Effect of selective β-adrenoceptor blockade and surgical resection of the celiac-superior mesenteric ganglion complex on delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats

PubMed Central

Vinagre, A.M.; Collares, E.F.

2016-01-01

There is evidence for participation of peripheral β-adrenoceptors in delayed liquid gastric emptying (GE) induced in rats by dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At). The present study aimed to determine whether β-adrenoceptors are involved in delayed GE induced by phenylpyrazole derivatives and the role of the prevertebral sympathetic nervous system in this condition. Male Wistar rats weighing 220-280 g were used in the study. In the first experiment rats were intravenously pretreated with vehicle (V), atenolol 30 mg/kg (ATE, β1-adrenergic antagonist), or butoxamine 25 mg/kg (BUT, β2-adrenergic antagonist). In the second experiment, rats were pretreated with V or SR59230A 2 mg/kg (SRA, β3-adrenergic antagonist). In the third experiment, rats were subjected to surgical resection of the celiac-superior mesenteric ganglion complex or to sham surgery. The groups were intravenously treated with saline (S), 240 µmol/kg Dp, AA, or At, 15 min after pretreatment with the antagonists or V and nine days after surgery. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol red 10 min after gavage. The %GR (means±SE, n=6) values indicated that BUT abolished the effect of Dp (BUT+Dp vs V+Dp: 35.0%±5.1% vs 56.4%±2.7%) and At (BUT+At vs V+At: 33.5%±4.7% vs 52.9%±2.6%) on GE, and significantly reduced (P<0.05) the effect of AA (BUT+AA vs V+AA: 48.0%±5.0% vs 65.2%±3.8%). ATE, SRA, and sympathectomy did not modify the effects of treatments. These results suggest that β2-adrenoceptor activation occurred in delayed liquid gastric emptying induced by the phenylpyrazole derivatives dipyrone, 4-aminoantipyrine, and antipyrine. Additionally, the released neurotransmitter did not originate in the celiac-superior mesenteric ganglion complex. PMID:26840714

Molecular modeling of the inhibition of enzyme PLA2 from snake venom by dipyrone and 1-phenyl-3-methyl-5-pyrazolone

NASA Astrophysics Data System (ADS)

Silva, S. L. Da; Comar, M., Jr.; Oliveira, K. M. T.; Chaar, J. S.; Bezerra, E. R. M.; Calgarotto, A. K.; Baldasso, P. A.; Veber, C. L.; Villar, J. A. F. P.; Oliveira, A. R. M.; Marangoni, S.

Phospholipases A2 (PLA2) are enzymes that trigger the degradation cascade of the arachidonic acid, leading to the formation of pro-inflammatory eicosanoids. The selective inhibition of PLA2s is crucial in the search for a more efficient anti-inflammatory drug with fewer side effects than the drugs currently used. Hence, we studied the influences caused by two pyrazolonic inhibitors: dipyrone (DIP) and 1-phenyl-3-methyl-5-pyrazolone (PMP) on the kinetic behavior of PLA2 from Crotalus adamanteus venom. Molecular modeling results, by DFT and MM approaches, showed that DIP is strongly associated to the active site of PLA2 through three hydrogen bonds, whereas PMP is associated to the enzyme just through hydrophobic interactions. In addition, only PMP presents an intramolecular hydrogen bond that make difficult the formation of more efficient interactions with PLA2. These results help in the understanding of the experimental observations. Experimentally, the results showed that PLA2 from C. adamanteus present a typical Michaelian behavior. In addition, the calculated kinetic parameters showed that, in the presence of DIP or PMP, the maximum enzymatic velocity (VMAX) value was kept constant, whereas the Michaelis constant (KM) values increased and the inhibition constant (KI) decreased, indicating competitive inhibition. These results show that the phenyl-pyrazolonic structures might help in the development and design of new drugs able to selectively inhibit PLA2.

Tramadol wound infiltration is not different from intravenous tramadol in children: a randomized controlled trial.

PubMed

Giraldes, Ana Laura Albertoni; Sousa, Angela Maria; Slullitel, Alexandre; Guimarães, Gabriel Magalhães Nunes; Santos, Melina Geneviève Mary Egan; Pinto, Renata Evangelista; Ashmawi, Hazem Adel; Sakata, Rioko Kimiko

2016-02-01

The purpose of this trial was to assess if tramadol wound infiltration is superior to intravenous (IV) tramadol after minor surgical procedures in children because tramadol seems to have local anesthetic-like effect. Randomized double-blind controlled trial. Postanesthesia care unit. Forty children, American Society of Anesthesiologists physical status I or II, scheduled to elective inguinal hernia repair. Children were randomly distributed in 1 of 2 groups: IV tramadol (group 1) or subcutaneous infiltration with tramadol (group 2). At the end of the surgery, group 1 received 2 mg/kg tramadol (3 mL) by IV route and 3-mL saline into the surgical wound; group 2 received 2 mg/kg tramadol (3 mL) into the surgical wound and 3-mL saline by IV route. In the postanesthesia care unit, patients were evaluated for pain intensity, nausea and vomiting, time to first rescue medication, and total rescue morphine and dipyrone consumption. Pain scores measured during the postanesthesia recovery time were similar between groups. Time to first rescue medication was shorter, but not statistically significant in the IV group. The total dose of rescue morphine and dipyrone was also similar between groups. We concluded that tramadol was effective in reducing postoperative pain in children, and there was no difference in pain intensity, nausea and vomiting, or somnolence regarding IV route or wound infiltration. Copyright © 2016 Elsevier Inc. All rights reserved.

Importance of MS selectivity and chromatographic separation in LC-MS/MS-based methods when investigating pharmaceutical metabolites in water. Dipyrone as a case of study.

PubMed

Ibáñez, M; Gracia-Lor, E; Sancho, J V; Hernández, F

2012-08-01

Pharmaceuticals are emerging contaminants of increasing concern because of their presence in the aquatic environment and potential to reach drinking-water sources. After human and/or veterinary consumption, pharmaceuticals can be excreted in unchanged form, as the parent compound, and/or as free or conjugated metabolites. Determination of most pharmaceuticals and metabolites in the environment is commonly made by liquid chromatography (LC) coupled to mass spectrometry (MS). LC coupled to tandem MS is the technique of choice nowadays in this field. The acquisition of two selected reaction monitoring (SRM) transitions together with the retention time is the most widely accepted criterion for a safe quantification and confirmation assay. However, scarce attention is normally paid to the selectivity of the selected transitions as well as to the chromatographic separation. In this work, the importance of full spectrum acquisition high-resolution MS data using a hybrid quadrupole time-of-flight analyser and/or a suitable chromatographic separation (to reduce the possibility of co-eluting interferences) is highlighted when investigating pharmaceutical metabolites that share common fragment ions. For this purpose, the analytical challenge associated to the determination of metabolites of the widely used analgesic dipyrone (also known as metamizol) in urban wastewater is discussed. Examples are given on the possibilities of reporting false positives of dypirone metabolites by LC-MS/MS under SRM mode due to a wrong assignment of identity of the compounds detected. Copyright © 2012 John Wiley & Sons, Ltd.

Analysis of analgesic, antipyretic, and nonsteroidal anti-inflammatory drug use in pediatric prescriptions.

PubMed

Ferreira, Tânia R; Lopes, Luciane C

2016-01-01

Data on clinical practice in pediatrics on the use of analgesic, antipyretic, and nonsteroidal anti-inflammatory drugs considering the best available evidence and regulatory-agency approved use are uncertain. This study aimed to determine the frequency of prescription of these drugs according to the best scientific evidence and use approved by regulatory agencies. This was a cross-sectional study of 150 pediatric prescriptions containing analgesic, antipyretic, and nonsteroidal anti-inflammatory drugs, followed by interview with caregivers at 18 locations (nine private drugstores and nine Basic Health Units of the Brazilian Unified Health System). The assessed outcomes included recommended use or use with no contraindication, indications with benefit evidence, and health surveillance agency-approved use. Data were analyzed in electronic databases and the variables were summarized by simple frequency. A total of 164 analgesic, antipyretic, and nonsteroidal anti-inflammatory drugs were prescribed to 150 children aged 1-4 years (38.6%). Dipyrone was included in 82 (54.6%) and ibuprofen in 40 (26.6%) prescriptions. Non-recommended uses were identified in 15% of prescriptions and contraindicated uses were observed in 13.3%. Nimesulide (1.5%) is still prescribed to children younger than 12 years. The dose was incorrect in 74.3% of prescriptions containing dipyrone. Of the 211 reported clinical indications, 56 (26.5%) had no evidence of benefit according to the best available scientific evidence and 66 (31.3%) had indications not approved by the regulatory agencies. There are significant discrepancies between clinical practice and recommended use of analgesic, antipyretic, and nonsteroidal anti-inflammatory drugs in pediatrics. Copyright © 2015 Sociedade Brasileira de Pediatria. Published by Elsevier Editora Ltda. All rights reserved.

Who gets dipyrone (metamizole) in Germany? Prescribing by age, sex and region.

PubMed

Hoffmann, F; Meinecke, P; Freitag, M H; Glaeske, G; Schulze, J; Schmiemann, G

2015-06-01

Metamizole (dipyrone) is an analgesic that has been the focus of considerable controversy regarding its safety. Because of potentially life-threatening blood disorders such as agranulocytosis, it has been withdrawn in many countries but not in Germany, where prescribing even increased over recent years. We aimed to evaluate prescribing of metamizole in Germany with respect to age, sex and regional variations. Using data of a statutory health insurance, we analysed a cohort of 1·7 million persons who were insured at least 1 day in each quarter of 2009. Outcome of interest was the outpatient prescription prevalence, for example the proportion of persons receiving at least one prescription of metamizole. A total of 6·8% received metamizole with a higher prescribing prevalence in females (7·8% vs. 6·0%). The prevalence increased with age up to 26·7% in persons ≥85 years (men: 21·1%; and women: 30·4%). We found large regional variations with higher prevalences in the northern part of Germany. Most of the prescriptions were issued by general practitioners (78·9%). 58·3% were liquid oral formulations with considerable regional variations ranging between 32·3% in Mecklenburg-West Pomerania and 67·3% in North Rhine-Westphalia. Overall, liquid oral forms are much more often prescribed in the western than in the eastern part of Germany. Metamizole - a drug with a relatively narrow indication - is often prescribed in Germany with relevant differences by age, sex and region. Qualitative studies should clarify reasons for this. Further quantitative research should investigate small-area variations, indications and treatment durations. © 2015 John Wiley & Sons Ltd.

Antinociceptive activity of Tibouchina pereirae, an endemic plant from the Brazilian semiarid region.

PubMed

Dias, Êuder Reis; Dias, Thays de Lima Matos Freire; Alexandre-Moreira, Magna Suzana; Branco, Alexsandro

The anti-nociceptive activity of an extract of Tibouchina pereirae Aubl (AETP) was investigated using two models of chemically induced pain, viz. the acetic acid-induced writhing and the formalin test, respectively, with dipyrone and indomethacin as reference drugs, respectively. In the acetic acid-induced writhing test, AETP application (100 mg/kg) caused a significant reduction of writhing produced by acetic acid. In the formalin test, AETP reduced the formalin effects significantly only in the late phase. These findings thus indicate the involvement of AETP only in peripheral antinociceptive mechanisms. In addition, AETP exhibited good antioxidant activity (EC50 approx. 15 μg/mL) in the DPPH free radical scavenging assay.

Dipyrone in association with atropine inhibits the effect on gastric emptying induced by hypoglycemia in rats

PubMed Central

Collares, E.F.; Vinagre, A.M.; Collares-Buzato, C.B.

2017-01-01

Atropine (AT) and dipyrone (Dp) induce a delay of gastric emptying (GE) of liquids in rats by inhibiting muscarinic receptors and activating β2-adrenergic receptors, respectively. The objective of the present study was to determine the effects of pretreatment with AT and Dp, given alone or in combination, on the effect of hypoglycemia in the liquid GE in rats. Male Wistar adult rats (280-310 g) were pretreated intravenously with AT, Dp, AT plus Dp or their vehicle and then treated 30 min later with iv insulin or its vehicle (n=8-10 animals/group). Thirty min after treatment, GE was evaluated by determining, in awake rats, the percent gastric retention (%GR) of a saline meal labeled with phenol red administered by gavage. The results indicated that insulin induced hypoglycemia in a dose-dependent manner resulting in a significant reduction in %GR of liquid only at the highest dose tested (1 U/kg). Pretreatment with AT significantly increased %GR in the rats treated with 1 U/kg insulin. Surprisingly, after pretreatment with AT, the group treated with the lowest dose of insulin (0.25 U/kg) displayed significantly lower %GR compared to its control (vehicle-treated group), which was not seen in the non-pretreated animals. Pretreatment with Dp alone at the dose of 40 mg/kg induced an increase in %GR in both vehicle and 0.25 U/kg-treated rats. A higher dose of Dp alone (80 mg/kg) significantly reduced the effect of a marked hypoglycemia induced by 1 U/kg of insulin on GE while in combination with AT the effect was completely abolished. The results with AT suggest that moderate hypoglycemia may render the inhibitory mechanisms of GE ineffective while Dp alone and in combination with AT significantly overcame the effect of hypoglycemia on GE. PMID:28876363

Antinociceptive effect of systemically administered dipyrone (metamizol), magnesium chloride or both in a murine model of cancer.

PubMed

Brito, B E; Vazquez, E; Taylor, P; Alvarado, Y; Vanegas, H; Millan, A; Tortorici, V

2017-03-01

Opioid effectiveness to treat cancer pain is often compromised by the development of tolerance and the occurrence of undesirable side effects, particularly during long-term treatment. Hence, the search for more efficient analgesics remains a necessity. The main goal of this study was to relieve neuropathic symptoms associated with tumour growth by administering the non-opioid analgesic dipyrone (DIP) alone or in combination with magnesium chloride (MgCl 2 ), an adjuvant that blocks the NMDA receptor channel. Mice were inoculated with a melanoma cell line (B16-BL6) in the left thigh and two protocols were used to evaluate the effect of DIP (270 mg/kg), MgCl 2 (200 mg/kg), or the combination DIP-MgCl 2 . In the therapeutic protocol the drugs, alone or combined, were administered once tumour had promoted increased nociception. In the preventive protocol, drugs were administered prior to the appearance of the primary tumour. Tumour growth was assessed with a caliper and nociception was determined using behavioural tests. DIP promoted antinociception only at the beginning of both protocols due to the development of tolerance. The combination DIP-MgCl 2 improved the antinociceptive effect, avoiding tolerance and reducing tumour growth in the preventive treatment, more efficiently than each compound alone. These results suggest that DIP-MgCl 2 may represent a safe, affordable and accessible option to reduce tumour growth and to treat cancer pain avoiding the risk of tolerance, without the typical complications of opioids agents, particularly when long-term treatment is required. This study shows a non-opioid analgesic combined with an adjuvant as a therapeutic option to treat cancer pain. The avoidance of antinociceptive tolerance when repeated administration is required, as well as tumor growth reduction, are additional advantages to be considered. © 2016 European Pain Federation - EFIC®.

Oral Myiasis Caused by Cochliomyia hominivorax in a Disabled Person.

PubMed

Novo-Neto, José Pereira; Dos Santos, Fabiano de Sant'Ana; Pontes, Ana Emília Farias; Ribeiro, Fernando Salimon; Scannavino, Fábio Luiz Ferreira; Martins, Alex Tadeu

2015-01-01

Myiasis is a parasitic disease caused by developing maggots of fly species, which can infect humans. Patients with special needs, especially those with severe neuropsychomotor limitations, may have oral manifestations of this disease. Here, we present a clinical case in which a disabled person was affected by oral myiasis caused by Cochliomyia hominivorax. Maggots were found in two ulcerated lesions, a 2 cm diameter lesion in the maxilla and a 6 cm diameter lesion in the mandible. Forty-five maggots were removed during inspection, whereas 75 maggots were surgically removed under general anesthesia with nasotracheal intubation. Dipyrone, ivermectin, and clindamycin were prescribed, and the patient remained hospitalized for 3 days. Seven days after surgical intervention, no maggots were observed. Our study emphasizes that dentists must recognize the symptoms and behaviors of parasitic diseases that affect the oral cavity.

The prevalence and characterization of self-medication for obtaining pain relief among undergraduate nursing students.

PubMed

Souza, Layz Alves Ferreira; da Silva, Camila Damázio; Ferraz, Gisely Carvalho; Sousa, Fátima Aparecida Emm Faleiros; Pereira, Lílian Varanda

2011-01-01

This study investigates the prevalence of self-medication among undergraduate nursing students seeking to relieve pain and characterizes the pain and relief obtained through the used medication. This epidemiological and cross-sectional study was carried out with 211 nursing students from a public university in Goiás, GO, Brazil. A numerical scale (0-10) measured pain intensity and relief. The prevalence of self-medication was 38.8%. The source and main determining factor of this practice were the student him/herself (54.1%) and lack of time to go to a doctor (50%), respectively. The most frequently used analgesic was dipyrone (59.8%) and pain relief was classified as good (Md=8.5;Max=10;Min=0). The prevalence of self-medication was higher than that observed in similar studies. Many students reported that relief obtained through self-medication was good, a fact that can delay the clarification of a diagnosis and its appropriate treatment.

Peripheral analgesic sites of action of anti-inflammatory drugs.

PubMed

Ferreira, S H

2002-07-01

Inflammatory signs and symptoms of redness, swelling, heat and pain are due to the effects of inflammatory mediators released during the inflammatory response. Depending on the type of injurious stimuli and the tissue involved, the array of mediators may differ but eicosanoids are involved in the genesis of inflammatory pain. They are responsible for the hypersensitisation of the nociceptors (allodynialhyperalgesia). The basic mechanism of analgesic action of nonsteroidal anti-inflammatory drugs results from the inhibition of prostaglandin synthesis (prostacyclin or PGE2), thus preventing nociceptor threshold lowering. Because there is a temporal hierarchy in the release of inflammatory mediators, there are several targets for the action of peripheral acting analgesics before and after the inhibition of prostaglandin synthesis. Blockade of the release and inhibition of inducible cyclooxygenase explain the analgesic action of glucocorticoids. Nimesulide also has an inhibitory action on the cascade of hypersensitising cytokines. Some analgesics, such as dipyrone, flurbiprofen or diclofenac, act directly upon ongoing inflammatory hypersensitisation. Those analgesics restore the nociceptor by stimulating the arginine/NO/cGMP/K(ATP) channel pathway.

Discovery of phenylsulfonylfuroxan derivatives as gamma globin inducers by histone acetylation.

PubMed

Melo, Thais Regina Ferreira de; Kumkhaek, Chutima; Fernandes, Guilherme Felipe Dos Santos; Lopes Pires, Maria Elisa; Chelucci, Rafael Consolin; Barbieri, Karina Pereira; Coelho, Fernanda; Capote, Ticiana Sidorenko de Oliveira; Lanaro, Carolina; Carlos, Iracilda Zeppone; Marcondes, Sisi; Chegaev, Konstantin; Guglielmo, Stefano; Fruttero, Roberta; Chung, Man Chin; Costa, Fernando Ferreira; Rodgers, Griffin P; Dos Santos, Jean Leandro

2018-05-28

N-oxide derivatives 5(a-b), 8(a-b), and 11(a-c) were designed, synthesized and evaluated in vitro and in vivo as potential drugs that are able to ameliorate sickle cell disease (SCD) symptoms. All of the compounds demonstrated the capacity to releasing nitric oxide at different levels ranging from 0.8 to 30.1%, in vivo analgesic activity and ability to reduce TNF-α levels in the supernatants of monocyte cultures. The most active compound (8b) protected 50.1% against acetic acid-induced abdominal constrictions, while dipyrone, which was used as a control only protected 35%. Compounds 8a and 8b inhibited ADP-induced platelet aggregation by 84% and 76.1%, respectively. Both compounds increased γ-globin in K562 cells at 100 μM. The mechanisms involved in the γ-globin increase are related to the acetylation of histones H3 and H4 that is induced by these compounds. In vitro, the most promising compound (8b) was not cytotoxic, mutagenic and genotoxic. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Idiosyncratic drug-induced agranulocytosis or acute neutropenia.

PubMed

Andrès, Emmanuel; Maloisel, Frédéric

2008-01-01

Idiosyncratic drug-induced agranulocytosis or acute neutropenia is an adverse event resulting in a neutrophil count of under 0.5 x 10/l. Patients with such severe neutropenia are likely to experience life-threatening and sometimes fatal infections. Over the last 20 years, the incidence of idiosyncratic drug-induced agranulocytosis or acute neutropenia has remained stable at 2.4-15.4 cases per million, despite the emergence of new causative drugs: antibiotics (beta-lactam and cotrimoxazole), antiplatelet agents (ticlopidine), antithyroid drugs, sulfasalazine, neuroleptics (clozapine), antiepileptic agents (carbamazepine), nonsteroidal anti-inflammatory agents and dipyrone. Drug-induced agranulocytosis remains a serious adverse event due to the occurrence of severe sepsis with severe deep infections (such as pneumonia), septicemia and septic shock in around two thirds of patients. In this setting, old age (>65 years), septicemia or shock, metabolic disorders such as renal failure, and a neutrophil count under 0.1 x 10/l are poor prognostic factors. Nevertheless with appropriate management using preestablished procedures, with intravenous broad-spectrum antibiotic therapy and hematopoietic growth factors, the mortality rate is currently around 5%. Given the increased life expectancy and subsequent longer exposure to drugs, as well as the development of new agents, healthcare professionals should be aware of this adverse event and its management.

Pharmacological Basis for Traditional Use of the Lippia thymoides

PubMed Central

Silva, Fabrício Souza; Menezes, Pedro Modesto Nascimento; de Sá, Pedro Guilherme Souza; Oliveira, André Luís de Santana; Souza, Eric Alencar Araújo; Bamberg, Vinicius Martins; de Oliveira, Henrique Ribeiro; de Oliveira, Sheilla Andrade; Araújo, Roni Evêncio e; Uetanabaro, Ana Paula Trovatti; Silva, Tânia Regina dos Santos; Almeida, Jackson Roberto Guedes da Silva; Lucchese, Angélica Maria

2015-01-01

The aim of this study was to evaluate crude extracts and fractions from leaves and stems of Lippia thymoides and to validate their use in folk medicine. In vitro antioxidant and antimicrobial activities and in vivo wound healing in rats, baker yeast-induced fever in young rats, and acute oral toxicity in mice assays were realized. The crude extracts and their dichloromethane and ethyl acetate fractions had potent radical-scavenging activity against the DPPH but were not effective in the β-carotene bleaching method. The dichloromethane fraction from the leaves extract showed the broadest spectrum of activity against S. aureus, B. cereus, and C. parapsilosis. The animals treated with crude extracts showed no difference in wound healing when compared with the negative control group. The crude extract from leaves (1200 mg/kg) has equal efficacy in reducing temperature in rats with hyperpyrexia compared to dipyrone (240 mg/kg) and is better than paracetamol (150 mg/kg). In acute toxicity test, crude extract of leaves from Lippia thymoides exhibited no mortality and behavioral changes and no adverse effects in male and female mice. This work validates the popular use of Lippia thymoides for treating the wound and fever, providing a source for biologically active substances. PMID:25892998

Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit

PubMed Central

de Melo, Thais Regina Ferreira; Chelucci, Rafael Consolin; Pires, Maria Elisa Lopes; Dutra, Luiz Antonio; Barbieri, Karina Pereira; Bosquesi, Priscila Longhin; Trossini, Gustavo Henrique Goulart; Chung, Man Chin; dos Santos, Jean Leandro

2014-01-01

A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs. PMID:24714090

Non-prescription (OTC) oral analgesics for acute pain - an overview of Cochrane reviews.

PubMed

Moore, R Andrew; Wiffen, Philip J; Derry, Sheena; Maguire, Terry; Roy, Yvonne M; Tyrrell, Laila

2015-11-04

Non-prescription (over-the-counter, or OTC) analgesics (painkillers) are used frequently. They are available in various brands, package sizes, formulations, and dose. They can be used for a range of different types of pain, but this overview reports on how well they work for acute pain (pain of short duration, usually with rapid onset). Thirty-nine Cochrane reviews of randomised trials have examined the analgesic efficacy of individual drug interventions in acute postoperative pain. To examine published Cochrane reviews for information about the efficacy of pain medicines available without prescription using data from acute postoperative pain. We identified OTC analgesics available in the UK, Australia, Canada, and the USA by examining online pharmacy websites. We also included some analgesics (diclofenac potassium, dexketoprofen, dipyrone) of importance in parts of the world, but not currently available in these jurisdictions.We identified systematic reviews by searching the Cochrane Database of Systematic Reviews (CDSR) on The Cochrane Library through a simple search strategy. All reviews were overseen by a single review group, had a standard title, and had as their primary outcome numbers of participants with at least 50% pain relief over four to six hours compared with placebo. From individual reviews we extracted the number needed to treat for an additional beneficial outcome (NNT) for this outcome for each drug/dose combination, and also calculated the success rate to achieve at least 50% of maximum pain relief. We also examined the number of participants experiencing any adverse event, and whether the incidence was different from placebo. We found information on 21 different OTC analgesic drugs, doses, and formulations, using information from 10 Cochrane reviews, supplemented by information from one non-Cochrane review with additional information on ibuprofen formulations (high quality evidence). The lowest (best) NNT values were for combinations of ibuprofen plus paracetamol, with NNT values below 2. Analgesics with values close to 2 included fast acting formulations of ibuprofen 200 mg and 400 mg, ibuprofen 200 mg plus caffeine 100 mg, and diclofenac potassium 50 mg. Combinations of ibuprofen plus paracetamol had success rates of almost 70%, with dipyrone 500 mg, fast acting ibuprofen formulations 200 mg and 400 mg, ibuprofen 200 mg plus caffeine 100 mg, and diclofenac potassium 50 mg having success rates above 50%. Paracetamol and aspirin at various doses had NNT values of 3 or above, and success rates of 11% to 43%. We found no information on many of the commonly available low dose codeine combinations.The proportion of participants experiencing an adverse event were generally not different from placebo, except for aspirin 1000 mg and (barely) ibuprofen 200 mg plus caffeine 100 mg. For ibuprofen plus paracetamol, adverse event rates were lower than with placebo. There is a body of reliable evidence about the efficacy of some of the most commonly available drugs and doses widely available without prescription. The postoperative pain model is predominantly pain after third molar extraction, which is used as the industry model for everyday pain. The proportion of people with acute pain who get good pain relief with any of them ranges from around 70% at best to less than 20% at worst; low doses of some drugs in fast acting formulations were among the best. Adverse events were generally no different from placebo. Consumers can make an informed choice based on this knowledge, together with availability and price. Headache and migraine were not included in this overview.

Aqueous root extracts from Mimosa albida Humb. & Bonpl. ex Willd display antinociceptive activity in mice.

PubMed

Rejón-Orantes, J C; Suaréz, D P Perdomo; Rejón-Rodríguez, A; Hernández, S Hernández; Liévano, O E García; Rodríguez, D López; de la Mora, M Pérez

2013-09-16

In this work, we study whether aqueous extracts from the roots of Mimosa albida Humb. & Bonpl. ex Willd, a plant known in the Highlands of Chiapas, Mexico as "Lotóm chíx" are endowed with both antinociceptive and anxiolytic effects. ICR mice were systemically treated with aqueous extracts from Mimosa albida and the reference compounds (diazepam, dipyrone and/or fentanyl) and their behavior was evaluated in several behavioral tests. Administration of aqueous extracts from the roots of Mimosa albida resulted in a reduction of the nociception elicited in mice by both the hot plate (12.5, 25 and 50 mg/kg; i.p.) and the acetic acid-induced writhing (25 and 50 mg/kg; i.p.) tests. No effects were however observed both in the elevated plus-maze and hole board test (3.2, 12.5 and 25 mg/kg; i.p.). In contrast, both locomotion (open field test) and motor coordination (rotarod test) were affected at doses (50, 100 y 200 mg/kg; i.p.) higher than those having antinociceptive effects. These data suggest that in mice the systemic administration of low doses of aqueous extracts from the roots of Mimosa albida results in antinociceptive effects in several models of pain through mechanisms that do not involve the opioid system pathway. These results support the ethnopharmacological use of Mimosa albida in popular medicine. © 2013 Elsevier Ireland Ltd. All rights reserved.

Multicentre evaluation of postoperative pain control after 24hours in three hospitals of Colombia.

PubMed

Machado-Alba, Jorge Enrique; Machado-Duque, Manuel Enrique; Ramírez-Sarmiento, Javier Orlando

To determine the intensity of pain in operated patients using a visual analogue scale and identify variables associated with lack of pain control in three cities in Colombia. A cross-sectional study in patients over the age of 18 years, between January 1 st and September 30 th 2014, in 3 clinics in Colombia. The intensity of postoperative pain using a visual analogue scale at 24hours after surgery was recorded. Socio-demographic, clinical and pharmacological variables were taken into account. SPSS 22.0 was used for the analysis. 460 patients were evaluated, mean age 47.6±17.4 years, and 63.3% were female. The mean pain level was 23.8±17.4mm, with 91 (19.8% of patients) with moderate or greater pain (i.e., lack of pain control). Tramadol was the most used analgesic, followed by dipyrone and diclofenac. 53.0% were treated with monotherapy. Compliance with the dosing regimen of the first analgesic (OR: 0.53; 95% CI: 0.294 to .988; p=.046) was statistically significantly associated with a decreased risk of poorly controlled pain. Pain intensity and the proportion of patients with uncontrolled pain at 24hours after surgery show better results than other studies previously published in the country. There must be insistence on the administration of analgesia within a suitable interval in order to improve pain control. Copyright © 2017 Elsevier España, S.L.U. All rights reserved.

Fast track endoscopic thoracic sympathicotomy.

PubMed

Duarte, João Bosco Vieira; Kux, Peter; Castro, Carlos H V; Cruvinel, Marcos G C; Costa, José R R

2003-12-01

The length of hospital stay is an important factor of cost and psychological discomfort in the treatment of hyperhidrosis by endoscopic thoracic sympathicotomy (ETS). Our experience enrolls 1587 patients operated on an outpatient basis in the last 10 years and seven months. This study aimed to confirm that ETS can be performed on an outpatient basis. Fifty-two consecutive patients (30 males and 22 females) were submitted to ETS under general anesthesia using a single lumen endotracheal tube, with lung collapse by intrapleural injection of CO(2). The sympathetic chain and the communicating rami were severed at different levels according to hyperhidrosis location. Patients were physical state American Society of Anesthesiologists 1 and 2. Age varied between 13 and 55 years (27.3 +/- 10.2 years). They were monitored with ECG, SPO2, NIBP, expired CO(2), sevoflurane analyzer, and airway pressure. Normal saline (40.0 +/- 2.7 ml/kg) was infused intravenously. The drugs used were propofol, alfentanil, rocuronium, ondansetron, dexamethasone, dipyrone, cetoprofene and sevoflurane. Anesthesia and post-operative data were analyzed. Post-operative thoracic X-rays were taken in 20 patients before discharge. Anesthesia lasted 67.2 +/- 20.8 minutes, and the surgical procedure took 46.3 +/- 20.9 minutes. The patients stayed 18.0 +/- 11.0 minutes in the post-anaesthetic care unit and were discharged from hospital after 150.3 +/- 43.1 minutes. The only abnormal post-operative event observed was insignificant residual carbothorax, found in 2 (10%) of the thoracic X-rays taken. In conclusion, this study confirmed that ETS can be performed safely on an outpatient basis.

[Human Single Drug Exposures to Non-opioid Analgesics Reported to the Poisons Information Centre Erfurt from 2003 to 2012].

PubMed

Hentschel, H; Prasa, D; Bergmann, I; Enden, G; Plenert, B; Frimlova, G; Just, S; Liebetrau, G; Stürzebecher, A; Deters, M

2016-01-01

Because of their frequency, non-opioid analgesics (NOA) single drug exposures registered by Poisons Information Centre (PIC) Erfurt have been studied over a decade. A retrospective analysis of frequencies, circumstances of exposure, symptom severity, and age groups in NOA single drug exposures received by the PIC Erfurt from the beginning of 2003 to the end of 2012 was undertaken. Of all 4749 NOA single drug exposures, the 10 most frequent were caused by paracetamol (n=1 686), ibuprofen (n=1 439), acetylsalicylic acid (n=456), dipyrone (n=274), diclofenac (n=267), flupirtine (n=138), naproxen (n=41), etoricoxib (n=36), indomethacin (n=24), and dexketoprofen (n=19). Paracetamol single drug exposures increased from 158 in 2003 to 216 in 2007 and fell afterwards to 133 in 2012. Ibuprofen single drug exposures continously rose from 57 in 2003 to 258 in 2012. Adults were more often involved in NOA (53.8%) and all single drug exposures (54.1%) than children (45.9% and 45.6%, respectively). Suicidal attempts were more frequent in NOA (43.1%) than in all single drug exposures (34.2%), whereas accidental exposures or exposures in abuse were less often (33.4 and 0.2%, 46.0 and 0.9% respectively). NOA single drug exposures resulted mostly in none to minor symptoms (77.0%) and rarely in moderate (2.1%) or severe symptoms (1.0%). One adult was found dead after probable ingestion of 32 g of acetylsalicylic acid in suicidal intention. Because many NOA are over-the-counter drugs, it is difficult to obtain data on their use. PIC data could provide information on the NOA use in the population. © Georg Thieme Verlag KG Stuttgart · New York.

Case-crossover study of Burkholderia cepacia complex bloodstream infection associated with contaminated intravenous bromopride.

PubMed

Martins, Ianick Souto; Pellegrino, Flávia Lúcia Piffano Costa; Freitas, Andrea d'Avila; Santos, Marisa da Silva; Ferraiuoli, Giovanna Ianini d'Alemeida; Vasques, Márcia Regina Guimarães; Amorim, Efigenia Lourdes Teixeira; Oliveira, Sandra; Nouér, Simone Aranha; Cardoso, Fernando Luiz Lopes; Mascarenhas, Luiz Affonso; Magalhães, Ana Cristina Gouveia; Cleinman, Isabella Barbosa; Figueiredo, Agnes Marie Sá; Moreira, Beatriz Meurer

2010-05-01

To investigate an outbreak of healthcare-associated Burkholderia cepacia complex (BCC) primary bloodstream infections (BCC-BSI). Case-crossover study in a public hospital, a university hospital and a private hospital in Rio de Janeiro, Brazil, from March 2006 to May 2006. Twenty-five patients with BCC-BSI. After determining the date BCC-BSI symptoms started for each patient, 3 time intervals of data collection were defined, each one with a duration of 3 days: the case period, starting just before BCC-BSI symptoms onset; the control period, starting 6 days before BCC-BSI symptoms onset; and the washout period, comprising the 3 days between the case period and the control period. Exposures evaluated were intravascular solutions and invasive devices and procedures. Potential risk factors were identified by using the McNemar chi(2) adjusted test. Cultures of samples of potentially contaminated solutions were performed. BCC strain typing was performed by pulsed-field gel electrophoresis using SpeI. The statistical analysis revealed that the use of bromopride and dipyrone was associated with BCC-BSI. A total of 21 clinical isolates from 17 (68%) of the 25 patients and an isolate obtained from the bromopride vial were available for strain typing. Six pulsotypes were detected. A predominant pulsotype (A) accounted for 11 isolates obtained from 11 patients (65%) in the 3 study hospitals. Our investigation, using a case-crossover design, of an outbreak of BCC-BSI infections concluded it was polyclonal but likely caused by infusion of contaminated bromopride. The epidemiological finding was validated by microbiological analysis. After recall of contaminated bromopride vials by the manufacturer, the outbreak was controlled.

Self-medication in university students from the city of Rio Grande, Brazil

PubMed Central

2012-01-01

Background Self-medication is the use of medication without prescription, orientation, or supervision of a physician or dentist. Self-medication might become a serious health problem. The purpose of this study was to identify the prevalence and factors associated with self-medication among first and last-year students enrolled in healthcare and non-healthcare programs. Methods A cross-sectional study was conducted at Universidade Federal do Rio Grande (FURG), state of Rio Grande do Sul, Brazil. Of 830 students in the sample, 95% answered the questionnaire – 789 students enrolled in 10 undergraduate programs. Mean age was 22 ± 6.17 years. The students answered a questionnaire covering socio-economic and demographic variables, use of medication, and medication knowledge. Information was collected on the conditions treated with medication, the medications used, and attitude towards self-medication. Results Of 789 students, 86.4% self-medicated (88.5% of 446 healthcare students). There were no significant differences in self-medication between healthcare and non-healthcare students, nor between first and last-year students. Bivariate and multivariate analyses showed a significant association between self-medication and having children (p = 0.01), having a home pharmacy (p < 0.001) and adequate medication knowledge (p = 0.01). The most frequently used active ingredients were acetaminophen (paracetamol), dipyrone, aspirin, phytotherapic compounds, and tea. Illicit drug use was significantly associated with self-medication in the multivariate analysis. Conclusion The fact that being a healthcare student was associated with higher medication knowledge, but not with less self-medication, suggests that medication knowledge might contribute to increase self-medication. This should be taken into account when designing educational interventions relating to self-medication. PMID:22568959

Antinociceptive effect in mice of a hydroalcoholic extract of Neurolaena lobata (L.) R. Br. and its organic fractions.

PubMed

Gracioso, J S; Paulo, M Q; Hiruma Lima, C A; Souza Brito, A R

1998-12-01

An infusion of the aerial parts of Neurolaena lobata (L.) R. Br. (Compositae-Asteraceae) is used in Caribbean folk medicine to treat several kinds of pain. In this investigation we studied the acute oral toxicity of the hydroalcoholic extract of the plant and the antinociceptive effect of the extract and of its hexane- and chloroform-partitioned fractions, given orally, in nociception and inflammatory models in mice. No signs of toxicity were observed for oral doses up to 5000 mg kg(-1) in mice. Morphine hydrochloride (100 mg kg(-1)), dipyrone sodium (200 mg kg(-1)), the hydroalcoholic extract (1000 mg kg(-1)), and its chloroform- and hexane-partitioned fractions (100 mg kg(-1)) significantly inhibited acetic acid-induced abdominal constriction in mice (100, 95, 47, 62 and 60% inhibition, respectively when compared with the negative control). In the hot-plate test in mice, morphine hydrochloride, the chloroform- and hexane-partitioned fractions, but not the hydroalcoholic extract, resulted in a significant latency increase in all observation times. In the acetic acid-induced abdominal constriction in mice, pretreatment of the animals with naloxone significantly reversed the analgesic effect of morphine, but not that of the hydroalcoholic extract or of its hexane- and chloroform-partitioned fractions. Finally, administration of the hexane- and chloroform-partitioned fractions (100 mg kg(-1)) had a significant anti-oedematogenic effect on carrageenan-induced oedema in mice. These data show that the hydroalcoholic extract of N. lobata and, in particular, its partitioned fractions have significant analgesic properties when assessed through these pain models. Their antinociceptive effect might be the result of interference with the inflammatory process.

Effects of reference analgesics and psychoactive drugs on the noxious heat threshold of mice measured by an increasing-temperature water bath.

PubMed

Boros, Melinda; Benkó, Rita; Bölcskei, Kata; Szolcsányi, János; Barthó, Loránd; Pethő, Gábor

2013-12-01

The study aimed at validating an increasing-temperature water bath suitable for determining the noxious heat threshold for use in mice. The noxious heat threshold was determined by immersing the tail of the gently held awake mouse into a water container whose temperature was near-linearly increased at a rate of 24°C/min. until the animal withdrew its tail, that is, heating attained the noxious threshold. The effects of standard analgesic, neuroleptic and anxiolytic drugs were investigated in a parallel way on both the noxious heat threshold and the psychomotor activity assessed by the open field test. Morphine, diclofenac and metamizol (dipyrone) elevated the heat threshold of mice with minimum effective doses of 6, 30 and 1000 mg/kg i.p., respectively. These doses of morphine and diclofenac failed to induce any remarkable effect on psychomotor activity in the open field test while that of metamizol exerted a profound inhibition. The anxiolytic diazepam and the neuroleptic droperidol at doses evoking a mild and moderate, respectively, psychomotor inhibition failed to alter the heat threshold. Combination of a subliminal dose of morphine (regarding both antinociceptive and psychomotor inhibitory action) with diclofenac, metamizol, diazepam or droperidol at doses also subliminal regarding the thermal antinociceptive effect elevated the noxious heat threshold without major additional effects in the open field test. It is concluded that the increasing-temperature water bath is suitable for studying the thermal antinociceptive effects of morphine and diclofenac as well as the morphine-sparing action of diclofenac, metamizol, droperidol and diazepam. Behavioural testing is recommended when testing analgesics. © 2013 Nordic Pharmacological Society. Published by John Wiley & Sons Ltd.

Degradation of 4-aminoantipyrine by electro-oxidation with a boron-doped diamond anode: Optimization by central composite design, oxidation products and toxicity.

PubMed

de Melo da Silva, Lucas; Gozzi, Fábio; Sirés, Ignasi; Brillas, Enric; de Oliveira, Silvio Cesar; Machulek, Amilcar

2018-08-01

Electro-oxidation with electrogenerated H 2 O 2 (EO-H 2 O 2 ) was applied to treat acidic aqueous solutions of 4-aminoantipyrine (4-AA), a persistent drug metabolite of dipyrone, in sulfate medium. Trials were made using a boron-doped diamond anode in the presence of H 2 O 2 electrogenerated on site. A 2 4 central composite design (CCD) was employed to evaluate the effect of four independent variables, namely current density (j), pH, 4-AA concentration and electrolysis time, on the percentages of degradation and mineralization, as well as on mineralization current efficiency (MCE). Predicted responses agreed with observed values, showing linear trendlines with good R 2 and R 2 adj values. The degradation was optimum at j=77.5mAcm -2 , pH3.5 and 62.5mgL -1 4-AA, leading to 63% and 99% removal after 3 and 7min, respectively. For those solutions, the largest mineralization was found at j=77.5mAcm -2 , attaining 45% abatement at 175min. Low MCE values were obtained in all electrolyses. An initial route for 4-AA degradation is proposed based on one dimer and eleven aromatic and aliphatic intermediates detected in the treated solutions at pH3.5 by LC-MS. The initial 62.5mgL -1 solution at pH3.5 presented acute toxicity on Artemia salina larvae, with LC 50 =13.6mgL -1 , being substantially reduced after 3 and 7min of EO-H 2 O 2 at j=77.5mAcm -2 due to the formation of less toxic derivatives. Copyright © 2018 Elsevier B.V. All rights reserved.

Pain medication in German nursing homes: a whole lot of metamizole.

PubMed

Hoffmann, Falk; Schmiemann, Guido

2016-06-01

Prescribing of metamizole (dipyrone), an analgesic that has been withdrawn from the market or never approved in many countries owing to safety concerns, is high in elder persons in Germany. This study assessed the use of pain medications in German nursing homes with a special focus on prescribing patterns of metamizole. Using data of the 'Inappropriate Medication in Patients with Renal Insufficiency in Nursing Homes' (IMREN) study conducted between October 2014 and April 2015 in nursing homes in Bremen and Lower Saxony, we studied prescribing of analgesics including both scheduled and as-needed medications. For residents with scheduled medication, dosage and duration of use were analysed. A total of 852 residents from 21 nursing homes were included. They were on average 83.5 years old, and 76.5% were women; 73.8% received at least one analgesic with 70.3% obtaining World Health Organization step I drugs. The most frequently prescribed substances were metamizole (for 40.6%) and paracetamol (acetaminophen; 35.6%), with paracetamol given mostly as-needed. The proportion of residents receiving metamizole increased with age (up to 47.4% in persons aged 90 years and over). Of 143 residents with scheduled metamizole (16.8%), the mean daily dosage was 1843 mg (interquartile range [IQR]: 1500-2250); 66.9% received metamizole for at least 90 days and 23.2% for at least 365 days (mean duration 276 days; IQR: 59-314). There is a discrepancy between prescribing of metamizole for older persons, on the one hand, and evidence on comparative effectiveness and safety as well as approval and recommendations, on the other hand. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

Analytical methodologies based on LC-MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge.

PubMed

Boix, C; Ibáñez, M; Fabregat-Safont, D; Morales, E; Pastor, L; Sancho, J V; Sánchez-Ramírez, J E; Hernández, F

2016-01-01

In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, carbamazepine, 4-aminoantipyrine (4-AA), 4-acetyl aminoantipyrine (4-AAA), 4-formyl aminoantipyrine (4-FAA), venlafaxine and benzoylecgonine. The aqueous and solid phases of the sewage sludge were analyzed making use of Solid-Phase Extraction (SPE) and UltraSonic Extraction (USE) for sample treatment, respectively. The methods were validated at three concentration levels: 0.2, 2 and 20 μg L(-1) for the aqueous phase, and 50, 500 and 2000 μg kg(-1) for the solid phase of the sludge. In general, the method was satisfactorily validated, showing good recoveries (70-120%) and precision (RSD < 20%). Regarding the limit of quantification (LOQ), it was below 0.1 μg L(-1) in the aqueous phase and below 50 μg kg(-1) in the solid phase for the majority of the analytes. The method applicability was tested by analysis of samples from a wider study on degradation of emerging pollutants in sewage sludge under anaerobic digestion. The key benefits of these methodologies are: • SPE and USE are appropriate sample procedures to extract selected emerging contaminants from the aqueous phase of the sewage sludge and the solid residue. • LC-MS/MS is highly suitable for determining emerging contaminants in both sludge phases. • Up to our knowledge, the main metabolites of dipyrone had not been studied before in sewage sludge.

Prevalence of self-medication in Brazil and associated factors

PubMed Central

Arrais, Paulo Sérgio Dourado; Fernandes, Maria Eneida Porto; Pizzol, Tatiane da Silva Dal; Ramos, Luiz Roberto; Mengue, Sotero Serrate; Luiza, Vera Lucia; Tavares, Noemia Urruth Leão; Farias, Mareni Rocha; Oliveira, Maria Auxiliadora; Bertoldi, Andréa Dâmaso

2016-01-01

ABSTRACT OBJECTIVE To analyze the prevalence and associated factors regarding the use of medicines by self-medication in Brazil. METHODS This cross-sectional population-based study was conducted using data from the PNAUM (National Survey on Access, Use and Promotion of Rational Use of Medicines), collected between September 2013 and February 2014 by interviews at the homes of the respondents. All people who reported using any medicines not prescribed by a doctor or dentist were classified as self-medication practitioners. Crude and adjusted prevalence ratios (Poisson regression) and their respective 95% confidence intervals were calculated in order to investigate the factors associated with the use of self-medication by medicines. The independent variables were: sociodemographic characteristics, health conditions and access to and use of health services. In addition, the most commonly consumed medicines by self-medication were individually identified. RESULTS The self-medication prevalence in Brazil was 16.1% (95%CI 15.0–17.5), with it being highest in the Northeast region (23.8%; 95%CI 21.6–26.2). Following the adjusted analysis, self-medication was observed to be associated with females, inhabitants from the North, Northeast and Midwest regions and individuals that have had one, or two or more chronic diseases. Analgesics and muscle relaxants were the therapeutic groups most used for self-medication, with dipyrone being the most consumed medicines. In general, most of the medicines used for self-medication were classified as non-prescriptive (65.5%). CONCLUSIONS Self-medication is common practice in Brazil and mainly involves the use of non-prescription medicines; therefore, the users of such should be made aware of the possible risks. PMID:27982373

Transcutaneous electrical nerve stimulation for pain relief after liposuction: a randomized controlled trial.

PubMed

da Silva, Milla Pompilio; Liebano, Richard Eloin; Rodrigues, Victor Ales; Abla, Luiz Eduardo Felipe; Ferreira, Lydia Masako

2015-04-01

Liposuction is a common cosmetic surgical procedure, which requires analgesia for postoperative pain. Transcutaneous electrical nerve stimulation (TENS) has been used for postoperative pain relief; however, there is no evidence of its effectiveness in liposuction patients and this is the focus of this paper. A prospective, randomized, double-blind, controlled trial was conducted with 42 adult patients who underwent liposuction. Patients were randomly allocated to either the TENS group (active TENS) or control group (sham TENS). All patients received morphine (0.1 mg/kg) and dipyrone 1 g immediately after surgery; TENS was delivered 2 h later. The primary outcome was pain intensity. Secondary outcomes were analgesic requirement, number and types of adverse effects of TENS, quality of pain, treatment success, and patient satisfaction. Postoperative pain was measured using a visual analog scale (VAS) and the Brazilian version of the McGill Pain Questionnaire (Br-MPQ). Patients in the TENS group reported significantly lower pain intensity (P < 0.001, effect size = 0.92) compared with those in the control group. TENS significantly decreased the consumption of analgesics in the postoperative period (P < 0.001). No withdrawals or adverse effects were observed in the TENS group, but 33.3% of patients in the control group reported drowsiness and nausea. About 95 and 38% of patients in the TENS and control groups, respectively, were satisfied with the analgesic treatment. The results indicate that TENS is effective as an adjunct to analgesics for pain relief after liposuction. This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266.

Use of medicines and other products for therapeutic purposes among children in Brazil.

PubMed

Pizzol, Tatiane da Silva Dal; Tavares, Noemia Urruth Leão; Bertoldi, Andréa Dâmaso; Farias, Mareni Rocha; Arrais, Paulo Sergio Dourado; Ramos, Luiz Roberto; Oliveira, Maria Auxiliadora; Luiza, Vera Lucia; Mengue, Sotero Serrate

2016-12-01

To assess the prevalence of the use of medicines and other products for therapeutic purposes in the Brazilian pediatric population and test whether demographic, socioeconomic and health factors are associated with use. A cross-sectional population-based study (National Survey on Access, Use and Promotion of Rational Use of Medicines - PNAUM), including 7,528 children aged 12 or younger, living in urban areas in Brazil. Medicine use to treat chronic or acute diseases was reported by the primary caregiver present at the household interview. Associations between independent variables and medicine use were investigated by Poisson regression. The overall prevalence of medicine use was 30.7% (95%CI 28.3-33.1). The prevalence of medicine use for chronic diseases was 5.6% (95%CI 4.7-6.7) and for acute conditions, 27.1% (95%CI 24.8-29.4). The factors significantly associated with overall use were five years old or under, living in the Northeast region, having health insurance and using health services in the last 12 months (emergency visits and hospitalizations). The following were associated with drug use for chronic diseases: age ≥ 2 years, Southeast and South regions, and use of health services. For drug use in treating acute conditions, the following associated factors were identified: ≤ 5 years, North, Northeast or Midwest regions, health insurance, and one or more emergency visits. The most commonly used drugs among children under two years of age were paracetamol, ascorbic acid, and dipyrone; for children aged two years or over they were dipyrone, paracetamol, and amoxicillin. The use of medicine by children is considerable, especially in treating acute medical conditions. Children using drugs for chronic diseases have a different demographic profile from those using drugs for acute conditions in relation to gender, age, and geographic region. Estimar a prevalência de uso de medicamentos e outros produtos com finalidade terapêutica na população pediátrica brasileira e testar se fatores demográficos, socioeconômicos e médicos estão associados ao uso. Estudo transversal de base populacional (Pesquisa Nacional sobre Acesso, Utilização e Promoção do Uso Racional de Medicamentos - PNAUM), incluindo 7.528 crianças com 12 anos ou menos de idade, residentes na zona urbana do território brasileiro. O uso de medicamentos para tratar doenças crônicas ou agudas foi referido pelo principal cuidador da criança presente na entrevista domiciliar. Associações entre as variáveis independentes e o uso de medicamentos foram investigadas por meio de regressão de Poisson. A prevalência de uso global de medicamentos foi de 30,7% (IC95% 28,3-33,1). A prevalência de uso de medicamentos para doenças crônicas foi de 5,6% (IC95% 4,7-6,7) e para condições agudas, 27,1% (IC95% 24,8-29,4). Os fatores significativamente associados com o uso global foram ter no máximo cinco anos de idade, residir na região Nordeste, ter plano de saúde e utilizar serviços de saúde nos últimos 12 meses (consultas de emergência e internações). Associaram-se ao uso de medicamentos para doenças crônicas: idade ≥ 2 anos, regiões Sudeste e Sul e utilização de serviços de saúde. Para o uso de medicamentos em condições agudas, foram identificados os seguintes fatores associados: ≤ 5 anos, Norte, Nordeste ou Centro-Oeste, plano de saúde e uma ou mais consultas de emergência. Os medicamentos com maior prevalência de uso pelas crianças menores de dois anos foram paracetamol, ácido ascórbico e dipirona; nas crianças com 2 ou mais anos, foram dipirona, paracetamol e amoxicilina. O uso de medicamentos na população infantil é substancial, principalmente no tratamento de condições médicas agudas. As crianças usuárias de medicamentos para doenças crônicas apresentam perfil demográfico diferente das usuárias de medicamentos para condições agudas, em relação ao sexo, à idade e à região geográfica.

How natural are 'natural herbal remedies'? A Saudi perspective.

PubMed

Bogusz, Maciej J; al Tufail, Mohammed; Hassan, Huda

2002-01-01

There is a rapidly growing trend in the consumption of herbal remedies in industrialised and developing countries. Users of herbal remedies are at risk of toxicity and adverse interactions of herbal preparations due to their frequent contamination with metals and adulteration with synthetic drugs. The purpose of this study was to assess the quality of herbal remedies present on the market in Saudi Arabia in recent years. 247 herbal remedies and related preparations were examined from 2000-2001 at the Toxicology Laboratory, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia. Herbal powder samples were the most common sample type examined (n = 80), followed by complete, packed preparations (n = 59), single undescribed capsules or pills (n = 46), loose plant leaves or seeds (n = 28), creams (n = 18) and liquid or jelly samples (n = 16). All samples were subjected to toxicological screening for organic substances using gas chromatographic-mass spectrometric analysis, screening for heavy metals (arsenic, mercury, and lead) using inductive coupled plasma-mass spectrometry and microbiological examination. The preparations analysed were used to treat the following indications: leukaemia and other forms of cancer (n = 22); obesity (n = 18); diabetes mellitus (n = 14); rheumatic disorders (n = 14); skin pigmentation problems (n = 11); or to enhance male sexual activity (n = 9). In 123 cases, the indication of use was not known. 39 samples contained high concentrations of heavy metals. This was particularly striking in remedies used to treat leukaemia (arsenic content of 522-161,600 ppm) and in creams for whitening skin (mercury content of 5,700-126,000 ppm). Eight preparations contained synthetic drugs (e.g. benzodiazepines and tricyclic antidepressants in sedative preparations, cyproheptadine in a remedy to gain bodyweight, ibuprofen and dipyrone in herbal capsules used to treat rheumatism). 18 samples were contaminated with micro-organisms. 14 samples contained toxic substances of natural origin. Of the 247 examined preparations, 77 (i.e. over 30%) were disqualified due to high heavy metals content, bacterial contamination or presence of toxic organic substances. The study shows an urgent need to control the production, importing and selling of herbal preparations.

391 Description of Drug Allergy Study Conducted in a Teaching Hospital between October 2007 and March 2011

PubMed Central

Rodríguez Martínez, Consuelo Fernanda; Rubio, Alicia Sciaraffia

2012-01-01

Background The World Allergy Organization (WAO) in 2003 defined ‘drug allergy’ as an immunologically mediated drug hypersensitivity reaction. The mechanism of drug allergy may be either IgE or non-IgE mediated. The true incidence of drug allergy is not known. There are only few studies/datasets using standardized clinical questionnaires and validated in vivo or in vitro tests to confirm the diagnosis of drug allergy. Here we have analyzed the obtained results of in vivo test in suspected drug allergy patients. Methods Data from the Centre of Allergies of the Clinical Hospital of the Universidad de Chile between the months of October 2007 and March 2011 was obtained. The information of the protocols of drug executed, by defining as Protocol the study of a probable allergy by 2 or more procedures, which can be: Prick Test, intradermal reaction, specific IgE and/or Test Patch. Results For a total of 126 drug protocols, 25% of them were trivírica vaccine, 24% β-lactams, 21% local anaesthetics and 10% to general anesthesia (inductors, muscle relaxants and Latex). Of the total of patients undergoing protocols the most of them were women, there is no clear difference between the number of children and adults. The temporal distribution of protocols was stable between the months of October 2007 and March 2009 (15 protocols/semester), to then become variable, reaching values between 10 and 29 every 6 months. Of total protocols, 30.1% were positive; only one patient presented a mild adverse reaction (local welt). The β-lactams being most often the positive drugs. Protocols involving pethidine 100% was positive, diclofenac 33%, dipyrone, ketoprofen and hydrocortisone each one 25%. The most accomplished protocol was trivírica vaccine, resulting in 100% negative. Of all negative protocols 58% went to provocation, resulting in a 8% positive, including one provocation to the trívirica vaccine. Conclusions Methodologicall study is very important for a possible drug allergy, because history is not enough to certify the diagnosis. To do a provocation test to a negative protocol is crucial.

Determinants of self medication practices among pregnant women in Ibadan, Nigeria.

PubMed

Yusuff, Kazeem B; Omarusehe, Louis-Domeih

2011-10-01

To assess the frequency and evaluate the factors underlining self-medication with orthodox and herbal medicines among pregnant women in Ibadan, Nigeria. Setting Antenatal clinics at the major antenatal care facility in Ibadan, south-western Nigeria. A prospective cross-sectional study with a pre-tested 15-item structured questionnaire over a 12 week period among 1,650 pregnant women who attended antenatal clinics at a major antenatal care facility in Ibadan, south-western Nigeria. Data analysis was done with Chi-square, multivariate logistic regression and summary statistics. Frequency and major factors associated with self-medication in pregnancy. The response and completion rate was 96.6% (1,594) [mean age ± SD 27 ± 5.3 years]. The majority of the respondents were literate (92.6%), self-employed (61.5%) and in the third trimester (49.5%). A significant majority (63.8%) used self-medication (orthodox and herbal medicines) as their first response to perceived ill-health (P < 0.001). Self-medication in pregnancy was strongly associated with self-employment (OR: 3.8 (2.6-4.7), unemployment (OR: 2.6 (1.4-4.2) and third trimester of pregnancy (OR: 4.2 (3.1-5.6). The major over-the-counter medicines and potentially harmful prescription medicines kept at home for self-medication were Paracetamol, vitamins and haematinics; and piroxicam, dipyrone, chloramphenicol and Diazepam respectively. About one-third of the respondents who self-medicated (1,017) used local herbs (31.2%). The most frequent source of the medicines purchased during self-medication was patent medicine stores (55%). Mothers-in-law and relatives (41.3%) were the most frequently cited sources of advice during self-medication. Miscarriage/bleeding (44.3%) was the most frequently cited potential adverse effect that could occur with the use of certain medicines during pregnancy. Only 32% of respondents could identify medicines that are potentially harmful in pregnancy. Poorly guided self-medication with prescription, over-the-counter and herbal medicines is pervasive and significantly associated with gestational age and occupational pattern among pregnant women in Ibadan, south-western. A majority lacked the knowledge of potential adverse outcomes associated with the use of certain medicines, and the potentially harmful medicines to avoid during pregnancy.

Minimum Effective Concentration of Bupivacaine in Ultrasound-Guided Femoral Nerve Block after Arthroscopic Knee Meniscectomy: A Randomized, Double-Blind, Controlled Trial.

PubMed

Moura, Ed Carlos Rey; de Oliveira Honda, Claudio A; Bringel, Roberto Cesar Teixeira; Leal, Plinio da Cunha; Filho, Gasper de Jesus Lopes; Sakata, Rioko Kinmiko

2016-01-01

Adequate analgesia is important for early hospital discharge after meniscectomy. A femoral nerve block may reduce the need for systemic analgesics, with fewer side effects; however, motor block can occur. Ultrasound-guided femoral nerve block may reduce the required local anesthetic concentration, preventing motor block. The primary objective of this study was to determine the lowest effective analgesic concentration of bupivacaine in 50% (EC50) and in 90% (EC90) of patients for a successful ultrasound-guided femoral nerve block in arthroscopic knee meniscectomy. This was a prospective, randomized, double-blind, controlled trial. This study was conducted at Hospital São Domingos. A total of 52 patients undergoing arthroscopic knee meniscectomy were submitted to ultrasound-guided femoral nerve block using 22 mL bupivacaine. The bupivacaine concentration given to a study patient was determined by the response of the previous patient (a biased-coin design up-down sequential method). If the previous patient had a negative response, the bupivacaine concentration was increased by 0.05% for the next case. If the previous patient had a positive response, the next patient was randomized to receive the same bupivacaine concentration (with a probability of 0.89) or to have a decrease by 0.05% (with a probability of 0.11). A successful block was defined by a numerical pain intensity scale score < 4 (0 = no pain; 10 = worst imaginable pain) in 3 different evaluations. If the pain intensity score was = 4 (moderate or severe pain) at any time, the block was considered failed. General anesthesia was induced with 30 µg/kg alfentanil and 2 mg/kg propofol, followed by propofol maintanance, plus remifentanil if needed. Postoperative analgesia supplementation was performed with dipyrone; ketoprofen and tramadol were given if needed. The following parameters were evaluated: numerical pain intensity score, duration of analgesia, supplementary analgesic dose in 24 hours, and need for intraoperative remifentanil. The EC50 was 0.160 (95% CI: 0.150 - 0.189), and EC90 was 0.271 (95% CI: 0.196 - 0.300). There was no difference in numerical pain intensity score for the different concentrations of bupivacaine. A successful block was achieved in 45 patients, with no difference according to bupivacaine concentration. Time to first analgesic supplementation dose was longer for bupivacaine concentrations = 0.3% (543.8 ± 283.8 min.), compared to 0.25% (391.3 ± 177.8 min.) and < 0.25% (302.3 ± 210.1 min.). There were no differences in supplementary analgesic dose in 24 hours nor in the use of intraoperative remifentanil according to bupivacaine concentration. The analgesic effect was measured only during the first 2 hours. Bupivacaine EC50 for ultrasound-guided femoral nerve block was 0.160 (95% CI: 0.150 - 0.189), and EC90 was 0.271 (95% CI: 0.196 - 0.300).

Potential intravenous drug incompatibilities in a pediatric unit.

PubMed

Leal, Karla Dalliane Batista; Leopoldino, Ramon Weyler Duarte; Martins, Rand Randall; Veríssimo, Lourena Mafra

2016-01-01

To investigate potential intravenous drug incompatibilities and related risk factors in a pediatric unit. A cross-sectional analytical study conducted in the pediatric unit of a university hospital in Brazil. Data on prescriptions given to children aged 0-15 years from June to October 2014 were collected. Prescriptions that did not include intravenous drugs and prescriptions with incomplete dosage regimen or written in poor handwriting were excluded. Associations between variables and the risk of potential incompatibility were investigated using the Student's t test and ANOVA; the level of significance was set at 5% (p<0.05). Relative risks were calculated for each drug involved in potential incompatibility with 95% confidence interval. A total of 222 children participated in the study; 132 (59.5%) children were male and 118 (53.2%) were aged between 0 and 2 years. The mean length of stay was 7.7±2.3 days. Dipyrone, penicillin G and ceftriaxona were the most commonly prescribed drugs. At least one potential incompatibility was detected in about 85% of children (1.2 incompatibility/patient ratio). Most incompatibilities detected fell into the non-tested (93.4%), precipitation (5.5%), turbidity (0.7%) or chemical decomposition (0.4%) categories. The number of drugs and prescription of diazepam, phenytoin, phenobarbital or metronidazole were risk factors for potential incompatibility. Most pediatric prescriptions involved potential incompatibilities, with higher prevalence of non-tested incompatibilities. The number of drugs and prescription of diazepam, phenobarbital, phenytoin or metronidazole were risk factors for potential incompatibilities. Avaliar o potencial de incompatibilidade dos medicamentos intravenosos, identificando possíveis fatores de risco em uma unidade pediátrica. Trata-se de um estudo observacional analítico do tipo transversal realizado na unidade de pediatria de um hospital de ensino no Brasil. Os dados foram coletados de junho a outubro de 2014 a partir da análise das prescrições de crianças (0 a 15 anos) hospitalizadas. Foram excluídas prescrições sem medicamento intravenoso e com posologia incompletas ou grafia inadequada. A associação entre as variáveis e o risco de potenciais incompatibilidades foi determinada pelo teste t de Student e ANOVA, considerando significativo para p<0,05. Calculou-se o risco relativo com intervalo de confiança de 95% de cada medicamento envolvido. Duzentos e vinte e duas crianças participaram do estudo, 132 (59,5%) eram do gênero masculino, 118 (53,2%) tinham idade entre 0 a 2 anos e estiveram internados em média 7,7±2,3 dias. Os medicamentos mais prescritos foram dipirona, penicilina G e ceftriaxona. Quase 85% das crianças apresentaram ao menos uma potencial incompatibilidade, razão de 1,2 incompatibilidades/paciente. Os tipos de incompatibilidades mais comuns foram: não testada (93,4%), precipitação (5,5%), turbidez (0,7%) e decomposição química (0,4%). Os fatores associados a potenciais incompatibilidades foram: número de medicamentos e a prescrição dos medicamentos diazepam, fenitoína, fenobarbital e metronidazol. A maioria das prescrições pediátricas apresentou potenciais incompatibilidades e a incompatibilidade não testada foi o tipo mais comum. O número de medicamentos e a prescrição dos medicamentos diazepam, fenobarbital, fenitoína e metronidazol foram fatores de risco para potenciais incompatibilidades.

Prevalence of self-medication in Brazil and associated factors.

PubMed

Arrais, Paulo Sérgio Dourado; Fernandes, Maria Eneida Porto; Pizzol, Tatiane da Silva Dal; Ramos, Luiz Roberto; Mengue, Sotero Serrate; Luiza, Vera Lucia; Tavares, Noemia Urruth Leão; Farias, Mareni Rocha; Oliveira, Maria Auxiliadora; Bertoldi, Andréa Dâmaso

2016-12-01

To analyze the prevalence and associated factors regarding the use of medicines by self-medication in Brazil. This cross-sectional population-based study was conducted using data from the PNAUM (National Survey on Access, Use and Promotion of Rational Use of Medicines), collected between September 2013 and February 2014 by interviews at the homes of the respondents. All people who reported using any medicines not prescribed by a doctor or dentist were classified as self-medication practitioners. Crude and adjusted prevalence ratios (Poisson regression) and their respective 95% confidence intervals were calculated in order to investigate the factors associated with the use of self-medication by medicines. The independent variables were: sociodemographic characteristics, health conditions and access to and use of health services. In addition, the most commonly consumed medicines by self-medication were individually identified. The self-medication prevalence in Brazil was 16.1% (95%CI 15.0-17.5), with it being highest in the Northeast region (23.8%; 95%CI 21.6-26.2). Following the adjusted analysis, self-medication was observed to be associated with females, inhabitants from the North, Northeast and Midwest regions and individuals that have had one, or two or more chronic diseases. Analgesics and muscle relaxants were the therapeutic groups most used for self-medication, with dipyrone being the most consumed medicines. In general, most of the medicines used for self-medication were classified as non-prescriptive (65.5%). Self-medication is common practice in Brazil and mainly involves the use of non-prescription medicines; therefore, the users of such should be made aware of the possible risks. Analisar a prevalência e os fatores associados à utilização de medicamentos por automedicação no Brasil. Este estudo transversal de base populacional foi realizado com dados da Pesquisa Nacional de Acesso, Utilização e Promoção do Uso Racional de medicamentos (PNAUM), coletados de setembro de 2013 a fevereiro de 2014, por meio de entrevistas em domicílio. Todas as pessoas que referiram usar qualquer medicamento sem prescrição por médico ou dentista foram classificadas como praticantes de automedicação. Foram calculadas razões de prevalência bruta e ajustada (regressão de Poisson) e seus respectivos intervalos de confiança de 95% na investigação dos fatores associados ao consumo de medicamentos por automedicação. As variáveis independentes foram: aspectos sociodemográficos, de condições de saúde e de acesso e utilização de serviços de saúde. Adicionalmente, foram identificados os medicamentos mais consumidos por automedicação. A prevalência da automedicação no Brasil foi de 16,1% (IC95% 15,0-17,5), sendo maior na região Nordeste (23,8%; IC95% 21,6-26,2). Após análise ajustada, automedicação mostrou-se associada a ser do sexo feminino, pertencer às faixas etárias 10-19 anos, 20-29 anos, 40-59 anos e 60 anos ou mais, residir na região Norte, Nordeste ou Centro-Oeste, e ter uma ou duas ou mais doenças crônicas. Os analgésicos e os relaxantes musculares foram os grupos terapêuticos mais utilizados por automedicação, sendo a dipirona o fármaco mais consumido. No geral, a maioria dos medicamentos usados por automedicação foram classificados como isentos de prescrição (65,5%). A automedicação é prática corrente no Brasil e envolve, principalmente, o uso de medicamentos isentos de prescrição, devendo os usuários ficarem atentos aos seus possíveis riscos.