Uses

Flumazenil is indicated for the complete or partial reversal of benzodiazepine-induced sedation following general anesthesia, procedural sedation, or benzodiazepine overdose. It is approved for use in adults and in pediatric patients aged 1 to 17 years for reversal of conscious sedation.

Do not use if

Contraindicated in patients with hypersensitivity to flumazenil or benzodiazepines. Must not be used when benzodiazepines were given to control a life-threatening condition such as status epilepticus or raised intracranial pressure. Also contraindicated in patients with signs of serious cyclic antidepressant overdose.

Side effects

Serious adverse effects include seizures, particularly in patients on long-term benzodiazepine therapy or with cyclic antidepressant co-ingestion. Other effects include nausea, vomiting, dizziness, agitation, and injection-site pain. Deaths have been reported mainly in patients with serious underlying disease or polydrug overdose.

Warnings

Seizure risk is the most critical warning; risk is highest in patients with long-term benzodiazepine dependence or concomitant cyclic antidepressant overdose. Re-sedation may occur as flumazenil's effect wears off before the benzodiazepine is cleared. Use with individualized dosing and close monitoring.

How it works

Flumazenil is an imidazobenzodiazepine that competitively antagonizes benzodiazepines at the GABA/benzodiazepine receptor complex. It has negligible agonist activity in humans. Its duration of action is shorter than most benzodiazepines, so re-sedation may occur and repeat dosing or monitoring is required.

Storage

Store at 20°C to 25°C (68°F to 77°F). Protect from light. Do not freeze.