve the management of pain, but no such agent is yet available for clinical use. The aim of this study is to evaluate the potentiation of the anesthetic effect of neosaxitoxin, with bupivacaine or epinephrine in a randomized double-blind clinical trial. Ten healthy males were subcutaneously injected into the left and right forearms with a randomized pair of the following treatments: (i) bupivacaine (5 mg); (ii) neosaxitoxin (10 microg); (iii) neosaxitoxin (10 microg) plus bupivacaine (5 mg), and (iv) neosaxitoxin (10 microg) plus epinephrine (1:100.000), but all participant received all four formulations (in 2 ml; s.c.), with 1 month elapsing between the two round of experiments. A validated sensory and pain paradigm was used for evaluating the effect of the treatment 0-72 h after the injections, measuring sensory, pain, and mechanical touch perception threshold. The duration of the effect produced by combined treatments was longer than that by the single drugs. In conclusion, bupivacaine and epinephrine potentiate the local anesthetic effect of neosaxitoxin in humans when co-injected subcutaneously. The present results support the idea that neosaxitoxin is a new long-acting local pain blocker, with highly potential clinical use.

  5. Effectiveness of continuous wound infusion of local anesthetics after abdominal surgeries.

    PubMed

    Dhanapal, Baskaran; Sistla, Sarath Chandra; Badhe, Ashok Shankar; Ali, Sheikh Manwar; Ravichandran, Niranjan T; Galidevara, Indira

    2017-05-15

    To assess the effectiveness of continuous preperitoneal wound infusion of local anesthetic drug bupivacaine in providing pain relief, reducing opioid consumption, and enhancing postoperative recovery. Eligible patients were randomly allocated to two groups (study group: bupivacaine and control group: normal saline). There were 47 patients in each group. The patients received continuous infusion of either 0.25% bupivacaine or 0.9% normal saline at 6 mL/h, for 48 h, based on their group allocation, through a multiholed wound infiltration catheter placed preperitoneally. All patients also received intravenous morphine through patient-controlled analgesia pump. Pain scores at rest and on cough, morphine consumption, and peak expiratory flow rate were assessed at 12, 24, and 48 h postoperatively. The time to first perception of bowel sounds and first passage of flatus was noted. All patients were assessed for postoperative nausea and vomiting and any local or systemic complications. Chi-square test was used to compare categorical variables. The morphine consumption was compared using Student t-test, the visual analogue scale (VAS) scores were compared using repeated-measures analysis of variance. The mean total morphine consumption in the study group was significantly lower than the control group (18.8 ± 2.21 versus 30.8 ± 2.58 mg, P = 0.001). The median VAS scores were significantly lower in the study group than those in the control group both at rest (3 [1-4] versus 4 [2-5], P = 0.04) and during cough (4 [3-6] versus 6 [4-6] P = 0.03), except at 48 h, when the median VAS score at rest was similar (3 [1-4] versus 3 [2-4], P = 0.56). Bowel function returned earlier in study group (67.34 ± 2.61 versus 76.34 ± 5.29 h, P = 0.03). Postoperative nausea and vomiting was less in study group. Respiratory function, assessed by peak expiratory flow rate, was better in the study group (192.55 ± 12.93 versus 165.31 ± 9.32 mL, P = 0.03). The

  6. Mass-spectrometric monitoring of the intravenous anesthetic concentration in the breathing circuit of an anesthesia machine

    NASA Astrophysics Data System (ADS)

    Elizarov, A. Yu.; Levshankov, A. I.

    2011-04-01

    Interaction between inhalational anesthetic sevoflurane and an absorber of CO2 (soda lime) in the breathing circuit of an anesthesia machine during low-flow anesthesia (0.5 l of a fresh gaseous mixture per minute) is studied with the mass-spectrometric method. Monitoring data for the concentration of sevoflurane and three toxic products of sevoflurane decompositions (substances A, B, and C) during anesthesia in the inspiration-expiration regime are presented. The highest concentration of substance A is found to be 65 ppm. The biochemical blood analysis before and after anesthesia shows that nephropathy is related to the function of liver toxicity. It is found that inhalational anesthetic sevoflurane influences the concentration of intravenous hypnotic propofol in blood.

  7. Local anesthetics inhibit induction of ornithine decarboxylase by the tumor promoter 12-O-tetradecanoylphorbol 13-acetate.

    PubMed Central

    Yuspa, S H; Lichti, U; Ben, T

    1980-01-01

    The induction of ornithine decarboxylase (L-ornithine carboxy-lyase, EC 4.1.1.17) activity in mouse epidermal cells in vivo and in vitro occurs rapidly after exposure to the tumor promoter 12-O-tetradecanoylphorbol 13-acetate (TPA). This induction has characteristics of a cell surface receptor-mediated process. Local anesthetics modify a variety of cellular responses mediated by membrane receptors. When cultured mouse epidermal cells were exposed to the local anesthetics lidocaine, tetracaine, or procaine (0.1-1 mM), induction of the decarboxylase by TPA was inhibited by more than 90%. In vivo, lidocaine essentially abolishes the decarboxylase response of mouse epidermis when applied shortly after TPA. In contrast, local anesthetics have no effect on the enzyme's activity when added directly to the assay mixture and, in concert with TPA, have only a minimal effect on overall protein synthesis relative to controls. However, lidocaine has no effect on TPA-stimulated DNA synthesis in vitro (12-fold with or without lidocaine). Local anesthetics also markedly inhibit induction of the decarboxylase by ultraviolet light, which is probably not membrane mediated. Furthermore, in culture, lidocaine has only a small inhibitory effect on ornithine decarboxylase when given before TPA but is an effective inhibitor even when given up to 4-5 hr after the promoter, a time when decarboxylase activity has already increased. These findings suggest that local anesthetics, which are tertiary amines, do not act at the site of interaction of TPA and its putative receptor but may be acting specifically on polyamine biosynthesis. These drugs could be useful agents to determine the role of the polyamine pathway in tumor promotion. PMID:6933562

  8. Phimosis. Preputial plasty using transversal widening on the dorsal side with EMLA local anesthetic cream.

    PubMed

    Dessanti, Antonio; Ginesu, Giorgio; Iannuccelli, Marco; Balata, Antonio

    2005-04-01

    In the United States, the treatment of choice for the correction of phimosis is circumcision, whereas in European countries, the condition is usually treated by preputial plasty using Duhamel's method or modified versions. We report our experience in correcting phimosis by preputial plasty using transversal widening on the dorsal side with EMLA local anesthetic cream. Twenty-six patients with phimosis were operated on by preputial plasty, under local anesthesia with EMLA cream. A transversal incision is made on the dorsal side of the ring of prepuce, like 3 contiguous Ts, the middle one inverted with the long arm on the preputial mucosa side. The 2 small mucocutaneous flaps of the prepuce are separated and then sutured with interrupted stitches, thus transforming the incisions from T to V. No postoperative complications were observed. At 1-year follow-up, the cosmetic and functional results were satisfactory. The technique of preputial plasty that the authors present enlarges the stenotic ring of prepuce by a transversal widening on the dorsal side. The ring of prepuce obtained is wide and symmetrical on its dorsal and ventral sides and therefore cosmetically and functionally satisfactory. It is a good alternative to the more radical circumcision technique.

  9. Prolonged local anesthetic action through slow release from poly (lactic acid co castor oil).

    PubMed

    Sokolsky-Papkov, Marina; Golovanevski, Ludmila; Domb, Abraham J; Weiniger, Carolyn F

    2009-01-01

    To evaluate a new formulation of bupivacaine loaded in an injectable fatty acid based biodegradable polymer poly(lactic acid co castor oil) in prolonging motor and sensory block when injected locally. The polyesters were synthesized from DL: -lactic acid and castor oil with feed ratio of 4:6 and 3:7 w/w. Bupivacaine was dispersed in poly(fatty ester) liquid and tested for drug release in vitro. The polymer p(DLLA:CO) 3:7 loaded with 10% bupivacaine was injected through a 22G needle close to the sciatic nerve of ICR mice and the duration of sensory and motor nerve blockade was measured. The DL: -lactic acid co castor oil p(DLLA:CO) 3:7 released 65% of the incorporated bupivacaine during 1 week in vitro. Single injection of 10% bupivacaine loaded into this polymer caused motor block that lasted 24 h and sensory block that lasted 48 h. Previously we developed a ricinoleic acid based polymer with incorporated bupivacaine which prolonged anesthesia to 30 h. The new polymer poly(lactic acid co castor oil) 3:7 provides slow release of effective doses of the incorporated local anesthetic agent and prolongs anesthesia to 48 h.

  10. Effects of regional limb perfusion volume on concentrations of amikacin sulfate in synovial and interstitial fluid samples from anesthetized horses.

    PubMed

    Godfrey, Jennifer L; Hardy, Joanne; Cohen, Noah D

    2016-06-01

    OBJECTIVE To evaluate the effect of volume of IV regional limb perfusion (IVRLP) on amikacin concentrations in synovial and interstitial fluid of horses. ANIMALS 8 healthy adult horses. PROCEDURES Each forelimb was randomly assigned to receive IVRLP with 4 mL of amikacin sulfate solution (250 mg/mL) plus 56 mL (total volume, 60 mL) or 6 mL (total volume, 10 mL) of lactated Ringer solution. Horses were anesthetized, and baseline synovial and interstitial fluid samples were collected. A tourniquet was placed, and the assigned treatment was administered via the lateral palmar digital vein. Venous blood pressure in the distal portion of the limb was recorded. Additional synovial fluid samples were collected 30 minutes (just before tourniquet removal) and 24 hours after IVRLP began; additional interstitial fluid samples were collected 6 and 24 hours after IVRLP began. RESULTS 30 minutes after IVRLP began, mean amikacin concentration in synovial fluid was significantly greater for the large-volume (459 μg/mL) versus small-volume (70 μg/mL) treatment. Six hours after IVRLP, mean concentration in interstitial fluid was greater for the large-volume (723 μg/mL) versus small-volume (21 μg/mL) treatment. Peak venous blood pressure after large-volume IVRLP was significantly higher than after small-volume IVRLP, with no difference between treatments in time required for pressure to return to baseline. CONCLUSIONS AND CLINICAL RELEVANCE Study findings suggested that large-volume IVRLP would deliver more amikacin to metacarpophalangeal joints of horses than would small-volume IVRLP, without a clinically relevant effect on local venous blood pressure, potentially increasing treatment efficacy.

  11. The use of dye surrogates to illustrate local anesthetic drug sequestration by lipid emulsion: a visual demonstration of the lipid sink effect.

    PubMed

    Papadopoulou, Aikaterini; Willers, Johann W; Samuels, Theophilus L; Uncles, David R

    2012-01-01

    We hypothesized that by substituting a dye surrogate in place of local anesthetic, we could visually demonstrate dye sequestration by lipid emulsion that would be dependent on both dye lipophilicity and the amount of lipid emulsion used. We selected 2 lipophilic dyes, acid blue 25 and Victoria blue, with log P values comparable to lidocaine and bupivacaine, respectively. Each dye solution was mixed with combinations of lipid emulsion and water to emulate "lipid rescue" treatment at dye concentrations equivalent to fatal, cardiotoxic, and neurotoxic local anesthetic plasma concentrations. The lipid emulsion volumes added to each dye solution emulated equivalent intravenous doses of 100, 500, and 900 mL of 20% Intralipid in a 75-kg adult. After mixing, the samples were separated into a lipid-rich supernatant and a lipid-poor subnatant by heparin flocculation. The subnatants were isolated, and their colors compared against a graduated dye concentration scale. Lipid emulsion addition resulted in significant dye acquisition by the lipid compartment accompanied by a reduction in the color intensity of the aqueous phase that could be readily observed. The greatest amount of sequestration occurred with the dye possessing the higher log P value and the greatest amount of lipid emulsion. Our study provides a visual demonstration of the lipid sink effect. It supports the theory that lipid emulsion may reduce the amount of free drug present in plasma from concentrations associated with an invariably fatal outcome to those that are potentially survivable.

  12. Novel methods of local anesthetic delivery in the perioperative and postoperative setting-potential for fibrin hydrogel delivery.

    PubMed

    Kearney, Laura; Whelan, Derek; O'Donnell, Brian D; Clover, Anthony J P

    2016-12-01

    The benefits of high-quality postoperative analgesia are well documented and include earlier mobilization, fewer respiratory and cardiovascular complications, and shorter hospital stay. Local anesthesia-based acute pain regimens are at worst equal to and at best superior to opiate-based regimens from the perspective of analgesia. A multimodal approach limiting opioids by combining with local anesthetics has additional beneficial effect on outcomes such as nausea and vomiting, pruritus, gastrointestinal function, respiratory complications, and neutrophil function. Wound catheters providing continuous infiltration of local anesthetics offer a rational approach to effective perioperative analgesia, but their use is limited by a short duration of action. There is an identified need for further methods to optimize longer-acting delivery of these agents. This article reviews current and evolving longer-acting techniques and their limitations with particular focus on the potential advantages of a fibrin hydrogel-based system. Copyright © 2016 Elsevier Inc. All rights reserved.

  13. Probing the dynamics of complexed local anesthetics via neutron scattering spectroscopy and DFT calculations.

    PubMed

    Martins, Murillo L; Eckert, Juergen; Jacobsen, Henrik; Dos Santos, Éverton C; Ignazzi, Rosanna; de Araujo, Daniele Ribeiro; Bellissent-Funel, Marie-Claire; Natali, Francesca; Koza, Michael Marek; Matic, Aleksander; de Paula, Eneida; Bordallo, Heloisa N

    2017-05-30

    Since potential changes in the dynamics and mobility of drugs upon complexation for delivery may affect their ultimate efficacy, we have investigated the dynamics of two local anesthetic molecules, bupivacaine (BVC, C18H28N2O) and ropivacaine (RVC, C17H26N2O), in both their crystalline forms and complexed with water-soluble oligosaccharide 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The study was carried out by neutron scattering spectroscopy, along with thermal analysis, and density functional theory computation. Mean square displacements suggest that RVC may be less flexible in crystalline form than BVC, but both molecules exhibit very similar dynamics when confined in HP-β-CD. The use of vibrational analysis by density functional theory (DFT) made possible the identification of molecular modes that are most affected in both molecules by insertion into HP-β-CD, namely those of the piperidine rings and methyl groups. Nonetheless, the somewhat greater structure in the vibrational spectrum at room temperature of complexed RVC than that of BVC, suggests that the effects of complexation are more severe for the latter. This unique approach to the molecular level study of encapsulated drugs should lead to deeper understanding of their mobility and the respective release dynamics. Copyright © 2017 Elsevier B.V. All rights reserved.

  14. Molecular determinants of prokaryotic voltage-gated sodium channels for recognition of local anesthetics.

    PubMed

    Shimomura, Takushi; Irie, Katsumasa; Fujiyoshi, Yoshinori

    2016-08-01

    Local anesthetics (LAs) inhibit mammalian voltage-gated Na(+) channels (Navs) and are thus clinically important. LAs also inhibit prokaryotic Navs (BacNavs), which have a simpler structure than mammalian Navs. To elucidate the detailed mechanisms of LA inhibition to BacNavs, we used NavBh, a BacNav from Bacillus halodurans, to analyze the interactions of several LAs and quaternary ammoniums (QAs). Based on the chemical similarity of QA with the tertiary-alkylamine (TAA) group of LAs, QAs were used to determine the residues required for the recognition of TAA by NavBh. We confirmed that two residues, Thr220 and Phe227, are important for LA binding; a methyl group of Thr220 is important for recognizing both QAs and LAs, whereas Phe227 is involved in holding blockers at the binding site. In addition, we found that NavBh holds blockers in a closed state, consistent with the large inner cavity observed in the crystal structures of BacNavs. These findings reveal the inhibition mechanism of LAs in NavBh, where the methyl group of Thr220 provides the main receptor site for the TAA group and the bulky phenyl group of Phe227 holds the blockers inside the large inner cavity. These two residues correspond to the two LA recognition residues in mammalian Navs, which suggests the relevance of the LA recognition between BacNavs and mammalian Navs. © 2016 Federation of European Biochemical Societies.

  15. Investigation of local anesthetic and antimycobacterial activity of Ottonia martiana Miq. (Piperaceae).

    PubMed

    Cunico, Miriam M; Trebien, Herbert A; Galetti, Fábio C; Miguel, Obdulio G; Miguel, Marilis D; Auer, Celso G; Silva, Célio L; de Souza, Ana Olívia

    2015-01-01

    Ottonia martiana is a plant popularly known in Brazil by the use for toothache. Ethanolic extract (EE), hexane fraction (HF), dichloromethane fraction (DF) and piperovatine obtained from O. martiana were assayed in vitro and in vivo. The acute toxicity of EE was determined, and LD50 values of 164.5 and 65.0 mg/kg by the oral and intraperitoneal routes, respectively, indicated a high toxicity for EE in vivo, explaining its popular use by topical administration only. A local anesthetic-like effect of EE and its fractions was observed in experimental models using pain induction, and such effect involved an analgesic action. The antimycobacterial activity of EE, HF, DF and piperovatine was evaluated against Mycobacterium tuberculosis H37Rv ATCC 27924. EE, HF, DF, and piperovatine showed a potential antimycobacterial effect with MICs of 16.0, 62.0, 62.0 and 8.0 μg/mL, respectively. Piperovatine was more effective than the EE or the other fractions. The selectivity index (SI=IC50/MIC) values calculated for EE, HF, DF and piperovatine based on the MICs and the cytotoxicity against J774 macrophages (IC50 by MTT assay) revealed values of 6.43, 2.34, 1.5 and 9.66, respectively.

  16. The vanilloid receptor TRPV1 is activated and sensitized by local anesthetics in rodent sensory neurons.

    PubMed

    Leffler, Andreas; Fischer, Michael J; Rehner, Dietlinde; Kienel, Stephanie; Kistner, Katrin; Sauer, Susanne K; Gavva, Narender R; Reeh, Peter W; Nau, Carla

    2008-02-01

    Local anesthetics (LAs) block the generation and propagation of action potentials by interacting with specific sites of voltage-gated Na(+) channels. LAs can also excite sensory neurons and be neurotoxic through mechanisms that are as yet undefined. Nonspecific cation channels of the transient receptor potential (TRP) channel family that are predominantly expressed by nociceptive sensory neurons render these neurons sensitive to a variety of insults. Here we demonstrated that the LA lidocaine activated TRP channel family receptors TRPV1 and, to a lesser extent, TRPA1 in rodent dorsal root ganglion sensory neurons as well as in HEK293t cells expressing TRPV1 or TRPA1. Lidocaine also induced a TRPV1-dependent release of calcitonin gene-related peptide (CGRP) from isolated skin and peripheral nerve. Lidocaine sensitivity of TRPV1 required segments of the putative vanilloid-binding domain within and adjacent to transmembrane domain 3, was diminished under phosphatidylinositol 4,5-bisphosphate depletion, and was abrogated by a point mutation at residue R701 in the proximal C-terminal TRP domain. These data identify TRPV1 and TRPA1 as putative key elements of LA-induced nociceptor excitation. This effect is sufficient to release CGRP, a key component of neurogenic inflammation, and warrants investigation into the role of TRPV1 and TRPA1 in LA-induced neurotoxicity.

  17. The challenge of evaluating pain and a pre-incisional local anesthetic block

    PubMed Central

    Pascoe, Peter J.; Lascelles, B. Duncan X.; Kass, Philip H.

    2014-01-01

    Background. Our objective was to test the effectiveness of a local anesthetic line block administered before surgery in reducing postoperative pain scores in dogs undergoing ovariohysterectomy (OVHX). Methods. This study is a prospective, randomized, blinded, clinical trial involving 59 healthy female dogs. An algometric pressure-measuring device was used to determine nociceptive threshold, and compared to three subjective pain scales. Group L/B received a line block of lidocaine (4 mg/kg) and bupivacaine (1 mg/kg) subcutaneously in the area of the incision site and saline subcutaneously as premedication; group L/BM (positive control) received a similar block and morphine (0.5 mg/kg) subcutaneously for premedication; and group SS (negative control) received a saline line block and saline premedication. Criteria for rescue analgesia were defined before the study. Dogs were assessed prior to surgery, at extubation (time 0) and at 2, 4, 6, 8 and 24 h post-recovery. The data were analyzed with one-way ANOVA, and a Split Plot Repeated Measures ANOVA with one grouping factor and one repeat factor (time). P < 0.05 was considered statistically significant. Results. Approximately 33% of dogs required rescue analgesia at some point during the study, with no significant difference between groups. There was no significant difference between treatment groups with any assessment method. Conclusions. As there were no statistically significant differences between positive and negative controls, the outcome of this technique cannot be proven. PMID:24765575

  18. Local anesthetic and antiepileptic drug access and binding to a bacterial voltage-gated sodium channel.

    PubMed

    Boiteux, Céline; Vorobyov, Igor; French, Robert J; French, Christopher; Yarov-Yarovoy, Vladimir; Allen, Toby W

    2014-09-09

    Voltage-gated sodium (Nav) channels are important targets in the treatment of a range of pathologies. Bacterial channels, for which crystal structures have been solved, exhibit modulation by local anesthetic and anti-epileptic agents, allowing molecular-level investigations into sodium channel-drug interactions. These structures reveal no basis for the "hinged lid"-based fast inactivation, seen in eukaryotic Nav channels. Thus, they enable examination of potential mechanisms of use- or state-dependent drug action based on activation gating, or slower pore-based inactivation processes. Multimicrosecond simulations of NavAb reveal high-affinity binding of benzocaine to F203 that is a surrogate for FS6, conserved in helix S6 of Domain IV of mammalian sodium channels, as well as low-affinity sites suggested to stabilize different states of the channel. Phenytoin exhibits a different binding distribution owing to preferential interactions at the membrane and water-protein interfaces. Two drug-access pathways into the pore are observed: via lateral fenestrations connecting to the membrane lipid phase, as well as via an aqueous pathway through the intracellular activation gate, despite being closed. These observations provide insight into drug modulation that will guide further developments of Nav inhibitors.

  19. Electrocardiographic alterations during endosseous implant placement performed with local anesthetic agents.

    PubMed

    Romano, Marcelo Munhóes; Soares, Mario Sergio; Pastore, Carlos Alberto; de Oliveira Guaré, Renata; Adde, Carlos Alberto

    2009-01-01

    The purpose of this study was to analyze electrocardiographic alterations during dental implant surgeries when local anesthetic agents were used. Twenty implants were placed in 18 healthy patients. An electrocardiogram and Wincardio software were used to gather recordings from 12 static leads every 2 minutes, continuously record coronary artery (D2) derivations, and automatically measure the following electrocardiographic parameters: heart rate, duration and amplitude of the P wave, PR segment duration, ST segment deviation, QRS complex duration, and duration of the RR, QT, and corrected QT (QTc) intervals. Analysis of variance of the values obtained at the different stages showed significant differences (P<.05) for the heart rate and for the duration of the RR and QT intervals. The heart rate increased during the anesthesia, incision, and bone drilling stages, reaching a peak during drilling. Duration of the RR and QT intervals decreased during the incision and drilling stages. Among the electrocardiographic parameters individually assessed, several altered values were found for the duration of the P wave, the QRS complex, and the QT and QTc intervals. Sinusal tachycardia and bradycardia, sinusal arrhythmia, supraventricular extrasystole, ventricular extrasystole, and T-wave inversion were detected. Dental implant placement surgery may induce electrocardiographic alterations. The most frequently found arrhythmias were extrasystole and sinusal tachycardia. The anesthesia, incision, and bone drilling stages exhibited the highest heart rate values and the shortest durations of the RR and QT intervals.

  20. Do local anesthetics interact preferentially with membrane lipid rafts? Comparative interactivities with raft-like membranes.

    PubMed

    Tsuchiya, Hironori; Ueno, Takahiro; Mizogami, Maki; Takakura, Ko

    2010-08-01

    Membranous lipid bilayers have been reconsidered as the site of action of local anesthetics (LAs). Recent understanding of biomembranes indicates the existence of lipid raft microdomains enriched in cholesterol and sphingolipids as potential platforms for channels and receptors. Based on the hypothesis that LAs may interact preferentially with lipid rafts over non-raft membranes, we compared their effects on raft model membranes and cardiolipin-containing biomimetic membranes. Liposomes were prepared with phospholipids, sphingomyelin, cerebroside, and cholesterol to have compositions corresponding to lipid rafts and cardiomyocyte mitochondrial membranes. After reacting LAs (50-200 microM) with the membrane preparations, their interactivities were determined by measuring fluorescence polarization with 1,6-diphenyl-1,3,5-hexatriene. Although bupivacaine and lidocaine acted on different raft-like liquid-ordered membranes to reduce polarization values, their effects on biomimetic less ordered membranes were much greater. LAs interacted with biomimetic membranes with the potency being R(+)-bupivacaine > racemic bupivacaine > S(-)-bupivacaine > ropivacaine > lidocaine > prilocaine, which is consistent with the rank order of pharmacotoxicological potency. However, raft model membranes showed neither structure-dependence nor stereoselectivity. The relevance of membrane lipid rafts to LAs is questionable at least in their effects on raft-like liquid-ordered membranes.

  1. Thermal effect of sonophoresis for accelerating the analgesic effect of local anesthetics on rat tail nerve.

    PubMed

    Wu, Yi-Hui; Chen, Wen-Shiang; Luh, Jer-Junn; Chong, Fok-Ching

    2008-01-01

    Sonophoresis is an ultrasound transdermal drugs delivery system. The eutectic mixture of local anesthetics (EMLA) has been used clinically for anesthesia but requires at least one hour to take effect and lacks of analgesia's objective assessment. We proposed that sonophoresis could reduce the duration of EMLA analgesia effect onset and be assessed by sensory conduction studies. Thirty Wistar adult rats were randomized into normal, control, ultrasound-, and heat-treatment groups. Normal group was received no EMLA cream or ultrasound and heat treatment. The control group received the EMLA cream on the rat tail at 3.5 cm distal to the rat tail base for local anesthesia of tail nerve. Ultrasound- and heat-treatment groups were received ultrasound with different parameters and heat treatment, respectively, before EMLA cream applied. Sensory conduction studies of tail nerve were made before and after treatment every 5 min at least for 60 min in all rats. There was no significant difference between the EMLA control group and heat treatment group. All rats in ultrasound-treatment group exhibit significant difference with EMLA control group and heat-treatment group in time for decreased 20% SNCV except for the 2 W/cm(2), 25 min, 20% in ultrasound-treatment group having no significant difference with heat-treatment group. There was no significant difference between ultrasound-treatment subgroups. In the decrease of amplitude, only the 2 W/cm(2), 5 min, 100% and the 2 W/cm(2), 10 min, 50% in ultrasound-treatment group had significant difference between EMLA control and heat-treatment groups. We have objectively examined the sonophoresis effect of ultrasound by investigating the effects of EMLA. Applying ultrasound for 5 min reduces the onset time of EMLA analgesia from 60 min to less than 20 min. Ultrasound sonophoresis of analgesic drugs is potentially useful in the treatment of carpal tunnel syndrome, tooth extraction, and other applications of analgesia.

  2. Local-anesthetic like inhibition of the cardiac sodium channel Nav1.5 α-subunit by 5-HT3 receptor antagonists.

    PubMed

    Van't Klooster, Mariet P; Foadi, Nilufar; Hage, Axel; Stoetzer, Carsten; Wegner, Florian; Eberhardt, Mirjam; Leffler, Andreas

    2016-10-15

    5-hydroxytryptamine 3 receptor (5-HT3 receptor) antagonists are administered for prevention and therapy of nausea and vomiting. Although regarded as safe therapeutics, they can also provoke arrhythmias by prolonging the QRS interval. However, the mechanisms mediating this cardiotoxicity are poorly understood. Here we investigated effects of 5-HT3 receptor antagonists on the cardiac Na(+) channel Nav1.5. We explored the interaction of dolasetron, tropisetron, granisetron and ondansetron on the human α-subunit Nav1.5 heterologously expressed in HEK293 cells. Sodium currents were explored by means of whole-cell patch clamp recordings. All four substances inhibited the Nav1.5 in a concentration and state-dependent manner. Dolasetron displayed the lowest blocking efficacy, and tropisetron was the most potent blocker with a half maximum blocking concentration of 18µM for tonic block of inactivated channels. Tropisetron was also the most potent use-dependent inhibitor, and it also induced a strong open -channel block. Both tonic and use-dependent block by tropisetron were abbreviated on the local-anesthetic insensitive mutant Nav1.5-F1760A. Co-administration of tropisetron and the local anesthetic bupivacaine or the hypnotic propofol augmented inhibition of Nav1.5. Our data demonstrate that 5-HT3 receptor antagonists induce a local-anesthetic like inhibition of Nav1.5, and that they display different blocking efficacies. Reports on a relevant cardiotoxicity of dolasetron as opposed to other 5-HT3 receptor antagonists do not seem to correlate with a block of Nav1.5. As inhibition of Nav1.5 was enhanced by propofol and bupivacaine however, it is possible that a combined administration of Na(+) channel blockers and 5-HT3 receptor antagonists can provoke arrhythmias.

  3. Analysis of Efficacy Differences between Caudal and Lumbar Interlaminar Epidural Injections in Chronic Lumbar Axial Discogenic Pain: Local Anesthetic Alone vs. Local Combined with Steroids

    PubMed Central

    Manchikanti, Laxmaiah; Pampati, Vidyasagar; Benyamin, Ramsin M.; Boswell, Mark V.

    2015-01-01

    Study Design: Comparative assessment of randomized controlled trials of caudal and lumbar interlaminar epidural injections in chronic lumbar discogenic pain. Objective: To assess the comparative efficacy of caudal and lumbar interlaminar approaches of epidural injections in managing axial or discogenic low back pain. Summary of Background Data: Epidural injections are commonly performed utilizing either a caudal or lumbar interlaminar approach to treat chronic lumbar axial or discogenic pain, which is pain exclusive of that associated with a herniated intervertebral disc, or that is due to degeneration of the zygapophyseal joints, or due to dysfunction of the sacroiliac joints, respectively. The literature on the efficacy of epidural injections in managing chronic axial lumbar pain of presumed discogenic origin is limited. Methods: The present analysis is based on 2 randomized controlled trials of chronic axial low back pain not caused by disc herniation, radiculitis, or facet joint pain, utilizing either a caudal or lumbar interlaminar approach, with a total of 240 patients studied, and a 24-month follow-up. Patients were assigned to receive either local anesthetic only or local anesthetic with a steroid in each 60 patient group. Results: The primary outcome measure was significant improvement, defined as pain relief and functional status improvement of at least 50% from baseline, which was reported at 24-month follow-ups in 72% who received local anesthetic only with a lumbar interlaminar approach and 54% who received local anesthetic only with a caudal approach. In patients receiving local anesthetic with a steroid, the response rate was 67% for those who had a lumbar interlaminar approach and 68% for those who had a caudal approach at 12 months. The response was significantly better in the lumbar interlaminar group who received local anesthetic only, 77% versus 56% at 12 months and 72% versus 54% at 24 months. Conclusion: This assessment shows that in patients

  4. Dexmedetomidine Dose Dependently Enhances the Local Anesthetic Action of Lidocaine in Inferior Alveolar Nerve Block: A Randomized Double-Blind Study.

    PubMed

    Ouchi, Kentaro; Sugiyama, Kazuna

    2016-01-01

    Dexmedetomidine (DEX) dose dependently enhances the local anesthetic action of lidocaine in rats. We hypothesized that the effect might also be dose dependent in humans. We evaluated the effect of various concentrations of DEX with a local anesthetic in humans. Eighteen healthy volunteers were randomly assigned by a computer to receive 1.8 mL of 1 of 4 drug combinations: (1) 1% lidocaine with 2.5 ppm (parts per million) (4.5 μg) DEX, (2) lidocaine with 5.0 ppm (9.0 μg) DEX, (3) lidocaine with 7.5 ppm (13.5μg) DEX, or (4) lidocaine with 1:80,000 (22.5 μg) adrenaline (AD), to produce inferior alveolar nerve block. Pulp latency and lower lip numbness (for assessing onset and duration of anesthesia) were tested, and sedation level, blood pressure, and heart rate were recorded every 5 minutes for 20 minutes, and every 10 minutes from 20 to 60 minutes. Pulp latency of each tooth increased compared with baseline, from 5 to 15 minutes until 60 minutes. There were no significant intergroup differences at any time point. Anesthesia onset was not different between groups. Anesthesia duration was different between groups (that with DEX 7.5 ppm was significantly longer than that with DEX 2.5 ppm and AD; there was no difference between DEX 2.5 ppm and AD). Blood pressure decreased from baseline in the 5.0 and 7.5 ppm DEX groups at 30 to 60 minutes, although there was no hypotension; moreover, heart rate did not change in any group. Sedation score did not indicate deep sedation in any of the groups. Dexmedetomidine dose dependently enhances the local anesthetic action of lidocaine in humans. Dexmedetomidine at 2.5 ppm produces similar enhancement of local anesthesia effect as addition of 1:80,000 AD.

  5. The nicotinic acetylcholine receptor: Binding of nitroxide analogs of a local anesthetic and a photoactivatable analog of phosphatidylserine

    SciTech Connect

    Blanton, M.P.

    1989-01-01

    Electron spin resonance was used to contrast the accessibility of tertiary and quaternary amine local anesthetics to their high affinity binding site in the desensitized Torpedo californica acetylcholine receptor (AchR). Preincubation of AchR-rich membranes with agonist resulted in a substantial reduction in the initial association of the quaternary amine local anesthetic C6SLMEI with the receptor. The time-dependent reduction in association follows a biphasic exponential function having rate constants of 0.19 min{sup {minus}1} and 0.03 min{sup {minus}1}. In contrast, agonist preincubation did not produce a comparable decrease in the association of C6SL, a tertiary amine analog, with the AchR. The results are modeled in two ways: (1) A charge gate near the channel mouth in the desensitized receptor limits access of the permanently charged cationic local anesthetic (C6SLMEI), but not for the uncharged form of the tertiary amine anesthetic C6SL. (2) A hydrophobic pathway, possibly through a corridor in the annular lipid surrounding receptor subunits, allows the uncharged form of C6SL to reach the high affinity binding site in the AchR. A photoactivatable analog of phosphatidylserine {sup 125}I 4-azido salicylic acid-phosphatidylserine ({sup 125}I ASA-PS) was use to label both Torpedo californica acetylcholine receptor-rich membranes and reconstituted AchR membranes. All four subunits of the AchR were found to incorporate label, with the {alpha} subunit incorporating approximately twice as much as each of the other subunits on a per mole basis. The regions of the AchR {alpha} subunit that incorporate {sup 125}I ASA-PS were mapped by Staphylococcus aureus V8 protease digestion. Eighty-one per cent of the incorporated label was localized to 11.7 and 10.1 kdal V8 cleavage fragments.

  6. Analgesic Effect of Botulinum Toxin A in Myofascial Pain Syndrome Patients Previously Treated with Local Infiltration of Anesthetic and Steroids.

    PubMed

    Cartagena-Sevilla, Joaquín; García-Fernández, María R; Vicente-Villena, Juan P

    2016-12-01

    The purpose of this study was to evaluate the analgesic effect of botulinum toxin A (BoNTA) injections in patients with myofascial pain syndrome (MPS) who were previously treated with the local infiltration of anesthetic and steroids (LIAS). The study included a retrospective phase and a longitudinal open-label prospective phase, which were conducted on consecutive patients with MPS previously treated with the local infiltration of anesthetic (levobupivacaíne 0.25%) and steroids (triamcinolone 40 mg). Eligible patients were treated with a single intramuscular injection of BoNTA (Botox; Allergan, Inc., Irvine, CA). The treatment efficacy was determined according to the degree of pain relief obtained. Eighty-two patients met the inclusion/exclusion criteria and were included in the study. Successful results were obtained for 32 (39.0%) and 30 (36.6%) patients, during treatment with BoNTA and LIAS, respectively. The mean (standard deviation) length of the analgesic effect was significantly longer with BoNTA (29.6 [SD = 17.7] weeks) than with LIAS (8.5 [SD = 6.4] weeks), P <.0001. As regards the side effects, 19 (23.2%) patients reported transient soreness at the injection site for 2 to 3 days with BoNTA. The MPS patients previously treated with a local infiltration of anesthetic and steroids who then received a single injection of BoNTA experienced significantly reduced pain for a relatively long time.

  7. Continuous wound infusion of local anesthetic for the control of pain after elective abdominal colorectal surgery.

    PubMed

    Polglase, Adrian L; McMurrick, Paul J; Simpson, Paul J B; Wale, Roger J; Carne, Peter W G; Johnson, William; Chee, Justin; Ooi, Corrine W; Chong, Jennifer W D; Kingsland, Sally R; Buchbinder, Rachelle

    2007-12-01

    Local anesthetic wound infusion has been investigated in recent years as a potential alternative to standard analgesic regimens after major surgery. This study investigates the efficacy of a continuous wound infusion of ropivacaine in conjunction with best practice postoperative analgesia after midline laparotomy for abdominal colorectal surgery. We performed a randomized, participant and outcome assessor-blinded, placebo-controlled trial on patients presenting for major abdominal colorectal surgery at our institution between December 2003 and February 2006. Patients were allocated to receive ropivacaine 0.54 percent or normal saline via a dual catheter Painbuster Soaker (I-Flow Corporation, OH, USA) continuous infusion device into their midline laparotomy wound for 72 hours postoperatively. A total of 310 patients were included in this study. The continuous wound infusion of ropivacaine after abdominal colorectal surgery conveys minimal benefit compared with saline wound infusion. No statistically significant difference could be shown for: pain at rest, morphine usage, length of stay, mobility, nausea, or return of bowel function. There was a small, statistically significant difference in mean pain on movement on Day 1 for the ropivacaine group (adjusted mean difference -0.6 (range, -1.08 to -0.13)). Although this trend continued on Days 2 and 3, the differences between groups were no longer statistically significant. Management of pain after major abdominal colorectal surgery is best achieved through adopting a multimodal approach to analgesia. Delivery of ropivacaine to midline laparotomy wounds via a Painbuster Soaker device is safe, but we have not demonstrated any significant clinical advantage over current best practice.

  8. A National Survey of Undergraduate Suture and Local Anesthetic Training in the United Kingdom.

    PubMed

    Rufai, Sohaib R; Holland, Luke C; Dimovska, Eleonora O F; Bing Chuo, Cher; Tilley, Simon; Ellis, Harold

    2016-01-01

    Suturing is a skill expected to be attained by all medical students on graduation, according to the General Medical Council's (GMC) Tomorrow's Doctors. There are no GMC recommendations for the amount of suture training required at medical school nor the level of competence to be achieved. This study examines the state of undergraduate suture training by surveying a sample of medical students across the United Kingdom. We distributed a survey to 17 medical schools to be completed by undergraduates who have undergone curricular suture training. The survey included questions relating to career intention, hours of curricular suture training, hours of additional paid training, confidence in performing various suture techniques and knowledge of their indications. We also asked about the students' perceived proficiency at injecting local anesthetic and their overall opinion of medical school suture training. We received responses from 705 medical students at 16 UK medical schools. A total of 607 (86.1%) medical students had completed their scheduled curricular suture training. Among them, 526 (86.5%) students reported inadequate suture training in medical school and 133 (21.9%) students had paid for additional training. Results for all competence markers were significantly lower than the required GMC standards (p < 0.001). Students who had paid for additional training were significantly more confident across all areas examined (p < 0.001). Our study identified a deficiency in the curricular suture training provided to the medical students surveyed. These findings suggest that medical schools should provide more opportunities for students to develop their suturing skills to achieve the GMC standard. Copyright © 2015. Published by Elsevier Inc.

  9. Efficacy of postoperative continuous wound infiltration with local anesthetic after major abdominal surgery.

    PubMed

    Abadir, Adel R; Nicolas, Fred; Gharabawy, Ramiz; Shah, Trusha; Michael, Rafik

    2009-01-01

    The aim of this study was to evaluate the analgesic efficacy, safety, opioid sparing effects and improvement of respiratory function when using 0.2% ropivacaine continuous wound infiltration after major intra-abdominal surgery. Forty patients undergoing major intra-abdominal surgery requiring a midline incision of > or = 20 cm were enrolled into this IRB-approved, randomized, prospective controlled study. Group 1: 20 patients, parenteral analgesia (control group). Group II: 20 patients, with local anesthetic wound infiltration (pain pump group). At the end of the procedure, in the pain pump group of patients, a multi hole, 20-gauge catheter was inserted percutaneously, above the fascia. An initial dose of 10 ml of 0.2% ropivacaine was injected in the wound through the catheter. A device provided continuous delivery of 0.2% ropivacaine; the infusion was initiated at 6 ml/h for the following two days. The total "rescue" morphine and oxycodone/acetaminophen tablets administered were significantly lower in the pain pump group. At all time intervals, resting pain scores were significantly lower in the pain pump group when compared with the control group. However, at the 4-48 and 12-48 hours pain scores generated after leg raise and coughing, respectively, were significantly lower in group II. The patient vital capacities were insignificantly higher in group II. We conclude that after major abdominal surgery, infiltration and continuous wound instillation with 0.2% ropivacaine decreases postoperative pain, opioid requirements and oral analgesia. Early patient rehabilitation, hastening convalescence, and preventing respiratory complications are expected outcomes of this approach.

  10. Survey of responsible handling of local anesthetic in Indian dental operatory

    PubMed Central

    Rooban, Thavarajah; Rao, Umadevi Krishnamohan; Joshua, Elizabeth; Ranganathan, Kannan

    2013-01-01

    Background: Dental operatory requires handling of numerous toxic fluids such as denture acrylic monomer, alcohol and formalin for effective oral care delivery. The efficacy and responsible handling of such fluids has not been analyzed among Indian dentists and this study aims to address this lacunae. Materials and Methods: Closed ended questionnaire was distributed through email to Indian dentists in July 2012. After inclusion/exclusion criteria, 1484 practitioners constituted the study group with a response rate of 52%. Statistics: SPSS® Version 17.0 (SPSS-IBM Inc., IL, USA) was used to carry out statistical analysis. Descriptive statistics were presented. Chi square test was used to identify the association between the parameters; P ≤ 0.05 was considered as statistically significant. Results: Males (80.8%), undergraduates (78%), exclusive practitioners (81.2%), urban practitioners (68.5%) were the predominant respondents. Predominant of the respondents (97%) used local anesthetic (LA) from bottles. Eight percent have encountered instances of injecting formalin instead of LA in their settings. Safe disposal rules and regulations (P ≤ 0.05), opinion on injecting the other fluids instead of LA as a severe negligent act (P ≤ 0.05) were statistically significant between age groups. Educational status did not appear to influence the outcome. Only a third of the respondents were aware of the rules and regulations for safe disposal of empty LA bottles while 49.1% were not aware of them and willing to learn. Discussion: The lacunae in responsible handling of toxic fluids need to be addressed to prevent inadvertent and negligence suits against dentists, highlighting the need through continuing dental education programmes. PMID:24255564

  11. Mechanisms of use-dependent block of sodium channels in excitable membranes by local anesthetics.

    PubMed Central

    Starmer, C F; Grant, A O; Strauss, H C

    1984-01-01

    Many local anesthetics promote reduction in sodium current during repetitive stimulation of excitable membranes. Use-, frequency-, and voltage-dependent responses describe patterns of peak INa when pulse width, pulse frequency, and pulse amplitude are varied. Such responses can be viewed as reflecting voltage-sensitive shifts in equilibrium between conducting, unblocked channels and nonconducting, blocked channels. The modulated-receptor hypothesis postulates shifts in equilibrium as the result of a variable-affinity receptor and modified inactivation gate kinetics in drug-complexed channels. An alternative view considers drug blocking in the absence of these two features. We propose that drug binds to a constant-affinity channel receptor where receptor access is regulated by the channel gates. Specifically, we view channel binding sites as guarded by the channel gate conformation, so that unlike receptors where ligands have continuous access, blocking agent access is variable during the course of an action potential. During the course of an action potential, the m and h gates change conformation in response to transmembrane potential. Conducting channels with both gates open leave the binding site unguarded and thus accessible to drug, whereas nonconducting channels, with gates in the closed conformation, act to restrict drug access to unbound receptors and possibly to trap drug in drug-complexed channels. We develop analytical expressions characterizing guarded receptors as "apparently" variable-affinity binding sites and predicting shifts in "apparent" channel inactivation in the hyperpolarizing direction. These results were confirmed with computer simulations. Furthermore, these results are in quantitative agreement with recent investigations of lidocaine binding in cardiac sodium channels. PMID:6331543

  12. Local Anesthetics in the Gas-Phase the Rotational Spectrum of Butamben and Isobutamben

    NASA Astrophysics Data System (ADS)

    Vallejo-López, Montserrat; Ecija, Patricia; Caminati, Walther; Grabow, Jens-Uwe; Lesarri, Alberto; Cocinero, Emilio J.

    2016-06-01

    Benzocaine (BZ), butamben (BTN) and isobutamben (BTI) are local anesthetics characterized by a hydrophilic head and a lipophilic aliphatic tail linked by an aminobenzoate group. Previous rotational work on BZ (H2N-C6H4-COO-Et) showed that its ethyl aliphatic tail may adopt either in-plane (trans) or out of plane (gauche) conformations, with a low interconversion barrier below 50 cm-1. Here we extend the rotational study to BTN and BTI, isolated in a supersonic jet expansion and vaporized either by heating or UV ps-laser ablation methods. Both molecules share a 14 heavy-atoms skeleton, differing in their butyl (-(CH2)3-CH3) or isobutyl (-CH2-CH(CH3)2) four-carbon tail. We detected a single conformer for BTN and two conformers for BTI. The two molecules do not adopt an all-trans carbon skeleton. Conversely, the β-ethyl carbon in BTN is gauche. For BTI the β-carbon may be either trans or gauche. The microwave spectrum covered the cm- (BTN, BTI, 6-18 GHz) and mm-wave (BTW, 50-75 GHz) frequency ranges.In all the cases, rotational and centrifugal distortion constants as well as the diagonal elements of the 14N nuclear quadrupole coupling tensor were accurate determined and compared to the theoretical results (ab initio and DFT). No transitions belonging to configurations predicted as higher minima of the PES were found, pointing out that conformational interconversions may take place in the jet. A. Lesarri, S. T. Shipman, G. G. Brown, L. Alvarez-Valtierra, R. D. Suenram, B. H. Pate, Int. Symp. Mol. Spectrosc., 2008, Comm. RH07. E. Aguado, A. Longarte, E. Alejandro, J. A. Fernández, F. Castaño, J. Phys. Chem. A, 2006, 110, 6010.

  13. Magnesium sulfate diminishes the effects of amide local anesthetics in rat sciatic nerve block

    PubMed Central

    Hung, Yu-Chun; Chen, Chia-Ying; Lirk, Philipp; Wang, Chi-Fei; Cheng, Jen-Kun; Chen, Chien-Chuan; Wang, Ging Kuo; Gerner, Peter

    2007-01-01

    Background and Objectives Magnesium sulfate (MgSO4) is well-known as an antagonist of n-methyl-d-aspartate receptors and was used for intrathecal analgesia a century ago. However, the effects of MgSO4 combined with local anesthetics (LAs) on peripheral nerves are unclear. We tested the hypothesis that MgSO4 could be used as an adjuvant to prolong and intensify conduction block by amide-type LAs in a rat sciatic nerve block model. Further, the mechanism of possible synergy between LAs and MgSO4 was investigated in whole-cell mode patch-clamp experiments. Methods Sciatic nerves were exposed to 2%/73.9mM lidocaine, 0.25%/7.7mM bupivacaine, and 0.5%/15.4mM ropivacaine, with or without addition of 1.25%, 2.5%, or 5% MgSO4/50.7 mM, and nerve block characteristics were assessed. To elucidate the LA-MgSO4 interaction, voltage-dependent inactivation curves were determined in cultured rat GH3 cells expressing neuronal Na+ channels. Results Unexpectedly, the addition of MgSO4 overall significantly shortened the duration of blockade by lidocaine, bupivacaine, and ropivacaine. The steady-state inactivation of Na+ channels in the presence of 300 μM lidocaine was almost unchanged by the addition of 10 mM MgSO4, indicating that MgSO4 does not affect the potency of lidocaine toward the inactivated Na+ channel. Conclusions MgSO4 coadministered with amide-type LAs shortened the duration of sciatic nerve blockade in rats. Therefore, it does not seem to be useful as an adjuvant for peripheral nerve blockade. The mechanism of this observed antagonism is unclear, but appears to be independent of the action of LAs and MgSO4 at the LA receptor within the Na+ channel. PMID:17720112

  14. TASK channel deletion reduces sensitivity to local anesthetic-induced seizures

    PubMed Central

    Du, Guizhi; Chen, Xiangdong; Todorovic, Marko S.; Shu, Shaofang; Kapur, Jaideep; Bayliss, Douglas A.

    2011-01-01

    Background Local anesthetics (LAs) are typically used for regional anesthesia but can be given systemically to mitigate postoperative pain, supplement general anesthesia or prevent cardiac arrhythmias. However, systemic application or inadvertent intravenous injection can be associated with substantial toxicity, including seizure induction. The molecular basis for this toxic action remains unclear. Methods We characterized effects of different LAs on homomeric and heteromeric K+ channels containing TASK-1 (K2P3.1, KCNK3) and TASK-3 (K2P9.1, KCNK9) subunits in a mammalian expression system. In addition, we used TASK-1/TASK-3 knockout mice to test the possibility that TASK channels contribute to LA-evoked seizures. Results LAs inhibited homomeric and heteromeric TASK channels in a range relevant for seizure induction; channels containing TASK-1 subunits were most sensitive and IC50 values indicated a rank order potency of bupivacaine > ropivacaine ⟫ lidocaine. LAs induced tonic-clonic seizures in mice with the same rank order potency, but higher LA doses were required to evoke seizures in TASK knockout mice. For bupivacaine, which produced the longest seizure times, seizure duration was significantly shorter in TASK knockout mice; bupivacaine-induced seizures were associated with an increase in electroencephalogram power at frequencies <5 Hz in both wild type and TASK knockout mice. Conclusions These data suggest that increased neuronal excitability associated with TASK channel inhibition by LAs contributes to seizure induction. Since all LAs were capable of evoking seizures in TASK channel deleted mice, albeit at higher doses, the results imply that other molecular targets must also be involved in this toxic action. PMID:21946151

  15. Effectiveness of local anesthetic on postoperative pain in different levels of laparoscopic gynecological surgery.

    PubMed

    Selcuk, Selcuk; Api, Murat; Polat, Mesut; Arinkan, Arzu; Aksoy, Bilge; Akca, Tijen; Karateke, Ates

    2016-06-01

    The aim of this study was to assess the effects of preemptive and preclosure analgesia on postoperative pain intensity in patients undergoing different levels of laparoscopic surgery. Two hundred and twenty-six patients who underwent laparoscopic gynecological surgery were enrolled in this quasi-randomized, prospective, placebo controlled study. The operations were classified as level 1 or level 2 according to the extent of the surgery. Lidocaine 1 % was administered at the port sites before making the incision in the preincisional study group. In preincisional control group, same amount of saline was infiltrated in same manner. Lidocaine 1 % was infiltrated at the port site immediately after removing the trocars in preclosure study group. In preclosure control group, the same amount of saline was infiltrated in the same manner. Postoperative pain intensity was evaluated by linear visual analogue scale. It was found that preclosure lidocaine infiltration was more effective on postoperative pain intensity than its placebo group in level 1 and level 2 surgery groups at 1 and 2 h postoperatively. The administration of preincisional lidocaine improved postoperative pain scores significantly more than its placebo group in level 1 laparoscopic surgery group at 1 and 2 h postoperatively and in level 2 laparoscopic surgery group at 1 h postoperatively. Lidocaine infiltration at port sites had beneficial effects on pain intensity in the early postoperative period after laparoscopic gynecological surgery. However, the results of present study showed that the analgesic effect mechanism of local anesthetic was unrelated to the preemptive analgesia hypothesis.

  16. Local Anesthetic Activity from Extracts, Fractions and Pure Compounds from the Roots of Ottonia anisum Spreng. (Piperaceae).

    PubMed

    López, Kelvin S E; Marques, André M; Moreira, Davyson DE L; Velozo, Leosvaldo S; Sudo, Roberto T; Zapata-Sudo, Gisele; Guimarães, Elsie F; Kaplan, Maria Auxiliadora C

    2016-01-01

    Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage) is demonstrated for the first time in vivo guinea pig model. Phytochemical investigation led to the isolation of three amides (pipercallosidine, piperine and valeramide) and in an enriched mixture of seven amides (valeramide, 4,5-dihydropiperlonguminine, N-isobutil-6-piperonil-2-hexenamide, piperovatine, dihydropipercallosidine, pipercallosidine and pipercallpsine). Our findings demonstrated the anesthetic potential for the methanolic extract from roots, its n-hexane partition and amides from O. anisum and it is in agreement with ethnobotanical survey.

  17. Cytotoxicity of solid lipid nanoparticles and nanostructured lipid carriers containing the local anesthetic dibucaine designed for topical application

    NASA Astrophysics Data System (ADS)

    Barbosa, R. M.; da Silva, C. M. G.; Bella, T. S.; de Araújo, D. R.; Marcato, P. D.; Durán, N.; de Paula, E.

    2013-04-01

    Dibucaine (DBC) is powerful long-lasting local anesthetic, but it is also considered fairly toxic to the CNS. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) have attracted attention as carriers for drug delivery. The aim of this study was to develop and to evaluate the cytotoxic activity of DBC-loaded SLN and NLC against 3T3 fibroblast and HaCat keratinocyte cells. The SLN and NLC had myristyl myristate and Liponate®GC as their lipid matrices, respectively, plus a surfactant. SLN and NLC were characterized in terms in their diameter, size distribution, surface charge and DBC encapsulation efficiency. The particle size of SLN and NLC were around 234.33 and 166.62 nm, respectively. The polydispersity index was kept below 0.2 for both nanomaterials. Negative surface charges were observed for both nanoparticles, which decreased in the presence of the anesthetic. Encapsulation efficiency reached 76% and 90%, respectively, in SLN and NLC. DBC alone was found to be toxic to 3T3 and HaCat cells in culture. However, NLC and SLN loaded DBC decreased its intrinsic cytotoxic effect against 3T3 and HaCat cells. In conclusion, encapsulation of DBC in SLN and NLC decreased the in vitro toxicity of the local anesthetic, indicating the potential of these nanocarriers for clinical applications.

  18. The influence of a local anesthetic containing vasoconstrictor on microtensile bond strengths of two adhesive systems to human dentin in situ.

    PubMed

    Harnirattisai, Choltacha; Luangaram, Chumpol; Kuphasuk, Watcharaporn; Senawongse, Pisol

    2010-02-01

    To evaluate the bond strengths of an etch-and-rinse adhesive and a self-etching adhesive to human dentin in vitro and under two in situ conditions: non-anesthetization and anesthetization of the teeth with a local anesthetic containing vasoconstrictor. An in situ study was performed on 49 maxillary premolars scheduled for extraction due to orthodontic reasons. For the bond strength test, occlusal cavities were prepared either with or without a local anesthetic containing vasoconstrictor. The cavities were bonded with Adper Single Bond or Clearfil SE Bond and filled with a resin composite, Filtek Z250. The teeth were then extracted, sectioned, trimmed, and tested for microtensile bond strength. For the observation of dentin surfaces, 20 premolars were used. The impressions of the cavity floors in the anesthetized and non-anesthetized groups were taken before and after acid etching. The replicas were observed under a scanning electron microscope. In vitro, the bond strength test and the SEM observation were also carried out on 24 extracted premolars with the same procedures used in the in situ study. The bond strengths of the two adhesives bonded to dentin in situ were significantly lower than those in vitro. When both adhesives were tested under in situ conditions, there were no significant differences between the bond strengths to dentin of anesthetized and non-anesthetized groups (p > 0.05). No fluid droplets were found on dentin on the cavity floor prepared in vitro, either before or after acid-etching. For the unetched dentin prepared in situ, fluid droplets were found and covered on the smear layer in anesthetized and non-anesthetized groups, but the droplets were slightly larger in the non-anesthetized group. In the non-anesthetized, acid-etched group, dentin surfaces were covered with coalescent dentinal fluid in most specimens. However, in the anesthetized, acid-etched group, patent tubules and some dentinal fluid were observed on the surfaces. It was

  19. Efficacy of parental application of eutectic mixture of local anesthetics for intravenous insertion.

    PubMed

    Koh, J L; Fanurik, D; Stoner, P D; Schmitz, M L; VonLanthen, M

    1999-06-01

    To demonstrate that parent application of eutectic mixture of local anesthetics (EMLA) results in equal reduction of the pain of intravenous (IV) placement compared with clinician application of EMLA, and to assess potential difficulties with parental application. A 2 x 2 randomized block design was used, with 41 children divided into two age groups (5-12 years vs 13-18 years) and randomized to one of two experimental groups (parent-applied EMLA vs clinician-applied EMLA). All children were scheduled to have outpatient gastrointestinal endoscopies with IV sedation. EMLA was placed at least 60 minutes before IV insertion either by the parent or a clinician, depending on the experimental group assignment. Outcome measures were child pain ratings and observed behavioral distress ratings. Parents and children were interviewed to determine parent and child anxiety levels in anticipation of the IV insertion, previous needle stick experience, and previous difficulty coping. Feasibility outcomes included technical difficulty with application of EMLA and appearance of the EMLA cream and occlusive covering. Pain ratings and behavioral distress ratings in the low to moderate range for all groups and ws and were consistent w previous empiric reports of EMLA outcome. There were no significant differences in pain or distress ratings for either the age or the experimental groups. Parent ratings of their child's previous difficulty coping was related to the level of behavioral distress exhibited before (r =.50), during (r =.32) and after (r =.44) the IV insertion. In addition, children's anxiety ratings about IV insertion seemed to differ among groups (although not statistically significant for post hoc comparisons), with the most anxiety reported by the younger children when clinicians applied the EMLA and by older children when parents applied the EMLA. Parent application of EMLA appears to be as effective as clinician application in reducing children's pain and distress

  20. Evaluation of cerebrospinal fluid lactate and plasma lactate concentrations in anesthetized dogs with and without intracranial disease

    PubMed Central

    Caines, Deanne; Sinclair, Melissa; Wood, Darren; Valverde, Alexander; Dyson, Doris; Gaitero, Luis; Nykamp, Stephanie

    2013-01-01

    The objectives of this study were to establish a reference interval for canine cerebrospinal fluid lactate (CSFL) and to compare CSFL and plasma lactate (PL) concentrations in anesthetized dogs with and without intracranial disease. Using a prospective study, canine blood and cerebrospinal fluid were collected for lactate analysis in 11 dogs with intracranial disease after undergoing magnetic resonance imaging (MRI) (Group ID-MRI), in 10 healthy dogs post-MRI (Group H-MRI), and in 39 healthy dogs after induction of anesthesia (Group H-Sx). Dogs were anesthetized for the procedures using different anesthetic protocols. Neurological scores (NS) and sedation scores (SS) were assessed pre-anesthesia in ID-MRI dogs. The CSFL reference interval [90% confidence interval (CI) for lower and upper limits] was 1.1 (1.0 to 1.2) to 2.0 (2.0 to 2.1) mmol/L. Mean ± SD CSFL concentrations were: ID-MRI, 2.1 ± 0.8; H-MRI, 1.6 ± 0.4; and H-Sx, 1.6 ± 0.2 mmol/L. There was a tendency for higher CSFL in dogs in the ID-MRI group than in those in the H-MRI or H-Sx groups (P = 0.12). There was agreement between CSFL and PL in ID-MRI dogs (P = 0.007), but not in dogs in H-MRI (P = 0.5) or H-Sx (P = 0.2). Of the ID-MRI dogs, those with worse NS had higher CSFL (r2 = 0.44). The correlation between CSFL and PL in dogs with intracranial disease and between worse NS and higher CSFL warrants further investigation into the use of CSFL and PL for diagnostic and prognostic purposes. PMID:24124273

  1. The effect of different vasoconstrictors and local anesthetic solutions on substance P expression in human dental pulp.

    PubMed

    Caviedes-Bucheli, Javier; Rojas, Paola; Escalona, Mirna; Estrada, Andres; Sandoval, Carolina; Rivero, Claudia; Lombana, Nelson; Muñoz, Hugo Roberto

    2009-05-01

    The purpose of this study was to quantify the effect of the infiltration injection of different vasoconstrictor and anesthetic solutions on substance P (SP) expression in healthy human dental pulp. Thirty pulp samples were obtained from healthy upper premolars in which extraction was indicated for orthodontic reasons and were randomly assigned into three groups of 10 samples each: 2% lidocaine with 1:80,000 epinephrine (Lido group), 3% Prilocaine with 1:200000 felypressin (Prilo group); and 4% Prilocaine without vasoconstrictor (Prilo-no-VC group). All teeth were extracted 10 minutes after anesthetic application. Pulp samples were processed and SP was measured by radioimmunoassay. SP expression for the Lido, Prilo, and Prilo-no-VC groups were 616.49, 663.76, and 760.79 pmol/mg pulp tissue, respectively. Analysis of variance showed statistically significant differences between groups (p = 0.001). Tukey Honestly Significant Difference (HSD) post hoc tests showed significant statistical differences between the Prilo-no-VC group and the Lido group (p < 0.01) and between the Prilo-no-VC group and the Prilo group (p < 0.05). It can be concluded that infiltration injection of local anesthetics with vasoconstrictor attenuate SP expression in human dental pulp.

  2. Clinical parameters of the local anesthetic effects of bupivacaine applied with and without a vasoconstrictor in oral implantology.

    PubMed

    Duka, Milos; Lazić, Zoran; Stamatović, Novak; Tatić, Zoran; Bubalo, Marija; Veljović, Milić

    2007-09-01

    Bupivacaine (Marcaine), homologue of mepivacaine, chemically related to lidocaine, is used as a local anesthetic for local infiltration, peripheral nerve block, retrobulbar block, symphathetic block, and caudal and epidural anesthesia. The aim of this investigation was to determine and to compare clinical parameters of the local anesthetic effects of bupivacaine applied with and without a vasoconstrictor. This investigation included a total of 30 randomly selected patients, who ranged in age from 30-60 years, with partial or total anodontia in the molar region of the mandible. These patients with total or partial edentulous molar part of the mandible, scheduled for dental implantation placement, were asked to participate in the study. In the first phase of the investigation, the patients were subjected to local anesthesia with 3.5 cm3 of 0.5% bupivacaine with a vasoconstrictor (adrenalin, 1: 200,000) in the right side of the mandible. After administering local anesthesia, the placement of blade, cylindrical, transdental (B.C.T.) implants was performed. In the second stage of the investigation, in 7-10 days period after the first oral surgery, the patients were subjected to local anesthesia with 3.5 cm3 of 0.5% bupivacaine, but without a vasoconstrictor, in the left side of the mandible. After administering local anesthesia, the placement of B.C.T. implants was performed. During the performance of both oral surgery procedures, the following clinical parameters of the local anesthetic effects were monitored: latent period, duration and the potency of anesthesia, and the evaluation of the postoperative pain level. The latent period under local anesthesia with 3.5 cm3 of 0.5% bupivacaine and vasoconstrictor was statistically significantly shorter than without vasoconstrictor. The duration of local anesthesia was longer without vasoconstrictor. There was no difference in the potency of anesthesia with or without a vasoconstrictor, while the lowest level of postoperative

  3. Cartridge syringe vs computer controlled local anesthetic delivery system: Pain related behaviour over two sequential visits - a randomized controlled trial.

    PubMed

    Thoppe-Dhamodhara, Yogesh-Kumar; Asokan, Sharath; John, Baby-John; Pollachi-Ramakrishnan, GeethaPriya; Ramachandran, Punithavathy; Vilvanathan, Praburajan

    2015-10-01

    Local anesthetic injection is one of the most anxiety provoking procedure in dentistry. Knowledge about change in pain related behaviour during consecutive visits helps in and scheduling of treatment procedures and management of children in dental clinic. To compare the pain perception, behavioural response and the associated change in physiological parameters while receiving local anesthesia injection with cartridge syringe and computer controlled local anesthetic delivery system (CCLAD) over two consecutive visits. In this randomized controlled cross over trial, 120 children aged 7 - 11 years were randomly divided into group A: receiving injections with CCLAD during first visit; group B: receiving injections with cartridge syringe during first visit. The physiological parameters (heart rate and blood pressure) were recorded before and during injection procedure. Objective evaluation of disruptive behaviour and subjective evaluation of pain perceived were done using Face Legs Activity Cry Consolability (FLACC) scale and modified facial image scale (FIS) respectively. No statistical difference in pain response (p= 0.164) and disruptive behaviour (p = 0.120) between cartridge syringe and CCLAD injections were seen during the first visit although the latter showed lesser scores. However, during the second visit there were significant increase in pain response (p = 0.004) and disruptive behaviour (p = 0.006) in cartridge syringe group with an associated increase in heart rate. Injections with CCLAD produced lesser pain ratings and disruptive behaviour than cartridge syringe in children irrespective of order of visit. Behaviour, cartridge syringe, CCLAD, local anesthesia.

  4. Effects of one minimum alveolar anesthetic concentration sevoflurane on cerebral metabolism, blood flow, and CO2 reactivity in cardiac patients.

    PubMed

    Mielck, F; Stephan, H; Weyland, A; Sonntag, H

    1999-08-01

    We investigated the cerebral hemodynamic effects of 1 minimum alveolar anesthetic concentration (MAC) sevoflurane anesthesia in nine male patients scheduled for elective coronary bypass grafting. For measurement of cerebral blood flow (CBF), a modified Kety-Schmidt saturation technique was used with argon as an inert tracer gas. Measurements of CBF were performed before the induction of anesthesia and 30 min after induction under normocapnic, hypocapnic, and hypercapnic conditions. Compared with the awake state under normocapnic conditions, sevoflurane reduced the mean cerebral metabolic rate of oxygen by 47% and the mean cerebral metabolic rate of glucose by 39%. Concomitantly, CBF was reduced by 38%, although mean arterial pressure was kept constant. Significant changes in jugular venous oxygen saturation were absent. Hypocapnia and hypercapnia caused a 51% decrease and a 58% increase in CBF, respectively. These changes in CBF caused by variation of Paco2 indicate that cerebrovascular CO2 reactivity persists during 1 MAC sevoflurane anesthesia. We used a modified Kety-Schmidt saturation technique to investigate the effects of 1 minimum alveolar anesthetic concentration (MAC) sevoflurane on cerebral blood flow, metabolism, and CO2 reactivity in cardiac patients. We found that the global cerebral blood flow and global cerebral metabolic rate of oxygen remained coupled and that cerebrovascular CO2 reactivity is not impaired by the administration of 1 MAC sevoflurane.

  5. Efficacy of Benzocaine 20% Topical Anesthetic Compared to Placebo Prior to Administration of Local Anesthesia in the Oral Cavity: A Randomized Controlled Trial.

    PubMed

    de Freiras, Guilherme Camponogara; Pozzobon, Roselaine Terezinha; Blaya, Diego Segatto; Moreira, Carlos Heitor

    2015-01-01

    The aim of the present study was to compare the effects of a topical anesthetic to a placebo on pain perception during administration of local anesthesia in 2 regions of the oral cavity. A split-mouth, double-blind, randomized clinical trial design was used. Thirty-eight subjects, ages 18-50 years, American Society of Anesthesiologists I and II, received 4 anesthetic injections each in regions corresponding to the posterior superior alveolar nerve (PSA) and greater palatine nerve (GPN), totaling 152 sites analyzed. The side of the mouth where the topical anesthetic (benzocaine 20%) or the placebo was to be applied was chosen by a flip of a coin. The needle used was 27G, and the anesthetic used for administration of local anesthesia was 2% lidocaine with 1:100,000 epinephrine. After receiving the administration of local anesthesia, each patient reported pain perception on a visual analog scale (VAS) of 100-mm length. The results showed that the topical anesthetic and the placebo had similar effects: there was no statistically significant VAS difference between the PSA and the GPN pain ratings. A higher value on the VAS for the anesthesia of the GPN, relative to the PSA, was observed for both groups. Regarding gender, male patients had higher values on the VAS compared with female patients, but these differences were not meaningful. The topical anesthetic and the placebo had similar effects on pain perception for injection of local anesthesia for the PSA and GPN.

  6. Efficacy of Benzocaine 20% Topical Anesthetic Compared to Placebo Prior to Administration of Local Anesthesia in the Oral Cavity: A Randomized Controlled Trial

    PubMed Central

    de Freiras, Guilherme Camponogara; Pozzobon, Roselaine Terezinha; Blaya, Diego Segatto; Moreira, Carlos Heitor

    2015-01-01

    The aim of the present study was to compare the effects of a topical anesthetic to a placebo on pain perception during administration of local anesthesia in 2 regions of the oral cavity. A split-mouth, double-blind, randomized clinical trial design was used. Thirty-eight subjects, ages 18–50 years, American Society of Anesthesiologists I and II, received 4 anesthetic injections each in regions corresponding to the posterior superior alveolar nerve (PSA) and greater palatine nerve (GPN), totaling 152 sites analyzed. The side of the mouth where the topical anesthetic (benzocaine 20%) or the placebo was to be applied was chosen by a flip of a coin. The needle used was 27G, and the anesthetic used for administration of local anesthesia was 2% lidocaine with 1:100,000 epinephrine. After receiving the administration of local anesthesia, each patient reported pain perception on a visual analog scale (VAS) of 100-mm length. The results showed that the topical anesthetic and the placebo had similar effects: there was no statistically significant VAS difference between the PSA and the GPN pain ratings. A higher value on the VAS for the anesthesia of the GPN, relative to the PSA, was observed for both groups. Regarding gender, male patients had higher values on the VAS compared with female patients, but these differences were not meaningful. The topical anesthetic and the placebo had similar effects on pain perception for injection of local anesthesia for the PSA and GPN. PMID:26061572

  7. EFFECTS OF TRAMADOL ON THE MINIMUM ANESTHETIC CONCENTRATION OF ISOFLURANE IN WHITE-EYED PARAKEETS (PSITTACARA LEUCOPHTHALMUS).

    PubMed

    Escobar, André; da Rocha, Rozana Wendler; Midon, Monica; de Almeida, Ricardo Miyasaka; Filho, Darcio Zangirolami; Werther, Karin

    2017-06-01

    The aim of this study was to determine the minimum anesthetic concentration (MAC) of isoflurane, and to investigate if tramadol changes the isoflurane MAC in white-eyed parakeets (Psittacara leucophthalmus). Ten adult birds weighing 157 ± 9 g were anesthetized with isoflurane in oxygen under mechanical ventilation. Isoflurane concentration for the first bird was adjusted to 2.2%, and after 15 min an electrical stimulus was applied in the thigh area to observe the response (movement or nonmovement). Isoflurane concentration for the subsequent bird was increased by 10% if the previous bird moved, or decreased by 10% if the previous bird did not move. This procedure was performed serially until at least four sequential crossover events were detected. A crossover event was defined as a sequence of two birds with different responses (positive or negative) to the electrical stimulus. Isoflurane MAC was calculated as the mean isoflurane concentration value at the crossover events. After 1 wk, the same birds were reanesthetized with isoflurane and MAC was determined at 15 and 30 min after intramuscular administration of 10 mg/kg of tramadol using the same method. A paired t-test (P < 0.05%) was used to detect significant differences for MAC between treatments. Isoflurane MAC in this population of white-eyed parakeets was 2.47 ± 0.09%. Isoflurane MAC values 15 and 30 min after tramadol administration were indistinguishable from each other (pooled value was 2.50 ± 0.18%); they were also indistinguishable from isoflurane MAC without tramadol. The isoflurane MAC value in white-eyed parakeets is higher than reported for other bird species. Tramadol (10 mg/kg, i.m.) does not change isoflurane MAC in these birds.

  8. Comparison of the efficacy of saline, local anesthetics, and steroids in epidural and facet joint injections for the management of spinal pain: A systematic review of randomized controlled trials

    PubMed Central

    Manchikanti, Laxmaiah; Nampiaparampil, Devi E.; Manchikanti, Kavita N.; Falco, Frank J.E.; Singh, Vijay; Benyamin, Ramsin M.; Kaye, Alan D.; Sehgal, Nalini; Soin, Amol; Simopoulos, Thomas T.; Bakshi, Sanjay; Gharibo, Christopher G.; Gilligan, Christopher J.; Hirsch, Joshua A.

    2015-01-01

    Background: The efficacy of epidural and facet joint injections has been assessed utilizing multiple solutions including saline, local anesthetic, steroids, and others. The responses to these various solutions have been variable and have not been systematically assessed with long-term follow-ups. Methods: Randomized trials utilizing a true active control design were included. The primary outcome measure was pain relief and the secondary outcome measure was functional improvement. The quality of each individual article was assessed by Cochrane review criteria, as well as the criteria developed by the American Society of Interventional Pain Physicians (ASIPP) for assessing interventional techniques. An evidence analysis was conducted based on the qualitative level of evidence (Level I to IV). Results: A total of 31 trials met the inclusion criteria. There was Level I evidence that local anesthetic with steroids was effective in managing chronic spinal pain based on multiple high-quality randomized controlled trials. The evidence also showed that local anesthetic with steroids and local anesthetic alone were equally effective except in disc herniation, where the superiority of local anesthetic with steroids was demonstrated over local anesthetic alone. Conclusion: This systematic review showed equal efficacy for local anesthetic with steroids and local anesthetic alone in multiple spinal conditions except for disc herniation where the superiority of local anesthetic with steroids was seen over local anesthetic alone. PMID:26005584

  9. Intraneural injection of a test dose of local anesthetic in peripheral nerves - does it induce histological changes in nerve tissue?

    PubMed

    Wiesmann, T; Steinfeldt, T; Exner, M; Nimphius, W; De Andres, J; Wulf, H; Schwemmer, U

    2017-01-01

    Most anesthesiologists use the injection of a test dose of local anesthetic in order to evaluate the final needle tip position. Thus, the intraneural injection of a full dose can be avoided. The aim of this study was to analyze whether an intraneural injection of a test dose of bupivacaine could trigger histological changes. Intraneural injections under direct vision were performed in 40 brachial plexus nerves in seven anesthetized pigs. Tibial nerves served as positive and negative controls. Two milliliter of bupivacaine 0.5% was injected in three nerves on the left brachial plexus. For control of local anesthetic's toxicity Ringer's solution was applied intraneurally on the right side. After maintaining 48 h of general anesthesia, the nerves were resected. The specimens were processed for histological examination and assessed for inflammation (hematoxylin and eosin stain, CD68-immunohistochemistry) and myelin damage (Kluver-Barrera stain). The degree of nerve injury was rated on a scale from 0 (no injury) to 4 (severe injury). Statistical analysis showed no significant differences between the bupivacaine group [median (interquartile range) 1 (1-1.5)] and the Ringer's solution group [1 (0.5-2) P = 0.772]. Mild myelin alteration was found in 12.5% of all specimens following intraneural injection, irrespective of the applied substance. "In our experimental study, intraneural injection of 2 ml of bupivacaine or Ringer's solution showed comparable mild inflammation. Nevertheless, inflammation can only be prevented by strictly avoiding nerve perforation followed by intraneural injection, as mechanical nerve perforation is a key factor for evolving inflammation. © 2016 The Acta Anaesthesiologica Scandinavica Foundation. Published by John Wiley & Sons Ltd.

  10. Efficacy of articaine and lidocaine in a primary intraligamentary injection administered with a computer-controlled local anesthetic delivery system.

    PubMed

    Berlin, Jeffrey; Nusstein, John; Reader, Al; Beck, Mike; Weaver, Joel

    2005-03-01

    The purpose of this prospective, randomized, double-blind study was to compare the anesthetic efficacy of the intraligamentary injection of 4% articaine with 1:100,000 epinephrine and of 2% lidocaine with 1:100,000 epinephrine, administered with computer-controlled local anesthetic delivery system, in mandibular posterior teeth. Using a crossover design, intraligamentary injections of 1.4 mL of 4% articaine with 1:100,000 epinephrine and of 1.4 mL of 2% lidocaine with 1:100,000 epinephrine were randomly administered with a computer-controlled local anesthetic delivery system, in a double-blind manner on the mesial and distal aspects of a mandibular first molar, at 2 separate appointments to 51 subjects. A pulp tester was used to test for anesthesia, in 2-minute cycles for 60 minutes, of the mandibular first and second molars and second premolar. Anesthesia was considered successful when 2 consecutive 80 readings (highest output) were obtained within 20 minutes. Successful pulpal anesthesia was obtained 86% of the time for the first molar using the articaine solution and 74% of the time using the lidocaine solution. There were no significant differences (P > .05) between the articaine and lidocaine solutions. The mean onset times of pulpal anesthesia for the first molar were 1.3 minutes with articaine solution and 2.2 minutes with lidocaine solution. Duration of pulpal anesthesia for the first molar was 34 minutes for the articaine solution and 31 minutes for the lidocaine solution. The efficacy of 4% articaine with 1:100,000 epinephrine was similar to the efficacy of 2% lidocaine with 1:100,000 epinephrine for intraligamentary injections.

  11. Effect of cuffed and uncuffed endotracheal tubes on the oropharyngeal oxygen and volatile anesthetic agent concentration in children.

    PubMed

    Raman, Vidya; Tobias, Joseph D; Bryant, Jason; Rice, Julie; Jatana, Kris; Merz, Meredith; Elmaraghy, Charles; Kang, D Richard

    2012-06-01

    Over the past 5 years, there has been a change in the clinical practice of pediatric anesthesiology with a transition to the use of cuffed instead of uncuffed endotracheal tubes (ETTs) in infants and children. As the trachea is sealed, one advantage is to eliminate the contamination of the oropharynx with oxygen which should be advantageous during adenotonsillectomy where there is a risk of airway fire. The current study prospectively assesses the oropharyngeal oxygen and volatile anesthetic agent concentration during adenotonsillectomy in infants and children. Following the induction of general anesthesia in patients scheduled for adenoidectomy, tonsillectomy or adenotonsillectomy, the trachea was intubated. The use of a cuffed or uncuffed ETT and the use of spontaneous (SV) or positive pressure ventilation (PPV) were at the discretion of the anesthesia team. The oxygen concentration was kept at 100% oxygen until the study was completed. Following placement of the mouth gag, the otolaryngolist placed into the oropharynx a small bore catheter, which was attached to a standard anesthesia gas monitoring device which sampled the gas at 150mL/min. The concentration of the oxygen and the concentration of the anesthetic agent in the oropharynx were measured for 5 breaths. The cohort for the study included 200 patients ranging in age from 1 to 18 years. With the use of a cuffed ETT and either SV or PPV, the oxygen concentration in the oropharynx was 20-21% and the volatile agent concentration was 0% in all 118 patients. With the use of an uncuffed ETT and the administration of 100% oxygen, there was significant contamination of the oropharynx noted during both PPV and SV. The mean oxygen concentration was 71% during PPV with an uncuffed ETT and 65% during SV with an uncuffed ETT. In these patients, the oropharyngeal oxygenation concentration exceeded 30% in 73 of the 82 patients (89%). The oropharyngeal oxygen and agent concentration was greater when the leak around the

  12. 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.

  13. Monitoring cerebral oxygenation and local field potential with a variation of isoflurane concentration in a rat model

    PubMed Central

    Choi, Dong-Hyuk; Shin, Teo Jeon; Kim, Seonghyun; Bae, Jayyoung; Cho, Dongrae; Ham, Jinsil; Park, Ji-Young; Kim, Hyoung-Ihl; Jeong, Seongwook; Lee, Boreom; Kim, Jae Gwan

    2016-01-01

    We aimed to investigate experimentally how anesthetic levels affect cerebral metabolism measured by near-infrared spectroscopy (NIRS) and to identify a robust marker among NIRS parameters to discriminate various stages of anesthetic depth in rats under isoflurane anesthesia. In order to record the hemodynamic changes and local field potential (LFP) in the brain, fiber-optic cannulae and custom-made microelectrodes were implanted in the frontal cortex of the skull. The NIRS and LFP signals were continuously monitored before, during and after isoflurane anesthesia. As isoflurane concentration is reduced, the level of oxyhemoglobin and total hemoglobin concentrations of the frontal cortex decreased gradually, while deoxyhemoglobin increased. The reflectance ratio between 730nm and 850nm and burst suppression ratio (BSR) correspond similarly with the change of oxyhemoglobin during the variation of isoflurane concentration. These results suggest that NIRS signals in addition to EEG may provide a possibility of developing a new anesthetic depth index. PMID:27867719

  14. Non-centralized and functionally localized nervous system of ophiuroids: evidence from topical anesthetic experiments

    PubMed Central

    Sato, Eiki; Kano, Takeshi; Aonuma, Hitoshi; Ishiguro, Akio

    2017-01-01

    ABSTRACT Ophiuroids locomote along the seafloor by coordinated rhythmic movements of multi-segmented arms. The mechanisms by which such coordinated movements are achieved are a focus of interest from the standpoints of neurobiology and robotics, because ophiuroids appear to lack a central nervous system that could exert centralized control over five arms. To explore the underlying mechanism of arm coordination, we examined the effects of selective anesthesia to various parts of the body of ophiuroids on locomotion. We observed the following: (1) anesthesia of the circumoral nerve ring completely blocked the initiation of locomotion; however, initiation of single arm movement, such as occurs during the retrieval of food, was unaffected, indicating that the inability to initiate locomotion was not due to the spread of the anesthetic agent. (2) During locomotion, the midsegments of the arms periodically made contact with the floor to elevate the disc. In contrast, the distal segments of the arms were pointed aborally and did not make contact with the floor. (3) When the midsegments of all arms were anesthetized, arm movements were rendered completely uncoordinated. In contrast, even when only one arm was left intact, inter-arm coordination was preserved. (4) Locomotion was unaffected by anesthesia of the distal arms. (5) A radial nerve block to the proximal region of an arm abolished coordination among the segments of that arm, rendering it motionless. These findings indicate that the circumoral nerve ring and radial nerves play different roles in intra- and inter-arm coordination in ophiuroids. PMID:28412715

  15. Relief of Injection Pain During Delivery of Local Anesthesia by Computer-Controlled Anesthetic Delivery System for Periodontal Surgery: Randomized Clinical Controlled Trial.

    PubMed

    Chang, Hyeyoon; Noh, Jiyoung; Lee, Jungwon; Kim, Sungtae; Koo, Ki-Tae; Kim, Tae-Il; Seol, Yang-Jo; Lee, Yong-Moo; Ku, Young; Rhyu, In-Chul

    2016-07-01

    Pain from local anesthetic injection makes patients anxious when visiting a dental clinic. This study aims to determine differences in pain according to types of local anesthetizing methods and to identify the possible contributing factors (e.g., dental anxiety, stress, and sex). Thirty-one patients who underwent open-flap debridement in maxillary premolar and molar areas during treatment for chronic periodontitis were evaluated for this study. A randomized, split-mouth, single-masked clinical trial was implemented. The dental anxiety scale (DAS) and perceived stress scale (PSS) were administered before surgery. Two lidocaine ampules for each patient were used for local infiltration anesthesia (supraperiosteal injection). Injection pain was measured immediately after local infiltration anesthesia using the visual analog pain scale (VAS) questionnaire. Results from the questionnaire were used to assess degree of pain patients feel when a conventional local anesthetic technique (CNV) is used compared with a computer-controlled anesthetic delivery system (CNR). DAS and PSS did not correlate to injection pain. VAS scores were lower for CNR than for CNV regardless of the order in which anesthetic procedures were applied. VAS score did not differ significantly with sex. Pearson coefficient for correlation between VAS scores for the two procedures was 0.80, also indicating a strong correlation. Within the limitations of the present study, relief from injection pain is observed using CNR.

  16. Image intensifier-guided injection of corticosteroid and local anesthetic agent for the treatment of recalcitrant plantar fasciitis.

    PubMed

    Atkins, Kate L; Chin, Kuen Foo; Noorani, Ali M; Nairn, David S

    2010-08-01

    Plantar fasciitis is the most common cause of plantar heel pain. The condition is potentially self-limiting and can respond to conservative treatment, but patients may opt for surgery if the treatments fail. Surgical intervention is associated with potential complications. This study set out to explore the efficacy of the specific nonsurgical intervention offered to treatment-resistant cases in a local clinical setting. The technique involves image intensifier-guided injection of corticosteroid and local anesthetic agents under general anesthesia. Nineteen patients with recalcitrant plantar fasciitis of over 12 months' duration received injections. A simple follow-up questionnaire was given to patients after the procedure that focused on their subjective opinion of any change in their pain. They were also asked if the injection had solved their problems with heel pain. The improvements that the patients reported were found to be statistically significant (P = .012).

  17. Molecular Insights into the Local Anesthetic Receptor within Voltage-Gated Sodium Channels Using Hydroxylated Analogs of Mexiletine

    PubMed Central

    Desaphy, Jean-François; Dipalma, Antonella; Costanza, Teresa; Carbonara, Roberta; Dinardo, Maria Maddalena; Catalano, Alessia; Carocci, Alessia; Lentini, Giovanni; Franchini, Carlo; Camerino, Diana Conte

    2011-01-01

    , these results confirm our former hypothesis by showing that the presence of hydroxyl groups to the aryloxy moiety of mexiletine greatly reduced sodium channel block, and provide molecular insights into the intimate interaction of local anesthetics with their receptor. PMID:22403541

  18. Continuous wound infusion of local anesthetic and steroid after major abdominal surgery: study protocol for a randomized controlled trial.

    PubMed

    Bugada, Dario; De Gregori, Manuela; Compagnone, Christian; Muscoli, Carolina; Raimondi, Ferdinando; Bettinelli, Silvia; Avanzini, Maria Antonietta; Cobianchi, Lorenzo; Peloso, Andrea; Baciarello, Marco; Dagostino, Concetta; Giancotti, Luigino A; Ilari, Sara; Lauro, Filomena; Grimaldi, Stefania; Tasciotti, Ennio; Fini, Massimo; Saccani Jotti, Gloria M R; Meschi, Tiziana; Fanelli, Guido; Allegri, Massimo

    2015-08-14

    Inflammatory response is one of the key components of pain perception. Continuous infusion (CWI) of local anesthetics has been shown to be effective in controlling pain and reducing postoperative morphine consumption, but the effect of adding a potent anti-inflammatory drug (such as a steroid) has never been addressed. In our study, we want to investigate the effect of CWI with local anesthetic + methylprednisolone on acute and persistent pain, correlating clinical data with biomarkers of inflammation and genetic background. After approval by their institutional review board, three hospitals will enroll 120 patients undergoing major abdominal surgery in a randomized, double-blind, phase III study. After a 24-h CWI of ropivacaine 0.2 % + methylprednisolone 1 mg/kg, patients will be randomly assigned to receive either ropivacaine + steroid or placebo for the next 24 h. Then, patient-controlled CWI with only ropivacaine 0.2 % or placebo (according to the group of randomization) is planned after 48 h up to 7 days (bolus 10 ml, lock-out 1 h, maximum dose of 40 ml in 4 h). Morphine equivalent consumption up to 7 days will be analyzed, together with any catheter- or drug-related side effect. Persistent post-surgical pain (PPSP) incidence will also be investigated. Our primary endpoint is analgesic consumption in the first 7 days after surgery; we will evaluate, as secondary endpoints, any catheter- or drug-related side effect, genotype/phenotype correlations between some polymorphisms and postoperative outcome in terms of morphine consumption, development of the inflammatory response, and incidence of PPSP. Finally, we will collect, in a subgroup of patients, wound exudate samples by micro-dialysis, blood samples, and urine samples up to 72 h to investigate local and systemic inflammation and oxidative stress. This is a phase III trial to evaluate the safety and efficacy of wound infusion with steroid and local anesthetic. The study is aimed also to evaluate how long this

  19. The effect of buffering on pain and duration of local anesthetic in the face: A double-blind, randomized controlled trial

    PubMed Central

    Afolabi, Oluwatola; Murphy, Amanda; Chung, Bryan; Lalonde, Donald H

    2013-01-01

    BACKGROUND: The acidity of lidocaine preparations is believed to contribute to the pain of local anesthetic injection. OBJECTIVE: To investigate the effect of buffering lidocaine on the pain of injection and duration of anesthetic effect. METHODS: A double-blind, randomized trial involving 44 healthy volunteers was conducted. The upper lip was injected with a solution of: lidocaine 1% (Xylocaine, AstraZeneca, Canada, Inc) with epinephrine; and lidocaine 1% with epinephrine and 8.4% sodium bicarbonate. Volunteers reported pain of injection and duration of anesthetic effect. RESULTS: Twenty-six participants found the unbuffered solution to be more painful. Fifteen participants found the buffered solution to be more painful; the difference was not statistically significant. Twenty-one volunteers reported duration of anesthetic effect. The buffered solution provided longer anesthetic effect than the unbuffered solution (P=0.004). CONCLUSION: Although buffering increased the duration of lidocaine’s anesthetic effect in this particular model, a decrease in the pain of the injection was not demonstrated, likely due to limitations of the study. PMID:24497759

  20. Anesthetic Efficacy of Different Ropivacaine Concentrations for Inferior Alveolar Nerve Block

    PubMed Central

    El-Sharrawy, Eman; Yagiela, John A

    2006-01-01

    This study was conducted on 72 American Society of Anesthesiologists class 1 patients scheduled for extraction of a mandibular third molar after inferior alveolar nerve block. Each patient was randomly administered one of the following ropivacaine concentrations: 0.75%, 0.5%, 0.375%, or 0.25% (18 patients per group). Onset of block (mean ± SD) was rapid for both 0.75% (1.4 ± 0.4 minutes) and 0.5% (1.7 ± 0.5 minutes) ropivacaine but significantly slower for the 0.375% (4.2 ± 2.5 minutes) and 0.25% (10.7 ± 3.0 minutes) concentrations. Tooth extraction was performed successfully with the 0.5% and 0.75% concentrations, and supplemental injections were not required. Second injections, however, were required with 0.375% ropivacaine. Anesthesia was unsuccessful in 13 patients given 0.25% ropivacaine even after 3 injections. The mean durations of soft tissue anesthesia were 3.3 ± 0.3 hours and 3.0 ± 0.3 hours for the 0.75% and 0.5% concentrations, but significantly shorter with more dilute concentrations. The duration of analgesia showed a similar pattern, with the 0.75% and 0.5% concentrations producing prolonged analgesia of 6.0 ± 0.4 hours and 5.6 ± 0.4 hours. These results indicate that 0.5% and 0.75% concentrations were effective for intraoral nerve blockade, with both a rapid onset and prolonged duration of pain control. PMID:16722277

  1. Anesthetic efficacy of different ropivacaine concentrations for inferior alveolar nerve block.

    PubMed

    El-Sharrawy, Eman; Yagiela, John A

    2006-01-01

    This study was conducted on 72 American Society of Anesthesiologists class 1 patients scheduled for extraction of a mandibular third molar after inferior alveolar nerve block. Each patient was randomly administered one of the following ropivacaine concentrations: 0.75%, 0.5%, 0.375%, or 0.25% (18 patients per group). Onset of block (mean +/- SD) was rapid for both 0.75% (1.4 +/- 0.4 minutes) and 0.5% (1.7 +/- 0.5 minutes) ropivacaine but significantly slower for the 0.375% (4.2 +/- 2.5 minutes) and 0.25% (10.7 +/- 3.0 minutes) concentrations. Tooth extraction was performed successfully with the 0.5% and 0.75% concentrations, and supplemental injections were not required. Second injections, however, were required with 0.375% ropivacaine. Anesthesia was unsuccessful in 13 patients given 0.25% ropivacaine even after 3 injections. The mean durations of soft tissue anesthesia were 3.3 +/- 0.3 hours and 3.0 +/- 0.3 hours for the 0.75% and 0.5% concentrations, but significantly shorter with more dilute concentrations. The duration of analgesia showed a similar pattern, with the 0.75% and 0.5% concentrations producing prolonged analgesia of 6.0 +/- 0.4 hours and 5.6 +/- 0.4 hours. These results indicate that 0.5% and 0.75% concentrations were effective for intraoral nerve blockade, with both a rapid onset and prolonged duration of pain control.

  2. Postoperative Pain Management after Spinal Fusion Surgery: An Analysis of the Efficacy of Continuous Infusion of Local Anesthetics

    PubMed Central

    Reynolds, Richard A. K.; Legakis, Julie E.; Tweedie, Jillian; Chung, YoungKey; Ren, Emily J.; BeVier, Patricia A.; Thomas, Ronald L.; Thomas, Suresh T.

    2013-01-01

    Spinal fusion surgery is a major surgery that results in severe postoperative pain, therefore pain reduction is a primary concern. New strategies for pain management are currently under investigation and include multimodal treatment. A 3-year retrospective analysis of patients with idiopathic scoliosis undergoing spinal fusion surgery was performed at our hospital, assessing patient pain scores, opioid use, and recovery. We evaluated the effect of adding continuous infusion of local anesthetics (CILA) to a postoperative pain management protocol that includes intraoperative intrathecal morphine, as well as postoperative patient-controlled analgesia and oral opioid/acetaminophen combination. The study compared 25 patients treated according to the standard protocol, with 62 patients treated with CILA in addition to the pain management protocol. Patients in the CILA group used nearly 0.5 mg/kg less opioid analgesics during the first 24 hours after surgery. PMID:24436846

  3. Severe post-burn neck contracture release and skin graft harvest using tumescent local anaesthesia as the sole anesthetic technique.

    PubMed

    Prasad, Mukesh Kumar; Puneet, Pulak; Rani, Kanchan; Shree, Divya

    2012-02-01

    Severe post-burn contractures in the neck often cause anatomical distortion and restriction of neck movements, resulting in varying degrees of difficulty in airway management. Any mode of anesthesia that may obviate the need for imperative airway control may be desirable in such situations in which a difficult airway may be anticipated. Here we present one such situation where tumescent local anesthesia was employed to manage a case of severe post-burn neck contractures posted for contracture release and split-skin grafting. The other benefits of this method were minimal blood loss and excellent postoperative analgesia. In conclusion, it can be emphasized that the application of tumescent anesthesia is an important anesthetic tool in patients with predicted difficult airway management.

  4. The Effect of 2 Injection Speeds on Local Anesthetic Discomfort During Inferior Alveolar Nerve Blocks

    PubMed Central

    de Souza Melo, Marcelo Rodrigo; Sabey, Mark Jon Santana; Lima, Carla Juliane; de Almeida Souza, Liane Maciel; Groppo, Francisco Carlos

    2015-01-01

    This randomized double-blind crossover trial investigated the discomfort associated with 2 injection speeds, low (60 seconds) and slow (100 seconds), during inferior alveolar nerve block by using 1.8 mL of 2% lidocaine with 1 : 100,000 epinephrine. Three phases were considered: (a) mucosa perforation, (b) needle insertion, and (c) solution injection. Thirty-two healthy adult volunteers needing bilateral inferior alveolar nerve blocks at least 1 week apart were enrolled in the present study. The anesthetic procedure discomfort was recorded by volunteers on a 10-cm visual analog scale in each phase for both injection speeds. Comparison between the 2 anesthesia speeds in each phase was performed by paired t test. Results showed no statistically significant difference between injection speeds regarding perforation (P = .1016), needle placement (P = .0584), or speed injection (P = .1806). The discomfort in all phases was considered low. We concluded that the 2 injection speeds tested did not affect the volunteers' pain perception during inferior alveolar nerve blocks. PMID:26398126

  5. Anesthesia with Isoflurane and Sevoflurane in the Crested Serpent Eagle (Spilornis cheela hoya): Minimum Anesthetic Concentration, Physiological Effects, Hematocrit, Plasma Chemistry and Behavioral Effects

    PubMed Central

    CHAN, Fang-Tse; CHANG, Geng-Ruei; WANG, Hsien-Chi; HSU, Tien-Huan

    2013-01-01

    ABSTRACT The initial goal of this study was to determine the minimum anesthetic concentration (MAC) for isoflurane (ISO) and sevoflurane (SEVO) for the crested serpent eagle. Next, we compared the anesthetic effects of each on the physiological effects, hematocrit, plasma chemistry values and behavior in spontaneously breathing captive adult crested serpent eagles. Sixteen eagles were randomly allocated to two groups for anesthesia with ISO (n=8) or SEVO (n=8). First, we measured the MAC values of ISO and SEVO, and four weeks later, we investigated the effect of each on the physiological effects, hematocrit (HCT) and plasma chemistry values. The MAC values of ISO and SEVO for crested serpent eagles were 1.46 ± 0.30 and 2.03 ± 0.32%, respectively. The results revealed no significant differences between the two anesthetics in induction time, while time of extubation to recovery was significantly shorter with SEVO. A time-related increase in end-tidal CO2 and decreases in body temperature and respiratory rates were observed during anesthesia with each anesthetic. There were no significant differences between the effect of the two anesthetics on heart rate, hematocrit, plasma chemistry values or respiration, although each caused minor respiration depression. We concluded that SEVO is a more effective inhalant agent than ISO for use in eagles, showing the most rapidest induction and recovery from anesthesia. PMID:23955396

  6. Prophylactic Antiarrhythmic Effect of Anesthetics at Subanesthetic Concentration on Epinephrine-Induced Arrhythmias in Rats after Brain Death

    PubMed Central

    Miyata, Yuka; Iwasaki, Mitsuo; Yamanaka, Hiroo; Sato, Masanori; Kamibayashi, Takahiko; Fujino, Yuji

    2015-01-01

    The present study using brain death model of rats was designed to examine whether prophylactic administration of volatile anesthetics and propofol prevent the epinephrine-induced arrhythmias. A Fogarty catheter was placed intracranially for induction of brain death. After brain death, the rats were randomly assigned to five groups: the control group (no anesthetics), the sevoflurane group (0.8%), the isoflurane group (0.5%), the halothane group (0.3%), and the propofol group (195 μg·kg−1 ·min−1). These anesthetics were about 30% of ED50 of each anesthetic. The arrhythmogenic dose of epinephrine was determined in each anesthetic group. In addition, we examined left ventricular levels of connexin 43 phosphorylation 30 min after administration of each anesthetic with Western blot analysis. The arrhythmogenic dose of epinephrine in the sevoflurane group was significantly higher than that in the control group, while the arrhythmogenic dose of epinephrine in any other anesthetic group was not different. On the other hand, the ratio of phosphorylated-connexin 43/total connexin 43 was also similar among the study groups. Thus, prophylactic administration of subanesthetic dose of sevoflurane is effective in preventing epinephrine-induced arrhythmias after brain death, but phosphorylation of connexin is not involved in the antiarrhythmic property of sevoflurane. PMID:25654113

  7. Prophylactic antiarrhythmic effect of anesthetics at subanesthetic concentration on epinephrine-induced arrhythmias in rats after brain death.

    PubMed

    Miyata, Yuka; Iwasaki, Mitsuo; Yamanaka, Hiroo; Sato, Masanori; Kamibayashi, Takahiko; Fujino, Yuji; Hayashi, Yukio

    2015-01-01

    The present study using brain death model of rats was designed to examine whether prophylactic administration of volatile anesthetics and propofol prevent the epinephrine-induced arrhythmias. A Fogarty catheter was placed intracranially for induction of brain death. After brain death, the rats were randomly assigned to five groups: the control group (no anesthetics), the sevoflurane group (0.8%), the isoflurane group (0.5%), the halothane group (0.3%), and the propofol group (195 μg·kg(-1) ·min(-1)). These anesthetics were about 30% of ED50 of each anesthetic. The arrhythmogenic dose of epinephrine was determined in each anesthetic group. In addition, we examined left ventricular levels of connexin 43 phosphorylation 30 min after administration of each anesthetic with Western blot analysis. The arrhythmogenic dose of epinephrine in the sevoflurane group was significantly higher than that in the control group, while the arrhythmogenic dose of epinephrine in any other anesthetic group was not different. On the other hand, the ratio of phosphorylated-connexin 43/total connexin 43 was also similar among the study groups. Thus, prophylactic administration of subanesthetic dose of sevoflurane is effective in preventing epinephrine-induced arrhythmias after brain death, but phosphorylation of connexin is not involved in the antiarrhythmic property of sevoflurane.

  8. Concentrating partial entanglement by local operations

    NASA Astrophysics Data System (ADS)

    Bennett, Charles H.; Bernstein, Herbert J.; Popescu, Sandu; Schumacher, Benjamin

    1996-04-01

    If two separated observers are supplied with entanglement, in the form of n pairs of particles in identical partly entangled pure states, one member of each pair being given to each observer, they can, by local actions of each observer, concentrate this entanglement into a smaller number of maximally entangled pairs of particles, for example, Einstein-Podolsky-Rosen singlets, similarly shared between the two observers. The concentration process asymptotically conserves entropy of entanglement-the von Neumann entropy of the partial density matrix seen by either observer-with the yield of singlets approaching, for large n, the base-2 entropy of entanglement of the initial partly entangled pure state. Conversely, any pure or mixed entangled state of two systems can be produced by two classically communicating separated observers, drawing on a supply of singlets as their sole source of entanglement.

  9. The anesthetic interaction of propofol and sevoflurane on the minimum alveolar concentration preventing motor movement (MACNM) in dogs.

    PubMed

    Singsank-Coats, Jill; Seddighi, Reza; Rohrbach, Barton W; Cox, Sherry K; Egger, Christine M; Doherty, Thomas J

    2015-04-01

    The objective of this study was to determine the effects of propofol on the minimum alveolar concentration of sevoflurane needed to prevent motor movement (MAC(NM)) in dogs subjected to a noxious stimulus using randomized crossover design. Six, healthy, adult beagles (9.2 ± 1.3 kg) were used. Dogs were anesthetized with sevoflurane on 3 occasions, at weekly intervals, and baseline MAC(NM) (MAC(NM-B)) was determined on each occasion. Propofol treatments were administered as loading dose (LD) and constant rate infusion (CRI) as follows: Treatment 1 (T1) was 2 mg/kg body weight (BW) and 4.5 mg/kg BW per hour; T2 was 4 mg/kg BW and 9 mg/kg BW per hour; T3 was 8 mg/kg BW and 18 mg/kg BW per hour, respectively. Treatment MAC(NM) (MAC(NM-T)) determination was initiated 60 min after the start of the CRI. Two venous blood samples were collected and combined at each MAC(NM-T) determination for measurement of blood propofol concentration using high-performance liquid chromatography method (HPLC). Data were analyzed using a mixed-model ANOVA and are presented as least square means (LSM) ± standard error of means (SEM). Propofol infusions in the range of 4.5 to 18 mg/kg BW per hour resulted in mean blood concentrations between 1.3 and 4.4 μg/mL, and decreased (P < 0.05) sevoflurane MAC(NM) in a concentration-dependent manner. The percentage decrease in MAC(NM) was 20.5%, 43.0%, and 68.3%, with corresponding blood propofol concentrations of 1.3 ± 0.3 μg/mL, 2.5 ± 0.3 μg/mL, and 4.4 ± 0.3 μg/mL, for T1, T2, and T3, respectively. Venous blood propofol concentrations were strongly correlated (r = 0.855, P < 0.0001) with the decrease in MAC(NM). In dogs, propofol decreased the sevoflurane MAC(NM) in a concentration-dependent manner.

  10. Survey of Navy Dental Clinics: Materiel Complaints Regarding Carbide Burs and Local Anesthetics,

    DTIC Science & Technology

    1986-12-01

    Dental Materials and Devices. Revised American Dental Association specification no. 23 for dental excavating burs. JADA 90:459, Feb. 1975. 4. Personal...185. 6. Kaufman, E., Weinstein, P., and Milgrom, P. Difficulties in achieving local anesthesia. JADA 108:205-208, 1984. 7. Personal communication

  11. Calcitonin as an Additive to Local Anesthetic and Steroid Injection Using a Modified Coronoid Approach in Trigeminal Neuralgia.

    PubMed

    Elsheikh, Nabil Ail; Amr, Yasser M

    2016-01-01

    Pharmacotherapy is the main treatment for management of trigeminal neuralgia. However, many patients become refractory to drugs. The present study aimed to evaluate the effect of adding calcitonin to local anesthetic and methylprednisolone using a modified coronoid approach in management of trigeminal neuralgia pain involving the mandibular and/or maxillary branches. Randomized double blind clinical trial. Hospital outpatient setting. Thirty-three patients received maxillary and mandibular blocks by a modified coronoid approach. Patients were allocated into 2 groups. Group 1 received a block with 3 mL of lidocaine 0.5% plus 40 mg of methylprednisolone and another syringe contained 1 mL of 0.9% saline. Group 2 received a block with 3 mL of lidocaine 0.5% plus 40 mg of methylprednisolone and another syringe contained 50 international units of calcitonin. Pain was evaluated by visual analog scale (VAS) before the block (basal), at 2 weeks, one month after the procedure, and monthly for one year. Duration of the effective pain relief of the first block (VAS = 3) was reported. Repeated blockade was allowed for any patient reporting a VAS > 30 mm during one year of follow-up and the number of blocks were reported. Adverse effects were also reported. A significantly longer duration of effective pain relief was noticed in group 2 compared with group 1 (P < 0.0004) while the duration of effective pain relief of the second block in group 1 was 28.5 ± 8.9 weeks. Four patients did not need repeated blocks in group 1 versus 15 in group 2. Six patients received 2 blocks versus 2 patients in each group, respectively. Moreover, 6 patients needed 3 blocks in group1 versus none in group 2. No serious adverse events were reported during or after the interventional procedure. VAS was comparable in both groups (P > 0.05). Small sample size. Calcitonin may be a useful additive to local anesthetic and steroid in management of trigeminal neuralgia. Also, a modified coronoid approach for

  12. The catheter-over-needle assembly facilitates delivery of a second local anesthetic bolus to prolong supraclavicular brachial plexus block without time-consuming catheterization steps: a randomized controlled study.

    PubMed

    Ip, Vivian H Y; Tsui, Ban C H

    2013-07-01

    Single-shot delivery of a supraclavicular brachial plexus block is effective for providing outpatient surgical anesthesia; however, patients generally must use oral analgesics to control pain shortly after discharge from the hospital. Catheterized delivery of supraclavicular blocks can be challenging to perform. We aimed to show that administering a second postoperative bolus of local anesthetic through a catheter placed by a catheter-over-needle assembly not only avoids time-consuming steps but also provides an extended analgesic effect compared with the traditional single-shot approach. Patients were randomized into two groups: one group received a single-shot supraclavicular block with 25-30 mL of local anesthetic (1.5% lidocaine and 0.125% bupivacaine mixture), while the other group received a supraclavicular block via a catheter-over-needle assembly with the same volume and concentration of local anesthetic as for the single-shot block, which was followed by a second bolus of analgesic solution (0.2 % ropivacaine 20 mL) administered postoperatively through the catheter before its removal. The duration between the initial bolus and onset of pain was measured as well as the duration of pain relief from the last bolus. Thirty patients were enrolled and randomized into the single-shot supraclavicular block group (n = 15) and the catheter-over-needle group (n = 15). One patient withdrew from the study, and five patients were lost to follow-up. We observed no significant difference between the two groups in time to perform the blocks. The mean (standard deviation [SD]) times were 3.1 (1.9) min and 4.4 (2.7) min for the top-up group and single-shot group, respectively (single-shot took 1.3 min longer than the catheter-over-needle group; 95% confidence interval [CI]: -0.65 to 3.25; P = 0.17). The mean (SD) duration of analgesia, measured from the beginning of the local anesthetic bolus to the onset of pain requiring rescue analgesia was 617.5 (288) min in the catheter

  13. Continuous Transversus Abdominis Plane Nerve Blocks: Does Varying Local Anesthetic Delivery Method-Automatic Repeated Bolus Versus Continuous Basal Infusion-Influence the Extent of Sensation to Cold?: A Randomized, Triple-Masked, Crossover Study in Volunteers.

    PubMed

    Khatibi, Bahareh; Said, Engy T; Sztain, Jacklynn F; Monahan, Amanda M; Gabriel, Rodney A; Furnish, Timothy J; Tran, Johnathan T; Donohue, Michael C; Ilfeld, Brian M

    2017-04-01

    administration technique (continuous basal versus hourly bolus) when using ropivacaine 0.2% and TAP catheters at 8 mL/h and 24 mL every 3 hours significantly influences the cutaneous effects after 6 hours of administration. Additional research is required to determine whether changing variables (eg, local anesthetic concentration, basal infusion rate, bolus dose volume, and/or interval) would provide different results.

  14. Inferior alveolar nerve block by injection into the pterygomandibular space anterior to the mandibular foramen: radiographic study of local anesthetic spread in the pterygomandibular space.

    PubMed Central

    Okamoto, Y.; Takasugi, Y.; Moriya, K.; Furuya, H.

    2000-01-01

    We studied the spread of local anesthetic solution in the inferior alveolar nerve block by the injection of local anesthetic solution into the pterygomandibular space anterior to the mandibular foramen (anterior technique). Seventeen volunteers were injected with 1.8 mL of a mixture containing lidocaine and contrast medium utilizing the anterior technique. The course of spread was traced by fluoroscopy in the sagittal plane, and the distribution area was evaluated by lateral cephalograms and horizontal computed tomography. The results indicate that the contrast medium mixture spreads rapidly in the pterygomandibular space to the inferior alveolar nerve in the subjects who exhibited inferior alveolar nerve block effect. We concluded that the anesthetic effect due to the anterior technique was produced by the rapid distribution of anesthetic solution in the pterygomandibular space toward the mandibular foramen, and individual differences in the time of onset of analgesia may be due to differences in the histologic perineural tissues. Images Figure 1 Figure 2 Figure 3 PMID:11432178

  15. Effect of Addition of Fentanyl and Clonidine to Local Anesthetic Solution in Peribulbar Block

    PubMed Central

    Nehra, Poonam; Oza, Vrinda; Parmar, Vandana; Fumakiya, Pooja

    2017-01-01

    Objective: To compare the effect of addition of fentanyl and clonidine as adjuvants to bupivacaine and lignocaine in peribulbar block. Methods: The study was conducted on 105 adult patients of either sex, of ASA grade I and II undergoing ophthalmic surgeries. Patients were randomly divided into 3 groups of 35 each. All the patients were given peribulbuar block with 5ml lignocaine 2% +3 ml bupivacaine 0.5% +1 ml hyaluronidase (250 IU). In addition to this 1 ml normal saline was added to Group S, 25 μg fentanyl to Group F and 25 μg clonidine to Group C. Onset and duration of globe and lid akinesia, duration of sensory blockage and analgesia, hemodynamic parameters, number of rescue analgesic and visual analogue score were recorded. Results: The mean time of onset of globe and lid akinesia was significantly faster in group F and group C compared to group S, mean duration of globe and lid akinesia was longer in Group F (207.71 + 13.54 and 143.14 + 7.86 min) and group C (213.52 + 14.52 and 162.06 + 17.1 min) compared to group S (117.78 + 10.42 and 87.64 + 9.76 min). The mean duration of analgesia was significantly longer in group F (217.71 + 12.67) and C (258.82 + 14.50 min) as compared to group S (131.39 + 9.63 min). Conclusion: Addition of fentanyl or clonidine as adjuvant to local anaesthetic in peribulbar block provides faster onset and prolonged analgesia compared to local anaesthetic alone. PMID:28405129

  16. Effect of dexmedetomidine injected into the oral mucosa in combination with lidocaine on local anesthetic potency in humans: a crossover double-blind study.

    PubMed

    Yamane, Ayaka; Higuchi, Hitoshi; Tomoyasu, Yumiko; Ishii-Maruhama, Minako; Maeda, Shigeru; Miyawaki, Takuya

    2015-04-01

    Recently, attention has been paid to dexmedetomidine, a selective α-2 adrenoceptor agonist, as a possible additive for local anesthesia. However, the effect of locally injected dexmedetomidine on the anesthetic action in humans has not fully been clarified. Thus, the purpose of the present study was to evaluate the effect of dexmedetomidine injected into the oral mucosa in combination with lidocaine on local anesthetic potency in humans. Twenty healthy volunteers were included in the present crossover double-blinded study. Lidocaine solution or lidocaine plus dexmedetomidine solution was submucosally injected into the alveolar mucosa in a crossover and double-blinded manner. The local anesthetic effect of the solutions was evaluated by measuring the current perception threshold (CPT) in the oral mucosa for 120 minutes after injection. Furthermore, the sedation level, blood pressure, and heart rate of the volunteers were evaluated. For statistical analysis, the Wilcoxon signed rank test and 2-way repeated measures analysis of variation were used. The CPT was increased with the 2 solutions and peaked 10 minutes after injection. CPT values 10 and 20 minutes after injection of lidocaine plus dexmedetomidine solution were considerably higher than those with lidocaine solution. The duration of an important increase in the CPT after injection with lidocaine plus dexmedetomidine solution was longer than that with lidocaine. Furthermore, the area under the time curve of CPT was considerably higher with lidocaine plus dexmedetomidine solution than with lidocaine solution. No volunteer showed a change in sedation level, blood pressure, or heart rate after injection with either test solution throughout the experiment. The present study showed that a combination of dexmedetomidine plus lidocaine considerably enhances the local anesthetic potency of lidocaine without any major influences on the cardiovascular system when locally injected into the oral mucosa. Copyright © 2015

  17. Oxidative stress, metabolomics profiling, and mechanism of local anesthetic induced cell death in yeast.

    PubMed

    Boone, Cory H T; Grove, Ryan A; Adamcova, Dana; Seravalli, Javier; Adamec, Jiri

    2017-02-03

    The World Health Organization designates lidocaine as an essential medicine in healthcare, greatly increasing the probability of human exposure. Its use has been associated with ROS generation and neurotoxicity. Physiological and metabolomic alterations, and genetics leading to the clinically observed adverse effects have not been temporally characterized. To study alterations that may lead to these undesirable effects, Saccharomyces cerevisiae grown on aerobic carbon sources to stationary phase was assessed over 6h. Exposure of an LC50 dose of lidocaine, increased mitochondrial depolarization and ROS/RNS generation assessed using JC-1, ROS/RNS specific probes, and FACS. Intracellular calcium also increased, assessed by ICP-MS. Measurement of the relative ATP and ADP concentrations indicates an initial 3-fold depletion of ATP suggesting an alteration in the ATP:ADP ratio. At the 6h time point the lidocaine exposed population contained ATP concentrations roughly 85% that of the negative control suggesting the surviving population adapted its metabolic pathways to, at least partially restore cellular bioenergetics. Metabolite analysis indicates an increase of intermediates in the pentose phosphate pathway, the preparatory phase of glycolysis, and NADPH. Oxidative stress produced by lidocaine exposure targets aconitase decreasing its activity with an observed decrease in isocitrate and an increase citrate. Similarly, increases in α-ketoglutarate, malate, and oxaloacetate imply activation of anaplerotic reactions. Antioxidant molecule glutathione and its precursor amino acids, cysteine and glutamate were greatly increased at later time points. Phosphatidylserine externalization suggestive of early phase apoptosis was also observed. Genetic studies using metacaspase null strains showed resistance to lidocaine induced cell death. These data suggest lidocaine induces perpetual mitochondrial depolarization, ROS/RNS generation along with increased glutathione to combat the

  18. Comparative evaluation of effectiveness of intra-pocket anesthetic gel and injected local anesthesia during scaling and root planing - A split-mouth clinical trial.

    PubMed

    Chintala, Kalyan; Kumar, Sandhya Pavan; Murthy, K Raja V

    2017-01-01

    Pain control is an important outcome measure for successful periodontal therapy. Injected local anesthesia has been used to secure anesthesia for scaling and root planing (SRP) and continues to be the anesthetic of choice for pain control. Alternatively, intra-pocket anesthetic gel has been used as an anesthetic during SRP. Hence, this clinical trial was done to compare the effectiveness of intra-pocket anesthetic gel and injected local anesthesia during SRP and also to assess the influence of intra-pocket anesthetic gel on treatment outcomes in chronic periodontitis patients. Fifteen systemically healthy chronic periodontitis patients were recruited. The dental quadrants on right side received either intra-pocket 20% benzocaine gel (Gel group) or infiltration/block by 2% lidocaine with 1:80,000 adrenaline (injection group). Quadrants on the left side received the alternative. Pain perception and patients preference for the type of anesthesia was recorded. Clinical parameters: plaque index, modified gingival index, modified sulcular bleeding index, probing pocket depth, and clinical attachment level were recorded at baseline and 1 month after treatment. No difference was observed in visual analog scale (P > 0.05) and verbal rating scale (P > 0.05) pain perception between gel group and injection group. A slightly increased preference to gel as anesthesia (53% vs. 47%) was observed. The treatment outcome after SRP did not show a significant difference between gel and injection group (P > 0.05). Intra-pocket administration of 20% benzocaine gel may be effective for pain control during SRP and may offer an alternative to conventional injection anesthesia.

  19. β-Cyclodextrin-Propyl Sulfonic Acid Catalysed One-Pot Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles as Local Anesthetic Agents.

    PubMed

    Ran, Yan; Li, Ming; Zhang, Zong-Ze

    2015-11-12

    Some functionalized 1,2,4,5-tetrasubstituted imidazole derivatives were synthesized using a one-pot, four component reaction involving 1,2-diketones, aryl aldehydes, ammonium acetate and substituted aromatic amines. The synthesis has been efficiently carried out in a solvent free medium using β-cyclodextrin-propyl sulfonic acid as a catalyst to afford the target compounds in excellent yields. The local anesthetic effect of these derivatives was assessed in comparison to lidocaine as a standard using a rabbit corneal and mouse tail anesthesia model. The three most potent promising compounds were subjected to a rat sciatic nerve block assay where they showed considerable local anesthetic activity, along with minimal toxicity. Among the tested analogues, 4-(1-benzyl-4,5-diphenyl-1H-imidazol-2-yl)-N,N-dimethylaniline (5g) was identified as most potent analogue with minimal toxicity. It was further characterized by a more favourable therapeutic index than the standard.

  20. 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.

  1. Absolute determination of local tropospheric OH concentrations

    NASA Technical Reports Server (NTRS)

    Armerding, Wolfgang; Comes, Franz-Josef

    1994-01-01

    Long path absorption (LPA) according to Lambert Beer's law is a method to determine absolute concentrations of trace gases such as tropospheric OH. We have developed a LPA instrument which is based on a rapid tuning of the light source which is a frequency doubled dye laser. The laser is tuned across two or three OH absorption features around 308 nm with a scanning speed of 0.07 cm(exp -1)/microsecond and a repetition rate of 1.3 kHz. This high scanning speed greatly reduces the fluctuation of the light intensity caused by the atmosphere. To obtain the required high sensitivity the laser output power is additionally made constant and stabilized by an electro-optical modulator. The present sensitivity is of the order of a few times 10(exp 5) OH per cm(exp 3) for an acquisition time of a minute and an absorption path length of only 1200 meters so that a folding of the optical path in a multireflection cell was possible leading to a lateral dimension of the cell of a few meters. This allows local measurements to be made. Tropospheric measurements have been carried out in 1991 resulting in the determination of OH diurnal variation at specific days in late summer. Comparison with model calculations have been made. Interferences are mainly due to SO2 absorption. The problem of OH self generation in the multireflection cell is of minor extent. This could be shown by using different experimental methods. The minimum-maximum signal to noise ratio is about 8 x 10(exp -4) for a single scan. Due to the small size of the absorption cell the realization of an open air laboratory is possible in which by use of an additional UV light source or by additional fluxes of trace gases the chemistry can be changed under controlled conditions allowing kinetic studies of tropospheric photochemistry to be made in open air.

  2. Absolute determination of local tropospheric OH concentrations

    NASA Technical Reports Server (NTRS)

    Armerding, Wolfgang; Comes, Franz-Josef

    1994-01-01

    Long path absorption (LPA) according to Lambert Beer's law is a method to determine absolute concentrations of trace gases such as tropospheric OH. We have developed a LPA instrument which is based on a rapid tuning of the light source which is a frequency doubled dye laser. The laser is tuned across two or three OH absorption features around 308 nm with a scanning speed of 0.07 cm(exp -1)/microsecond and a repetition rate of 1.3 kHz. This high scanning speed greatly reduces the fluctuation of the light intensity caused by the atmosphere. To obtain the required high sensitivity the laser output power is additionally made constant and stabilized by an electro-optical modulator. The present sensitivity is of the order of a few times 10(exp 5) OH per cm(exp 3) for an acquisition time of a minute and an absorption path length of only 1200 meters so that a folding of the optical path in a multireflection cell was possible leading to a lateral dimension of the cell of a few meters. This allows local measurements to be made. Tropospheric measurements have been carried out in 1991 resulting in the determination of OH diurnal variation at specific days in late summer. Comparison with model calculations have been made. Interferences are mainly due to SO2 absorption. The problem of OH self generation in the multireflection cell is of minor extent. This could be shown by using different experimental methods. The minimum-maximum signal to noise ratio is about 8 x 10(exp -4) for a single scan. Due to the small size of the absorption cell the realization of an open air laboratory is possible in which by use of an additional UV light source or by additional fluxes of trace gases the chemistry can be changed under controlled conditions allowing kinetic studies of tropospheric photochemistry to be made in open air.

  3. Continuous Femoral Nerve Blocks: Varying Local Anesthetic Delivery Method (Bolus versus Basal) to Minimize Quadriceps Motor Block while Maintaining Sensory Block

    PubMed Central

    Charous, Matthew T.; Madison, Sarah J.; Suresh, J.; Sandhu, NavParkash S.; Loland, Vanessa J.; Mariano, Edward R.; Donohue, Michael C.; Dutton, Pascual H.; Ferguson, Eliza J.; Ilfeld, Brian M.

    2011-01-01

    Background Whether the method of local anesthetic administration for continuous femoral nerve blocks —basal infusion versus repeated hourly bolus doses —influences block effects remains unknown. Methods Bilateral femoral perineural catheters were inserted in volunteers (n = 11). Ropivacaine 0.1% was administered through both catheters concurrently: a 6-h continuous 5 ml/h basal infusion on one side and 6 hourly bolus doses on the contralateral side. The primary endpoint was the maximum voluntary isometric contraction (MVIC) of the quadriceps femoris muscle at Hour 6. Secondary end points included quadriceps MVIC at other time points, hip adductor MVIC, and cutaneous sensation 2 cm medial to the distal quadriceps tendon in the 22 h following local anesthetic administration initiation. Results Quadriceps MVIC for limbs receiving 0.1% ropivacaine as a basal infusion declined by a mean (SD) of 84% (19) compared with 83% (24) for limbs receiving 0.1% ropivacaine as repeated bolus doses between baseline and Hour 6 (paired t test P = 0.91). Intrasubject comparisons (left vs. right) reflected a lack of difference as well: the mean basal-bolus difference in quadriceps MVIC at Hour 6 was −1.1% (95% CI −22.0 to 19.8%). The similarity did not reach our a priori threshold for concluding equivalence, which was the 95% CI falling within ± 20%. There were similar minimal differences in the secondary endpoints during local anesthetic administration. Conclusions This study did not find evidence to support the hypothesis that varying the method of local anesthetic administration —basal infusion versus repeated bolus doses —influences continuous femoral nerve block effects to a clinically significant degree. PMID:21394001

  4. Application of carbon nanosorbent for PRiME pass-through cleanup of 10 selected local anesthetic drugs in human plasma samples.

    PubMed

    Ma, Jian-Bo; Zhao, Li-Ming; Rui, Qiu-Hong; Liao, Yu-Feng; Chen, Yan-Min; Xu, Jin; Zhu, Yan; Zhao, Yong-Gang

    2017-04-01

    A novel PRiME (process, robustness, improvements, matrix effects, ease of use) pass-through cleanup procedure has been developed to improve the existing commercially available designs. Carbon nanosorbents, i.e., magnetic modified carboxyl-graphene (Mag-CG) and magnetic modified carboxyl-carbon nanotubes (Mag-CCNTs), have been synthesised and evaluated in PRiME pass-through cleanup procedure for human plasma prior to analysis of 10 selected local anesthetic drugs by liquid chromatography-tandem quadrupole mass spectrometry (LC-MS/MS). The matrix effect, an interesting phenomenon of ion suppression for local anesthetic drugs containing ester group and ion enhancement for other drugs containing acylamino group, has been minimized using carbon nanosorbents PRiME pass-through cleanup procedure. Under the optimal conditions, the obtained results show higher cleanup efficiency of the carbon nanosorbents with recoveries between 70.2% and 126%. Furthermore, the carbon nanosorbents are also evaluated for reuse up to 80-100 times. The limits of quantification (LOQs) for local anesthetic drugs are in the range of 0.024-0.15 μg/L. Validation results on linearity, specificity, accuracy, and precision, as well as the application to the analysis of lidocaine in five patients recruited from the lung cancer demonstrate the applicability to clinical studies.

  5. Comparative evaluation of endodontic pressure syringe, insulin syringe, jiffy tube, and local anesthetic syringe in obturation of primary teeth: An in vitro study

    PubMed Central

    Hiremath, Mallayya C.; Srivastava, Pooja

    2016-01-01

    Purpose: The purpose of this in vitro study was to compare four methods of root canal obturation in primary teeth using conventional radiography. Materials and Methods: A total of 96 root canals of primary molars were prepared and obturated with zinc oxide eugenol. Obturation methods compared were endodontic pressure syringe, insulin syringe, jiffy tube, and local anesthetic syringe. The root canal obturations were evaluated by conventional radiography for the length of obturation and presence of voids. The obtained data were analyzed using Chi-square test. Results: The results showed significant differences between the four groups for the length of obturation (P < 0.05). The endodontic pressure syringe showed the best results (98.5% optimal fillings) and jiffy tube showed the poor results (37.5% optimal fillings) for the length of obturation. The insulin syringe (79.2% optimal fillings) and local anesthetic syringe (66.7% optimal fillings) showed acceptable results for the length of root canal obturation. However, minor voids were present in all the four techniques used. Conclusions: Endodontic pressure syringe produced the best results in terms of length of obturation and controlling paste extrusion from the apical foramen. However, insulin syringe and local anesthetic syringe can be used as effective alternative methods. PMID:27433062

  6. 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

  7. Local Anesthetic Microencapsulation.

    DTIC Science & Technology

    1983-03-18

    Polylactide Availability 2 2. Microencapsulation of Etidocaine-HCl 2 3. Porosimetry Measurements 2 B. Stability of Stored Microcapsules 8 C. In Vivo... Microencapsulation 3 Table 2 Etidocaine-HCl Microcapsules Size Distribution 4 Table 3 Porosimetry Data on Etidocaine-HCl Microcapsules (70% Drug, 106...rapid releasing etidocaine microcapsules can provide long term anesthesia (e.g., 4mg of microencapsulated etidocaine-HCl provided anesthesia after five

  8. Dimethyl sulfoxide with lignocaine versus eutectic mixture of local anesthetics: prospective randomized study to compare the efficacy of cutaneous anesthesia in shock wave lithotripsy.

    PubMed

    Kumar, Santosh; Kumar, Sunil; Ganesamoni, Raguram; Mandal, Arup K; Prasad, Seema; Singh, Shrawan K

    2011-06-01

    The objective of the study was to compare the efficacy of dimethyl sulfoxide (DMSO) mixed with lignocaine and eutectic mixture of local anesthetics (EMLA) cream as topically applied surface anesthetics in relieving pain during shock wave lithotripsy (SWL) in a prospective randomized study. Of the 160 patients, 80 patients received DMSO with lignocaine and 80 patients received EMLA cream, applied to the skin of the flank at the area of entry of shock waves. SWL was done with Seimens lithostar multiline lithotripter. The pain during the procedure was assessed using visual analog and verbal rating scores. The mean visual analog scale scores for the two groups were 3.03 for DMSO group and 4.43 for EMLA group. The difference of pain score on visual analog scale was statistically significant (p < 0.05). Similarly, the pain scores as rated on the verbal rating scale were also evaluated; the mean score on verbal rating scale were 2.34 for DMSO group and 3.00 for the EMLA group. The difference between the pain score on verbal rating scale was also found to be statistically significant (p < 0.05). Our study showed that DMSO with lignocaine is a better local anesthetic agent for SWL than EMLA cream. The stone fragmentation and clearance rates are also better in the DMSO group.

  9. Alterations in monitored vital constants induced by various local anesthetics in combination with different vasoconstrictors in the surgical removal of lower third molars.

    PubMed

    Carrera, I; Mestre, R; Berini, L; Gay-Escoda, C

    2000-01-01

    The purpose of this study was to observe the hemodynamic changes during surgical extraction of lower third molars induced by three local anesthetics solutions associated with different vasoconstrictors. A double-blind observational and longitudinal study was made of 45 healthy adult volunteers subjected to surgical removal of an impacted lower third molar under local anesthesia. Three groups were established (n = 15) according to the anesthetic solution and associated vasoconstrictor administered (4% articaine + epinephrine 1:200,000; 3% mepivacaine without vasoconstrictor; and 3% prilocaine + felypressin 1:1,850,000). Heart rate, systolic and diastolic pressure, and oxygen saturation were recorded at different times before, during and at the end of surgery, along with the type and amount of anesthetic solution administered. The study variables were found to be more stable with articaine + epinephrine 1:200,000, although the three studied solutions caused no significant hemodynamic changes with respect to the basal values when administered in healthy patients subjected to surgical removal of a lower third molar.

  10. (/sup 3/H)Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs

    SciTech Connect

    McNeal, E.T.; Lewandowski, G.A.; Daly, J.W.; Creveling, C.R.

    1985-03-01

    (/sup 3/H)Batrachotoxinin A benzoate ((/sup 3/H)BTX-B) binds with high affinity to sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex. In this preparation, local anesthetics competitively antagonize the binding of (/sup 3/H)BTX-B. The potencies of some 40 classical local anesthetics and a variety of catecholamine, histamine, serotonin, adenosine, GABA, glycine, acetylcholine, and calcium antagonists, tranquilizers, antidepressants, barbiturates, anticonvulsants, steroids, vasodilators, antiinflammatories, anticoagulants, analgesics, and other agents have been determined. An excellent correlation with the known local anesthetic activity of many of these agents indicate that antagonism of binding of (/sup 3/H)BTX-B binding provides a rapid, quantitative, and facile method for the screening and investigation of local anesthetic activity.

  11. Comparative Analysis of Local Anesthesia with 2 Different Concentrations of Adrenaline: A Randomized and Single Blind Study

    PubMed Central

    Managutti, Anil; Prakasam, Michael; Puthanakar, Nagraj; Menat, Shailesh; Shah, Disha; Patel, Harsh

    2015-01-01

    Background: Local anesthetic agents are more commonly used in dentistry to have painless procedure during surgical intervention in bone and soft tissue. There are many local anesthetic agents available with the wide selection of vaso-constrictive agents that improve the clinical efficacy and the duration of local anesthesia. Most commonly lignocaine with adrenaline is used in various concentrations. Systemically adrenaline like drugs can cause a number of cardiovascular disturbances while most are short lived, permanent injury or even death may follow in drug induced ventricular fibrillation, myocardial infarction or cerebro-vascular accidents. This study compared the efficacy and cardiovascular effects with the use of 2% lignocaine with two different concentrations. Materials and Methods: Forty patients underwent extractions of mandibular bilateral teeth using 2% lignocaine with two different concentrations - one with 1:80000 and the other with 1:200000. Results: There was no significant difference in the efficacy and duration with the 2% lignocaine with 2 different concentrations. 2% lignocaine with 1:80000 adrenaline concentration has significantly increased the heart rate and blood pressure especially systolic compared with the lignocaine with 1:200000. Conclusion: Though 2% lignocaine with 1:80000 is widely used in India, 1:200000 adrenaline concentrations do not much affect the cardiovascular parameters. So it is recommended to use 2% lignocaine with 1:200000 for cardiac patients. PMID:25878474

  12. Feasibility of resectoscopic operative hysteroscopy in a UK outpatient clinic using local anesthetic and traditional reusable equipment, with patient experiences and comparative cost analysis.

    PubMed

    Penketh, Richard J A; Bruen, Elizabeth M; White, Judith; Griffiths, Anthony N; Patwardhan, Asmita; Lindsay, Peter; Hill, Sarah; Carolan-Rees, Grace

    2014-01-01

    To assess procedural success, patient acceptability, and cost-saving potential of operative hysteroscopy using conventional equipment and local anesthetic in an outpatient clinic. Feasibility study/service evaluation (Canadian Task Force classification II-3). Outpatient (office) clinic in a large UK teaching hospital. One hundred eighteen women with diagnosed or suspected intrauterine myomas or polyps. Operative hysteroscopy (122 monopolar resection procedures using 8- or 10-mm diameter rigid resectoscopes with glycine solution for uterine irrigation) with the patient under local anesthesia in an outpatient (office) clinic. Procedural success, duration of procedure, pathologic measurements, glycine irrigant deficit, patient pain scores and satisfaction, and comparative costs were recorded. Success of outpatient procedures was 90% (110 of 122 attempted), with a significantly reduced median procedure duration compared with a surgical setting using local (-7 minutes; p = .009) or general (-12.5 minutes; p < .001) anesthetic. Glycine irrigant absorption was low (median deficit, 0 mL), and no deficit was observed in 81% of patients. Mean (SD) estimated disease volume was comparable to that of hysteroscopic resection procedures in a surgical setting (3.38 [5.09] cm(3)), and weight was 1.8 (1.84) g. Patients tolerated the procedure well and reported low pain scores (highest median periprocedure pain measurement was 1.25 of 10), and 7-day follow-up satisfaction responses were positive. Retrospective cost analysis demonstrated that operative resection in an outpatient clinic was less expensive than in a surgical setting using general anesthetic (-$1003) or local anaesthetic (-$234). Reduced staff costs were the primary reason for this saving. Operative hysteroscopic resection of myomas and polyps is feasible and well tolerated by patients in an outpatient/office setting using local anaesthetic and conventional equipment. The outpatient procedure is less expensive and its

  13. Effect of tramadol as an adjuvant to local anesthetics for brachial plexus block: A systematic review and meta-analysis.

    PubMed

    Shin, Hye Won; Ju, Bum Jun; Jang, Yoo Kyung; You, Hae Seun; Kang, Hyun; Park, Ji Yong

    2017-01-01

    Tramadol, a 4-phenyl-piperidine analog of codeine, has a unique action in that it has a central opioidergic, noradrenergic, serotonergic analgesic, and peripheral local anesthetic (LA) effect. Many studies have reported contradictory findings regarding the peripheral analgesic effect of tramadol as an adjuvant to LA in brachial plexus block (BPB). This meta-analysis aimed to evaluate the effects of tramadol as an adjunct to LA in BPB during shoulder or upper extremity surgery. We searched the PubMed, EMBASE, Cochrane, KoreaMed databases, and Google Scholar for eligible randomized controlled trials (RCTs) that compared BPB with LA alone and BPB with LA and tramadol. Primary outcomes were the effects of tramadol as an adjuvant on duration of sensory block, motor block, and analgesia. Secondary outcomes were the effects of tramadol as an adjuvant on time to onset of sensory block and motor block and on adverse effects. We performed the meta-analysis using Review Manager 5.3 software. We identified 16 RCTs with 751 patients. BPB with tramadol prolonged the duration of sensory block (mean difference [MD], -61.5 min; 95% CI, -95.5 to -27.6; P = 0.0004), motor block (MD, -65.6 min; 95% CI, -101.5 to -29.7; P = 0.0003), and analgesia (MD, -125.5 min; 95% CI, -175.8 to -75.3; P < 0.0001) compared with BPB without tramadol. Tramadol also shortened the time to onset of sensory block (MD, 2.1 min; 95% CI, 1.1 to 3.1; P < 0.0001) and motor block (MD, 1.2 min; 95% CI, 0.2 to 2.1; P = 0.010). In subgroup analysis, the duration of sensory block, motor block, and analgesia was prolonged for BPB with tramadol 100 mg (P < 0.05) but not for BPB with tramadol 50 mg. The quality of evidence was high for duration of analgesia according to the GRADE system. Adverse effects were comparable between the studies. In upper extremity surgery performed under BPB, use of tramadol 100 mg as an adjuvant to LA appears to prolong the duration of sensory block, motor block, and analgesia, and shorten

  14. Anesthetic strategy during endovascular therapy: General anesthesia or conscious sedation? (GOLIATH - General or Local Anesthesia in Intra Arterial Therapy) A single-center randomized trial.

    PubMed

    Simonsen, Claus Z; Sørensen, Leif H; Juul, Niels; Johnsen, Søren P; Yoo, Albert J; Andersen, Grethe; Rasmussen, Mads

    2016-12-01

    Endovascular therapy after acute ischemic stroke due to large vessel occlusion is now standard of care. There is equipoise as to what kind of anesthesia patients should receive during the procedure. Observational studies suggest that general anesthesia is associated with worse outcomes compared to conscious sedation. However, the findings may have been biased. Randomized clinical trials are needed to determine whether the choice of anesthesia may influence outcome. The objective of GOLIATH (General or Local Anestesia in Intra Arterial Therapy) is to examine whether the choice of anesthetic regime during endovascular therapy for acute ischemic stroke influence patient outcome. Our hypothesis is that that conscious sedation is associated with less infarct growth and better functional outcome. GOLIATH is an investigator-initiated, single-center, randomized study. Patients with acute ischemic stroke, scheduled for endovascular therapy, are randomized to receive either general anesthesia or conscious sedation. The primary outcome measure is infarct growth after 48-72 h (determined by serial diffusion-weighted magnetic resonance imaging). Secondary outcomes include 90-day modified Rankin Scale score, time parameters, blood pressure variables, use of vasopressors, procedural and anesthetic complications, success of revascularization, radiation dose, and amount of contrast media. Choice of anesthesia may influence outcome in acute ischemic stroke patients undergoing endovascular therapy. The results from this study may guide future decisions regarding the optimal anesthetic regime for endovascular therapy. In addition, this study may provide preliminary data for a multicenter randomized trial. © 2016 World Stroke Organization.

  15. Mirrored bilateral slow-wave cortical activity within local circuits revealed by fast bihemispheric voltage-sensitive dye imaging in anesthetized and awake mice.

    PubMed

    Mohajerani, Majid H; McVea, David A; Fingas, Matthew; Murphy, Timothy H

    2010-03-10

    Spontaneous slow-wave oscillations of neuronal membrane potential occur about once every second in the rodent cortex and may serve to shape the efficacy of evoked neuronal responses and consolidate memory during sleep. However, whether these oscillations reflect the entrainment of all cortical regions via propagating waves or whether they exhibit regional and temporal heterogeneity that reflects processing in local cortical circuits is unknown. Using voltage-sensitive dye (VSD) imaging within an adult C57BL/6J mouse cross-midline large craniotomy preparation, we recorded this depolarizing activity across most of both cortical hemispheres simultaneously in both anesthetized and quiet awake animals. Spontaneous oscillations in the VSD signal were highly synchronized between hemispheres, and acallosal I/LnJ mice indicated that synchrony depended on the corpus callosum. In both anesthetized and awake mice (recovered from anesthesia), the oscillations were not necessarily global changes in activity state but were made up of complex local patterns characterized by multiple discrete peaks that were unevenly distributed across cortex. Although the local patterns of depolarizing activity were complex and changed over tens of milliseconds, they were faithfully mirrored in both hemispheres in mice with an intact corpus callosum, to perhaps ensure parallel modification of related circuits in both hemispheres. We conclude that within global rhythms of spontaneous activity are complex events that reflect orchestrated processing within local cortical circuits.

  16. Blood glucose determination in normal and alloxan-diabetic rats after administration of local anesthetics containing vasoconstrictors.

    PubMed

    Esmerino, L A; Ranali, J; Rodrigues, A L

    1998-01-01

    Normal and alloxan-diabetic rats were injected submucously in the posterior region of the upper jaw with bupivacaine (1.28 mg/kg) containing adrenaline (0.0012 mg/kg), or lignocaine (5.14 mg/kg) containing noradrenaline (0.005 mg/kg). Blood glucose was determined at zero (before administration), 0.5, 1, 2, 3 and 4 hours after the administration of the anesthetics. Statistical analysis (ANOVA and Tukey's test, P < 0.05) showed significant differences between treatments at 1 hour in normal rats. Bupivacaine with adrenaline induced a significantly greater blood glucose level than lignocaine with noradrenaline. The effect was significant but of short duration. In alloxan-diabetic rats, anesthetics containing adrenaline or noradrenaline did not induce increased blood glucose levels.

  17. Opioids added to local anesthetics for single-shot intrathecal anesthesia in patients undergoing minor surgery: a meta-analysis of randomized trials.

    PubMed

    Pöpping, Daniel M; Elia, Nadia; Marret, Emmanuel; Wenk, Manuel; Tramèr, Martin R

    2012-04-01

    Opioids are widely used as additives to local anesthetics for intrathecal anesthesia. Benefit and risk remain unclear. We systematically searched databases and bibliographies to February 2011 for full reports of randomized comparisons of any opioid added to any intrathecal local anesthetic with the local anesthetic alone in adults undergoing surgery (except cesarean section) and receiving single-shot intrathecal anesthesia without general anesthesia. We included 65 trials (3338 patients, 1932 of whom received opioids) published between 1983 and 2010. Morphine (0.05-2mg) and fentanyl (10-50 μg) added to bupivacaine were the most frequently tested. Duration of postoperative analgesia was prolonged with morphine (weighted mean difference 503 min; 95% confidence interval [CI] 315 to 641) and fentanyl (weighted mean difference 114 min; 95% CI 60 to 168). Morphine decreased the number of patients needing opioid analgesia after surgery and decreased pain intensity to the 12th postoperative hour. Morphine increased the risk of nausea (number needed to harm [NNH] 9.9), vomiting (NNH 10), urinary retention (NNH 6.5), and pruritus (NNH 4.4). Fentanyl increased the risk of pruritus (NNH 3.3). With morphine 0.05 to 0.5mg, the NNH for respiratory depression varied between 38 and 59 depending on the definition of respiratory depression chosen. With fentanyl 10 to 40 μg, the risk of respiratory depression was not significantly increased. For none of these effects, beneficial or harmful, was there evidence of dose-responsiveness. Consequently, minimal effective doses of intrathecal morphine and fentanyl should be sought. For intrathecal buprenorphine, diamorphine, hydromorphone, meperidine, methadone, pentazocine, sufentanil, and tramadol, there were not enough data to allow for meaningful conclusions.

  18. A novel approach to scavenging anesthetic gases in rodent surgery.

    PubMed

    Nesbitt, Jeffrey C; Krageschmidt, Dale A; Blanco, Michael C

    2013-01-01

    Laboratory animal procedures using gas anesthetics may amass elevated waste gas concentrations in operating rooms if controls are not implemented for capturing and removing the vapors. Area sampling using an infrared analyzer indicated isoflurane concentrations likely to exceed occupational exposure guidelines. Our study showed environmental concentrations of oxygen as high as 40% and isoflurane concentrations >100 ppm when no controls or merely passive controls were utilized. These extraneous isoflurane emissions were determined to be originating from the pre-procedural induction process as well as the gas delivery nose cone. A novel waste gas collection cylinder was designed to enclose the gas delivery nose cone and animal head during the administration of anesthetic gases. The vented cylinder utilized a house vacuum to remove the waste anesthetic gases from the surgical field. A commercially available induction chamber designed to be actively and externally exhausted was used to lower concentrations during the induction process. With implementation of local exhaust ventilation controls, waste anesthetic gas concentrations decreased to below recommended occupational exposure levels. In vitro (sham) testing compared favorably to in vivo measurements validating the reduction capability of active ventilation during rodent anesthetic administration. In vivo isoflurane reductions for the induction chamber emissions, the operating room, and the surgeon's breathing zone were 95%, 60%, and 53%, respectively. The same measurements for an in vitro procedure were 98%, 84%, and 87%, respectively.

  19. Perioperative pain management after fibular free flap harvesting for head-and-neck reconstruction using mini-catheters to inject local anesthetic: A pilot study.

    PubMed

    Ferri, Andrea; Varazzani, Andrea; Valente, Adriana; Pedrazzi, Giuseppe; Bianchi, Bernardo; Ferrari, Silvano; Sesenna, Enrico

    2017-06-24

    Fibular donor site pain management in the early postoperative period can help minimize complications, patient discomfort, and agitation. Traditional management of postoperative pain consists of systemic administration of opioids and NSAIDS. The use of local anesthetics in addition to systemic analgesics has the potential to improve pain control. Purpose of the study is to evaluate the efficacy of mini-catheters used to inject local anesthetic into the fibular donor site after flap harvesting for reconstruction of the head-and-neck area. Prospective study on 31 patients (mean age 52 years) treated for head and neck reconstruction with fibula free flap using minicatheter for local anesthetic injection in the early postoperative time. A bolus of chirochaine (0.125% w/v; 20 mL) was injected through the catheter before the patient regained consciousness. Postoperatively, three consecutive injections (20 mL each) were administered 8, 16, and 24 h after surgery. Pain evaluation before and after local anesthetic injection is used to assess efficacy and overall pain control. No major or minor complication occurred. Mean pain value was 1.69. At 8 h, the pain scores before injection ranged from 0 to 10 (mean 4.13 ± 3.06). After injection, the pain scores ranged from 0 to 5 (mean 1 ± 1.34). Similarly, at 16 h, the pain scores ranged from 0 to 8 (mean 2.77 ± 2.42) before injection and from 0 to 6 (mean 0.42 ± 1.2) thereafter. At 24 h, the initial pain score ranged from 0 to 6 (mean 1.71 ± 1.74) and from 0 to 1 (mean 0.1 ± 0.3) after drug administration. Pre and postinjection pain scores differences were statistically significant after all three injections (P < .001). Minicatheter seems to be easy, safe, and efficient when used to control pain after fibular free-flap harvesting. © 2017 Wiley Periodicals, Inc.

  20. Effects of Methadone on the Minimum Anesthetic Concentration of Isoflurane, and Its Effects on Heart Rate, Blood Pressure and Ventilation during Isoflurane Anesthesia in Hens (Gallus gallus domesticus).

    PubMed

    Escobar, André; da Rocha, Rozana Wendler; Pypendop, Bruno Henri; Zangirolami Filho, Darcio; Sousa, Samuel Santos; Valadão, Carlos Augusto Araújo

    2016-01-01

    The aim of this study was to measure the temporal effects of intramuscular methadone administration on the minimum anesthetic concentration (MAC) of isoflurane in hens, and to evaluate the effects of the isoflurane-methadone combination on heart rate and rhythm, blood pressure and ventilation. Thirteen healthy adult hens weighing 1.7 ± 0.2 kg were used. The MAC of isoflurane was determined in each individual using the bracketing method. Subsequently, the reduction in isoflurane MAC produced by methadone (3 or 6 mg kg(-1), i.m.) was determined by the up-and-down method. Stimulation was applied at 15 and 30 minutes, and at 45 minutes if the bird had not moved at 30 minutes. Isoflurane MAC reduction was calculated at each time point using logistic regression. After a washout period, birds were anesthetized with isoflurane and methadone, 6 mg kg(-1) i.m. was administered. Heart rate and rhythm, respiratory rate, blood gas values and invasive blood pressure were measured at 1.0 and 0.7 isoflurane MAC, and during 45 minutes after administration of methadone once birds were anesthetized with 0.7 isoflurane MAC. Fifteen minutes after administration of 3 mg kg(-1) of methadone, isoflurane MAC was reduced by 2 (-9 to 13)% [logistic regression estimate (95% Wald confidence interval)]. Administration of 6 mg kg(-1) of methadone decreased isoflurane MAC by 29 (11 to 46)%, 27 (-3 to 56)% and 10 (-8 to 28)% after 15, 30 and 45 minutes, respectively. Methadone (6 mg kg(-1)) induced atrioventricular block in three animals and ventricular premature contractions in two. Methadone caused an increase in arterial blood pressure and arterial partial pressure of carbon dioxide, while heart rate and pH decreased. Methadone, 6 mg kg(-1) i.m. significantly reduced isoflurane MAC by 30% in hens 15 minutes after administration. At this dose, methadone caused mild respiratory acidosis and increase in systemic blood pressure.

  1. Effects of Methadone on the Minimum Anesthetic Concentration of Isoflurane, and Its Effects on Heart Rate, Blood Pressure and Ventilation during Isoflurane Anesthesia in Hens (Gallus gallus domesticus)

    PubMed Central

    Pypendop, Bruno Henri; Zangirolami Filho, Darcio; Sousa, Samuel Santos; Valadão, Carlos Augusto Araújo

    2016-01-01

    The aim of this study was to measure the temporal effects of intramuscular methadone administration on the minimum anesthetic concentration (MAC) of isoflurane in hens, and to evaluate the effects of the isoflurane-methadone combination on heart rate and rhythm, blood pressure and ventilation. Thirteen healthy adult hens weighing 1.7 ± 0.2 kg were used. The MAC of isoflurane was determined in each individual using the bracketing method. Subsequently, the reduction in isoflurane MAC produced by methadone (3 or 6 mg kg-1, IM) was determined by the up-and-down method. Stimulation was applied at 15 and 30 minutes, and at 45 minutes if the bird had not moved at 30 minutes. Isoflurane MAC reduction was calculated at each time point using logistic regression. After a washout period, birds were anesthetized with isoflurane and methadone, 6 mg kg-1 IM was administered. Heart rate and rhythm, respiratory rate, blood gas values and invasive blood pressure were measured at 1.0 and 0.7 isoflurane MAC, and during 45 minutes after administration of methadone once birds were anesthetized with 0.7 isoflurane MAC. Fifteen minutes after administration of 3 mg kg-1 of methadone, isoflurane MAC was reduced by 2 (-9 to 13)% [logistic regression estimate (95% Wald confidence interval)]. Administration of 6 mg kg-1 of methadone decreased isoflurane MAC by 29 (11 to 46)%, 27 (-3 to 56)% and 10 (-8 to 28)% after 15, 30 and 45 minutes, respectively. Methadone (6 mg kg-1) induced atrioventricular block in three animals and ventricular premature contractions in two. Methadone caused an increase in arterial blood pressure and arterial partial pressure of carbon dioxide, while heart rate and pH decreased. Methadone, 6 mg kg-1 IM significantly reduced isoflurane MAC by 30% in hens 15 minutes after administration. At this dose, methadone caused mild respiratory acidosis and increase in systemic blood pressure. PMID:27018890

  2. Comparison of local anesthetic efficacy of tramadol hydrochloride (with adrenaline) versus plain tramadol hydrochloride in the extraction of upper molar teeth.

    PubMed

    Al-Haideri, Yahya A A

    2013-12-01

    To evaluate the efficacy of local anesthesia using tramadol hydrochloride (HCl) with versus without adrenaline in the extraction of upper molar teeth. This was a double-blinded study that included 100 patients who required extraction of 1 upper molar by the conventional method and were allocated randomly into 1 of 2 groups: in group A (n = 50), each patient received an initial dose of drug A (tramadol HCl 50 mg and adrenalin 0.0225 mg diluted to 1.8 mL by distilled water); in group B (n = 50), each patient received an initial dose of drug B (tramadol HCl 50 mg diluted to 1.8 mL by distilled water). Degree of pain during tooth extraction, duration of surgery, and total number of cartridges used were recorded intraoperatively. Postoperatively, patients were instructed to record any adverse effects, such as nausea or vomiting, on the first day of the operation. There were significant differences in the number of cartridges used and the degree of intraoperative pain. However, there was no significant difference in duration of surgery or side effects. The results of this study suggest that tramadol HCl in combination with adrenaline can be used as an alternative local anesthetic in oral and maxillofacial surgery when, for some unusual reason, a patient cannot receive a conventional local anesthetic. Copyright © 2013 American Association of Oral and Maxillofacial Surgeons. Published by Elsevier Inc. All rights reserved.

  3. Low flow oxygen therapy from a portable oxygen concentrator or an oxygen cylinder effectively treats hypoxemia in anesthetized white-tailed deer (Odocoileus virginianus).

    PubMed

    Fahlman, Asa; Caulkett, Nigel; Woodbury, Murray; Duke-Novakovski, Tanya; Wourms, Vincent

    2014-06-01

    For treatment of hypoxemia, delivery of the minimum effective oxygen flow rate is advantageous during field anesthesia because it prolongs the life of the oxygen cylinder. Portable oxygen concentrators as the oxygen source require less logistical considerations than cylinders and are a safer alternative during helicopter field work because they are nonexplosive devices. The objective of this study was to evaluate low oxygen flow rates by continuous or pulsed intranasal delivery for treatment of hypoxemia in anesthetized white-tailed deer (Odocoileus virginianus). Nine captive adult female deer (body mass 56-72 kg) were physically restrained in a drop-floor chute and hand injected intramuscularly with medetomidine (0.1-0.14 mg/kg) and ketamine (2.5-4.3 mg/kg). Intranasal oxygen was delivered from an oxygen cylinder at continuous flow rates of 1 and 2 L/min or from a battery driven oxygen concentrator (EverGo Portable Oxygen Concentrator, Respironics) with pulse-dose delivery (maximum capacity of 1.05 L/min). The pulse-dose setting (pulse volume 12-70 ml) was adjusted according to the respiratory rate. Arterial blood gases were analyzed before, during, and after O2 supplementation. A 10-min washout period was allowed between treatment groups. All three treatments adequately treated hypoxemia. The partial pressure of arterial oxygenation increased significantly from baseline values of 55 +/- 10 to 115 +/- 31 mm Hg during supplementation from the oxygen concentrator, to 138 +/- 21 mm Hg during supplementation from the oxygen cylinder at 1 L/min, and to 201 +/- 42 mm Hg at 2 L/min. In conclusion, low flow rates of intranasal oxygen supplemented continuously from an oxygen cylinder or by pulsed delivery from a portable oxygen concentrator effectively treated hypoxemia in anesthetized white-tailed deer.

  4. Improving entanglement concentration of Gaussian states by local displacements

    SciTech Connect

    Fiurasek, Jaromir

    2011-07-15

    We investigate entanglement concentration of continuous-variable Gaussian states by local single-photon subtractions combined with local Gaussian operations. We first analyze the local squeezing-enhanced entanglement-concentration protocol proposed very recently by Zhang and van Loock [arXiv:1103.4500] and discuss the mechanism by which local squeezing before photon subtraction helps to increase the entanglement of the output state of the protocol. We next show that a similar entanglement improvement can be achieved by using local coherent displacements instead of single-mode squeezing.

  5. Prediction of movement following noxious stimulation during 1 minimum alveolar anesthetic concentration isoflurane/nitrous oxide anesthesia by means of middle latency auditory evoked responses.

    PubMed

    Leistritz, L; Kochs, E; Galicki, M; Witte, H

    2002-06-01

    This paper investigates the applicability of generalized dynamic neural networks for the design of a two-valued anesthetic depth indicator during isoflurane/nitrous oxide anesthesia. The indicator construction is based on the processing of middle latency auditory evoked responses (MLAER) in combination with the observation of the patient's movement reaction to skin incision. The framework of generalized dynamic neural networks does not require any data preprocessing, visual data inspection or subjective feature extraction. The study is based on a data set of 106 patients scheduled for elective surgery under isoflurane/nitrous oxide anesthesia. The processing of the measured MLAER is performed by a recurrent neural network that transforms the MLAER signals into signals having a very uncomplex structure. The evaluation of these signals is self-evident, and yields to a simple threshold classifier. Using only evoked potentials before the pain stimulus, the patient's reaction could be predicted with a probability of 81.5%. The MLAER is closely associated to the patient's reaction to skin incision following noxious stimulation during 1 minimum alveolar anesthetic concentration isoflurane/nitrous oxide anesthesia. In combination with other parameters, MLAER could contribute to an objective and trustworthy movement prediction to noxious stimulation.

  6. Effect of mepivacaine in an infraorbital nerve block on minimum alveolar concentration of isoflurane in clinically normal anesthetized dogs undergoing a modified form of dental dolorimetry.

    PubMed

    Snyder, Christopher J; Snyder, Lindsey B C

    2013-01-15

    To evaluate the effects of a routinely used infraorbital nerve block, performed for dental procedures, on the anesthetic requirement for isoflurane in dogs. Prospective controlled study. 8 healthy adult Beagles. Dogs were anesthetized with isoflurane, and the minimum alveolar concentration (MAC) of isoflurane was established. A modification of a well-established method of stimulating the dental pulp, dental dolorimetry, was used to deliver a noxious stimulus (electrical stimulation) for isoflurane MAC determination. Once the isoflurane MAC was established, an infraorbital nerve block was performed with mepivacaine. The isoflurane MAC was then determined with the addition of the nerve block. Measurements of heart rate and mean arterial blood pressure were obtained at specified time points (baseline and prevention and elicitation of purposeful movement) during the determination of MAC and in response to the noxious stimulus. The mean ± SD isoflurane MAC without an infraorbital nerve block was 1.12 ± 0.13%. Isoflurane MAC with the regional mepivacaine anesthesia was 0.86 ± 0.11%. A significant reduction in isoflurane MAC (23%) was seen after the infraorbital nerve block, compared with results before the nerve block. With the exception of baseline measurements, no significant differences were found between treatments (isoflurane alone vs isoflurane with regional mepivacaine anesthesia) in heart rate or mean arterial blood pressure before or after the noxious stimulus. The significant reduction in MAC of isoflurane supported the practice of the addition of regional anesthesia for painful dental procedures to reduce the dose-dependent cardiorespiratory effects of general anesthesia.

  7. 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.

  8. Vasoconstrictors in local anesthesia for dentistry.

    PubMed

    Sisk, A L

    1992-01-01

    Addition of a vasoconstrictor to a local anesthetic may have several beneficial effects: a decrease in the peak plasma concentration of the local anesthetic agent, increase in the duration and the quality of anesthesia, reduction of the minimum concentration of anesthetic needed for nerve block, and decrease of blood loss during surgical procedures. The addition of a vasoconstrictor to a local anesthetic may also have detrimental effects. A review of the literature indicates that vasoconstrictor concentrations in local anesthetics marketed for dental use in the United States are not always optimal to achieve the purposes for which they are added. In most cases, a reduced concentration of vasoconstrictor could achieve the same goal as the marketed higher concentration, with less side-effect liability.

  9. Vasoconstrictors in local anesthesia for dentistry.

    PubMed Central

    Sisk, A. L.

    1992-01-01

    Addition of a vasoconstrictor to a local anesthetic may have several beneficial effects: a decrease in the peak plasma concentration of the local anesthetic agent, increase in the duration and the quality of anesthesia, reduction of the minimum concentration of anesthetic needed for nerve block, and decrease of blood loss during surgical procedures. The addition of a vasoconstrictor to a local anesthetic may also have detrimental effects. A review of the literature indicates that vasoconstrictor concentrations in local anesthetics marketed for dental use in the United States are not always optimal to achieve the purposes for which they are added. In most cases, a reduced concentration of vasoconstrictor could achieve the same goal as the marketed higher concentration, with less side-effect liability. PMID:8250339

  10. Optically measured NADH concentrations are unaffected by propofol induced EEG silence during transient cerebral hypoperfusion in anesthetized rabbits.

    PubMed

    Wang, Mei; Agarwal, Sachin; Mayevsky, Avraham; Joshi, Shailendra

    2011-06-17

    The neuroprotective benefit of intra-operative anesthetics is widely described and routinely aimed to invoke electroencephalographic (EEG) silence in anticipation of transient cerebral ischemia. Previous rat survival studies have questioned an additional benefit from achieving EEG silence during transient global cerebral hypoperfusion. Surgical preparation on twelve New Zealand white rabbits under ketamine-propofol anesthesia, included placement of skull screws for bilateral EEG monitoring, skull shaving for laser Doppler probes, and a 5 mm diameter right temporal craniotomy for the NADH probe. Transient global cerebral hypoperfusion was achieved with bilateral internal carotid artery occlusion and pharmacologically induced systemic hypotension. All animals acted as controls, and had cerebral hypoperfusion under baseline propofol anesthesia with an active EEG. Thereafter, animals were randomized to receive bolus injection of intracarotid (3-5 mg) or intravenous (10-20 mg) 1% propofol to create EEG silence for 1-2 min. The data collected at baseline, peak hypoperfusion, and 5 and 10 min post hypoperfusion was analyzed by repeated measures ANOVA with post hoc Bonferroni-Dunn test. Eleven of the twelve rabbits completed the protocol. Hemodynamics and cerebral blood flow changes were comparable in all the animals. Compared to controls, the increase in NADH during ischemia was unaffected by EEG silence with either intravenous or intraarterial propofol. We failed to observe any significant additional attenuation of the elevation in NADH levels with propofol induced EEG silence during transient global cerebral hypoperfusion. This is consistent with previous rat survival studies showing that EEG silence was not required for full neuroprotective effects of pentothal anesthesia. Copyright © 2011 Elsevier B.V. All rights reserved.

  11. Holter ECG assessment of the effects of three different local anesthetic solutions on cardiovascular system in the sedated dental patients with coronary artery disease.

    PubMed

    Zeytinoğlu, Mert; Tuncay, Ümit; Akay, M Cemal; Soydan, İnan

    2013-08-01

    The purpose of the study is to compare the effects of lidocaine alone, epinephrine-combined lidocaine and prilocaine with octapressin on the cardiovascular system during minor oral surgery of sedated cardiac dental patients under local anesthesia. Connected to a Holter electrocardiogram (ECG) monitor for a total of 5 hours starting 1 hour before the procedure, twenty patients with high risk of coronary artery disease were included in the prospective cohort study. All the patients had three operations at 3 different appointments with at least one-week intervals and each operation was performed under local anesthesia achieved by 3.6 mL of 3% prilocaine with octapressin, 3.6 mL of 2% lidocaine with 1:80.000 epinephrine and 3.6 mL of 2% lidocaine without a vasoconstrictor. Data of the Holter ECG device assessed at the end of every hour and evaluated statistically. Repeated measures ANOVA, Friedman test, and Wilcoxon signed ranks test were used to perform statistical analysis. Heart-rate showed significant differences between lidocaine with epinephrine and pure lidocaine in an hour following the injection (p<0.05 for all). Cardiac rhythm showed significant differences between prilocaine with octapressin and pure lidocaine at the second hour after its administration (p<0.05 for all). There were no significant differences between 3 local anesthetics in terms of ST segment deviation. In minor oral operation on the sedated patients with cardiac disease, the use of 3.6 mL or a less amount of local anesthetic injection containing epinephrine appears to be a predictable and safe method.

  12. [Studies on local anesthetics. Part 183: micellization and thermodynamic parameters of heptacainium chloride in the solution of potassium bromide].

    PubMed

    Andriamainty, F; Cizmárik, J; Malík, I; Horvat, S

    2008-06-01

    The critical micellar concentration (CMC) of the local anaesthetic agent heptacainium chloride in the solution of KBr was determined by the spectrophotometric method in the UV region of the spectrum at the temperature range of t = 20-40 degrees C and pH = 4.5-5.0. The dependence of CMC on the temperature T turned out forming the U-shape with the minimum at the temperature of t = 25 degrees C. The parabolic dependence of CMC on the temperature T was drawn by the fitting of the values using the polynomial function and the so-called power law equation. The CMC dependence on the temperature T was fitted by the second degree polynomial function. The obtained parabolic equations were applied to the "phase separation model", so the following thermodynamic parameters could be calculated: standard Gibbs free energy (deltaG), enthalpy (deltaH degrees), and entropy (deltaS degrees). The thermodynamic parameters were further used to determine the so-called entropy-enthalpy compensation of the systems under study. The compensation temperature was in the following range: (301 +/- 1-303 +/- 3)K. Then the temperature dependence of the enthalpy (deltaH degrees) and entropy (-TdeltaS degrees) contributions to the standard Gibbs free energy (deltaG degrees) for all prepared concentrations of the compound were calculated.

  13. [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.

  14. Does the Application of Heat Gel Pack After Eutectic Mixture of Local Anesthetic Cream Improve Venipuncture or Intravenous Cannulation Success Rate in Children? A Randomized Control Trial.

    PubMed

    Schreiber, Silvana; Cozzi, Giorgio; Patti, Giuseppa; Taddio, Andrea; Montico, Marcella; Pierobon, Chiara; Barbi, Egidio

    2017-07-17

    Needle-related procedures are the most common sources of pain for children in the hospital setting. The most used topical anesthetic, eutectic mixture of local anesthetic (EMLA) cream, may cause transient vasoconstriction. It has been postulated that this vasoconstriction may decrease vein visualization. The application of heat gel pack after removal of EMLA cream in the site of venipuncture counteracts the vasoconstriction, improving vein visualization. We assessed using a prospective randomized controlled trial whether the application of heat gel pack increases the needle procedure success rate. The primary study outcome was procedural success rate at the first attempt. The study enrolled 400 children, 200 of whom applied heat gel pack after removing EMLA (treatment group) and 200 did not (control group). Procedural success rate at the first attempt, vein perception before procedure, procedural pain, and adverse events were recorded in both groups. Eighty-eight percent of the procedures were successful at the first attempt in the treatment group and 89% in the control group (P = 0.876). Vein perception was not significantly different in the 2 groups (P = 0.081). Pain score after the procedure was similar in the 2 groups. This study shows that the application of heat gel pack after removal of EMLA cream does not improve venipuncture or intravenous cannulation success rate.

  15. A Review of Local Anesthetic Systemic Toxicity Cases Since Publication of the American Society of Regional Anesthesia Recommendations: To Whom It May Concern.

    PubMed

    Vasques, Francesco; Behr, Astrid U; Weinberg, Guy; Ori, Carlo; Di Gregorio, Guido

    2015-01-01

    Local anesthetic systemic toxicity (LAST) occurrence may cross several medical specialties. In 2010, the American Society of Regional Anesthesia and Pain Medicine (ASRA) published the first algorithm on LAST management, introducing the use of lipid emulsion (ILE) treatment. In the present study, we retrieved the cases of LAST published between ASRA guidelines dissemination and March 2014. We analyzed the reported clinical manifestations of LAST, characteristics of affected patients, onset time of toxicity, and clinical setting. We also focused on the treatment measures that were applied in the different cases, especially on the use of ILE and adherence to ASRA recommendations. Despite the limits of a review of case reports, the present study calls attention to the insidious nature of LAST, especially its atypical manifestations, and shows that ILE may currently be underadministered in daily clinical practice, especially in nonanesthesiology practice.

  16. Comparison of orbital muscle akinesia caused by rocuronium versus hyaluronidase mixed to the local anesthetic in single injection peribulbar block for cataract surgery

    PubMed Central

    Messeha, Medhat M.; Elhesy, Abd-Elmonem

    2015-01-01

    Background: The aim of this study was to compare orbital muscle akinesia caused by rocuronium versus hyaluronidase when mixed with the local anesthetic in single-injection peribulbar anesthesia (PBA). Patients and Methods: Sixty patients were included in the study and subjected to cataract extraction using phacoemulsification technique with intraocular lens implantation. Group I received peribulbar block with 5 ml mixture of 30 IU/ml hyaluronidase and 2% lidocaine. Group II received peribulbar block with 5 ml mixture of rocuronium 5 mg and 2% lidocaine. The onset and duration of akinesia were assessed; the akinesia score at 2, 5, and 10 min was measured after injection. The need for supplementary injection was also recorded. Results and Conclusion: PBA using a mixture of rocuronium and lidocaine provides optimal globe akinesia and faster establishment of suitable conditions to start eye surgery and shortens the block onset time as compared with the addition of hyaluronidase to lidocaine. PMID:26712977

  17. Effects of local anesthetic on the time between analgesic boluses and the duration of labor in patient-controlled epidural analgesia: prospective study of two ultra-low dose regimens of ropivacaine and sufentanil.

    PubMed

    Costa-Martins, José Manuel; Dias, Cláudia Camila; Pereira, Marco; Tavares, Jorge

    2015-01-01

    Patient-controlled epidural analgesia with low concentrations of anesthetics is effective in reducing labor pain. The aim of this study was to assess and compare two ultra-low dose regimens of ropivacaine and sufentanil (0.1% ropivacaine plus 0.5 μg.ml-1 sufentanil vs. 0.06% ropivacaine plus 0.5 μg.ml-1 sufentanil) on the intervals between boluses and the duration of labor. In this non-randomized prospective study, conducted between January and July 2010, two groups of parturients received patient-controlled epidural analgesia: Group I (n = 58; 1 mg.ml-1 ropivacaine + 0.5 μg.ml-1 sufentanil) and Group II (n = 57; 0.6 mg.ml-1 ropivacaine + 0.5 μg.ml-1 sufentanil). Rescue doses of ropivacaine at the concentration of the assigned group without sufentanil were administered as necessary. Pain, local anesthetic requirements, neuraxial blockade characteristics, labor and neonatal outcomes, and maternal satisfaction were recorded. The ropivacaine dose was greater in Group I (9.5 [7.7-12.7] mg.h-1 vs. 6.1 [5.1-9.8 mg.h-1], p < 0.001). A time increase between each bolus was observed in Group I (beta = 32.61 min, 95% CI [25.39; 39.82], p < 0.001), whereas a time decrease was observed in Group II (beta = -1.40 min, 95% CI [-2.44; -0.36], p = 0.009). The duration of the second stage of labor in Group I was significantly longer than that in Group II (78 min vs. 65 min, p < 0.001). Parturients receiving 0.06% ropivacaine exhibited less evidence of cumulative effects and exhibited faster second stage progression than those who received 0.1% ropivacaine.

  18. Anesthetic action of volatile anesthetics by using Paramecium as a model.

    PubMed

    Zhou, Miaomiao; Xia, Huimin; Xu, Younian; Xin, Naixing; Liu, Jiao; Zhang, Shihai

    2012-06-01

    Although empirically well understood in their clinical administration, volatile anesthetics are not yet well comprehended in their mechanism studies. A major conundrum emerging from these studies is that there is no validated model to assess the presumed candidate sites of the anesthetics. We undertook this study to test the hypothesis that the single-celled Paramecium could be anesthetized and served as a model organism in the study of anesthetics. We assessed the motion of Paramecium cells with Expert Vision system and the chemoresponse of Paramecium cells with T-maze assays in the presence of four different volatile anesthetics, including isoflurane, sevoflurane, enflurane and ether. Each of those volatiles was dissolved in buffers to give drug concentrations equal to 0.8, 1.0, and 1.2 EC50, respectively, in clinical practice. We could see that after application of volatile anesthetics, the swimming of the Paramecium cells was accelerated and then suppressed, or even stopped eventually, and the index of the chemoresponse of the Paramecium cells (denoted as I ( che )) was decreased. All of the above impacts were found in a concentration-dependent fashion. The biphasic effects of the clinical concentrations of volatile anesthetics on Paramecium simulated the situation of high species in anesthesia, and the inhibition of the chemoresponse also indicated anesthetized. In conclusion, the findings in our studies suggested that the single-celled Paramecium could be anesthetized with clinical concentrations of volatile anesthetics and therefore be utilized as a model organism to study the mechanisms of volatile anesthetics.

  19. 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

  20. Comparison of cardiorespiratory variables in dorsally recumbent horses anesthetized with guaifenesin-ketamine-xylazine spontaneously breathing 50% or maximal oxygen concentrations.

    PubMed

    Karrasch, Nicole M; Hubbell, John A E; Aarnes, Turi K; Bednarski, Richard M; Lerche, Phillip

    2015-04-01

    This study compared cardiorespiratory variables in dorsally recumbent horses anesthetized with guaifenesin-ketamine-xylazine and spontaneously breathing 50% or maximal (> 90%) oxygen (O2) concentrations. Twelve healthy mares were randomly assigned to breathe 50% or maximal O2 concentrations. Horses were sedated with xylazine, induced to recumbency with ketamine-diazepam, and anesthesia was maintained with guaifenesin-ketamine-xylazine to effect. Heart rate, arterial blood pressures, respiratory rate, lithium dilution cardiac output (CO), inspired and expired O2 and carbon dioxide partial pressures, and tidal volume were measured. Arterial and mixed-venous blood samples were collected prior to sedation (baseline), during 30 minutes of anesthesia, 10 minutes after disconnection from O2, and 30 minutes after standing. Shunt fraction, O2 delivery, and alveolar-arterial O2 partial pressures difference [P(A-a)O2] were calculated. Recovery times were recorded. There were no significant differences between groups in cardiorespiratory parameters or in P(A-a)O2 at baseline or 30 minutes after standing. Oxygen partial pressure difference in the 50% group was significantly less than in the maximal O2 group during anesthesia.

  1. The effect of midazolam on the recovery quality, recovery time and the minimum alveolar concentration for extubation in the isoflurane-anesthetized pig.

    PubMed

    Kleine, S A; Quandt, J E; Hofmeister, E H; Peroni, J

    2015-04-01

    There are no reported studies evaluating the effect of midazolam on recovery quality, recovery time or minimum alveolar concentration (MAC) at which extubation occurs (MAC extubation). Our hypotheses were that midazolam administered prior to recovery would decrease MAC extubation, prolong recovery time but provide a smoother recovery. Sixteen Yorkshire pigs were anesthetized with isoflurane for approximately 5 h. The end-tidal isoflurane concentration was then stabilized at 1.4% for 20 min. Pigs were randomly assigned to receive midazolam or saline. The vaporizer was decreased by 10% every 10 min until extubation. Pigs were declared awake by a blinded observer and were assigned a recovery score by the same observer. Mean MAC extubation was not significantly different for pigs receiving saline prior to recovery compared with those pigs receiving midazolam. The overall mean MAC extubation for both groups was 0.6 ± 0.4 vol%. Time to extubation was not significantly longer with midazolam (124 ± 36 min) compared with the saline group (96 ± 61 min; P = 0.09). Recovery score was not significantly different between groups (midazolam, 0.86 ± 1.1; saline 0.5 ± 0.5; P = 0.26). In conclusion, midazolam did not affect MAC extubation. There was no advantage of administering midazolam in the recovery period when performing step-down titration of isoflurane anesthesia. © The Author(s) 2014 Reprints and permissions: sagepub.co.uk/journalsPermissions.nav.

  2. Comparison of cardiorespiratory variables in dorsally recumbent horses anesthetized with guaifenesin-ketamine-xylazine spontaneously breathing 50% or maximal oxygen concentrations

    PubMed Central

    Karrasch, Nicole M.; Hubbell, John A.E.; Aarnes, Turi K.; Bednarski, Richard M.; Lerche, Phillip

    2015-01-01

    This study compared cardiorespiratory variables in dorsally recumbent horses anesthetized with guaifenesin-ketamine-xylazine and spontaneously breathing 50% or maximal (> 90%) oxygen (O2) concentrations. Twelve healthy mares were randomly assigned to breathe 50% or maximal O2 concentrations. Horses were sedated with xylazine, induced to recumbency with ketamine-diazepam, and anesthesia was maintained with guaifenesin-ketamine-xylazine to effect. Heart rate, arterial blood pressures, respiratory rate, lithium dilution cardiac output (CO), inspired and expired O2 and carbon dioxide partial pressures, and tidal volume were measured. Arterial and mixed-venous blood samples were collected prior to sedation (baseline), during 30 minutes of anesthesia, 10 minutes after disconnection from O2, and 30 minutes after standing. Shunt fraction, O2 delivery, and alveolar-arterial O2 partial pressures difference [P(A-a)O2] were calculated. Recovery times were recorded. There were no significant differences between groups in cardiorespiratory parameters or in P(A-a)O2 at baseline or 30 minutes after standing. Oxygen partial pressure difference in the 50% group was significantly less than in the maximal O2 group during anesthesia. PMID:25829559

  3. Benzocaine as an anesthetic for striped bass

    USGS Publications Warehouse

    Gilderhus, Philip A.; Lemm, Carol A.; Woods, L. Curry

    1991-01-01

    Benzocaine was tested as an anesthetic on juvenile and mature adult striped bass (Morone saxatilis ). Concentrations of 55 mg/L at 22 degree C to 80 mg/L at 11 degree C effectively anesthetized fish in about 3 min. Recovery was more rapid as temperature increased. Fish survived concentrations of twice the effective concentration and exposure times up to 60 min at the effective concentration. Striped bass required higher concentrations for anesthetization than had been previously demonstrated for salmonid fishes, but safety margins for both concentration and exposure time were wider than for the salmonids.

  4. Efficacy of Local Anesthetic With Dexamethasone on the Quality of Recovery Following Total Extraperitoneal Bilateral Inguinal Hernia Repair: A Randomized Clinical Trial.

    PubMed

    Sakamoto, Bryan; Harker, Gene; Eppstein, Andrew C; Gwirtz, Kenneth

    2016-12-01

    Quality of recovery (directly associated with patient satisfaction) is an important clinical outcome measurement and a surrogate of anesthetic/surgical care quality. To compare the efficacy of a transversus abdominis plane (TAP) block with dexamethasone sodium phosphate and preperitoneal instillation of local anesthetic (PILA) with dexamethasone vs control on postoperative quality of recovery following a bilateral total extraperitoneal inguinal hernia repair (TEP-IHR) (>24 hours). Secondary objectives included efficacy of this technique on postoperative opioid use, nausea and vomiting, and pain scores. Conducted from November 2013 to August 2015, this randomized, prospective, single-blinded study compared 2 groups (a TAP block and PILA) with a standard anesthetic technique with no regional technique (control) following bilateral TEP-IHR. This study at the Veterans Affairs Medical Center (Indianapolis, Indiana) included patients ages 18 to 80 years with an American Society of Anesthesiologists physical status of 1 to 3 scheduled for an outpatient bilateral TEP-IHR. Nurses assigning pain scores and administrating opioids for pain and staff anesthesiologists administering the Quality of Recovery-40 (QoR-40) questionnaire were blinded. Patients randomized to receive a TAP block with local anesthetics and dexamethasone, PILA with dexamethasone, or no regional technique (3 groups). Patient's response to the QoR-40 questionnaire following a TEP-IHR surgery. The mean (SD) ages in the TAP block (n = 19), PILA (n = 24), and control (n = 23) groups were 58.2 (9.4) years, 62.5 (8.1) years, and 62.9 (7.8) years, respectively. The global QoR-40 scores on postoperative day 1 for the TAP block group (median [interquartile range (IQR)], 178 [173-188]) were comparable with the control group (median [IQR], 174 [150-181]), while the PILA group had better global QoR-40 scores (median [IQR], 184 [175.5-190.75]) (P = .002). The effects of the TAP block and PILA on pain in

  5. Children's behavioral pain reactions during local anesthetic injection using cotton-roll vibration method compared with routine topical anesthesia: A randomized controlled trial

    PubMed Central

    Bagherian, Ali; Sheikhfathollahi, Mahmood

    2016-01-01

    Background: Topical anesthesia has been widely advocated as an important component of atraumatic administration of intraoral local anesthesia. The aim of this study was to use direct observation of children's behavioral pain reactions during local anesthetic injection using cotton-roll vibration method compared with routine topical anesthesia. Materials and Methods: Forty-eight children participated in this randomized controlled clinical trial. They received two separate inferior alveolar nerve block or primary maxillary molar infiltration injections on contralateral sides of the jaws by both cotton-roll vibration (a combination of topical anesthesia gel, cotton roll, and vibration for physical distraction) and control (routine topical anesthesia) methods. Behavioral pain reactions of children were measured according to the author-developed face, head, foot, hand, trunk, and cry (FHFHTC) scale, resulting in total scores between 0 and 18. Results: The total scores on the FHFHTC scale ranged between 0-5 and 0-10 in the cotton-roll vibration and control methods, respectively. The mean ± standard deviation values of total scores on FHFHTC scale were lower in the cotton-roll vibration method (1.21 ± 1.38) than in control method (2.44 ± 2.18), and this was statistically significant (P < 0.001). Conclusion: It may be concluded that the cotton-roll vibration method can be more helpful than the routine topical anesthesia in reducing behavioral pain reactions in children during local anesthesia administration. PMID:27274349

  6. Can the choice of the local anesthetic have an impact on ambulatory surgery perioperative costs? Chloroprocaine for popliteal block in outpatient foot surgery.

    PubMed

    Saporito, Andrea; Anselmi, Luciano; Borgeat, Alain; Aguirre, José A

    2016-08-01

    Short-acting regional anesthetics have already been successfully used for peripheral nerve blocks in an ambulatory surgery setting. However, the impact on direct and indirect perioperative costs comparing 2 different short-acting local anesthetics has not been performed yet. Observational, prospective, case-control, cost-minimization study. Operating room, regional hospital One hundred adult American Society of Anesthesiologists status I-III patients scheduled for popliteal block after minor ambulatory foot surgery. Application of 30 mL chloroprocaine 3% or of 30 mL mepivacaine 1.5% for anesthesia. Cost-minimization evaluation. Direct and indirect perioperative costs were calculated. Block success, onset time and block duration, patient satisfaction, and unplanned outpatient visits or readmissions after discharge were also assessed. Onset time (sensory: 4.3 ± 2.4 vs 11.5 ± 3.2 minutes; motor: 7.1 ± 3.7 vs 18.4 ± 4.5 minutes) and block duration (sensory: 105 ± 26 vs 317 ± 46 minutes; motor: 91 ± 25 vs 216 ± 31 minutes) were significantly shorter (P < .001) when chloroprocaine 3% was used. This translated to P < .001, basically due to a faster discharge home 55 ± 1 vs 175 ± 2 minutes; P < .001) in favor of chloroprocaine 3%, without negatively affecting either block efficacy or patients satisfaction. There were no unplanned outpatient visits or readmissions and no complications in the follow-up at 6 weeks. We conclude that the more expensive chloroprocaine 3% for ambulatory foot surgery can reduce total perioperative costs and reduce length of stay in outpatient patients. Moreover, the saved time and personal resources could be used for additional cases, further increasing the revenues of an ambulatory surgical center. Copyright © 2016 Elsevier Inc. All rights reserved.

  7. Comment on "Local impermeant anions establish the neuronal chloride concentration".

    PubMed

    Voipio, Juha; Boron, Walter F; Jones, Stephen W; Hopfer, Ulrich; Payne, John A; Kaila, Kai

    2014-09-05

    Glykys et al. (Reports, 7 February 2014, p. 670) conclude that, rather than ion transporters, "local impermeant anions establish the neuronal chloride concentration" and thereby determine "the magnitude and direction of GABAAR currents at individual synapses." If this were possible, perpetual ion-motion machines could be constructed. The authors' conclusions conflict with basic thermodynamic principles.

  8. A clinical study to evaluate the efficacy of ELA-Max (4% liposomal lidocaine) as compared with eutectic mixture of local anesthetics cream for pain reduction of venipuncture in children.

    PubMed

    Eichenfield, Lawrence F; Funk, Ann; Fallon-Friedlander, Sheila; Cunningham, Bari B

    2002-06-01

    A double-randomized, blinded crossover trial was performed to assess the efficacy of ELA-Max (4% liposomal lidocaine) as compared with eutectic mixture of local anesthetics (EMLA) for pain relief during pediatric venipuncture procedures. Safety was assessed by evaluation for topical or systemic effects and measurement of serum lidocaine concentrations. A total of 120 children who were scheduled for repeat venipuncture for non-study-related reasons at 2 sites participated in the study. Patients were doubly randomized to treatment regimen (study medication application time of either 30 or 60 minutes) and to the order of application of the topical anesthetics for each venipuncture. The primary outcome measures were the child's rating of pain immediately after the venipuncture procedures using a 100-mm visual analog scale (VAS) tool and the parent's and blinded research observer's Observed Behavioral Distress scores. Both ELA-Max and EMLA seemed to alleviate venipuncture pain. There was no clinically or statistically significant difference in the patient VAS scores within the 30-minute or 60-minute treatment groups, and there was no clinical or statistical difference in VAS scores between the 30-minute ELA-Max treatment without occlusion and the 60-minute EMLA treatment with occlusion. There were no clinically or statistically significant differences between treatment with ELA-Max and EMLA in parental or blinded researcher Observed Behavioral Distress scores, the most frequent response at any observation time being "no distress." This study demonstrates that a 30-minute application of ELA-Max without occlusion is as safe and as effective for ameliorating pain associated with venipuncture as a 60-minute application of the prescription product EMLA requiring occlusion.

  9. Effectiveness of various formulations of local anesthetics and additives for topical anesthesia – a prospective, randomized, double-blind, placebo-controlled study

    PubMed Central

    Weilbach, Christian; Hoppe, Christian; Karst, Matthias; Winterhalter, Michael; Raymondos, Konstantinos; Schultz, Arthur; Rahe-Meyer, Niels

    2017-01-01

    Background Topical anesthesia is used to control pain associated with many procedures in medicine. Today, the product most commonly applied for topical anesthesia in Germany is EMLA® (lidocaine/prilocaine). However, since prilocaine is a methemoglobin-inducing agent, there are limitations to its use, especially in neonates and infants. The aim of this study was to evaluate the effect of prilocaine and lidocaine as well as propylene glycol, a penetration enhancer, and trometamol, a buffer substance, in anesthetic creams. Patients and methods Twenty-nine healthy adults participated in this study. Standardized creams with eight different compositions were applied and left for 20, 40 or 60 min. After exposure to standardized painful stimuli (blunt/sharp with pressures of 0.2, 0.4 or 0.8 N), subjects rated the experimental pain using a visual analog scale. Results Significant results were only found with an exposure time of 60 min and a stamp pressure of 0.8 N. At a concentration of 20%, lidocaine was more effective compared to placebo and equally effective compared to lidocaine/prilocaine in controlling pain. The analgesic effect of the cream containing lidocaine 10% and additional trometamol was significantly superior to that of placebo and non-inferior to that of lidocaine/prilocaine. In this study, the penetration enhancer propylene glycol did not accelerate the onset of the analgesic effect. In contrast, the addition of trometamol (Tris/THAM) accelerated the onset of the effect compared to the native formulation (at 0.4 and 0.8 N). In all of the adult subjects of this study, the minimum exposure time was 60 min for any of the tested topical anesthetic creams. Conclusion The results of this study indicate that a cream containing 20% lidocaine, 38% trometamol and 10% propylene glycol may be used as an alternative to lidocaine/prilocaine with a comparable effect and without the need to extend exposure time. PMID:28546768

  10. 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

  11. State of the art: regional anesthesia using anesthetic admixtures.

    PubMed

    Fetzer-Fowler, S

    1992-08-01

    Aging, high-risk, and ambulatory patients comprise a growing population of surgical candidates. The advantages of regional anesthesia for these patients has promoted technological and pharmacological advances. As new anesthetic agents are developed, methods to improve existing local anesthetics continue. This article reviews the current practice of local anesthetic admixtures. The physiological action of the local anesthetics and their additives is explained relative to their chemical properties. The advantages and risks when adding bicarbonate and epinephrine are described. Nursing implications for the care of the patient receiving regional anesthesia using admixtures are reviewed. An actual case report is presented to demonstrate the clinical application of local anesthetic admixtures.

  12. Binding site and affinity prediction of general anesthetics to protein targets using docking.

    PubMed

    Liu, Renyu; Perez-Aguilar, Jose Manuel; Liang, David; Saven, Jeffery G

    2012-05-01

    The protein targets for general anesthetics remain unclear. A tool to predict anesthetic binding for potential binding targets is needed. In this study, we explored whether a computational method, AutoDock, could serve as such a tool. High-resolution crystal data of water-soluble proteins (cytochrome C, apoferritin, and human serum albumin), and a membrane protein (a pentameric ligand-gated ion channel from Gloeobacter violaceus [GLIC]) were used. Isothermal titration calorimetry (ITC) experiments were performed to determine anesthetic affinity in solution conditions for apoferritin. Docking calculations were performed using DockingServer with the Lamarckian genetic algorithm and the Solis and Wets local search method (http://www.dockingserver.com/web). Twenty general anesthetics were docked into apoferritin. The predicted binding constants were compared with those obtained from ITC experiments for potential correlations. In the case of apoferritin, details of the binding site and their interactions were compared with recent cocrystallization data. Docking calculations for 6 general anesthetics currently used in clinical settings (isoflurane, sevoflurane, desflurane, halothane, propofol, and etomidate) with known 50% effective concentration (EC(50)) values were also performed in all tested proteins. The binding constants derived from docking experiments were compared with known EC(50) values and octanol/water partition coefficients for the 6 general anesthetics. All 20 general anesthetics docked unambiguously into the anesthetic binding site identified in the crystal structure of apoferritin. The binding constants for 20 anesthetics obtained from the docking calculations correlate significantly with those obtained from ITC experiments (P = 0.04). In the case of GLIC, the identified anesthetic binding sites in the crystal structure are among the docking predicted binding sites, but not the top ranked site. Docking calculations suggest a most probable binding site

  13. Comparative, double-blind, controlled study of intra-articular hyaluronic acid (Hyalubrix) injections versus local anesthetic in osteoarthritis of the hip.

    PubMed

    Migliore, Alberto; Massafra, Umberto; Bizzi, Emanuele; Vacca, Francesca; Martin-Martin, Severino; Granata, Mauro; Alimonti, Andrea; Tormenta, Sandro

    2009-01-01

    Comparison of intra-articular bacterial-derived hyaluronic acid (Hyalubrix) (HA) with local analgesia (mepivacaine) for osteoarthritis (OA) of the hip. A pilot prospective, double-blind, 6-month randomized trial of 42 patients with hip OA. HA or mepivacaine was administered twice (once a month) under ultrasound guidance. Efficacy measurements included the Lequesne's algofunctional index, a visual analog scale for pain, concomitant use of analgesia, patient and physician global measurement, and safety. Patients in the HA group exhibited a significantly reduced Lequesne's algofunctional index 3 and 6 months after treatment (P < 0.001) and significantly reduced visual analog scale pain scores 3 and 6 months after treatment (P < 0.05) compared with the local anesthetic group. All primary and secondary measures were significantly improved versus baseline, but other than the above were not different from each other at 3 or 6 months. Adverse effects were minimal. This comparative study suggests a beneficial effect and safety of intra-articular HA in the management of hip OA. ISRCTN39397064.

  14. Comparative, double-blind, controlled study of intra-articular hyaluronic acid (Hyalubrix®) injections versus local anesthetic in osteoarthritis of the hip

    PubMed Central

    2009-01-01

    Introduction Comparison of intra-articular bacterial-derived hyaluronic acid (Hyalubrix®) (HA) with local analgesia (mepivacaine) for osteoarthritis (OA) of the hip. Methods A pilot prospective, double-blind, 6-month randomized trial of 42 patients with hip OA. HA or mepivacaine was administered twice (once a month) under ultrasound guidance. Efficacy measurements included the Lequesne's algofunctional index, a visual analog scale for pain, concomitant use of analgesia, patient and physician global measurement, and safety. Results Patients in the HA group exhibited a significantly reduced Lequesne's algofunctional index 3 and 6 months after treatment (P < 0.001) and significantly reduced visual analog scale pain scores 3 and 6 months after treatment (P < 0.05) compared with the local anesthetic group. All primary and secondary measures were significantly improved versus baseline, but other than the above were not different from each other at 3 or 6 months. Adverse effects were minimal. Conclusions This comparative study suggests a beneficial effect and safety of intra-articular HA in the management of hip OA. Trial registration number ISRCTN39397064. PMID:20003205

  15. A randomized controlled trail comparing the efficacy of 0.5% centbucridine to 2% lignocaine as local anesthetics in dental extractions.

    PubMed

    Mansuri, Samir; Bhayat, Ahmed; Omar, Esam; Jarab, Fadi; Ahmed, Mohammad Sami

    2011-01-01

    The development of local anesthesia in dentistry has marked the beginning of a new era in terms of pain control. Lignocaine is the most commonly used local anesthetic (LA) agent even though it has a vasodilative effect and needs to be combined with adrenaline. Centbucridine is a non-ester, non amide group LA and has not been comprehensively studied in the dental setting and the objective was to compare it to Lignocaine. This was a randomized study comparing the onset time, duration, depth and cardiovascular parameters between Centbucridine (0.5%) and Lignocaine (2%). The study was conducted in the dental outpatient department at the Government Dental College in India on patients attending for the extraction of lower molars. A total of 198 patients were included and there were no significant differences between the LAs except those who received Centbucridine reported a significantly longer duration of anesthesia compared to those who received Lignocaine. None of the patients reported any side effects. Centbucridine was well tolerated and its substantial duration of anesthesia could be attributed to its chemical compound. Centbucridine can be used for dental procedures and can confidently be used in patients who cannot tolerate Lignocaine or where adrenaline is contraindicated.

  16. Noninvasive investigation of skin local hypothermia influence upon local oxygenation and hemoglobin concentration

    NASA Astrophysics Data System (ADS)

    Douplik, Alexandre Y.; Kessler, Manfred D.; Kakihana, Yasuyuki; Krug, Alfons

    1997-08-01

    Functional evaluation of local hemoglobin concentration and hemoglobin oxygenation based on back scattering spectra from human skin in vivo have been obtained in visible range (502 - 628 nm) by a rapid microlightguide spectrometer (EMPHO II) with step 250 micrometer. Analysis of received results has shown that during local cooling there is two nearly simultaneous reactions: reduction of hemoglobin concentration and increase of hemoglobin oxygenation level. In a case when one has used previous heating of planning place for cooling, reduction of hemoglobin concentration is expressed higher by 22 - 33%.

  17. Does pain relief by CT-guided indirect cervical nerve root injection with local anesthetics and steroids predict pain relief after decompression surgery for cervical nerve root compression?

    PubMed

    Antoniadis, Alexander; Dietrich, Tobias J; Farshad, Mazda

    2016-10-01

    The relationship of pain relief from a recently presented CT-guided indirect cervical nerve root injection with local anesthetics and steroids to surgical decompression as a treatment for single-level cervical radiculopathy is not clear. This retrospective study aimed to compare the immediate and 6-week post-injection effects to the short- and long-term outcomes after surgical decompression, specifically in regard to pain relief. Patients (n = 39, age 47 ± 10 years) who had undergone CT-guided indirect injection with local anesthetics and steroids as an initial treatment for single cervical nerve root radiculopathy and who subsequently needed surgical decompression were included retrospectively. Pain levels (VAS scores) were monitored before, immediately after, and 6 weeks after injection (n = 34), as well as 6 weeks (n = 38) and a mean of 25 months (SD ± 12) after surgical decompression (n = 36). Correlation analysis was performed to find potential associations of pain relief after injection and after surgery to investigate the predictive value of post-injection pain relief. There was no correlation between immediate pain relief after injection (-32 ± 27 %) and 6 weeks later (-7 ± 19 %), (r = -0.023, p = 0.900). There was an association by tendency between immediate pain relief after injection and post-surgical pain relief at 6 weeks (-82 ± 27 %), (r = 0.28, p = 0.08). Pain relief at follow-up remained high at -70 ± 21 % and was correlated with the immediate pain amelioration effect of the injection (r = 0.37, p = 0.032). Five out of seven patients who reported no pain relief from injection had a pain relief from surgery in excess of 50 %. The amount of immediate radiculopathic pain relief after indirect cervical nerve root injection is associated with the amount of pain relief achieved at long-term follow-up after surgical decompression of single-level cervical radiculopathy

  18. Effect of bispectral index versus end-tidal anesthetic gas concentration-guided protocol on time to tracheal extubation for halothane-based general anesthesia

    PubMed Central

    Jain, Neena; Mathur, Pooja Rawat; Khan, Shoyeb; Khare, Arvind; Mathur, Veena; Sethi, Surendra

    2016-01-01

    Background and Aims: Early extubation is a desirable goal after general anesthesia. Very few studies have compared the effect of bispectral index (BIS) monitoring versus standard end-tidal anesthetic gas (ETAG) concentration monitoring on tracheal extubation time for halothane-based anesthesia. The aim of this study was to compare the effect of BIS versus ETAG-guided anesthesia on time to tracheal extubation for halothane-based anesthesia in general surgical setting. Methods: This was a randomized, controlled double-blind study. Sixty patients with the American Society of Anesthesiologists physical status Class 1 or 2, receiving halothane-based general anesthesia were randomized to BIS-guided (n = 30) and ETAG-guided anesthesia (n = 30). Time to tracheal extubation was measured. In BIS group, BIS value was kept between 40 and 60 while in ETAG group; ETAG value was kept between 0.7 and 1.3 minimum alveolar concentration. The two groups were compared using Student's t-test, and P < 0.05 was considered statistically significant. Data were processed and analyzed using SPSS version 17 software. Results: Mean time to tracheal extubation was significantly longer in BIS group (9.63 ± 3.02 min) as compared to ETAG group (5.29 ± 1.51 min), mean difference 4.34 min with 95% confidence interval (3.106, 5.982) (P < 0.05). Conclusion: In our study, the extubation time was significantly longer in BIS-guided anesthesia as compared to ETAG-guided anesthesia. ETAG monitoring promotes earlier extubation of patients as compared to BIS monitoring during halothane anesthesia. PMID:27746557

  19. Profiling the local carrier concentration across a semiconductor quantum dot

    SciTech Connect

    Walrath, J. C.; Lin, Yen-Hsiang; Huang, S.; Goldman, R. S.

    2015-05-11

    We profile the local carrier concentration, n, across epitaxial InAs/GaAs quantum dots (QDs) consisting of 3D islands on top of a 2D alloy layer. We use scanning thermoelectric microscopy to measure a profile of the temperature gradient-induced voltage, which is converted to a profile of the local Seebeck coefficient, S. The S profile is then converted to a conduction band-edge profile and compared with Poisson-Schrodinger band-edge simulations. Our combined computational-experimental approach suggests a reduced carrier concentration in the QD center in comparison to that of the 2D alloy layer. The relative roles of free carrier trapping and/or dopant expulsion are discussed.

  20. Noble gas binding to human serum albumin using docking simulation: nonimmobilizers and anesthetics bind to different sites.

    PubMed

    Seto, Tomoyoshi; Isogai, Hideto; Ozaki, Masayuki; Nosaka, Shuichi

    2008-10-01

    Nonimmobilizers are structurally similar to anesthetics, but do not produce anesthesia at clinically relevant concentrations. Xenon, krypton, and argon are anesthetics, whereas neon and helium are nonimmobilizers. The structures of noble gases with anesthetics or nonimmobilizers are similar and their interactions are simple. Whether the binding site of anesthetics differs from that of nonimmobilizers has long been a question in molecular anesthesiology. We investigated the binding sites and energies of anesthetic and nonimmobilizer noble gases in human serum albumin (HSA) because the 3D structure of HSA is well known and it has an anesthetic binding site. The computational docking simulation we used searches for binding sites and calculates the binding energy for small molecules and a template molecule. Xenon, krypton, and argon were found to bind to the enflurane binding site of HSA, whereas neon and helium were found to bind to sites different from the xenon binding site. Rare gas anesthetic binding was dominated by van der Waals energy, while nonimmobilizer binding was dominated by solvent-effect energy. Binding site preference was determined by the ratios of local binding energy (van der Waals energy) and nonspecific binding energy (solvent-effect energy) to the total binding energy. van der Waals energy dominance is necessary for anesthetic binding. This analysis of binding energy components provides a rationale for the binding site difference of anesthetics and nonimmobilizers, reveals the differences between the binding interactions of anesthetics and nonimmobilizers, may explain pharmacological differences between anesthetics and nonimmobilizers, and provide an understanding of anesthetic action at the atomic level.

  1. People, Places, Power: Medicaid Concentration and Local Political Participation.

    PubMed

    Michener, Jamila D

    2017-10-01

    The geographic concentration of disadvantage is a key mechanism of inequity. In the United States, the spatial patterning of disadvantage renders it more than the sum of its individual parts and disproportionately harms economically and racially marginalized Americans. This article focuses specifically on the political effects of Medicaid beneficiaries being concentrated in particular locales. After offering a framework for conceptualizing the community-wide consequences of such policy concentration, I analyze aggregate multiyear data to examine the effect of Medicaid density on county-level voter turnout and local organizational strength. I find that, as the proportion of county residents enrolled in Medicaid increases, the prevalence of civic and political membership associations declines and aggregate rates of voting decrease. These results suggest that, if grassroots political action is to be part of a strategy to achieve health equity, policy makers and local organizations must make efforts to counteract the sometimes demobilizing "place-based" political effects of "people-based" policies such as Medicaid. Copyright © 2017 by Duke University Press.

  2. Anesthetics interacting with lipid rafts.

    PubMed

    Bandeiras, Cátia; Serro, Ana Paula; Luzyanin, Konstantin; Fernandes, Anabela; Saramago, Benilde

    2013-01-23

    The exact mechanism by which anesthetics induce cell membrane-mediated modifications is still an open question. Although the fluidization effect of the anesthetic molecules on the cellular membrane is widely recognized, it is not known if anesthetics show any preference for specific membrane domains, namely the lipid rafts. The importance of these membrane micro-domains derives from the fact that they have been associated with cell signaling pathways, as well as with specific drug interactions. The objective of this work is to contribute for the elucidation of this question through the comparison of the anesthetic interactions with membranes of various lipid compositions. Liposomes prepared with an equimolar mixture of POPC, sphingomyelin and cholesterol, were chosen as models for lipid rafts. The interactions of these liposomes with two local anesthetics, tetracaine and lidocaine, and one general anesthetic, propofol, were studied. The effect of cholesterol was investigated by comparing anesthetic interactions with POPC/SM liposomes and POPC/SM/CHOL liposomes. The following experimental techniques were used: quartz crystal microbalance with dissipation, differential scanning calorimetry and phosphorus nuclear magnetic resonance. Although the liposomes investigated by the different techniques are not in the same conditions, it is possible to assemble the information obtained from all experimental techniques employed to reach a general conclusion. Tetracaine interacts more with raftlike domains, lidocaine induces stronger modifications on POPC/SM liposomes and the results for propofol are not fully conclusive but it seems to be the least prone to lipid interactions. The results were compared with those obtained with DMPC-containing liposomes, reported in a previous work.

  3. 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.

  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. Novel serine-based gemini surfactants as chemical permeation enhancers of local anesthetics: A comprehensive study on structure-activity relationships, molecular dynamics and dermal delivery.

    PubMed

    Teixeira, Raquel S; Cova, Tânia F G G; Silva, Sérgio M C; Oliveira, Rita; do Vale, M Luísa C; Marques, Eduardo F; Pais, Alberto A C C; Veiga, Francisco J B

    2015-06-01

    This work aims at studying the efficacy of a series of novel biocompatible, serine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine, combining an experimental and computational approach. The surfactants consist of gemini molecules structurally related, but with variations in headgroup charge (nonionic vs. cationic) and in the hydrocarbon chain lengths (main and spacer chains). In vitro permeation and molecular dynamics studies combined with cytotoxicity profiles were performed to investigate the permeation of both drugs, probe skin integrity, and rationalize the interactions at molecular level. Results show that these enhancers do not have significant deleterious effects on the skin structure and do not cause relevant changes on cell viability. Permeation across the skin is clearly improved using some of the selected serine-based gemini surfactants, namely the cationic ones with long alkyl chains and shorter spacer. This is noteworthy in the case of ropivacaine hydrochloride, which is not easily administered through the stratum corneum. Molecular dynamics results provide a mechanistic view of the surfactant action on lipid membranes that essentially corroborate the experimental observations. Overall, this study suggests the viability of these serine-based surfactants as suitable and promising delivery agents in pharmaceutical formulations. Copyright © 2015. Published by Elsevier B.V.

  6. The interaction between pindolol and epinephrine contained in local anesthetic solution to the left ventricular diastolic filling velocity in normal subjects.

    PubMed Central

    Niwa, H.; Shibutani, T.; Hori, T.; Kim, Y.; Akita, M.; Matsuura, H.

    1996-01-01

    To evaluate the interaction between the nonselective beta-blocker, pindolol, and epinephrine contained in a local anesthetic solution, the left ventricular diastolic filling velocity was examined with pulsed Doppler echocardiography. Arterial blood pressure (BP), the R-R interval on the electrocardiogram (RR), and Doppler echo-cardiographic measurements were recorded in seven healthy volunteers after 45 micrograms of epinephrine contained in lidocaine (L-E) was injected in the maxilla after pretreatment with 5 mg of pindolol. The administration of L-E caused the elevation of BP and an increase in RR interval. Peak early (E) and peak atrial (A) filling velocities decreased, whereas isovolumic relaxation time (IVRT) and diastolic filling period (DFP) were prolonged. Although the ratio of E to A (E/A) remained unchanged, E/A/DFP was reduced. In contrast, when L-E was given without pindolol pretreatment, RR interval was shortened and BP was unchanged. The increase of both E and A velocities and the shortening of both IVRT and DFP were observed. E/A remained unchanged but E/A/DFP was increased. These results suggested that L-E caused opposite effects on the left ventricular filling velocity in the presence or absence of pindolol. We conclude that epinephrine activates the left ventricular relaxation rate but impairs it in the presence of pindolol. Images Figure 1 PMID:10323111

  7. Concentration independent modulation of local micromechanics in a fibrin gel.

    PubMed

    Kotlarchyk, Maxwell A; Shreim, Samir G; Alvarez-Elizondo, Martha B; Estrada, Laura C; Singh, Rahul; Valdevit, Lorenzo; Kniazeva, Ekaterina; Gratton, Enrico; Putnam, Andrew J; Botvinick, Elliot L

    2011-01-01

    Methods for tuning extracellular matrix (ECM) mechanics in 3D cell culture that rely on increasing the concentration of either protein or cross-linking molecules fail to control important parameters such as pore size, ligand density, and molecular diffusivity. Alternatively, ECM stiffness can be modulated independently from protein concentration by mechanically loading the ECM. We have developed a novel device for generating stiffness gradients in naturally derived ECMs, where stiffness is tuned by inducing strain, while local mechanical properties are directly determined by laser tweezers based active microrheology (AMR). Hydrogel substrates polymerized within 35 mm diameter Petri dishes are strained non-uniformly by the precise rotation of an embedded cylindrical post, and exhibit a position-dependent stiffness with little to no modulation of local mesh geometry. Here we present the device in the context of fibrin hydrogels. First AMR is used to directly measure local micromechanics in unstrained hydrogels of increasing fibrin concentration. Changes in stiffness are then mapped within our device, where fibrin concentration is held constant. Fluorescence confocal imaging and orbital particle tracking are used to quantify structural changes in fibrin on the micro and nano levels respectively. The micromechanical strain stiffening measured by microrheology is not accompanied by ECM microstructural changes under our applied loads, as measured by confocal microscopy. However, super-resolution orbital tracking reveals nanostructural straightening, lengthening, and reduced movement of fibrin fibers. Furthermore, we show that aortic smooth muscle cells cultured within our device are morphologically sensitive to the induced mechanical gradient. Our results demonstrate a powerful cell culture tool that can be used in the study of mechanical effects on cellular physiology in naturally derived 3D ECM tissues.

  8. Concentration Independent Modulation of Local Micromechanics in a Fibrin Gel

    PubMed Central

    Alvarez-Elizondo, Martha B.; Estrada, Laura C.; Singh, Rahul; Valdevit, Lorenzo; Kniazeva, Ekaterina; Gratton, Enrico; Putnam, Andrew J.; Botvinick, Elliot L.

    2011-01-01

    Methods for tuning extracellular matrix (ECM) mechanics in 3D cell culture that rely on increasing the concentration of either protein or cross-linking molecules fail to control important parameters such as pore size, ligand density, and molecular diffusivity. Alternatively, ECM stiffness can be modulated independently from protein concentration by mechanically loading the ECM. We have developed a novel device for generating stiffness gradients in naturally derived ECMs, where stiffness is tuned by inducing strain, while local mechanical properties are directly determined by laser tweezers based active microrheology (AMR). Hydrogel substrates polymerized within 35 mm diameter Petri dishes are strained non-uniformly by the precise rotation of an embedded cylindrical post, and exhibit a position-dependent stiffness with little to no modulation of local mesh geometry. Here we present the device in the context of fibrin hydrogels. First AMR is used to directly measure local micromechanics in unstrained hydrogels of increasing fibrin concentration. Changes in stiffness are then mapped within our device, where fibrin concentration is held constant. Fluorescence confocal imaging and orbital particle tracking are used to quantify structural changes in fibrin on the micro and nano levels respectively. The micromechanical strain stiffening measured by microrheology is not accompanied by ECM microstructural changes under our applied loads, as measured by confocal microscopy. However, super-resolution orbital tracking reveals nanostructural straightening, lengthening, and reduced movement of fibrin fibers. Furthermore, we show that aortic smooth muscle cells cultured within our device are morphologically sensitive to the induced mechanical gradient. Our results demonstrate a powerful cell culture tool that can be used in the study of mechanical effects on cellular physiology in naturally derived 3D ECM tissues. PMID:21629793

  9. Generation of local concentration gradients by gas-liquid contacting.

    PubMed

    de Jong, Jorrit; Verheijden, Pascal W; Lammertink, Rob G H; Wessling, Matthias

    2008-05-01

    We present a generic concept to create local concentration gradients, based on the absorption of gases or vapors in a liquid. A multilayer microfluidic device with crossing gas and liquid channels is fabricated by micromilling and used to generate multiple gas-liquid contacting regions, separated by a hydrophobic membrane. Each crossing can acts as both a microdosing and microstripping region. Furthermore, the liquid and gas flow rate can be controlled independently of each other. The focus of this conceptual article is on the generation of pH gradients, by locally supplying acidic or basic gases/vapors, such as carbon dioxide, hydrochloric acid, and ammonia, visualized by pH-sensitive dyes. Stationary and moving gradients are presented in devices with 500-microm channel width, depths of 200-400 microm, and lengths of multiple centimeters. It is shown that the method allows for multiple consecutive switching gradients in a single microchannel. Absorption measurements in a microcontactor with the model system CO2/water are presented to indicate the dependence of gas absorption rate on channel depth and residence time. Achievable concentration ranges are ultimately limited by the solubility of used components. The reported devices are easy to fabricate, and their application is not limited to pH gradients. Two proof of principles are demonstrated to indicate new opportunities: (i) local crystallization of NaCl using HCl vapor and (ii) consecutive reactions of ammonia with copper(II) ions in solution.

  10. Kinetics of the inhibition of acetylcholinesterase from desert cobra (Walterinnesia aegyptia) venom by local anesthetics: procaine and tetracaine.

    PubMed

    al-Jafari, A A; Kamal, M A; Duhaiman, A S; Alhomida, A S

    1996-10-01

    The kinetic parameters of W. aegyptia venom acetylcholinesterase (AChE) inhibition by procaine and tetracaine hydrochloride were investigated in the present study. Procaine and tetracaine reversibly inhibited the AChE activity in a concentration-dependent manner, the IC50 being about 0.28 and 0.04 mM, respectively. The Michaelis-Menten constant (K(m)) for the hydrolysis of acetylthiocholine iodide was found to be 0.051 mM with Vmax 10.2 mumole/min/mg protein. Both K(m) and Vmax were affected by procaine while only Vmax decreased with tetracaine. A Lineweaver-Burk plot and its secondary replot indicated that the nature of the inhibition is of the linear mixed type for procaine which is considered to be a mixture of competitive and noncompetitive types while the inhibition was noncompetitive for tetracaine. The values of Ki(slope) and K(intercept were estimated as 0.133 mM and 0.451 mM for procaine and 7.2 x 10(-3) mM for tetracaine, respectively, by the secondary replots of the Lineweaver-Burk plot.

  11. Imaging local scatterer concentrations by the Nakagami statistical model.

    PubMed

    Tsui, Po-Hsiang; Chang, Chien-Cheng

    2007-04-01

    The ultrasonic B-mode image is an important clinical tool used to examine the internal structures of the biological tissue. Due to the fact that the conventional B-scans cannot fully reflect the nature of the tissue, some useful quantitative parameters have been applied to quantify the properties of the tissue. Among various possibilities, the Nakagami parameter was demonstrated to have an outstanding ability to detect the variation of the scatterer concentration. This study is aimed to develop a scatterer concentration image based on the Nakagami parameter map to assist in the B-mode image for tissue characterization. In particular, computer simulations are carried out to generate phantoms of different scatterer concentrations and echogenicity coefficients and their B-mode and Nakagami parametric images are compared to evaluate the performance of the Nakagami image in differentiating the properties of the scatterers. The simulated results show that the B-mode image would be affected by the system settings and user operations, whereas the Nakagami parametric image provides a comparatively consistent image result when different diagnosticians use different dynamic ranges and system gains. This is largely because the Nakagami image formation is only based on the backscattered statistics of the ultrasonic signals in local tissues. Such an imaging principle allows the Nakagami image to quantify the local scatterer concentrations in the tissue and to extract the backscattering information from the regions of the weaker echoes that may be lost in the B-mode image. These findings suggest that the Nakagami image can be combined with the use of the B-mode image simultaneously to visualize the tissue structures and the scatterer properties for a better medical diagnosis.

  12. The active titration method for measuring local hydroxyl radical concentration

    NASA Technical Reports Server (NTRS)

    Sprengnether, Michele; Prinn, Ronald G.

    1994-01-01

    We are developing a method for measuring ambient OH by monitoring its rate of reaction with a chemical species. Our technique involves the local, instantaneous release of a mixture of saturated cyclic hydrocarbons (titrants) and perfluorocarbons (dispersants). These species must not normally be present in ambient air above the part per trillion concentration. We then track the mixture downwind using a real-time portable ECD tracer instrument. We collect air samples in canisters every few minutes for roughly one hour. We then return to the laboratory and analyze our air samples to determine the ratios of the titrant to dispersant concentrations. The trends in these ratios give us the ambient OH concentration from the relation: dlnR/dt = -k(OH). A successful measurement of OH requires that the trends in these ratios be measureable. We must not perturb ambient OH concentrations. The titrant to dispersant ratio must be spatially invariant. Finally, heterogeneous reactions of our titrant and dispersant species must be negligible relative to the titrant reaction with OH. We have conducted laboratory studies of our ability to measure the titrant to dispersant ratios as a function of concentration down to the few part per trillion concentration. We have subsequently used these results in a gaussian puff model to estimate our expected uncertainty in a field measurement of OH. Our results indicate that under a range of atmospheric conditions we expect to be able to measure OH with a sensitivity of 3x10(exp 5) cm(exp -3). In our most optimistic scenarios, we obtain a sensitivity of 1x10(exp 5) cm(exp -3). These sensitivity values reflect our anticipated ability to measure the ratio trends. However, because we are also using a rate constant to obtain our (OH) from this ratio trend, our accuracy cannot be better than that of the rate constant, which we expect to be about 20 percent.

  13. The active titration method for measuring local hydroxyl radical concentration

    NASA Technical Reports Server (NTRS)

    Sprengnether, Michele; Prinn, Ronald G.

    1994-01-01

    We are developing a method for measuring ambient OH by monitoring its rate of reaction with a chemical species. Our technique involves the local, instantaneous release of a mixture of saturated cyclic hydrocarbons (titrants) and perfluorocarbons (dispersants). These species must not normally be present in ambient air above the part per trillion concentration. We then track the mixture downwind using a real-time portable ECD tracer instrument. We collect air samples in canisters every few minutes for roughly one hour. We then return to the laboratory and analyze our air samples to determine the ratios of the titrant to dispersant concentrations. The trends in these ratios give us the ambient OH concentration from the relation: dlnR/dt = -k(OH). A successful measurement of OH requires that the trends in these ratios be measureable. We must not perturb ambient OH concentrations. The titrant to dispersant ratio must be spatially invariant. Finally, heterogeneous reactions of our titrant and dispersant species must be negligible relative to the titrant reaction with OH. We have conducted laboratory studies of our ability to measure the titrant to dispersant ratios as a function of concentration down to the few part per trillion concentration. We have subsequently used these results in a gaussian puff model to estimate our expected uncertainty in a field measurement of OH. Our results indicate that under a range of atmospheric conditions we expect to be able to measure OH with a sensitivity of 3x10(exp 5) cm(exp -3). In our most optimistic scenarios, we obtain a sensitivity of 1x10(exp 5) cm(exp -3). These sensitivity values reflect our anticipated ability to measure the ratio trends. However, because we are also using a rate constant to obtain our (OH) from this ratio trend, our accuracy cannot be better than that of the rate constant, which we expect to be about 20 percent.

  14. Exploring the structure of the voltage-gated Na+ channel by an engineered drug access pathway to the receptor site for local anesthetics.

    PubMed

    Lukacs, Peter; Gawali, Vaibhavkumar S; Cervenka, Rene; Ke, Song; Koenig, Xaver; Rubi, Lena; Zarrabi, Touran; Hilber, Karlheinz; Stary-Weinzinger, Anna; Todt, Hannes

    2014-08-01

    Despite the availability of several crystal structures of bacterial voltage-gated Na(+) channels, the structure of eukaryotic Na(+) channels is still undefined. We used predictions from available homology models and crystal structures to modulate an external access pathway for the membrane-impermeant local anesthetic derivative QX-222 into the internal vestibule of the mammalian rNaV1.4 channel. Potassium channel-based homology models predict amino acid Ile-1575 in domain IV segment 6 to be in close proximity to Lys-1237 of the domain III pore-loop selectivity filter. The mutation K1237E has been shown previously to increase the diameter of the selectivity filter. We found that an access pathway for external QX-222 created by mutations of Ile-1575 was abolished by the additional mutation K1237E, supporting the notion of a close spatial relationship between sites 1237 and 1575. Crystal structures of bacterial voltage-gated Na(+) channels predict that the side chain of rNaV1.4 Trp-1531 of the domain IV pore-loop projects into the space between domain IV segment 6 and domain III pore-loop and, therefore, should obstruct the putative external access pathway. Indeed, mutations W1531A and W1531G allowed for exceptionally rapid access of QX-222. In addition, W1531G created a second non-selective ion-conducting pore, bypassing the outer vestibule but probably merging into the internal vestibule, allowing for control by the activation gate. These data suggest a strong structural similarity between bacterial and eukaryotic voltage-gated Na(+) channels. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc.

  15. Exploring the Structure of the Voltage-gated Na+ Channel by an Engineered Drug Access Pathway to the Receptor Site for Local Anesthetics*

    PubMed Central

    Lukacs, Peter; Gawali, Vaibhavkumar S.; Cervenka, Rene; Ke, Song; Koenig, Xaver; Rubi, Lena; Zarrabi, Touran; Hilber, Karlheinz; Stary-Weinzinger, Anna; Todt, Hannes

    2014-01-01

    Despite the availability of several crystal structures of bacterial voltage-gated Na+ channels, the structure of eukaryotic Na+ channels is still undefined. We used predictions from available homology models and crystal structures to modulate an external access pathway for the membrane-impermeant local anesthetic derivative QX-222 into the internal vestibule of the mammalian rNaV1.4 channel. Potassium channel-based homology models predict amino acid Ile-1575 in domain IV segment 6 to be in close proximity to Lys-1237 of the domain III pore-loop selectivity filter. The mutation K1237E has been shown previously to increase the diameter of the selectivity filter. We found that an access pathway for external QX-222 created by mutations of Ile-1575 was abolished by the additional mutation K1237E, supporting the notion of a close spatial relationship between sites 1237 and 1575. Crystal structures of bacterial voltage-gated Na+ channels predict that the side chain of rNaV1.4 Trp-1531 of the domain IV pore-loop projects into the space between domain IV segment 6 and domain III pore-loop and, therefore, should obstruct the putative external access pathway. Indeed, mutations W1531A and W1531G allowed for exceptionally rapid access of QX-222. In addition, W1531G created a second non-selective ion-conducting pore, bypassing the outer vestibule but probably merging into the internal vestibule, allowing for control by the activation gate. These data suggest a strong structural similarity between bacterial and eukaryotic voltage-gated Na+ channels. PMID:24947510

  16. Comparison of interscalene brachial plexus block and intra-articular local anesthetic administration on postoperative pain management in arthroscopic shoulder surgery.

    PubMed

    Aksu, Recep; Biçer, Cihangir; Ülgey, Ayşe; Bayram, Adnan; Güneş, Işın; Güney, Ahmet; Yıldırım, Mustafa Denizhan; Gökahmetoğlu, Günhan; Yıldız, Karamehmet

    2015-01-01

    In this study, the aim was to compare postoperative analgesia effects of the administration of ultrasound-guided interscalene brachial plexus block and intra-articular bupivacaine carried out with bupivacaine. In the first group of patients 20 mL 0.25% bupivacaine and ultrasound-guided interscalene brachial plexus block (ISPB) were applied, while 20 mL 0.25% bupivacaine was given via intra-articular (IA) administration to the second group patients after surgery. Patients in the third group were considered the control group and no block was performed. Patient-controlled analgesia (PCA) with morphine was used in all three groups for postoperative analgesia. In the ISPB group, morphine consumption in the periods between 0-4, 6-12 and 12-24 postoperative hours and total consumption within 24h was lower than in the other two groups. Morphine consumption in the IA group was lower than in the control group in the period from 0 to 6h and the same was true for total morphine consumption in 24h. Postoperative VASr scores in the ISPB group were lower than both of the other groups in the first 2h and lower than the control group in the 4th and 6th hours (p<0.05). In the IA group, VASr and VASm scores in the 2nd, 4th and 6th hours were lower than in the control group (p<0.05). Interscalene brachial plexus block was found to be more effective than intra-articular local anesthetic injection for postoperative analgesia. Copyright © 2014 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  17. Regional anesthesia and lipid resuscitation for local anesthetic systemic toxicity in China: results of a survey by the orthopedic anesthesia group of the Chinese Society Of Anesthesiology.

    PubMed

    Xu, Mao; Jin, Shanliang; Li, Zhengqian; Xu, Xuzhong; Wang, Xiuli; Zhang, Lan; Feng, Zeguo; Yu, Buwei; Liu, Jin; Guo, Xiangyang

    2016-01-04

    Intravenous lipid emulsions have been introduced for the management of patients with Local Anesthetic Systemic Toxicity (LAST). These emulsions have been stated as a first-line treatment in the guidelines of several international anesthesia organizations. Nevertheless, the adoption of lipid rescue therapy by Chinese practitioners remains unknown. We, therefore, evaluated the current approaches to treat LAST and the use of lipid rescue therapy among anesthesiologists in China. In September 2013, a 23-question survey on regional anesthesia practice and availability of lipid emulsions was sent by e-mail to directors or designated individuals at 41 academic anesthesiology departments listed by the orthopedic anesthesia group of the Chinese Society of Anesthesiology. Responses were received from 36 of the 41 (88 %) anesthesiology departments. To simplify the analysis, responses were divided into two groups according to the annual percentage of patients who received regional anesthesia (RA) for orthopedic anesthesia: 14 departments (39%) with high-utilization (≥ 50%) and 22 departments (61%) low-utilization (<50%) of RA. Ropivacaine and bupivacaine were the common drugs used for RA, which were independent of RA utilization. Interestingly, ultrasound-guided techniques were much more frequently used in low-utilization institutions than in high-utilization institutions (P = 0.025). Lipid emulsion was readily available in 8 of the 36 (22%) responding institutions, with 7 of the other 28 (25%) institutions planning to stock lipid emulsion. No differences in lipid availability and storage plans were observed between high- and low-utilization institutions. Lipid resuscitation was performed in five of the eight departments that had lipid emulsion. Eleven patients were successfully resuscitated and one was not. Lipid emulsion is not widely available in China to treat LAST resulted from RA for orthopedic patients. Efforts are required to promote lipid rescue therapy nationwide

  18. Role of the Local Anesthetic Receptor in the State-Dependent Inhibition of Voltage-Gated Sodium Channels by the Insecticide Metaflumizone

    PubMed Central

    von Stein, Richard T.

    2012-01-01

    Sodium channel inhibitor (SCI) insecticides selectively target voltage-gated sodium (Nav) channels in the slow-inactivated state by binding at or near the local anesthetic receptor within the sodium channel pore. Metaflumizone is a new insecticide for the treatment of fleas on domesticated pets and has recently been reported to block insect sodium channels in the slow-inactivated state, thereby implying that it is also a member of the SCI class. Using the two-electrode voltage-clamp technique, we examined metaflumizone inhibition of rat Nav1.4 sodium channels expressed in Xenopus laevis oocytes. Metaflumizone selectively inhibited Nav1.4 channels at potentials that promoted slow inactivation and shifted the voltage dependence of slow inactivation in the direction of hyperpolarization. Metaflumizone perfusion at a hyperpolarized holding potential also shifted the conductance-voltage curve for activation in the direction of depolarization and antagonized use-dependent lidocaine inhibition of fast-inactivated sodium channels, actions not previously observed with other SCI insecticides. We expressed mutated Nav1.4/F1579A and Nav1.4/Y1586A channels to investigate whether metaflumizone shares the domain IV segment S6 (DIV-S6) binding determinants identified for other SCI insecticides. Consistent with previous investigations of SCI insecticides on rat Nav1.4 channels, the F1579A mutation reduced sensitivity to block by metaflumizone, whereas the Y1586A mutation paradoxically increased the sensitivity to metaflumizone. We conclude that metaflumizone selectively inhibits slow-inactivated Nav1.4 channels and shares DIV-S6 binding determinants with other SCI insecticides and therapeutic drugs. However, our results suggest that metaflumizone interacts with resting and fast-inactivated channels in a manner that is distinct from other compounds in this insecticide class. PMID:22127519

  19. An ultrasonographic assessment of nerve stimulation-guided median nerve block at the elbow: a local anesthetic spread, nerve size, and clinical efficacy study.

    PubMed

    Dufour, Eric; Cymerman, Alexandre; Nourry, Gérard; Balland, Nicolas; Couturier, Christian; Liu, Ngai; Dreyfus, Jean-François; Fischler, Marc

    2010-08-01

    Nerve stimulation is an effective technique for peripheral nerve blockade. However, the local anesthetic (LA) distribution pattern obtained with this blind approach is unknown and may explain its clinical effects. One hundred patients received a median nerve block at the elbow using a nerve stimulator approach. After correct needle placement defined by a minimal stimulating current < or = 0.5 mA (2 Hz, 0.1 millisecond), 6 mL lidocaine 1.5%with epinephrine 1:200,000 was injected. A linear 5- to 13-MHz probe (12L-RS) was used to assess a cross-section area of median nerve, which was calculated by 3 consecutive measurements before and after injection, and LA circumferential spread around the nerve during static and longitudinal examination. Intraneural injection defined as an increase in nerve area was detected using an iterative method for outlier detection. Results of sensory tests (cold and light touch) on 3 nerve territories and of motor blockade were compared with the imaging aspects. We performed clinical neurological examination at 3 days and 1 month after block. Nerve swelling, considered significant when an increase in cross-sectional area was > or = 75%, was observed in 43 patients. Nerve swelling associated with a circumferential LA spread image, present in 37 patients, was associated with a sensory success rate of 86%. The success rate was 34% for 32 patients in whom none of these signs was visualized. A circumferential spread around a nonswollen nerve, present in 25 patients, was followed by a sensory success rate of 76% within the 30-minute evaluation period. No major early neurological complications were observed. Nerve stimulation does not prevent intraneural injection. In the absence of intraneural injection, the presence of circumferential LA spread image seemed predictive of successful sensory block in almost 75% of the cases within the 30-minute evaluation period.

  20. Mutations in the transmembrane helix S6 of domain IV confer cockroach sodium channel resistance to sodium channel blocker insecticides and local anesthetics.

    PubMed

    Jiang, Dingxin; Du, Yuzhe; Nomura, Yoshiko; Wang, Xingliang; Wu, Yidong; Zhorov, Boris S; Dong, Ke

    2015-11-01

    Indoxacarb and metaflumizone are two sodium channel blocker insecticides (SCBIs). They preferably bind to and trap sodium channels in the slow-inactivated non-conducting state, a mode of action similar to that of local anesthetics (LAs). Recently, two sodium channel mutations, F1845Y (F(4i15)Y) and V1848I (V(4i18)I), in the transmembrane segment 6 of domain IV (IVS6), were identified to be associated with indoxacarb resistance in Plutella xylostella. F(4i15) is known to be critical for the action of LAs on mammalian sodium channels. Previously, mutation F(4i15)A in a cockroach sodium channel, BgNav1-1a, has been shown to reduce the action of lidocaine, a LA, but not the action of SCBIs. In this study, we introduced mutations F(4i15)Y and V(4i18)A/I individually into the cockroach sodium channel, BgNav1-1a, and conducted functional analysis of the three mutants in Xenopus oocytes. We found that both the F(4i15)Y and V(4i18)I mutations reduced the inhibition of sodium current by indoxacarb, DCJW (an active metabolite of indoxacarb) and metaflumizone. F(4i15)Y and V(4i18)I mutations also reduced the use-dependent block of sodium current by lidocaine. In contrast, substitution V(4i18)A enhanced the action metaflumizone and lidocaine. These results show that both F(4i15)Y and V(4i18)I mutations may contribute to target-site resistance to SCBIs, and provide the first molecular evidence for common amino acid determinants on insect sodium channels involved in action of SCBIs and LA. Copyright © 2015 Elsevier Ltd. All rights reserved.

  1. Tetrodotoxin-sensitive α-subunits of voltage-gated sodium channels are relevant for inhibition of cardiac sodium currents by local anesthetics.

    PubMed

    Stoetzer, C; Doll, T; Stueber, T; Herzog, C; Echtermeyer, F; Greulich, F; Rudat, C; Kispert, A; Wegner, F; Leffler, A

    2016-06-01

    The sodium channel α-subunit (Nav) Nav1.5 is regarded as the most prevalent cardiac sodium channel required for generation of action potentials in cardiomyocytes. Accordingly, Nav1.5 seems to be the main target molecule for local anesthetic (LA)-induced cardiotoxicity. However, recent reports demonstrated functional expression of several "neuronal" Nav's in cardiomyocytes being involved in cardiac contractility and rhythmogenesis. In this study, we examined the relevance of neuronal tetrodotoxin (TTX)-sensitive Nav's for inhibition of cardiac sodium channels by the cardiotoxic LAs ropivacaine and bupivacaine. Effects of LAs on recombinant Nav1.2, 1.3, 1.4, and 1.5 expressed in human embryonic kidney cell line 293 (HEK-293) cells, and on sodium currents in murine, cardiomyocytes were investigated by whole-cell patch clamp recordings. Expression analyses were performed by reverse transcription PCR (RT-PCR). Cultured cardiomyocytes from neonatal mice express messenger RNA (mRNA) for Nav1.2, 1.3, 1.5, 1.8, and 1.9 and generate TTX-sensitive sodium currents. Tonic and use-dependent block of sodium currents in cardiomyocytes by ropivacaine and bupivacaine were enhanced by 200 nM TTX. Inhibition of recombinant Nav1.5 channels was similar to that of TTX-resistant currents in cardiomyocytes but stronger as compared to inhibition of total sodium current in cardiomyocytes. Recombinant Nav1.2, 1.3, 1.4, and 1.5 channels displayed significant differences in regard to use-dependent block by ropivacaine. Finally, bupivacaine blocked sodium currents in cardiomyocytes as well as recombinant Nav1.5 currents significantly stronger in comparison to ropivacaine. Our data demonstrate for the first time that cardiac TTX-sensitive sodium channels are relevant for inhibition of cardiac sodium currents by LAs.

  2. Efficacy of subpleural continuous infusion of local anesthetics after thoracoscopic pulmonary resection for primary lung cancer compared to intravenous patient-controlled analgesia

    PubMed Central

    Jung, Joonho; Haam, Seokjin

    2016-01-01

    Background This study compared the efficacy and side effects of intravenous patient-controlled analgesia (IV-PCA) with those of a subpleural continuous infusion of local anesthetic (ON-Q system) in patients undergoing thoracoscopic pulmonary resection for primary lung cancer. Methods We retrospectively reviewed 66 patients who underwent thoracoscopic pulmonary resection for primary lung cancer from January 2014 to August 2015 (36 in the IV-PCA group and 30 in the ON-Q group). The numeric pain intensity scale (NPIS), additional IV injections for pain control, side effects, and early discontinuation of the pain control device were compared. Results There were no differences in the general characteristics of the two groups. The NPIS scores gradually decreased with time (P<0.001), but the two groups had differences in pattern of NPIS scores (P=0.111). There were no differences in the highest NPIS score during admission (4.75±2.35 vs. 5.27±1.87, P=0.334) or the number of additional IV injections for pain control in the same period (0.72±0.94 for IV-PCA vs. 0.83±0.65 for ON-Q; P=0.575). Side effects such as nausea, dizziness, and drowsiness were significantly more frequent with IV-PCA (36.1% vs. 10.0%, P=0.014), and early discontinuation of the pain control device was more frequent in the IV-PCA group (33.3% vs. 6.7%, P=0.008). Conclusions The ON-Q system was equivalent to the IV-PCA for postoperative pain control after thoracoscopic pulmonary resection for primary lung cancer, and it also had fewer effects and early discontinuations. PMID:27499973

  3. Mutations M287L and Q266I in the Glycine Receptor α1 Subunit Change Sensitivity to Volatile Anesthetics in Oocytes and Neurons, but Not the Minimal Alveolar Concentration in Knockin Mice

    PubMed Central

    Borghese, Cecilia M.; Xiong, Wei; Oh, S. Irene; Ho, Angel; Mihic, S. John; Zhang, Li; Lovinger, David M.; Homanics, Gregg E.; Eger, Edmond I; Harris, R. Adron

    2012-01-01

    Background Volatile anesthetics (VAs) alter the function of key central nervous system proteins but it is not clear which, if any, of these targets mediates the immobility produced by VAs in the face of noxious stimulation. A leading candidate is the glycine receptor, a ligand-gated ion channel important for spinal physiology. VAs variously enhance such function, and blockade of spinal GlyRs with strychnine affects the minimal alveolar concentration (an anesthetic EC50) in proportion to the degree of enhancement. Methods We produced single amino acid mutations into the glycine receptorα1 subunit that increased (M287L, third transmembrane region) or decreased (Q266I, second transmembrane region) sensitivity to isoflurane in recombinant receptors, and introduced such receptors into mice. The resulting knockin mice presented impaired glycinergic transmission, but heterozygous animals survived to adulthood, and we determined the effect of isoflurane on glycine-evoked responses of brain stem neurons from the knockin mice, and the minimal alveolar concentration for isoflurane and other VAs in the immature and mature knockin mice. Results Studies of glycine-evoked currents in brain stem neurons from knock-in mice confirmed the changes seen with recombinant receptors. No increases in the minimal alveolar concentration were found in knockin mice, but the minimal alveolar concentration for isoflurane and enflurane (but not halothane) decreased in 2-week-old Q266I mice. This change is opposite to the one expected for a mutation that decreases the sensitivity to volatile anesthetics. Conclusion Taken together, these results indicate that glycine receptors containing the α1 subunit are not likely to be crucial for the action of isoflurane and other VAs. PMID:22885675

  4. Evaluation of Efficacy of Bone Scan With SPECT/CT in the Management of Low Back Pain: A Study Supported by Differential Diagnostic Local Anesthetic Blocks.

    PubMed

    Jain, Anuj; Jain, Suruchi; Agarwal, Anil; Gambhir, Sanjay; Shamshery, Chetna; Agarwal, Amita

    2015-12-01

    Conventional radiologic modalities provide details only about the anatomic aspect of the various structures of the spine. Frequently the structures that show abnormal morphology may not be the cause of low back pain (LBP). Functional imaging in the form of bone scan along with single photon emission computerized tomography (SPECT/CT) may be helpful in identifying structures causing pain, whether morphologically normal or not. The objective of this study is to evaluate the role of bone scan with SPECT/CT in management of patients with LBP. This is randomized double-blinded controlled study performed on 80 patients with LBP aged 20 to 80 years, ASA physical status I to III. Patients were randomized into bone scan and control groups consisting of 40 patients each. On the basis of the clinical features and radiologic findings a clinical diagnosis was made. After making a clinical diagnosis, the patients in bone scan group were subjected to bone scan with SPECT/CT. On the basis of the finding of the bone scan and SPECT/CT, a new working diagnosis was made and intervention was performed according to the new working diagnosis. Diagnostic blocks in the control group were given based on clinical diagnosis. Controlled comparative diagnostic blocks were performed with local anesthetic. The pain score just after the diagnostic block and at the time of discharge (approximately 4 h later) was recorded; the pain relief was recorded in percentage. In both the groups, sacroilitis was the most common diagnosis followed by facet joint arthropathy. The number of patients obtaining pain relief of >50% was significantly higher in the bone scan-positive group as compared with the control group. Three new clinical conditions were identified in the bone scan group. These conditions were multiple myeloma, avascular necrosis of the femoral head, and ankylosing spondylitis. Bone scan with SPECT/CT was found to complement the clinical workup of patients with LBP. Inclusion of bone scan with

  5. A critical residue for isoform difference in tetrodotoxin affinity is a molecular determinant of the external access path for local anesthetics in the cardiac sodium channel

    PubMed Central

    Sunami, Akihiko; Glaaser, Ian W.; Fozzard, Harry A.

    2000-01-01

    Membrane-impermeant quaternary derivatives of lidocaine (QX222 and QX314) block cardiac Na+ channels when applied from either side of the membrane, but they block neuronal and skeletal muscle channels poorly from the outside. To find the molecular determinants of the cardiac external QX access path, mutations of adult rat skeletal muscle (μ1) and rat heart (rH1) Na+ channels were studied by two-electrode voltage clamp in Xenopus oocytes. Mutating the μ1 domain I P-loop Y401, which is the critical residue for isoform differences in tetrodotoxin block, to the heart sequence (Y401C) allowed outside QX222 block, but its mutation to brain type (Y401F) showed little block. μ1-Y401C accelerated recovery from block by internal QX222. Block by external QX222 in μ1-Y401C was diminished by chemical modification with methanethiosulfonate ethylammonium (MTSEA) to the outer vestibule or by a double mutant (μ1-Y401C/F1579A), which altered the putative local anesthetic binding site. The reverse mutation in heart rH1-C374Y reduced outside QX314 block and slowed dissociation of internal QX222. Mutation of μ1-C1572 in IVS6 to Thr, the cardiac isoform residue (C1572T), allowed external QX222 block, and accelerated recovery from internal QX222 block, as reported. Blocking efficacy of outside QX222 in μ1-Y401C was more than that in μ1-C1572T, and the double mutant (μ1-Y401C/C1572T) accelerated internal QX recovery more than μ1-Y401C or μ1-C1572T alone. We conclude that the isoform-specific residue (Tyr/Phe/Cys) in the P-loop of domain I plays an important role in drug access as well as in tetrodotoxin binding. Isoform-specific residues in the IP-loop and IVS6 determine outside drug access to an internal binding site. PMID:10681444

  6. Anesthetic Diffusion Through Lipid Membranes Depends on the Protonation Rate

    PubMed Central

    Pérez-Isidoro, Rosendo; Sierra-Valdez, F. J.; Ruiz-Suárez, J. C.

    2014-01-01

    Hundreds of substances possess anesthetic action. However, despite decades of research and tests, a golden rule is required to reconcile the diverse hypothesis behind anesthesia. What makes an anesthetic to be local or general in the first place? The specific targets on proteins, the solubility in lipids, the diffusivity, potency, action time? Here we show that there could be a new player equally or even more important to disentangle the riddle: the protonation rate. Indeed, such rate modulates the diffusion speed of anesthetics into lipid membranes; low protonation rates enhance the diffusion for local anesthetics while high ones reduce it. We show also that there is a pH and membrane phase dependence on the local anesthetic diffusion across multiple lipid bilayers. Based on our findings we incorporate a new clue that may advance our understanding of the anesthetic phenomenon. PMID:25520016

  7. Anesthetic diffusion through lipid membranes depends on the protonation rate.

    PubMed

    Pérez-Isidoro, Rosendo; Sierra-Valdez, F J; Ruiz-Suárez, J C

    2014-12-18

    Hundreds of substances possess anesthetic action. However, despite decades of research and tests, a golden rule is required to reconcile the diverse hypothesis behind anesthesia. What makes an anesthetic to be local or general in the first place? The specific targets on proteins, the solubility in lipids, the diffusivity, potency, action time? Here we show that there could be a new player equally or even more important to disentangle the riddle: the protonation rate. Indeed, such rate modulates the diffusion speed of anesthetics into lipid membranes; low protonation rates enhance the diffusion for local anesthetics while high ones reduce it. We show also that there is a pH and membrane phase dependence on the local anesthetic diffusion across multiple lipid bilayers. Based on our findings we incorporate a new clue that may advance our understanding of the anesthetic phenomenon.

  8. Concentrating entanglement by local actions: Beyond mean values

    NASA Astrophysics Data System (ADS)

    Lo, Hoi-Kwong; Popescu, Sandu

    2001-02-01

    Suppose two distant observers Alice and Bob share a pure bipartite quantum state. By applying local operations and communicating with each other using a classical channel, Alice and Bob can manipulate it into some other states. Previous investigations of entanglement manipulations have been largely limited to a small number of strategies and their average outcomes. Here we consider a general entanglement manipulation strategy, and go beyond the average property. For a pure entangled state shared between two separated persons Alice and Bob, we show that the mathematical interchange symmetry of the Schmidt decomposition can be promoted into a physical symmetry between the actions of Alice and Bob. Consequently, the most general (multistep two-way-communications) strategy of entanglement manipulation of a pure state is, in fact, equivalent to a strategy involving only a single (generalized) measurement by Alice followed by one-way communications of its result to Bob. We also prove that strategies with one-way communications are generally more powerful than those without communications. In summary, one-way communications is necessary and sufficient for entanglement manipulations of a pure bipartite state. The supremum probability of obtaining a maximally entangled state (of any dimension) from an arbitrary state is determined, and a strategy for achieving this probability is constructed explicitly. One important question is whether collective manipulations in quantum mechanics can greatly enhance the probability of large deviations from the average behavior. We answer this question in the negative by showing that, given n pairs of identical partly entangled pure states (\\|Ψ>) with entropy of entanglement E(\\|Ψ>), the probability of getting nK [K>E(\\|Ψ>)] singlets out of entanglement concentration tends to zero as n tends to infinity.

  9. [Brain protection by anesthetics].

    PubMed

    Adachi, Naoto

    2006-05-01

    Many investigators have attempted to protect the brain against ischemia by reducing the cerebral metabolic rate using anesthetic agents. However, the magnitude of suppression of the cerebral metabolic rate does not correlate with neuroprotective effects of anesthetics, suggesting that other factors besides reduction in the cerebral metabolic rate contribute to the protection. Facilitation of protein synthesis, GABAergic activity, and anti-oxidant action are likely factors responsible for beneficial effects of barbiturates and propofol. Although the brain is protected during anesthesia, anesthetics cannot provide effects sufficiently enough to recover damage caused by severe ischemia. Further, no desired outcome has been reported by treatments after ischemic events.

  10. Comparative analysis of tissue reactions to anesthetic solutions: histological analysis in subcutaneous tissue of rats.

    PubMed Central

    Ribeiro, Paulo Domingos; Sanches, Marcio Giampietro; Okamoto, Tetuo

    2003-01-01

    Postanesthetic pain is a relatively common complication after local anesthesia. This complication may be caused by the anesthetic technique or by the anesthetic solution used. Tissue reactions induced by the anesthetic solutions may be one of the factors resulting in pain after anesthesia. The objective of this study was to comparatively analyze tissue reactions induced by different anesthetic solutions in the subcutaneous tissue of rats. The following solutions were utilized: 2% lidocaine without vasoconstrictor; a 0.5% bupivacaine solution with 1:200,000 adrenaline; a 4% articaine solution and 2% mepivacaine, both with 1:100,000 adrenaline; and a 0.9% sodium chloride solution as a control. Sterilized absorbent paper cones packed inside polyethylene tubes were soaked in the solutions and implanted in the subcutaneous region. The sacrifice periods were 1, 2, 5, and 10 days after surgery. The specimens were prepared and stained with hematoxylin and eosin for histological analysis. The results showed that there is a difference in tissue irritability produced by the local anesthetic solutions. The results also showed that there is no relation between the concentration of the drug and the inflammatory intensity, that the mepivacaine and articaine solutions promoted less inflammatory reaction than the bupivacaine, and that the lidocaine solution produced the least intense inflammation. Images Figure 1 Figure 2 Figure 3 Figure 4 Figure 5 Figure 6 Figure 7 Figure 8 Figure 9 Figure 10 Figure 11 PMID:14959905

  11. Effects of using the posterior or anterior approaches to the lumbar plexus on the minimum effective anesthetic concentration (MEAC) of mepivacaine required to block the femoral nerve: a prospective, randomized, up-and-down study.

    PubMed

    Cappelleri, Gianluca; Aldegheri, Giorgio; Ruggieri, Francesco; Carnelli, Franco; Fanelli, Andrea; Casati, Andrea

    2008-01-01

    To evaluate if psoas compartment block requires a larger concentration of mepivacaine to block the femoral nerve than does an anterior 3-in-1 femoral nerve block. Forty eight patients undergoing anterior cruciate ligament repair were randomly allocated to receive an anterior 3-in-1 femoral block (femoral group, n = 24) or a posterior psoas compartment block (psoas group, n = 24) with 30 mL of mepivacaine. The concentration of the injected solution was varied for consecutive patients using an up-and-down staircase method (initial concentration: 1%; up-and-down steps: 0.1%). The minimum effective anesthetic concentration of mepivacaine blocking the femoral nerve in 50% of cases (ED(50)) was 1.06% +/- 0.31% (95% confidence interval [CI], 0.45%-1.68%) in the femoral group and 1.03% +/- 0.21% (95% CI, 0.6%-1.45%) in the psoas group (P = .83). The lateral femoral cutaneous and obturator nerves were blocked in 4 (16%) and 5 (20%) femoral group patients as compared with 20 (83%) and 19 (80%) psoas group patients (P = .005 and P = .0005, respectively). Intraoperative analgesic supplementation was required by 15 (60%) and 5 (20%) patients in the femoral and psoas groups, respectively (P = .01). Using a posterior psoas compartment approach to the lumbar plexus does not increase the minimum effective anesthetic concentration of mepivacaine required to block the femoral nerve as compared with the anterior 3-in-1 approach, and provides better quality of intraoperative anesthesia due to the more reliable block of the lateral femoral cutaneous and obturator nerves.

  12. [Effective volume of local anesthetics for fascia iliac compartment block: a double-blind, comparative study between 0.5% ropivacaine and 0.5% bupivacaine.].

    PubMed

    Helayel, Pablo Escovedo; Lobo, Giovanni; Vergara, Roberta; Conceição, Diogo Brüggemann da; Oliveira Filho, Getúlio Rodrigues de

    2006-10-01

    Fascia iliac compartment block is widely used as one of the anesthetic techniques used for surgical interventions of the hip, thigh, and knee. The majority of the studies have used fixed volumes of ropivacaine or bupivacaine. The objective of this study was to calculate the effective volume of 0.5% ropivacaine and 0.5% bupivacaine in 50% (EV50%), 95% (EV95), and 99% (EV99) of the cases to achieve fascia iliac compartment block. Fifty-one adults scheduled for elective surgical interventions of the hip, femoral diaphysis, and knee underwent fascia iliac compartment block. Patients were randomly assigned to receive either 0.5% ropivacaine (n = 25) or 0.5% bupivacaine (n = 26). The success of the block was defined as a complete sensitive block of the anterior, medial, and lateral regions of the thigh. The volume of the anesthetic was determined by Massey and Dixon's up-and-down method, while the effective volume was calculated by Massey and Dixon's formula (EV50) and by probits regression (EV50, EV95, and EV99). The volume of anesthetic capable of producing an effective nervous anesthesia in 50% of the cases, calculated by Massey and Dixon formula, were 28.79 mL (CI 95%: 26.31 - 31.5 mL) for ropivacaine, and 29.56 mL (CI 95%: 25.22 - 34.64 mL) for bupivacaine (p = 0.62). The effective volumes of ropivacaine capable of producing a blocking in 50%, 95%, and 99% of the cases were estimated by probits regression as 28.8 mL (27.2 - 30.4), 34.3 mL (32.5 - 37.3), and 36.6 mL (34.3 - 40.5), respectively. The corresponding volumes of bupivacaine were 29.5 mL (28.1 - 31.1), 36.1 mL (33.5 - 38.1), and 37.3 mL (35.1 - 41.3) (p > 0.05). The volumes of 0.5% ropivacaine and 0.5% bupivacaine with adrenaline 1:200,000 for the fascia iliac block are similar.

  13. Neurometric assessment of intraoperative anesthetic

    DOEpatents

    Kangas, Lars J.; Keller, Paul E.

    1998-01-01

    The present invention is a method and apparatus for collecting EEG data, reducing the EEG data into coefficients, and correlating those coefficients with a depth of unconsciousness or anesthetic depth, and which obtains a bounded first derivative of anesthetic depth to indicate trends. The present invention provides a developed artificial neural network based method capable of continuously analyzing EEG data to discriminate between awake and anesthetized states in an individual and continuously monitoring anesthetic depth trends in real-time. The present invention enables an anesthesiologist to respond immediately to changes in anesthetic depth of the patient during surgery and to administer the correct amount of anesthetic.

  14. Neurometric assessment of intraoperative anesthetic

    DOEpatents

    Kangas, L.J.; Keller, P.E.

    1998-07-07

    The present invention is a method and apparatus for collecting EEG data, reducing the EEG data into coefficients, and correlating those coefficients with a depth of unconsciousness or anesthetic depth, and which obtains a bounded first derivative of anesthetic depth to indicate trends. The present invention provides a developed artificial neural network based method capable of continuously analyzing EEG data to discriminate between awake and anesthetized states in an individual and continuously monitoring anesthetic depth trends in real-time. The present invention enables an anesthesiologist to respond immediately to changes in anesthetic depth of the patient during surgery and to administer the correct amount of anesthetic. 7 figs.

  15. Common medical illnesses that affect anesthesia and their anesthetic management.

    PubMed

    Agarwal, Ravi; Porter, Michael H; Obeid, George

    2013-08-01

    Patients undergoing an office-based anesthetic require a thorough preoperative evaluation to identify medical illnesses and undertake appropriate investigations or studies. This article addresses common medical illnesses seen in oral surgery offices and provides insight into their anesthetic management, concentrating on open-airway office-based anesthesia. Copyright © 2013 Elsevier Inc. All rights reserved.

  16. 40 CFR 52.1164 - Localized high concentrations-carbon monoxide.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 4 2010-07-01 2010-07-01 false Localized high concentrations-carbon... Localized high concentrations—carbon monoxide. (a) Not later than October 1, 1975, the Commonwealth shall... quality standards for carbon monoxide. Once such localized areas have been identified, the...

  17. 40 CFR 52.1164 - Localized high concentrations-carbon monoxide.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 4 2013-07-01 2013-07-01 false Localized high concentrations-carbon... Localized high concentrations—carbon monoxide. (a) Not later than October 1, 1975, the Commonwealth shall... quality standards for carbon monoxide. Once such localized areas have been identified, the...

  18. 40 CFR 52.1164 - Localized high concentrations-carbon monoxide.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 4 2011-07-01 2011-07-01 false Localized high concentrations-carbon... Localized high concentrations—carbon monoxide. (a) Not later than October 1, 1975, the Commonwealth shall... quality standards for carbon monoxide. Once such localized areas have been identified, the...

  19. 40 CFR 52.1164 - Localized high concentrations-carbon monoxide.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 4 2012-07-01 2012-07-01 false Localized high concentrations-carbon... Localized high concentrations—carbon monoxide. (a) Not later than October 1, 1975, the Commonwealth shall... quality standards for carbon monoxide. Once such localized areas have been identified, the...

  20. 40 CFR 52.1164 - Localized high concentrations-carbon monoxide.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 4 2014-07-01 2014-07-01 false Localized high concentrations-carbon... Localized high concentrations—carbon monoxide. (a) Not later than October 1, 1975, the Commonwealth shall... quality standards for carbon monoxide. Once such localized areas have been identified, the...

  1. Use of anesthetics associated to vasoconstrictors for dentistry in patients with cardiopathies. Review of the literature published in the last decade.

    PubMed

    Serrera Figallo, María A; Velázquez Cayón, Rocío T; Torres Lagares, Daniel; Corcuera Flores, Jose R; Machuca Portillo, Guillermo

    2012-04-01

    The use of local anesthetics associated to vasoconstrictor agents in dentistry is thoroughly justified and is widely extended, but we cannot ignore the fact that anesthetic infiltration poses risk of complications throughout the dental treatment period. The objective of the present review is to document the reported effects the use of the local anesthetics most widely employed in dentistry, with or without association to vasoconstrictor agents may have in patients with any sort of cardiopathy. We have searched for randomized clinical trials on the assessment of the cardiovascular effects of local anesthetics used in dentistry, without limits as regards age or sex, conducted in patients with any type of cardiopathy which were published during the last decade and were index-linked in Cochrane, Embase and Medline. We have found six randomized clinical trials index-linked in Medline and Cochrane in the past ten years. These trials compare different types of anesthetics: lidocaine 2%, mepivacaine 2%, prilocaine 2% , associated or not to different vasoconstrictor concentrations such as adrenaline or felypressin. The cardiopathies affecting the patients included in the different trials range from hypertension, ischemic heart disease, arrythmias, chronic coronary disease to heart transplantation. The use of anesthetics associated to vasoconstrictor agents is justified in the case of patients with cardiopathies (once we get over the period in which any type of dental manipulation is contraindicated) and in controlled hypertensive patients. In any case, we must be very careful with the choice and execution of the anesthetic technique, being it possible to use a dose between 1.8 and 3.6 ml, on a general basis. Further studies are necessary to establish the effects of these drugs on severe hypertensive patients or in patients with other more advanced cardiopathies. Key words:Vasoconstrictor agents, epinephrine/adverse effects, local anesthetics, dental restoration, oral

  2. Use of anesthetics associated to vasoconstrictors for dentistry in patients with cardiopathies. Review of the literature published in the last decade

    PubMed Central

    Serrera Figallo, María A.; Velázquez Cayón, Rocío T.; Corcuera Flores, Jose R.; Machuca Portillo, Guillermo

    2012-01-01

    Objective: The use of local anesthetics associated to vasoconstrictor agents in dentistry is thoroughly justified and is widely extended, but we cannot ignore the fact that anesthetic infiltration poses risk of complications throughout the dental treatment period. The objective of the present review is to document the reported effects the use of the local anesthetics most widely employed in dentistry, with or without association to vasoconstrictor agents may have in patients with any sort of cardiopathy. Study Design: We have searched for randomized clinical trials on the assessment of the cardiovascular effects of local anesthetics used in dentistry, without limits as regards age or sex, conducted in patients with any type of cardiopathy which were published during the last decade and were index-linked in Cochrane, Embase and Medline. Results: We have found six randomized clinical trials index-linked in Medline and Cochrane in the past ten years. These trials compare different types of anesthetics: lidocaine 2%, mepivacaine 2%, prilocaine 2% , associated or not to different vasoconstrictor concentrations such as adrenaline or felypressin. The cardiopathies affecting the patients included in the different trials range from hypertension, ischemic heart disease, arrythmias, chronic coronary disease to heart transplantation. Conclusions: The use of anesthetics associated to vasoconstrictor agents is justified in the case of patients with cardiopathies (once we get over the period in which any type of dental manipulation is contraindicated) and in controlled hypertensive patients. In any case, we must be very careful with the choice and execution of the anesthetic technique, being it possible to use a dose between 1.8 and 3.6 ml, on a general basis. Further studies are necessary to establish the effects of these drugs on severe hypertensive patients or in patients with other more advanced cardiopathies. Key words:Vasoconstrictor agents, epinephrine/adverse effects

  3. Determinants of volatile general anesthetic potency: a preliminary three-dimensional pharmacophore for halogenated anesthetics.

    PubMed

    Sewell, Jason C; Sear, John W

    2006-03-01

    We investigated the molecular basis for the immobilizing activity of halogenated volatile anesthetics using comparative molecular field analysis. In vivo potency data (expressed as minimum alveolar concentrations) for 69 structurally diverse anesthetics were obtained from the literature. The drugs were randomly divided into a training set (n = 52) used to derive the activity model and a test set (n = 17) used to independently assess the model's predictive power. The anesthetic structures were aligned so as to maximize their similarity in molecular shape and electrostatic potential to the most potent drug in the group, CF2H-(CF2)3-CH2OH. The conformers and alignments of the anesthetics with maximum similarity (calculated as Carbo indices) were retained and used to derive the comparative molecular field analysis models. The final model explained 94.2% of the variance in the observed activities of the training set compounds. The model showed good predictive capability for both the training set (cross-validated r2 = 0.705) and randomly excluded test set anesthetics (r2 = 0.837). Three-dimensional pharmacophoric maps were derived to identify the spatial distribution of key areas where steric and electrostatic interactions are important in determining immobilizing activity of the halogenated drugs and were compared with our previously published maps obtained for nonhalogenated volatile anesthetics.

  4. [Nine Biblical anesthetic premises.].

    PubMed

    Vale, Nilton Bezerra do; Delfino, José

    2003-02-01

    The authors produced a historical analysis of nine anesthesia-related premises described in the Bible more than 3,500 years ago (Old Testament). Anesthetic drugs and adjuvants, patients, anesthesiologists attitudes and techniques are discussed in the light of Biblical and modern science. To help understanding, the nine premises evaluated are correlated to the book of Bible citation: I - Jehovah, the pioneer of inhalational anesthesia - Gen 2; II - Alcoholic hypnosis and anesthesia - Prov 20, Gen 19, Marc 15; III - Anesthesia-related Chaos and Chronobiology - Gen 1, Ecles 3; IV - Anesthetic drugs Stereoisomerism - Ecle 42, Gen 1; V - Elijah s and Elisha s cardiopulmonary resuscitation - Gen 2, Kings III 17, Kings IV 4; VI - Tocoanalgesia - Gen 3, Rev 12, Gen 35 and Rachels post-partum death - Ex 1; VII - Jehovah s witnesses interpretation of blood transfusion forbiddance - Lev 7,17; VIII - Acidosis for epileptic seizure treatment - Math 17; IX - Death on the cross by hypovolemic shock - Marc 15, John 19. According to the anesthetic premises discussed, Holy Bible reading without fundamentalism shows no incompatibility between religion, science and anesthesia, except for Jehovah,s witnesses interpretation of Leviticus VII-XVII, by which they would lose eternal life because transfused blood is an impure food forbidden by Jehovah.

  5. Relationships of local lithium concentrations in drinking water to regional suicide rates in Italy.

    PubMed

    Pompili, Maurizio; Vichi, Monica; Dinelli, Enrico; Pycha, Roger; Valera, Paolo; Albanese, Stefano; Lima, Annamaria; De Vivo, Benedetto; Cicchella, Domenico; Fiorillo, Andrea; Amore, Mario; Girardi, Paolo; Baldessarini, Ross J

    2015-01-01

    Higher natural concentrations of lithium in drinking water may be associated with lower local rates of suicide. Lithium concentrations in drinking water were assayed by mass spectrometry at 145 sites in Italy, and compared with reported local suicide rates for men and women between 1980 and 2011. Lithium concentrations in drinking water averaged 5.28 [CI: 4.08-6.48] μg/L (0.761 [0.588-0.934] μEq/L) and ranged from 0.110 to 60.8 μg/L (1.58 to 8.76 μEq/L). Lithium concentrations and local suicide rates were not significantly inversely related, except in 1980-1989, particularly among women. A proposed association between trace lithium concentrations in drinking water and risk of suicide was only partially supported, and mechanisms for potential clinical effects of trace levels of lithium are unknown.

  6. Renin dynamics in adipose tissue: adipose tissue control of local renin concentrations.

    PubMed

    Fowler, Jason D; Krueth, Stacy B; Bernlohr, David A; Katz, Stephen A

    2009-02-01

    The renin-angiotensin system (RAS) has been implicated in a variety of adipose tissue functions, including tissue growth, differentiation, metabolism, and inflammation. Although expression of all components necessary for a locally derived adipose tissue RAS has been demonstrated within adipose tissue, independence of local adipose RAS component concentrations from corresponding plasma RAS fluctuations has not been addressed. To analyze this, we varied in vivo rat plasma concentrations of two RAS components, renin and angiotensinogen (AGT), to determine the influence of their plasma concentrations on adipose and cardiac tissue levels in both perfused (plasma removed) and nonperfused samples. Variation of plasma RAS components was accomplished by four treatment groups: normal, DOCA salt, bilateral nephrectomy, and losartan. Adipose and cardiac tissue AGT concentrations correlated positively with plasma values. Perfusion of adipose tissue decreased AGT concentrations by 11.1%, indicating that adipose tissue AGT was in equilibrium with plasma. Cardiac tissue renin levels positively correlated with plasma renin concentration for all treatments. In contrast, adipose tissue renin levels did not correlate with plasma renin, with the exception of extremely high plasma renin concentrations achieved in the losartan-treated group. These results suggest that adipose tissue may control its own local renin concentration independently of plasma renin as a potential mechanism for maintaining a functional local adipose RAS.

  7. Local Labor Market Characteristics and the Occupational Concentration of Different Sociodemographic Groups.

    ERIC Educational Resources Information Center

    Bloomquist, Leonard E.

    1990-01-01

    Analyzes concentration of employment opportunities for different socioeconomic groups in different local labor-market areas (LMAs). Uses regression analysis of 1980 census data. Finds rural LMAs offer fewer opportunities. Gender differences in occupational concentrations relate to industrial composition of labor market. Racial difference is…

  8. Medullary norepinephrine neurons modulate local oxygen concentrations in the bed nucleus of the stria terminalis

    PubMed Central

    Bucher, Elizabeth S; Fox, Megan E; Kim, Laura; Kirkpatrick, Douglas C; Rodeberg, Nathan T; Belle, Anna M; Wightman, R  Mark

    2014-01-01

    Neurovascular coupling is understood to be the underlying mechanism of functional hyperemia, but the actions of the neurotransmitters involved are not well characterized. Here we investigate the local role of the neurotransmitter norepinephrine in the ventral bed nucleus of the stria terminalis (vBNST) of the anesthetized rat by measuring O2, which is delivered during functional hyperemia. Extracellular changes in norepinephrine and O2 were simultaneously monitored using fast-scan cyclic voltammetry. Introduction of norepinephrine by electrical stimulation of the ventral noradrenergic bundle or by iontophoretic ejection induced an initial increase in O2 levels followed by a brief dip below baseline. Supporting the role of a hyperemic response, the O2 increases were absent in a brain slice containing the vBNST. Administration of selective pharmacological agents demonstrated that both phases of this response involve β-adrenoceptor activation, where the delayed decrease in O2 is sensitive to both α- and β-receptor subtypes. Selective lesioning of the locus coeruleus with the neurotoxin DSP-4 confirmed that these responses are caused by the noradrenergic cells originating in the nucleus of the solitary tract and A1 cell groups. Overall, these results support that non-coerulean norepinephrine release can mediate activity-induced O2 influx in a deep brain region. PMID:24714037

  9. Comparison of the efficacy and safety of 2% lidocaine HCl with different epinephrine concentration for local anesthesia in participants undergoing surgical extraction of impacted mandibular third molars: A multicenter, randomized, double-blind, crossover, phase IV trial.

    PubMed

    Karm, Myong-Hwan; Park, Fiona Daye; Kang, Moonkyu; Kim, Hyun Jeong; Kang, Jeong Wan; Kim, Seungoh; Kim, Yong-Deok; Kim, Cheul-Hong; Seo, Kwang-Suk; Kwon, Kyung-Hwan; Kim, Chul-Hwan; Lee, Jung-Woo; Hong, Sung-Woon; Lim, Mi Hyoung; Nam, Seung Kwan; Cho, Jae Min

    2017-05-01

    The most commonly impacted tooth is the third molar. An impacted third molar can ultimately cause acute pain, infection, tumors, cysts, caries, periodontal disease, and loss of adjacent teeth. Local anesthesia is employed for removing the third molar. This study aimed to evaluate the efficacy and safety of 2% lidocaine with 1:80,000 or 1:200,000 epinephrine for surgical extraction of bilateral impacted mandibular third molars. Sixty-five healthy participants underwent surgical extraction of bilateral impacted mandibular third molars in 2 separate visits while under local anesthesia with 2% lidocaine with different epinephrine concentration (1:80,000 or 1:200,000) in a double-blind, randomized, crossover trial. Visual analog scale pain scores obtained immediately after surgical extraction were primarily evaluated for the 2 groups receiving different epinephrine concentrations. Visual analog scale pain scores were obtained 2, 4, and 6 hours after administering an anesthetic. Onset and duration of analgesia, onset of pain, intraoperative bleeding, operator's and participant's overall satisfaction, drug dosage, and hemodynamic parameters were evaluated for the 2 groups. There were no statistically significant differences between the 2 groups in any measurements except hemodynamic factors (P >.05). Changes in systolic blood pressure and heart rate following anesthetic administration were significantly greater in the group receiving 1:80,000 epinephrine than in that receiving 1:200,000 epinephrine (P ≤.01). The difference in epinephrine concentration between 1:80,000 and 1:200,000 in 2% lidocaine liquid does not affect the medical efficacy of the anesthetic. Furthermore, 2% lidocaine with 1:200,000 epinephrine has better safety with regard to hemodynamic parameters than 2% lidocaine with 1:80,000 epinephrine. Therefore, we suggest using 2% lidocaine with 1:200,000 epinephrine rather than 2% lidocaine with 1:80,000 epinephrine for surgical extraction of impacted

  10. Local anesthetis and adjuvants in pediatric regional anesthesia.

    PubMed

    Mossetti, Valeria; Vicchio, Noemi; Ivani, Giorgio

    2012-06-01

    The pediatric loco-regional techniques are considered very safe and effective, first of all because they target the therapy directly to the site of surgery, decreasing the risks of intravenous analgesia. The quality of local anesthesia is influenced by structural and biophysical characteristics of local anesthetics drug, dose, site of injection, mixture of local anesthetics and possible addition of a vasoconstrictor or an adjuvant to prolong the analgesic effect. In children, unlike adults, small nerve diameters and short distance between Ranvier nodes permit to use large volumes and low concentrations of local anesthetics. The clinical practice has shown that in pediatric population, effective analgesia is obtained by 1% mepivacaine, 1% lidocaine and 0.25% bupivacaine or better 0.2% ropivacaine, 0.2-0.25% levobupivacaine. In addition, levobupivacaine and ropivacaine have a better profile in terms of safety in comparison to bupivacaine and are the local anesthetics of choice for the daily clinical practice also in children as in adults. Among the adjuvant, clonidine and ketamine showed the best pharmacokinetic and pharmacodynamic profiles of effective and safety, improving and prolonging the action of associated local anesthetics. Therefore, the use of enantiomers, in association with adjuvants as clonidine or ketamine, using the multimodal approach of integrated anesthesia, makes the clinical practice effective and safe in the pediatric operating rooms. This review focuses on the overview of local anesthetics and adjuvants used today in locoregional pediatric anesthesia, with an emphasis on the advantages and disadvantages of each drug.

  11. Pain fiber anesthetic reduces brainstem Fos after tooth extraction.

    PubMed

    Badral, B; Davies, A J; Kim, Y H; Ahn, J S; Hong, S D; Chung, G; Kim, J S; Oh, S B

    2013-11-01

    We recently demonstrated that pain-sensing neurons in the trigeminal system can be selectively anesthetized by co-application of QX-314 with the TRPV1 receptor agonist, capsaicin (QX cocktail). Here we examined whether this new anesthetic strategy can block the neuronal changes in the brainstem following molar tooth extraction in the rat. Adult male Sprague-Dawley rats received infiltration injection of anesthetic 10 min prior to lower molar tooth extraction. Neuronal activation was determined by immunohistochemistry for the proto-oncogene protein c-Fos in transverse sections of the trigeminal subnucleus caudalis (Sp5C). After tooth extraction, c-Fos-like immunoreactivity (Fos-LI) detected in the dorsomedial region of bilateral Sp5C was highest at 2 hrs (p < .01 vs. naïve ipsilateral) and declined to pre-injury levels by 8 hrs. Pre-administration of the QX cocktail significantly reduced to sham levels Fos-LI examined 2 hrs after tooth extraction; reduced Fos-LI was also observed with the conventional local anesthetic lidocaine. Pulpal anesthesia by infiltration injection was confirmed by inhibition of the jaw-opening reflex in response to electrical tooth pulp stimulation. Our results suggest that the QX cocktail anesthetic is effective in reducing neuronal activation following tooth extraction. Thus, a selective pain fiber 'nociceptive anesthetic' strategy may provide an effective local anesthetic option for dental patients in the clinic.

  12. Post-operative pain control for burn reconstructive surgery in a resource-restricted country with subcutaneous infusion of local anesthetics through a soaker catheter to the surgical site: Preliminary results.

    PubMed

    Fuzaylov, Gennadiy; Kelly, Tara L; Bline, Cheryl; Dunaev, Alexander; Dylewski, Maggie L; Driscoll, Daniel N

    2015-12-01

    Post-operative pain can significantly affect a patient's ability to recover following surgery. In this study we introduced the concept of post-operative pain evaluation of burn patients as well as a technique for placement and use of subcutaneous catheters for continuous infusion of local anesthetic to provide analgesia following skin harvest from the lateral thigh in a hospital in resource-restricted country--Ukraine. A total of 109 patients were enrolled in this study. In the control group 64 patients received the standard post-operative pain regimen of metamizole 1 g and/or ketorolac 3%- 30 mg at the discretion of the nursing staff. In the interventional group, 45 patients received the catheter infusion of local anesthetic by elastomeric pump which was placed intraoperatively; it continuously delivers a regulated flow 4-5 ml/h of procaine 0.5% for 48 h to a patient's surgical donor site with the standard pain regimen available for breakthrough pain. All patients were assessed post-operatively and in the peri-dressing change period by the nursing staff. Blood pressure, heart rate, and pain scores were documented based on the Wong-Baker Faces Pain Rating Scale. All data were analyzed using SAS version 9.3. The Student's t test and Fisher's exact test were used to assess differences between groups for continuous variables. The Mann-Whitney U Test was used to examine differences in pain scores between groups. A p value of <0.05 was considered significant. The median pain score immediately following surgery was 5.0 in the control group, which was significantly greater (p=0.03) than median pain score of 4.0 for the patients receiving continuous infusion of procaine. However, there is no statistically significant difference in the median pain score (3.0 and 3.0) after the initial dressing change (p=0.73). Our Ukrainian colleagues now have a method of objective pain assessment and a new technique in pain management. With assessment linked to intervention, improvement in

  13. Vapor Pressures of Anesthetic Agents at Temperatures Below 0°C and a Novel Anesthetic Delivery Device.

    PubMed

    Schenning, Katie J; Casson, Henry; Click, Sarah V; Brambrink, Lucas; Chatkupt, Thomas T; Alkayed, Nabil J; Hutchens, Michael P

    2017-02-01

    At room temperature, the vapor pressures of desflurane, isoflurane, and sevoflurane are well above the clinically useful range. We hypothesized that therapeutic concentrations of these agents could be achieved at temperatures below 0°C, but the vapor pressure-temperature relationship is unknown below 0. Second, we hypothesized that this relationship could be exploited to deliver therapeutic-range concentrations of anesthetic vapor. We therefore set out to determine the low temperature-vapor pressure relationships of each anesthetic agent, thereby identifying the saturated vapor concentration of each agent at any temperature below 0°C. To test our hypothesis, we measured the saturated vapor concentration at 1 atm of pressure for temperatures between -60 and 0°C, thus developing an empiric relationship for each agent. There was consistency in repeated experiments for all 3 agents. To test the empiric data, we constructed a digitally controlled thermoelectric anesthetic vaporizer, characterized the device, and used it to deliver anesthetic vapor to laboratory mice. We report, for the first time, the temperature-vapor pressure relationship at temperatures below 0°C for desflurane, isoflurane, and sevoflurane as well as the TMAC of these agents: the temperature at which the vapor pressure is equal to the minimum alveolar concentration. We describe the construction and limited validation of an anesthetic vaporizer prototype on the basis of this principle. We conclude that clinically relevant concentrations of volatile anesthetics may be achieved at low temperatures.

  14. The influence of the local oxygen vacancy concentration on the piezoresponse of strontium titanate thin films

    NASA Astrophysics Data System (ADS)

    Andrä, Michael; Gunkel, Felix; Bäumer, Christoph; Xu, Chencheng; Dittmann, Regina; Waser, Rainer

    2015-08-01

    In this study, the influence of the local oxygen vacancy concentration on piezoresponse force microscopy (PFM) measurements was investigated. Ultra-thin single-crystalline SrTiO3 thin films were deposited on niobium doped SrTiO3 substrates and analyzed using a combined PFM and local conductive atomic force microscopy (LC-AFM) measurement setup. After applying different polarization voltages between +/-2 V and +/-5 V to the thin films, we simultaneously observed an anomalous contrast in the piezoresponse amplitude and phase signal as well as a changed local conductivity in the exact same region. Since classic ferroelectricity can be excluded as the reason for the observed contrast, an influence of the local oxygen vacancy concentration on the piezoresponse is considered. Additionally, the surface potential was measured using Kelvin probe force microscopy (KPFM) revealing a change in surface potential in the regions of the applied voltage. The observed relaxation of the surface potential over time was fitted to a local oxidation reaction of the previously reduced regions of the ultra-thin SrTiO3 film. We propose a model that relates the local oxygen vacancy concentration to the surface potential. The influence of the oxygen vacancy concentration on the PFM measurements is explained.

  15. Computational modeling of temperature elevation and thermoregulatory response in the brains of anesthetized rats locally exposed at 1.5 GHz

    NASA Astrophysics Data System (ADS)

    Hirata, Akimasa; Masuda, Hiroshi; Kanai, Yuya; Asai, Ryuichi; Fujiwara, Osamu; Arima, Takuji; Kawai, Hiroki; Watanabe, Soichi; Lagroye, Isabelle; Veyret, Bernard

    2011-12-01

    The dominant effect of human exposures to microwaves is caused by temperature elevation ('thermal effect'). In the safety guidelines/standards, the specific absorption rate averaged over a specific volume is used as a metric for human protection from localized exposure. Further investigation on the use of this metric is required, especially in terms of thermophysiology. The World Health Organization (2006 RF research agenda) has given high priority to research into the extent and consequences of microwave-induced temperature elevation in children. In this study, an electromagnetic-thermal computational code was developed to model electromagnetic power absorption and resulting temperature elevation leading to changes in active blood flow in response to localized 1.457 GHz exposure in rat heads. Both juvenile (4 week old) and young adult (8 week old) rats were considered. The computational code was validated against measurements for 4 and 8 week old rats. Our computational results suggest that the blood flow rate depends on both brain and core temperature elevations. No significant difference was observed between thermophysiological responses in 4 and 8 week old rats under these exposure conditions. The computational model developed herein is thus applicable to set exposure conditions for rats in laboratory investigations, as well as in planning treatment protocols in the thermal therapy.

  16. The effectiveness of diclofenac gel and eutectic mixture of local anesthetic cream on vein puncture pain severity with vein catheter in patient undergoing cesarean section: A randomized, double-blind, placebo-controlled trial.

    PubMed

    Khalili, Sediqeh; Safavi, Mahboubeh; Rezaei, Rozita; Bidmeshki, Maria; Shirzad, Fatemeh; Nasiri, Mostafa

    2014-09-01

    This study was aimed to explore the effect of applying diclofenac gel and a eutectic mixture of local anesthetic (EMLA) cream on vein puncture pain severity with vein catheter in the patients undergoing cesarean section. The sample comprised 90 women undergoing elective cesarean section that referred to Imam Ali Hospital's maternity section in Amol city (Northern Iran). Data collection tools included visual analog scale for pain severity and a checklist for short term possible side-effects of diclofenac gel, EMLA cream and Vaseline ointment as placebo. The pain of vein puncture with diclofenac gel and EMLA cream was significantly lower than that with the Vaseline ointment (P = 0.001). Similarly, there was a significant difference between using diclofenac gel and EMLA cream in catheter insertion pain severity (P = 0.006). In addition, there was no short term possible side-effect with using diclofenac gel and Vaseline ointment, but a short term side-effect (blanching) was detected in 20% of subjects with EMLA cream. Compared to Vaseline cream, EMLA cream and diclofenac gel application significantly reduces the pain severity associated with vein catheter insertion. Use of diclofenac gel is preferred compared with EMLA cream, because of economics, more efficiency purpose, and no side-effects.

  17. Intrinsic Organization of the Anesthetized Brain

    PubMed Central

    Liang, Zhifeng; King, Jean; Zhang, Nanyin

    2012-01-01

    The neural mechanism of unconsciousness has been a major unsolved question in neuroscience despite its vital role in brain states like coma and anesthesia. The existing literature suggests that neural connections, information integration and conscious states are closely related. Indeed, alterations in several important neural circuitries and networks during unconscious conditions have been reported. However, how the whole-brain network is topologically reorganized to support different patterns of information transfer at unconscious states remains unknown. Here we directly compared whole-brain neural networks in an awake and an anesthetized state in rodents. Consistent with our previous report, the awake rat brain was organized in a non-trivial manner and conserved fundamental topological properties as the human brain. Strikingly, these topological features were well maintained in the anesthetized brain. Meanwhile, local neural networks were reorganized with altered local network properties. The connectional strength between brain regions was also considerably different between the awake and anesthetized conditions. Interestingly, we found that long-distance connections were not preferentially reduced in the anesthetized condition, arguing against the hypothesis that loss of long-distance connections is characteristic to unconsciousness. These findings collectively show that the integrity of the whole-brain network can be conserved between widely dissimilar physiologic states while local neural networks can flexibly adapt to new conditions. They also illustrate that the governing principles of intrinsic brain organization might represent fundamental characteristics of the healthy brain. With the unique spatial and temporal scales of rsfMRI, this study has opened a new avenue for understanding the neural mechanism of (un)consciousness. PMID:22836253

  18. Molecularly imprinted polymer in microextraction by packed sorbent for the simultaneous determination of local anesthetics: lidocaine, ropivacaine, mepivacaine and bupivacaine in plasma and urine samples.

    PubMed

    Daryanavard, Seyed Mosayeb; Jeppsson-Dadoun, Amin; Andersson, Lars I; Hashemi, Mahdi; Colmsjö, Anders; Abdel-Rehim, Mohamed

    2013-11-01

    This study presents the use of molecularly imprinted polymer (MIP) as packing material for microextraction by packed syringe (MEPS) to achieve higher extraction selectivity. Pentycaine was used as template for MIP. Development and validation of the determination of lidocaine, ropivacaine, mepivacaine and bupivacaine in human plasma and urine samples utilizing MIP-MEPS and liquid chromatography-tandem mass spectrometry (LC-MS/MS) were carried out. The MEPS MIP-cartridge could be used for 100 extractions before it was discarded. The extraction recovery ranged from 60 to 80%. The correlation coefficients values were >0.999 for all assays using lidocaine, ropivacaine, mepivacaine and bupivacaine in the calibration range 5-2000 nmol/L. The accuracy of the studied compounds, given as a percentage variation from the nominal concentration values, ranged from -4.9 to 8.4% using plasma and urine samples. The between-batch precision, given as the relative standard deviation, at three different concentrations (quality control samples) was ranged from -4.7 to 14.0% and from 1.8 to 12.7% in plasma and urine, respectively. The lower limit of quantification and limit of detection of the studied substances were 5.0 and 1.0 nm, respectively. Copyright © 2013 John Wiley & Sons, Ltd.

  19. Anesthetic Requirement is Increased in Redheads

    PubMed Central

    Liem, Edwin B.; Lin, Chun–Ming; Suleman, Mohammad–Irfan; Doufas, Anthony G.; Gregg, Ronald G.; Veauthier, Jacqueline M.; Loyd, Gary

    2005-01-01

    Background: Age and body temperature alter inhalational anesthetic requirement; however, no human genotype is associated with inhalational anesthetic requirement. There is an anecdotal impression that anesthetic requirement is increased in redheads. Furthermore, red hair results from distinct mutations of the melanocortin-1 receptor. We thus tested the hypothesis that the requirement for the volatile anesthetic desflurane is greater in natural redhead than in dark-haired women. Methods: We studied healthy women with bright red (n=10) or dark (n=10) hair. Blood was sampled for subsequent analyses of melanocortin-1 receptor alleles. Anesthesia was induced with sevoflurane and maintained with desflurane randomly set at an end-tidal concentration between 5.5 and 7.5%. After an equilibration period, a noxious electrical stimulation (100 Hz, 70 mA) was transmitted through bilateral intradermal needles. If the volunteer moved in response to stimulation, desflurane was increased by 0.5%; otherwise it was decreased by 0.5%. This was continued until volunteers “crossed-over” from movement to non-movement (or vice versa) four times. Individual logistic regression curves were used to determine desflurane requirement (P50). Desflurane requirements in the two groups were compared using Mann-Whitney nonparametric two-sample test; P < 0.05 was considered statistically significant. Results: The desflurane requirement in redheads (6.2 volume-percent [95% CI, 5.9 - 6.5]) was significantly greater than in dark-haired women (5.2 volume-percent [4.9 – 5.5], P = 0.0004). Nine of 10 redheads were either homozygous or compound heterozygotes for mutations on the melanocortin-1 receptor gene. Conclusions: Red hair appears to be a distinct phenotype linked to anesthetic requirement in humans that can also be traced to a specific genotype. PMID:15277908

  20. Selected Antimicrobial Activity of Topical Ophthalmic Anesthetics

    PubMed Central

    Reynolds, Margaret M.; Greenwood-Quaintance, Kerryl E.; Patel, Robin; Pulido, Jose S.

    2016-01-01

    Purpose Endophthalmitis is a rare complication of intravitreal injection (IVI). It is recommended that povidone-iodine be the last agent applied before IVI. Patients have reported povidone-iodine application to be the most bothersome part of IVIs. Topical anesthetics have been demonstrated to have antibacterial effects. This study compared the minimum inhibitory concentration (MIC) of topical anesthetic eye drops (proparacaine 0.5%, tetracaine 0.5%, lidocaine 2.0%) and the antiseptic, 5.0% povidone-iodine, against two organisms causing endophthalmitis after IVI. Methods Minimum inhibitory concentration values of topical anesthetics, povidone-iodine, preservative benzalkonium chloride (0.01%), and saline control were determined using five isolates of each Staphylococcus epidermidis and viridans group Streptococcus species (VGS). A broth microdilution technique was used with serial dilutions. Results Lidocaine (8.53 × 10−5mol/mL) had MICs of 4.27 to 8.53 × 10−5 mol/mL, and tetracaine (1.89 × 10−5 mol/mL) had MICs of 9.45 × 10−6 mol/mL for all isolates. Proparacaine (1.7 × 10−5 mol/mL) had MICs of 1.32 to 5.3 × 10−7 and 4.25 × 10−6 mol/mL for S. epidermidis and VGS, respectively). Benzalkonium chloride (3.52 × 10−7 mol/mL) had MICs of 1.86 × 10−9 to 1.1 × 10−8 and 4.40 × 10−8 mol/mL for S. epidermidis and VGS, respectively. Povidone-iodine (1.37 × 10−4 mol/mL) had MICs of 2.14 to 4.28 × 10−6 and 8.56 × 10−6 mol/mL for S. epidermidis and VGS, respectively. Conclusion Proparacaine was the anesthetic with the lowest MICs, lower than that of povidone-iodine. Benzalkonium chloride had lower MICs than proparacaine. All tested anesthetics and povidone-iodine inhibited growth of S. epidermidis and VGS at commercially available concentrations. Translational Relevance For certain patients, it could be possible to use topical anesthetic after povidone-iodine for comfort without inhibiting and perhaps contributing additional antimicrobial

  1. Solubility of Haloether Anesthetics in Human and Animal Blood

    PubMed Central

    Soares, Joao H. N.; Brosnan, Robert J.; Fukushima, Fabíola B.; Hodges, Joanne; Liu, Hong

    2012-01-01

    Background Anesthetic blood solubility predicts pharmacokinetics for inhaled agents and is essential for determination of blood anesthetic concentrations from end-tidal gas concentrations using Henry’s Law. Though used to model anesthetic effects in humans, there are limited interspecies solubility comparisons that include modern haloethers. This study aimed to measure hematocrit-adjusted blood:gas anesthetic partition coefficients (λB:G) for desflurane, sevoflurane, isoflurane, and methoxyflurane in humans and animals. Methods Whole blood was collected from 20 rats, 8 horses, and 4 each of cats, cattle, humans, dogs, goats, pigs, rabbits, and sheep. Plasma or cell volume was removed to adjust all samples to a packed cell volume of 40%. A single agent calibration gas headspace was added to blood in a glass syringe and was mixed and equilibrated at 37°C for 2 hours. Agent concentrations in the calibration gas and syringe headspace were measured using gas chromatography. Anesthetic solubility in saline, citrate-phosphate-dextrose-adenine, and olive oil were similarly measured. Results Except for goats, all animal species had at least one λB:G measurement that differed significantly from humans. For each agent, λB:G positively correlated with serum triglyceride concentrations, but this only explained 25% of interspecies variability. Desflurane was significantly less soluble in blood than sevoflurane in some species (e.g., humans) but not in others (e.g., rabbits). Conclusions Anesthetic partition coefficients differ significantly between humans and most animals for haloether anesthetics. Because of their similar λB:G values, goats may be a better animal model for inhaled anesthetic pharmacokinetics in people. PMID:22510863

  2. Effects of Topical Anesthetics on Pullularia pullulans and Debaryomyces hansenii

    PubMed Central

    Merdinger, Emanuel; Guthmann, Walter S.; Mangine, Francis W.

    1969-01-01

    The inhibitory effects of three topical anesthetics of various concentrations on the growth of Pullularia pullulans, Debaryomyces hansenii, and on pigment production by P. pullulans were investigated. The topical anesthetics were benoxinate hydrochloride, proparacaine hydrochloride, and tetracaine hydrochloride. In decreasing order, the inhibiting effects of the drugs on growth were benoxinate, tetracaine, and proparacaine for P. pullulans, and tetracaine, benoxinate, and proparacaine for D. hansenii. The pigment formation in P. pullulans was inhibited by the three drugs. PMID:5392897

  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. Dynamic characteristics of the cutaneous vasodilator response to a local external pressure application detected by the laser Doppler flowmetry technique on anesthetized rats

    NASA Astrophysics Data System (ADS)

    Humeau, Anne; Koitka, Audrey; Saumet, Jean-Louis; L'Huillier, Jean-Pierre

    2003-10-01

    The laser Doppler flowmetry technique has recently been used to report a significant transient increase of the cutaneous blood flow signal when a local non-noxious pressure is applied progressively on the skin (11.1 Pa/s). The present work analyses the dynamic characteristics of this vasodilatory reflex response on anaesthetised rats. A de-noising algorithm using wavelets is proposed to obtain accurate values of these dynamic characteristics. The blood flow peak and the time to reach this peak are computed on the de-noised recordings. The results show that the mean time to reach the peak of perfusion is 85.3 s (time t = 0 at the beginning of the pressure application). The mean peak value is 188.3 arbitrary units (a.u.), whereas the mean value of the perfusion before the pressure application is 113.4 a.u. The mean minimum value obtained at the end of the experiment is 60.7 a.u. This latter value is, on the average, reached 841.3 s after the beginning of the pressure application. The comparison of the dynamic characteristics, computed with the de-noising algorithm on signals obtained in other situations, will give a better understanding on some cutaneous lesions such as those present on diabetic people.

  5. A preferential delivery method to investigate direct neuromuscular blockade effect of inhaled anesthetics on skeletal muscle.

    PubMed

    Ye, Ling; Yang, Pingliang

    2017-04-01

    Inhaled anesthetics can enhance the effect of neuromuscular blocker, but whether inhaled anesthetics such as sevoflurane have a direct effect on skeletal muscle contractility is unknown. Selectively blocking skeletal muscle may prevent the interference effect of central nervous system. So we decided to evaluate a local application of neuromuscular blocker (NMB) atracurium to prevent the general effect on skeletal muscle. In part 1, sevoflurane (a inhaled anesthetic) minimum alveolar concentrations (MAC) of 1.0, 1.5 and 2.0 would be applied in succession. Neuromuscular function was assessed at each MAC. In part 2, patients are randomized into four groups: group1 (propofol+NMB, sevoflurane 0 MAC), and groups 2 to 4 (NMB+sevoflurane 1.0, 1.5 and 2.0 MAC respectively). In group 1, patients were anesthetized by propofol, then 0.01mg/kg atracurium was injected into the tested arm intravenously after the arterial blood flow was blocked using a tourniquet. For the other 3 groups, patients inhaled 1.0 MAC, 1.5 MAC, or 2.0 MAC of sevoflurane. Then 0.01mg/kg atracurium was injected. Neuromuscular function was recorded for the 4 groups. Neuromuscular function was assessed by acceleromyography measurement of evoked responses to train-of four (TOF) stimuli (2Hz for 2s applied every 12s) at the adductor pollicis using a TOF-Guard™ neuromuscular transmission monitor. If proven, our hypothesis would demonstrate the inhaled anesthetics have no direct effect on contractility but only by increasing the skeletal muscle sensitivity to NMB.

  6. Concentration gradient along scala tympani following the local application of gentamicin to the round window membrane

    PubMed Central

    Plontke, Stefan K.; Mynatt, Robert; Gill, Ruth M.; Borgmann, Stefan; Salt, Alec N.

    2008-01-01

    Objectives The distribution of gentamicin along the fluid spaces of the cochlea following local applications has never previously been demonstrated. Computer simulations have predicted that significant basal-apical concentration gradients might be expected and histological studies indicate that hair cell damage is greater at the base than at the apex following local gentamicin application. In the present study, gradients of gentamicin along the cochlea were measured. Methods A recently-developed method of sampling perilymph from the cochlear apex of guinea pigs was used, in which the samples represent fluid originating from different regions along scala tympani. Gentamicin concentration was determined in sequential apical samples which were taken following up to three hours of local application to the round window niche. Results Substantial gradients of gentamicin along the length of scala tympani were demonstrated and quantified, averaging more than 4000 times greater concentration at the base compared to the apex at the time of sampling. Peak concentrations and gradients for gentamicin varied considerably between animals, likely resulting from variations in round window membrane permeability and rates of perilymph flow. Conclusions The large gradients for gentamicin demonstrated here in guinea pigs account for how it is possible to suppress vestibular function in some patients with a local application of gentamicin without damaging auditory function. Variations in round window membrane permeability and in perilymph flow could account for why hearing losses are observed in some patients. PMID:17603318

  7. Pollution of ambient air by volatile anesthetics: a comparison of 4 anesthetic management techniques.

    PubMed

    Barberio, Joy C; Bolt, Jason D; Austin, Paul N; Craig, William J

    2006-04-01

    Long-term exposure to waste anesthetic gas (WAG) may lead to health problems. The purpose of this study was to compare WAG concentrations resulting from 4 combinations of fresh gas flow (FGF) and vaporizer settings during a simulated intravenous induction in which the anesthetic is deepened using a volatile anesthetic delivered via mask ventilation before intubation. By using a lung model, WAG was sampled 3 times each using 4 combinations and 3 volatile anesthetics: 3% sevoflurane, 2% isoflurane, and 6% desflurane. The combinations were FGF off/vaporizer on, FGF on/vaporizer off, both on, and both off. WAG was measured using a MIRAN Ambient Air Analyzer placed at a level approximating the anesthetist's head. One-way analysis of variance with a Student-Newman-Keuls post hoc test was used to compare the concentration of WAG among the combinations of FGF/vaporizer settings for each agent. Regardless of the agent, only the FGF on/vaporizer on combination at 60 seconds resulted in a statistically greater WAG level (P < .005). The results support using 3 of the 4 combinations examined when mask ventilation with a volatile agent accompanies intravenous induction. Future studies should examine other methods of controlling WAG levels and use time-weighted averages to help address clinical significance.

  8. The site of anesthetic action.

    PubMed

    Urban, B W

    2008-01-01

    The mechanisms of general anesthesia constitute one of the great unsolved problems of classical neuropharmacology. Since the discovery of general anesthesia, hundreds of substances have been tested and found to possess anesthetic activity. Anesthetics differ tremendously in their chemical, physical, and pharmacological properties, greatly varying in size, in chemically active groups, and in the combinations of interactions and chemical reactions that they can undergo. The large spectrum of targets makes it obvious that dealing with anesthetics pharmacologically is different from dealing with most other drugs used in pharmacology. Anesthetic potency often correlates with the lipophilicity of anesthetic compounds, i.e., their preference for dissolving in lipophilic phases. This suggests as a main characteristic of anesthetic interactions that they are weak and that for many of them there is overall an approximate balance of nonspecific hydrophobic interactions and weak specific polar interactions. These include various electrostatic (ions, permanent and induced dipoles, quadrupoles), hydrogen bonding, and hydrophobic interactions. There are many molecular targets of anesthetic action within the central nervous system, but there are many more still to be discovered. Molecular interaction sites postulated from functional studies include protein binding sites, protein cavities, lipid/protein interfaces, and protein/protein interfaces.

  9. Nondestructive Quantification of Local Plasticizer Concentration in PVC by (1)H NMR Relaxometry.

    PubMed

    Adams, Alina; Kwamen, Rance; Woldt, Benjamin; Graß, Michael

    2015-12-01

    The properties of plasticized poly(vinyl chloride) (PVC) , one of the most important polymers today, are strongly dictated by the concentration of plasticizer. Yet, it has been impossible to quantify this concentration at different positions inside a PVC product without its destruction because of a lack of suitable analytical methods. Thus, this paper introduces a simple, fast, and efficient way to determine truly nondestructively the concentration of plasticizer in PVC by single-sided nuclear magnetic resonance (NMR). With the help of correlation curves between the concentration of plasticizer inside nonaged PVC samples and the corresponding volume-averaged NMR parameters, single-sided NMR allows the quantification of the local concentration of plasticizer in aged PVC plates at different depths by spatially resolved relaxation measurements. The presented approach represents a fundamental step toward in situ characterization of plasticized PVC.

  10. Impact of closing Canada's largest point-source of mercury emissions on local atmospheric mercury concentrations.

    PubMed

    Eckley, Chris S; Parsons, Matthew T; Mintz, Rachel; Lapalme, Monique; Mazur, Maxwell; Tordon, Robert; Elleman, Robert; Graydon, Jennifer A; Blanchard, Pierrette; St Louis, Vincent

    2013-09-17

    The Flin Flon, Manitoba copper smelter was Canada's largest point source of mercury emissions until its closure in 2010 after ~80 years of operation. The objective of this study was to understand the variables controlling the local ground-level air mercury concentrations before and after this major point source reduction. Total gaseous mercury (TGM) in air, mercury in precipitation, and other ancillary meteorological and air quality parameters were measured pre- and postsmelter closure, and mercury speciation measurements in air were collected postclosure. The results showed that TGM was significantly elevated during the time period when the smelter operated (4.1 ± 3.7 ng m(-3)), decreased only 20% during the year following its closure, and remained ~2-fold above background levels. Similar trends were observed for mercury concentrations in precipitation. Several lines of evidence indicated that while smelter stack emissions would occasionally mix down to the surface resulting in large spikes in TGM concentrations (up to 61 ng m(-3)), the largest contributor to elevated TGM concentrations before and after smelter closure was from surface-air fluxes from mercury-enriched soils and/or tailings. These findings highlight the ability of legacy mercury, deposited to local landscapes over decades from industrial activities, to significantly affect local air concentrations via emissions/re-emissions.

  11. Anesthetic Concerns of Space Flight

    NASA Technical Reports Server (NTRS)

    Norfleet, William T.

    1999-01-01

    Anesthesiologists are acutely aware of the fact that, although a given surgical procedure may be relatively simple, the required anesthetic care is, in certain cases, extremely complex. This principle is particularly evident when one ponders the difficulties involved in providing even basic anesthetic care in microgravity. In this issue some of these difficulties through the evaluation of airway management techniques during water immersion are confronted, a simulation of the gravito-inertial conditions of space flight. As prelude for this paper, I would like to outline some of the challenges to be overcome before surgical, anesthetic, and critical care can be delivered beyond our home planet.

  12. A randomized, prospective, double-blind study to investigate the effectiveness of adding DepoMedrol to a local anesthetic injection in postmeniscectomy patients with osteoarthritis of the knee.

    PubMed

    Koyonos, Loukas; Yanke, Adam B; McNickle, Allison G; Kirk, Spencer S; Kang, Richard W; Lewis, Paul B; Cole, Brian J

    2009-06-01

    Patients with osteoarthritis of the knee are at risk for poorer outcomes after arthroscopic meniscectomy. Intra-articular corticosteroid injections have been shown to be efficacious both in patients with osteoarthritis and postarthroscopy patients. A postoperative, intra-articular methylprednisolone and lidocaine injection in patients with chondromalacia undergoing meniscectomy will improve patient-rated pain and function compared with control patients. Randomized, controlled trial; Level of evidence, 1. A total of 58 patients (59 knees) were randomized in a double-blinded fashion to receive either saline plus lidocaine (saline) or methylprednisolone plus lidocaine (steroid) after arthroscopic meniscectomy in which chondromalacia (modified Outerbridge grade 2 or higher) was confirmed. Preoperatively and at follow-up-6 weeks and 6, 9, and 12 months-patients underwent an examination and completed a subjective functioning survey. Scores were calculated using several validated scoring systems including the Lysholm, International Knee Documentation Committee (IKDC), and Short Form-12 (SF-12). No statistically significant differences were observed between the saline (n = 30) and steroid (n = 29) groups in their demographics and preoperative scores. At 6 weeks, the steroid group had higher scores than the saline group on multiple scales, including the IKDC. No differences in outcome scores existed at later time points. At 12 months, 86% of the steroid and 69% of the saline group were completely or mostly satisfied with the procedure (P = .01). In the saline group, 4 patients required reinjection and 2 underwent joint replacements within 12 months, while the steroid group had 3 reinjections and 2 meniscus transplants. The addition of a postoperative corticosteroid injection resulted in improved pain and function at an early time point; however, it provided no lasting difference compared with only local anesthetic injection.

  13. Local modulation of chemoattractant concentrations by single cells: dissection using a bulk-surface computational model

    PubMed Central

    Nolan, M.

    2016-01-01

    Chemoattractant gradients are usually considered in terms of sources and sinks that are independent of the chemotactic cell. However, recent interest has focused on ‘self-generated’ gradients, in which cell populations create their own local gradients as they move. Here, we consider the interplay between chemoattractants and single cells. To achieve this, we extend a recently developed computational model to incorporate breakdown of extracellular attractants by membrane-bound enzymes. Model equations are parametrized, using the published estimates from Dictyostelium cells chemotaxing towards cyclic AMP. We find that individual cells can substantially modulate their local attractant field under physiologically appropriate conditions of attractant and enzymes. This means the attractant concentration perceived by receptors can be a small fraction of the ambient concentration. This allows efficient chemotaxis in chemoattractant concentrations that would be saturating without local breakdown. Similar interactions in which cells locally mould a stimulus could function in many types of directed cell motility, including haptotaxis, durotaxis and even electrotaxis. PMID:27708760

  14. Waste gas monitor reduces wasted volatile anesthetic.

    PubMed

    Euliano, T Y; van Oostrom, J H; van der Aa, J

    1999-07-01

    The increasing focus on health care costs requires that all physicians evaluate practice behaviors. The primary emphasis in anesthesia has been limiting the use of expensive medications and interventions. Reducing waste is another approach, and volatile anesthetics are an appropriate target in that simple reduction of fresh gas-flow (FGF) rates is effective. A monitor that measures and displays the cost of wasted volatile anesthetic was developed and used to determine if real-time display of the cost would result in decreased FGF rates, which, in turn, would decrease wasted anesthetic. The waste gas monitor (WGM) measures flow rate at the anesthesia machine's scavenger port, integrates this with agent concentration, and displays the calculated cost, real-time, on a portable computer screen. The WGM equipment was attached to the anesthesia machine in the gynecologic surgery operating room (OR) and those cases performed under general endotracheal anesthesia and lasting longer than one hour were eligible for inclusion. First year anesthesiology residents assigned to the study OR as part of a non-specialty rotation, were the subjects of the study. For each resident, after data were collected from at least two eligible baseline cases (Baseline Phase, WGM not visible and resident unaware of its presence), the monitor was introduced and data collection continued for at least three more eligible cases (Visible Phase). Nine residents were initially enrolled, but due to scheduling difficulties only five residents completed the protocol. Data from cases using the WGM demonstrated a 50% decrease (3.58 +/- 1.34 l/min vs. 1.78 +/- 0.51 l/min (p = 0.009)) in the scavenger flow rates, which resulted in a 48% ($5.28 +/- 0.68 vs. $2.72 +/- 0.80 (p = 0.002)) decrease in hourly cost of wasted volatile anesthetic. There was no difference between the Baseline and Visible phases with regard to use of nitrous oxide or intravenous anesthetic agents. CONCLUSIONS. The WGM decreased wasted

  15. Face transplantation: Anesthetic challenges

    PubMed Central

    Dalal, Aparna

    2016-01-01

    Face transplantation is a complex vascular composite allotransplantation (VCA) surgery. It involves multiple types of tissue, such as bone, muscles, blood vessels, nerves to be transferred from the donor to the recipient as one unit. VCAs were added to the definition of organs covered by the Organ Procurement and Transplantation Network Final Rule and National Organ Transplant Act. Prior to harvest of the face from the donor, a tracheostomy is usually performed. The osteotomies and dissection of the midface bony skeleton may involve severe hemorrhagic blood loss often requiring transfusion of blood products. A silicon face mask created from the facial impression is used to reconstruct the face and preserve the donor’s dignity. The recipient airway management most commonly used is primary intubation of an existing tracheostoma with a flexometallic endotracheal tube. The recipient surgery usually averages to 19-20 h. Since the face is a very vascular organ, there is usually massive bleeding, both in the dissection phase as well as in the reperfusion phase. Prior to reperfusion, often, after one sided anastomosis of the graft, the contralateral side is allowed to bleed to get rid of the preservation solution and other additives. Intraoperative product replacement should be guided by laboratory values and point of care testing for coagulation and hemostasis. In face transplantation, bolus doses of pressors or pressor infusions have been used intraoperatively in several patients to manage hypotension. This article reviews the anesthetic considerations for management for face transplantation, and some of the perioperative challenges faced. PMID:28058213

  16. Large increases in attractant concentration disrupt the polar localization of bacterial chemoreceptors.

    PubMed

    Lamanna, Allison C; Ordal, George W; Kiessling, Laura L

    2005-08-01

    In bacterial chemotaxis, the chemoreceptors [methyl-accepting chemotaxis proteins (MCPs)] transduce chemotactic signals through the two-component histidine kinase CheA. At low but not high attractant concentrations, chemotactic signals must be amplified. The MCPs are organized into a polar lattice, and this organization has been proposed to be critical for signal amplification. Although evidence in support of this model has emerged, an understanding of how signals are amplified and modulated is lacking. We probed the role of MCP localization under conditions wherein signal amplification must be inhibited. We tested whether a large increase in attractant concentration (a change that should alter receptor occupancy from c. 0% to > 95%) would elicit changes in the chemoreceptor localization. We treated Escherichia coli or Bacillus subtilis with a high level of attractant, exposed cells to the cross-linking agent paraformaldehyde and visualized chemoreceptor location with an anti-MCP antibody. A marked increase in the percentage of cells displaying a diffuse staining pattern was obtained. In contrast, no increase in diffuse MCP staining is observed when cells are treated with a repellent or a low concentration of attractant. For B. subtilis mutants that do not undergo chemotaxis, the addition of a high concentration of attractant has no effect on MCP localization. Our data suggest that interactions between chemoreceptors are decreased when signal amplification is unnecessary.

  17. Nanoliposome encapsulated anesthetics for local anesthesia application.

    PubMed

    Vahabi, Sepideh; Eatemadi, Ali

    2017-02-01

    The systemic administration of opioids leads to potentially severe and undesirable and side effects like sedation and drowsiness, vomiting and nausea, allergies, respiratory depression, and neutrophil dysfunction. The application of nanotechnology in medical field has drawn a great attention in recent times. Several treatments available are tedious and expensive. Application of nanotechnology brings about faster cure and cost effectiveness. Nanoliposomes are one of the widely used names for nanoparticles used in medicine. Recently, nanoliposomes are used as a crucial novel drug delivery systems. The use of nanoliposomal formulation brings about a good results to pain control, rapid patient recovery, increased patient comfort, treatment costs reduction, and shortens length of hospitalization. This review presents a brief description about the achievements in the field of nanoscience and nanotechnology related to the application of nanoliposomes in anesthesia.

  18. Anesthetic approaches in carotid body tumor surgery

    PubMed Central

    Kavakli, Ali Sait; Ozturk, Nilgun Kavrut

    2016-01-01

    OBJECTIVE: Carotid body tumors (CBT) are benign tumors that originate from neural non-chromaffin cells that are typically localized near carotid bifurcation. Surgical removal of the tumor is the most appropriate treatment. General anesthesia is preferred anesthetic technique for CBT surgery. Basic elements of anesthetic management are protection of hemodynamic stability and maintaining cerebral perfusion pressure (CPP). The aim of this study was to evaluate anesthetic management of CBT surgery and present the literature knowledge. METHODS: The study included 10 consecutive patients with diagnosis of CBT who underwent surgery at Antalya Training and Research Hospital, in Antalya, Turkey, between 2013 and 2016. Preoperative demographic details; comorbidities; side of surgical site; duration of operation; length of intensive care unit (ICU) and hospital stay; change of intraoperative blood pressure; use of inotropic drugs, blood products, and analgesics; postoperative visual analogue scale (VAS) pain score; and complications were recorded. RESULTS: According to Shamblin classification, 3 tumors were type I and the remaining 7 were type II. Tumors were located on right side in 6 patients, and on left in 4. Blood loss sufficient to require transfusion was observed in 1 patient. Average intraoperative blood loss was 287±68 mL. Tachycardia and hypertension were observed in 1 patient; bradycardia and hypotension were seen in 4 patients. Infusion for inotropic support was administered to 1 patient. Mean duration of operation was 109±20 minutes. Mean VAS score was 4±1, mean ICU tramadol consumption was 80±25 mg. Duration of stay in ICU and hospital were 2.4±1.1 hours and 3.8±0.7 days, respectively. Mortality and neurological complications were not seen in postoperative period. CONCLUSION: CBT surgery requires close and complex anesthesia management. Protection of hemodynamic stability against sudden hemodynamic changes, monitoring, and maintaining CPP are the most

  19. 21 CFR 868.5880 - Anesthetic vaporizer.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 8 2012-04-01 2012-04-01 false Anesthetic vaporizer. 868.5880 Section 868.5880...) MEDICAL DEVICES ANESTHESIOLOGY DEVICES Therapeutic Devices § 868.5880 Anesthetic vaporizer. (a) Identification. An anesthetic vaporizer is a device used to vaporize liquid anesthetic and deliver a controlled...

  20. 21 CFR 868.5880 - Anesthetic vaporizer.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Anesthetic vaporizer. 868.5880 Section 868.5880...) MEDICAL DEVICES ANESTHESIOLOGY DEVICES Therapeutic Devices § 868.5880 Anesthetic vaporizer. (a) Identification. An anesthetic vaporizer is a device used to vaporize liquid anesthetic and deliver a controlled...

  1. 21 CFR 872.6100 - Anesthetic warmer.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 8 2014-04-01 2014-04-01 false Anesthetic warmer. 872.6100 Section 872.6100 Food... DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6100 Anesthetic warmer. (a) Identification. An anesthetic warmer is an AC-powered device into which tubes containing anesthetic solution are intended to be...

  2. 21 CFR 868.5880 - Anesthetic vaporizer.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 8 2011-04-01 2011-04-01 false Anesthetic vaporizer. 868.5880 Section 868.5880...) MEDICAL DEVICES ANESTHESIOLOGY DEVICES Therapeutic Devices § 868.5880 Anesthetic vaporizer. (a) Identification. An anesthetic vaporizer is a device used to vaporize liquid anesthetic and deliver a controlled...

  3. 21 CFR 872.6100 - Anesthetic warmer.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 8 2012-04-01 2012-04-01 false Anesthetic warmer. 872.6100 Section 872.6100 Food... DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6100 Anesthetic warmer. (a) Identification. An anesthetic warmer is an AC-powered device into which tubes containing anesthetic solution are intended to be...

  4. 21 CFR 868.5880 - Anesthetic vaporizer.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 8 2013-04-01 2013-04-01 false Anesthetic vaporizer. 868.5880 Section 868.5880...) MEDICAL DEVICES ANESTHESIOLOGY DEVICES Therapeutic Devices § 868.5880 Anesthetic vaporizer. (a) Identification. An anesthetic vaporizer is a device used to vaporize liquid anesthetic and deliver a controlled...

  5. 21 CFR 872.6100 - Anesthetic warmer.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Anesthetic warmer. 872.6100 Section 872.6100 Food... DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6100 Anesthetic warmer. (a) Identification. An anesthetic warmer is an AC-powered device into which tubes containing anesthetic solution are intended to be...

  6. 21 CFR 868.5880 - Anesthetic vaporizer.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 8 2014-04-01 2014-04-01 false Anesthetic vaporizer. 868.5880 Section 868.5880...) MEDICAL DEVICES ANESTHESIOLOGY DEVICES Therapeutic Devices § 868.5880 Anesthetic vaporizer. (a) Identification. An anesthetic vaporizer is a device used to vaporize liquid anesthetic and deliver a controlled...

  7. 21 CFR 872.6100 - Anesthetic warmer.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 8 2013-04-01 2013-04-01 false Anesthetic warmer. 872.6100 Section 872.6100 Food... DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6100 Anesthetic warmer. (a) Identification. An anesthetic warmer is an AC-powered device into which tubes containing anesthetic solution are intended to be...

  8. 21 CFR 872.6100 - Anesthetic warmer.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 8 2011-04-01 2011-04-01 false Anesthetic warmer. 872.6100 Section 872.6100 Food... DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6100 Anesthetic warmer. (a) Identification. An anesthetic warmer is an AC-powered device into which tubes containing anesthetic solution are intended to be...

  9. Altered states: psychedelics and anesthetics.

    PubMed

    Icaza, Eduardo E; Mashour, George A

    2013-12-01

    The psychedelic experience has been reported since antiquity, but there is relatively little known about the underlying neural mechanisms. A recent neuroimaging study on psilocybin revealed a pattern of decreased cerebral blood flow and functional disconnections that is surprisingly similar to that caused by various anesthetics. In this article, the authors review historical examples of psychedelic experiences induced by general anesthetics and then contrast the mechanisms by which these two drug classes generate altered states of consciousness.

  10. Evaluation of serum concentrations of the selected cytokines in patients with localized scleroderma

    PubMed Central

    Budzyńska-Włodarczyk, Jolanta; Michalska-Jakubus, Małgorzata M.; Kowal, Małgorzata

    2016-01-01

    Introduction Localized scleroderma is an autoimmune disease primarily affecting the skin. The cause of disease remains unexplained although environmental factors are implicated, which are likely to be responsible for activation of the endothelium and subsequent inflammation leading to excessive synthesis of collagen and extracellular matrix components. Aim To determine concentrations of interleukin (IL)-27, transforming growth factor (TGF)-β1, TGF-β2, IL-6, and sIL-6R in patients with localized scleroderma compared to controls and to assess the relations between their levels and laboratory markers. Material and methods The study encompassed 17 females with localized scleroderma (aged 25–67). The control group consisted of 30 age-matched healthy women. The blood was sampled from the basilic vein. Serum levels of cytokines were determined using ELISA. Results The TGF-β2 levels were found to be significantly lower in patients with localized scleroderma compared to controls. Concentrations of TGF-β1 were decreased in scleroderma patients when compared to controls but without statistical significance. There were no significant differences in serum IL-6, sIL-6R and IL-27 levels between patients and the control group; however, we found a significant positive correlation between the level of sIL-6 and ESR among subjects with localized scleroderma. Conclusions The findings of decreased serum levels of TGF-β1 and TGF-β2 in patients with localized scleroderma demonstrate a possible association of these cytokines with pathogenesis of the disease. The results suggest also that sIL-6R is likely to be involved in inflammation in patients with localized scleroderma. PMID:26985179

  11. Evaluation of serum concentrations of the selected cytokines in patients with localized scleroderma.

    PubMed

    Budzyńska-Włodarczyk, Jolanta; Michalska-Jakubus, Małgorzata M; Kowal, Małgorzata; Krasowska, Dorota

    2016-02-01

    Localized scleroderma is an autoimmune disease primarily affecting the skin. The cause of disease remains unexplained although environmental factors are implicated, which are likely to be responsible for activation of the endothelium and subsequent inflammation leading to excessive synthesis of collagen and extracellular matrix components. To determine concentrations of interleukin (IL)-27, transforming growth factor (TGF)-β1, TGF-β2, IL-6, and sIL-6R in patients with localized scleroderma compared to controls and to assess the relations between their levels and laboratory markers. The study encompassed 17 females with localized scleroderma (aged 25-67). The control group consisted of 30 age-matched healthy women. The blood was sampled from the basilic vein. Serum levels of cytokines were determined using ELISA. The TGF-β2 levels were found to be significantly lower in patients with localized scleroderma compared to controls. Concentrations of TGF-β1 were decreased in scleroderma patients when compared to controls but without statistical significance. There were no significant differences in serum IL-6, sIL-6R and IL-27 levels between patients and the control group; however, we found a significant positive correlation between the level of sIL-6 and ESR among subjects with localized scleroderma. The findings of decreased serum levels of TGF-β1 and TGF-β2 in patients with localized scleroderma demonstrate a possible association of these cytokines with pathogenesis of the disease. The results suggest also that sIL-6R is likely to be involved in inflammation in patients with localized scleroderma.

  12. Intraoperative awareness risk, anesthetic sensitivity, and anesthetic management for patients with natural red hair: a matched cohort study.

    PubMed

    Gradwohl, Stephen C; Aranake, Amrita; Abdallah, Arbi Ben; McNair, Paul; Lin, Nan; Fritz, Bradley A; Villafranca, Alex; Glick, David; Jacobsohn, Eric; Mashour, George A; Avidan, Michael S

    2015-04-01

    The red-hair phenotype, which is often produced by mutations in the melanocortin-1 receptor gene, has been associated with an increase in sedative, anesthetic, and analgesic requirements in both animal and human studies. Nevertheless, the clinical implications of this phenomenon in red-haired patients undergoing surgery are currently unknown. In a secondary analysis of a prospective trial of intraoperative awareness, red-haired patients were identified and matched with five control patients, and the relative risk for intraoperative awareness was determined. Overall anesthetic management between groups was compared using Hotelling's T(2) statistic. Inhaled anesthetic requirements were compared between cohorts by evaluating the relationship between end-tidal anesthetic concentration and the bispectral index with a linear mixed-effects model. Time to recovery was compared using Kaplan-Meier analysis, and differences in postoperative pain and nausea/vomiting were evaluated with Chi square tests. A cohort of 319 red-haired patients was matched with 1,595 control patients for a sample size of 1,914. There were no significant differences in the relative risk of intraoperative awareness (relative risk = 1.67; 95% confidence interval 0.34 to 8.22), anesthetic management, recovery times, or postoperative pain between red-haired patients and control patients. The relationship between pharmacokinetically stable volatile anesthetic concentrations and bispectral index values differed significantly between red-haired patients and controls (P < 0.001), but without clinical implications. There were no demonstrable differences between red-haired patients and controls in response to anesthetic and analgesic agents or in recovery parameters. These findings suggest that perioperative anesthetic and analgesic management should not be altered based on self-reported red-hair phenotype.

  13. A nonparametric approach to calculate critical micelle concentrations: the local polynomial regression method.

    PubMed

    López Fontán, J L; Costa, J; Ruso, J M; Prieto, G; Sarmiento, F

    2004-02-01

    The application of a statistical method, the local polynomial regression method, (LPRM), based on a nonparametric estimation of the regression function to determine the critical micelle concentration (cmc) is presented. The method is extremely flex