Flumazenil

From Health Encyclopedia

Use

benzodiazepine, inhibitor /antagonist

Facts (generated by robot; please edit if you find it inaccurate)

• Chemically, flumazenil is ethyl 8-fluoro-5, 6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a](1,4) benzodiazepine-3-carboxylate.
• Isolated in 1981, flumazenil is an imidazobenzodiazepine capable of blocking the centrally mediated effects of benzodiazepines at the receptor level.
• Following oral administration flumazenil is rapidly absorbed (peak concentrations are achieved after 20 to 90 minutes), but bioavailability is low (16%) due to significant presystemic elimination.
• Flumazenil is a recently discovered pharmacologic antagonist of the CNS effects of benzodiazepines.
• Flumazenil is a specific and competitive antagonist at the central benzodiazepine receptor, reversing all effects of benzodiazepine agonists without tranquillising or anticonvulsant actions.

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