Flumazenil - a specific antagonist of the benzodiazepines at the beginning of the 21st century. Is it needed?
Abstract
Flumazenil was developed in 1979 during search for new agonists of benzodiazepine receptors, which were discovered 2 years earlier in 1977. Flumazenil was registered in Switzerland in 1987 by Roche (brand name Anexate) as a benzodiazepine antagonist.
Similar drugs were tested to overcome its short-lasting effect. Only Sarmazol is used in veterinary anaesthesia, other derivates are used in experiments only.
Main boom of flumazenil use was in 80th and early 90th, later on its popularity decreased partly because of its high cost and short-lasting effect. Main indications of flumazenil are presented: reversal of paradoxical reaction to midazolam and antagonisation of conscious sedation induced by benzodiazepines.
Common dose 0.5 mg of flumazenil i.v. accelerates psychomotoric recovery after midazolam in 60 minutes. Intranasal and rectal application of flumazenil was also described, mainly in children.
Interesting effects of flumazenil are reversal of halothane induced sedation and potentiation of hypnotic effect of propofol and potentiation of antinociceptive effect of morphine.