Características do uso e da dependência de benzodiazepínicos entre usuários: atenção primária à saúde / Characteristics of benzodiazepine use and dependence: primary health care / Características del uso y la dependencia de las benzodiacepinas: la atención primaria de salud

Objetivo: analisar as características sociodemográficas, de história de uso e dependência de benzodiazepínicos. Método: estudo transversal, cuja amostra intencional foi composta de 219 usuários de benzodiazepínicos cadastrados em quatro equipes de saúde da família de um município da região Oeste de Minas Gerais. A coleta de dados foi realizada entre os meses de janeiro a maio de 2013, por meio da aplicação de um questionário semiestruturado. Para a tabulação e a análise descritiva dos dados utilizou-se os softwares Epidata 3.1 e EPINFO 6.04. Resultados: a maior parte de consumidores de benzodiazepínicos é do sexo feminino, com idade entre 53 e 60 anos. O Clonazepam foi o benzodiazepínico mais utilizado. Verificou-se que 181 indivíduos (82,6%) possuem dependência química de benzodiazepínicos. Conclusão: fatores como a imagem positiva, o baixo custo e troca de benzodiazepínicos, a medicalização de problemas pessoais, sóciofamiliares e profissionais, inadequações do tratamento contribuem para a dependência de benzodiazepínicos.

Objective: to analyze benzodiazepine users' socio-demographic characteristics, use history and dependence. Method: in this cross-sectional study of an intentional sample of 219 benzodiazepine users enrolled with four family health teams in the western Minas Gerais State, data was collected between January and May 2013 by applying an adapted questionnaire. Epidata 3.1 and EPINFO 6.04 software were used for data tabulation and descriptive analysis. Results: most of the benzodiazepine users were female, and 53 to 60 years old. Clonazepam was the benzodiazepine most commonly used, and 181 individuals (82.6%) were found to be chemically dependent on benzodiazepines. Conclusion: factors such as the positive image, low cost and swapping of benzodiazepines, medicalization of personal, social, family and professional problems, and treatment inadequacies contributed to benzodiazepine dependence..

Objetivo: analizar las características sociodemográficas, historial de uso y la dependencia de las benzodiacepinas. Métodos: estudio transversal, cuya muestra intencional fue compuesta por 219 usuarios de benzodiacepinas registrados en cuatro equipos de salud de la familia de una ciudad de la región oeste de Minas Gerais. La recolección de datos se llevó a cabo entre los meses de enero a mayo de 2013, mediante la aplicación de un cuestionario semiestructurado. Para la tabulación y el análisis descriptivo de los datos se utilizaron los softwares EpiData 3.1 y EPINFO 6.04. Resultados: la mayoría de los consumidores benzodiacepinas son mujeres, con edades comprendidas entre 53 y 60 años. El Clonazepam fue el benzodiacepínico más utilizado. Se encontró que 181 pacientes (82,6%) tienen dependencia química a benzodiacepinas. Conclusión: los factores tales como la imagen positiva, el bajo costo y el intercambio de las benzodiacepinas, la medicalización de los problemas personales, sociales-familiares y profesionales y las inadecuaciones del tratamiento contribuyen a la dependencia a las benzodiacepinas.

Flumazenil: a novel and potent benzodiazepine competitive receptor blocker

One of the most rewarding outcomes in the recent research in the field of benzodiazepines [BNZs] is the discovery of BNZ receptors and their association with GABA receptors, together with the discovery of some synthetic BNZ agonists andas antagonists. To the latter group belongs the 1,4-imidazodiazepine derivative-flumazenil which was introduced in 1981. It is shown to be competitive blocker for both types of BNZ receptors, namely, BNZ type-1 which are involved in the anxiolytic effects and BNZ type-2 which are involved in sedation and sleep. Administration of flumazenil [10 micro g/kgi.v] is shown to rapidly antagonize [within minutes] BNZ-induced anxiolytic, sedative,hypnotic, ataxic, anticonvulsant, amnestic and respiratory depressant effects. The major disadvantage of flumazenil is its rapid hepatic metabolism that curtails its oral use. Beside helping in reversal of BNZ- induced intoxication,the drug has been proven to be of value in the diagnosis of unconsciousness of unknown origin, to test for BNZs- involvement and in the improving of consciousness in some cases of hepatic coma. The introduction of flumazenil is expected to give an extended margin of safety to the use of BNZs, but it is hoped that it would not encourage the overwhelming use of these drugs

Reversal of benzodiazepine sedation with flumazenil in a patient with tetanus

A 54-year-old female patient admitted with a diagnosis of tetanus had her sedation reversed with an infusion of flumazenil. Flumazenil appears to be of use in reversal of sedation in patients with accumulation of benzodiazepine after prolonged administration.

Efecto de una beta lactama de 1.5 benzodiazepina sobre el sueño / Effect of a beta lactame of 1.5 benzodiacepine upon sleep

Existen numerosas substancias, de estructura química diversa que han sido utilizadas como inductoras de sueño. Sin embargo, debido a que producen efectos colaterales indeseables, constantemente son substituidas por fármacos de reciente creación. Este trabajo se llevó a cabo con el propósito de analizar el efecto sobre el sueño de una beta lactama de 1.5 benzodiazepina, administrada intraperitonealmente (0.9 mg/kg) a ratas wistar. Los resultados indican que esta substancia incrementa de manera significativa, tanto al sueño lento como al paradójico a expensas de la vigilia. La lactancia de la primera fase de sueño paradójico, se prolonga significativamente. Se concluye que esta substancia facilita la presencia de sueño, manifestándose su acción durante un período relativamente largo

Role of flumazenil in reversing the sedative effect of benzodiazepines in endoscopies: Salmaniya medical centre experience

Thirty seven patients undergoing endoscopic procedures were sedated with either midazolam 0.15mg-0.2mg/kg or diazepam 0.2-0.3 mg/kg intravenously. The sedative effect was reversed in 27 patients with flumazenil [Anexate] 0.2mg initially and then in incremental doses of 0.1mg. The remaining ten patients served as control group by allowing them to recover spontaneously. The efficacy of flumazenil was evaluated by the degree of sedation, comprehension and co-operation, orientation to space and time and re-sedation. The safety of flumazenil was evaluated by local and systemic tolerability. We conclude that flumazenil is a safe and effective benzodiazepine antagonist, and that the recovery of patients given this antagonist is both quick and complete

Flumazenil [anexate] versus non-specific benzodiazepines antagonist for recovery of patients using subjective and psychomotor assessments

80 patients were scheduled for minor surgical procedures [herniorrhaphy, cystolithotomy, excision of bladder ulcer or diagnostic cystoscope], their age ranged from 18-60 years of both sexes, they received benzodiazepines supplementation for regional anaesthesia. At the end of surgery sedation is reversed by flumazenil [Anexate], naloxone, aminophylline and placebo. The recovery was evaluated by recovery assessment of level of sedation, comprehension and co-peration, temporo-spatial orientation, cognitive and psychomotor tests and anterograde amnesia. The parameters are measured 5, 15, 30, 60, 120, 240 minutes after injection of the trial drug. Recovery score, comprehension and co-operation, orientation and psychomotor assessment showed marked and significant improvement after flumazenil in comparison with placebo, as regard the anterograde amnesia significant changes were noted between flumazenil and placebo; resedation was more with diazepam subgroups. There was no role for naloxone which was similar to placebo while aminophylline hasten the recovery from benzodiazepine sedation but more late if compared with flumazenil [30 minutes post-aminophylline versus 5 minutes post-flumazenil injection]

Naloxone as an antidote for benzodiazepine: an experimental and clinical study

This study evaluates the potential antidote action of naloxone on experimentally induced diazepam and flunitrazepam [benzodiazepines] intoxication in dogs. Its antidote effects is also evaluated in a clinical sample of 8 patients suffering from flunitrazepam intoxication. The clinical findings were suggestive of an antagonistic action of naloxone in flunitrazepam intoxication. It was also found that flunitrazepam exhibits a different pharmacological profile from other members of the benzodiazepine group. Our findings of a selective naloxane-flunitrazepam reversal need to be explained in relation to the mechanism of action of this benzodiazepine, as well as to the equated naloxane-opiates reversal

Memory modulation by brain benzodiazepines

1. Recent evidence indicates that post-training memory processes are down-regulated by benzodiazepine/GABA-A systems inthe amygdala, septum and hippocampus. Havituation and avoidance learning are accompanied by a decrease of benzodiazepine-like immunoreactivity in the three structures, explainable by a release of benzodiazepines. Immediate post-training microinjection of the benzodiazepine antagonist flumazenil into the hippocampus enhances retention of habituation. The post-training administration of glumazenil into any of the three structures enhances relation of avoidance learning. 2. The mode of operation of these systems was studied in detail in the amygdala using avoidance paradigms. The release of endogenous benzodiazepines during and particularly after training enhances sensitivity of local GABA-A receptors to muscimol, activation of the GABA-A receptors opens chloride channels that can be selectively blocked by picrotoxin and by Ro-4864. Training enhances, and fluazenil reduces, sensitivity of the amygdala to the amnestic effect of locally injected muscimol by a factor of 100. Post-training intra-amygdala administration of picrotoxin or Ro5-4864 enhances retention. 3. These findings suggest that the endogenous benzoidiazepine/GABA-A mechanisms that down-regulate memory int he amygdala, septum and hippocampus are activated in response to the anxiety and/or stress associated with each task. Memory lability which occurs in the psot-training period and characterizes consolidation would thus be a consequence of the brain's response to anxiety or stress