What is "flumazenil"

alt. (context pharmacology English) A benzodiazepine antagonist used to counter drowsiness caused by benzodiazepines. n. (context pharmacology English) A benzodiazepine antagonist used to counter drowsiness caused by benzodiazepines.

Flumazenil (also known as flumazepil, code name Ro 15-1788) is a selective benzodiazepine receptor antagonist primarily available by injection only, and the only GABAA negative allosteric modulator on the market today. It has antagonistic and antidote properties to therapeutically used benzodiazapenes, through competitive inhibition.

It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by the FDA on December 20, 1991. Flumazenil went off patent in 2008 so at present generic formulations of this drug are available. Intravenous flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual lozenge and topical cream has also been tested.