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flumazenil
V03AB25
Forms & Strengths
- Injectable solution: 0.1 mg/mL (5 mL, 10 mL vials)
Adult Dosing
- Reversal of general anesthesia: Initial 0.2 mg IV over 15 seconds; repeat 0.1 mg at 60-second intervals up to 1 mg total (usual dose 0.3-0.6 mg).
- Management of benzodiazepine overdose: Initial 0.2 mg IV over 30 seconds; if desired level of consciousness not obtained after 30 seconds, give 0.3 mg, then 0.5 mg at 60-second intervals up to 3 mg total.
Pediatric Dosing
- Reversal of general anesthesia (Ages >1 year): Initial 0.01 mg/kg (up to 0.2 mg) IV over 15 seconds; repeat 0.005 mg/kg up to max total dose of 1 mg or 0.05 mg/kg, whichever is lower.
- Management of benzodiazepine overdose (Ages >1 year): Initial 0.01 mg/kg (up to 0.2 mg) IV over 15 seconds; subsequent doses of 0.01 mg/kg (up to 0.2 mg) repeated at 60-second intervals up to max total dose of 1 mg.
Indications
- Complete or partial reversal of the sedative effects of benzodiazepines in general anesthesia
- Management of benzodiazepine overdose (known or suspected)
Mechanism of Action
- Competitive antagonist at the benzodiazepine recognition site on the GABA_A/benzodiazepine receptor complex
- Blocks central nervous system effects of benzodiazepines, nonbenzodiazepine hypnotics (e.g., zolpidem), and zaleplon
Contraindications
- Hypersensitivity to flumazenil or benzodiazepines
- Patients given benzodiazepines for control of potentially life-threatening conditions (e.g., status epilepticus)
- Patients showing signs of serious cyclic antidepressant overdose
Adverse Reactions
- Nausea and vomiting
- Dizziness, agitation, emotional lability, anxiety
- Headache, injection site pain
- Seizures in high-risk patients (e.g., long-term benzodiazepine users or cyclic antidepressant overdose)
- Withdrawal symptoms in benzodiazepine-dependent patients
Drug Interactions
- Reverses the sedative, cognitive, and psychomotor effects of benzodiazepines and benzodiazepine receptor agonists
- May precipitate severe benzodiazepine withdrawal syndrome in chronic users
- May precipitate seizures and cardiac arrhythmias in co-ingestions of cyclic antidepressants
Curated Content: Needs Vetting Before Put to Clinical Use