I. Basic Information
- English Name: Flumazenil
- CAS Number: 78755-81-4
- Molecular Formula: C15H14FN3O3
- Molecular Weight: 303.29 g/mol
- Synonyms: Anexate, Romazicon, Lanexat, Mazicon

II.  Pharmacological Actions

Flumazenil is a benzodiazepine antagonist used primarily for the reversal of benzodiazepine effects, particularly in cases of overdose or excessive sedation.

1.     Mechanism of Action:

o    Flumazenil competes with benzodiazepines for binding sites on the GABA (gamma-aminobutyric acid) receptor, specifically the benzodiazepine site. By binding to this site without activating the receptor, it effectively reverses the effects of benzodiazepines.

o    Since benzodiazepines enhance the inhibitory effects of GABA, flumazenil's inhibition leads to increased neuronal activity by preventing the benzodiazepines from exerting their calming effect.

2.     Clinical Uses:

o    Primarily used to treat benzodiazepine overdoses.

o    Reversal of benzodiazepine-induced sedation in medical or diagnostic procedures.

o    It is also used in anesthesia to help patients recover from the effects of benzodiazepine sedation more quickly.