Flumazenil is a benzodiazepine antagonist that is used for the complete or partial reversal of the sedative effects caused by benzodiazepines in various clinical settings, such as induced general anesthesia for diagnostic and therapeutic procedures. Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central...
- Mechanism
- Curator reviewed
Flumazenil, an imidazobenzodiazepine derivative, is a benzodiazepine antagonist. It competitively inhibits the benzodiazepine binding site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in man.
- Primary indication
- For the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, and where sedation has been produced with benzodiazepines for diagnostic and...Curator reviewed · 3 structured indications
- Formula / weight
- C15H14FN3O3 · 303.2884 g/mol (avg)
- First approval
- Canada, 2005 · United States, 1991
- Also known as
- Flumazepil
- Code names
- RO-15-1788 · RO 15-1788/000 · RO-1722 · RO-41-8157
Resolves to
OFBIFZUFASYYRE-UHFFFAOYSA-NSMILESCCOC(=O)C1=C2CN(C)C(=O)C3=C(C=CC(F)=C3)N2C=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Flumazenil, and which of those have an active Phase 3 trial?
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