Flumazenil

Other CNS Drugs · Benzodiazepine antagonist

Indications

Reversal of the central sedative effects of benzodiazepines in anaesthesia and in intensive care and diagnostic procedures.

Dosage

Adults: By IV injection, 200 mcg over 15 sec, then 100 mcg at 60 sec intervals if required, usual dose range, 300-600 mcg; max total dose 1 mg (2 mg in intensive care); question aetiology if no response to repeated doses. By IV infusion, if drowsiness recurs after injection, 100-400 mcg/hr, adjusted according to level of arousal. Children: Not recommended for children under 1 yr; not recommended for use by IV infusion in children; not recommended for children in intensive care. Reversal of sedative effects of benzodiazepines: IV injection over 15 sec: Neonate, 10 mcg/kg, repeat at 1-minute intervals if required; 1 mth-18 yr, 10 mcg/kg (max 200 mcg), repeated at 1-minute intervals if required, max total dose of 50 mcg/kg (1 mg), 2 mg in intensive care. IV infusion, if drowsiness recurs after injection: Neonate, 2-10 mcg/kg/hr, adjusted according to response; 1 mth-18 yr, 2-10 mcg/kg/hr,…

Administration

Administered IV over 15 to 30 seconds. To minimize pain at the injection site, flumazenil should be administered through a freely running IV infusion line into a large vein. Extravasation should be avoided. Compatibility: Dextrose 5%, NS, LR. Stability: Stored at controlled room temperature.

Adverse Effects

Nausea, vomiting and flushing; if wakening too rapid, agitation, anxiety and fear; transient increase in blood pressure and heart-rate in intensive care patients; very rarely convulsions (particularly in epileptics), hypotension, increased sweating, vertigo, headache, tremor, diplopia, strabismus, increased lacrimation.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Caution advised or effect undetermined. Contraindications: Epileptics who have received prolonged benzodiazepine therapy. Mixed intoxication with tricyclic and/or tetracyclic antidepressants. Precautions: Short-action (repeat doses may be necessary, benzodiazepine effects may persist for at least 24 hours); benzodiazepine dependence (may precipitate withdrawal symptoms); ensure neuromuscular blockade cleared before giving; avoid rapid injection in high-risk or anxious patients and following major surgery; hepatic impairment; severe head injury (rapid reversal of benzodiazepine sedation may increase risk of raised intracranial pressure); elderly, children. Anxiety.

Advice to Patient

Avoid activities that require alertness unless full effects of medication are known for 18-24 hours after discharge. Avoid alcohol and OTC medications for 10-24 hours after taking this medication. Contact prescriber if there is depression, agitation, fear, panic attack, difficulty in breathing, flushing, hyperventilation, lack of sleep, palpitations, or tremor.

Pharmacokinetics

Onset: IV: 1-2 mins. Duration: Variable. Absorption: Oral: Rapidly absorbed. Metabolism: Hepatic. Completely metabolized. Bioavailability: 20%. Half-life elimination: Terminal: 40-80 mins. Time to peak, plasma: IV: 6-10 mins. Oral: 20-90 mins. Excretion: Urine (mainly). Faeces (small amounts).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.