Flumazenil is the benzodiazepine antidote and can abruptly trigger withdrawal or seizures in dependent individuals. It should only be used with seizure management on standby and careful screening for mixed overdoses. Flumazenil competitively blocks the benzodiazepine site on the GABAA receptor. When used on benzodiazepine-tolerant individuals it can precipitate an abrupt, sometimes life-threatening withdrawal characterised by agitation, hypertension and generalised tonic-clonic seizures. Case series show neurologic adverse-event reporting odds ratios >1700 for withdrawal seizures in pharmacovigilance databases.
Flumaseniil molecular structure diagram from the DrugsPRO substance library.
Also known as: Anexate, Lanexat, Mazicon, Romazicon, Ro 15-1788
Classification
Chemical: Benzodiazepine
Chemical: Medicine
Tag: Antidote
Tag: Benzodiazepine-antagonist
Tag: Imidazobenzodiazepine
Tag: Not psychoactive
Tag: Pharmaceutical
Effects
Nausea Or Vomiting
Tremor
Abrupt Return Of Consciousness
Anxiety Or Panic
Dysphoria
Dizziness
Routes of Administration
Intravenous (Bolus)
Dosage
Threshold: 0.1 mg
Light: 0.2-0.3 mg
Common: 0.3-1 mg
Strong: 1-3 mg
Heavy: 3 mg
Duration
Onset: 0.02-0.03 h
Peak: 0.1-0.17 h
Offset: 1-2 h
After Effects: 6 h
Intravenous Infusion (Resedation Prevention)
Dosage
Threshold: 0.1 mg/h
Light: 0.2-0.5 mg/h
Common: 0.5-1 mg/h
Strong: 1-3 mg/h
Heavy: 3 mg/h
Duration
Offset: 1 h
After Effects: 6 h
Intranasal (Investigational / Pediatric)
Dosage
Threshold: 0.02 mg/kg
Light: 0.02-0.04 mg/kg
Common: 0.04-0.08 mg/kg
Strong: 0.08-0.10 mg/kg
Heavy: 0.10 mg/kg
Duration
Onset: 0.08-0.13 h
Peak: 0.17-0.33 h
Offset: 1-2 h
After Effects: 6 h
Harm Reduction
Check interactions before mixing substances, pay attention to dose spacing and hydration, and treat all dosage guidance as approximate rather than guaranteed safe.
Sources
Substance data is aggregated from the following public harm-reduction and reference sources.
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Flumazenil - DrugsPRO ainejuhend
Flumazenil: Flumazenil is the benzodiazepine antidote and can abruptly trigger withdrawal or seizures in dependent individuals. It should only be used with seizure management on standby and careful screening for mixed overdoses. Flumazenil competitively blocks the benzodiazepine site on the GABAA re
