Mechanism of action
Benzodiazepine antagonist.
Competitively binds to benzodiazepine site on the GABA receptor complex which antagonizes the CNS effect of benzodiazepines.
Indications and dose
Pharmacokinetics
Onset of action: 1–2 minutes
Duration of action: 19–50 minutes
Half-life of elimination: 40–80 minutes (increased in patients with impaired liver function)
Metabolism: Hepatic (complete metabolization)
Elimination: Kidneys (metabolites), Liver (5–10 %)
Directions for administration
Administer intravenously over 15 seconds or via infusion.
Repeated administration may be necessary as the half-life of benzodiazepines is usually greater.
Medicinal forms
Solution for injection/infusion (100 μg/ml)
- 1 vial = 5 ml (500 μg), 10 ml (1000 μg)
Side-effects
Confusion, nausea, dizziness, agitation
Abstinence syndrome
Palpitations, tachycardia, bradycardia
Flushing
Sweating
Diplopia
References
