Pharmacological and Clinical Evaluation of flumazenil Anexate

in anaesthesia and in the intensive care unit, benzodiazepines haveproven safe and effective agents for the induction and maintenance ofsedation for a variety of therapeutic goals. However, in these contexts,or in benzodiazepine overdose, it is often desirable to be able toterminate or interrupt sedation without waiting for the effect of thebenzodiazepine to become dissipated by normal metabolism andexcretion.Flumazenil, a l,4-imidazobenzodiazepine, is a highly effective,specific benzodiazepine antagonist which is indicated for use when theeffect of a benzodiazepine must be attenuated or terminated at a shorttime. It acts by displacing other benzodiazepines from the receptor siteby competitive inhibition.In this study, the pharmacological investigations demonstrated thatflumazenil had a dose dependent positive inotropic effect on isolatedperfused mammalian heart of rabbit. It was found also that flumazenilhad a dose dependent potentiation of noradrenaline induced contractionson isolated rabbit aortic spiral strip.