Drug intelligence / Profile preview

flumazenil

Development stage
Approved
Lead developer
Roche
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Flumazenil is a small molecule imidazobenzodiazepine derivative that acts as a selective benzodiazepine antagonist. It competitively inhibits the activity at the benzodiazepine recognition site on the Gamma-aminobutyric acid type A receptor (GABAA receptor), thereby reversing the central nervous system effects of benzodiazepines. Flumazenil is primarily used for the complete or partial reversal of sedation and psychomotor impairment caused by benzodiazepines, including in cases of overdose and for recovery from anesthesia or conscious sedation where benzodiazepines were administered. It does not reverse CNS depression caused by other agents such as barbiturates, ethanol, general anesthetics (not acting via the benzodiazepine site), or opioids. Flumazenil may also antagonize non-benzodiazepine "Z-drugs" like zolpidem and zopiclone due to their action at the same binding site[1][2][3][4][6][7].

Brand names
Romazicon
Other names
flumazenilflumazepil
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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