Benzodiazepine and anticonvulsant.
Acts on benzodiazepine receptor via GABA-A receptor and enhances its inhibitory effect through increased permeability for chloride ions.
Dose-related effect. Causes sedation, anxiolysis, anterograde amnesia, muscle relaxation and has an anticonvulsant effect. At higher doses causes cardiorespiratory depression.
Vomiting
Respiratory depression
Confusion
Drowsiness; excess sedation
Paradoxical agitation (more common in elderly)
Cardiovascular depression
Onset of action: Intravenous: 10 minutes; Intramuscular: 20-30 minutes
Duration of action: 6-8 hours
Bioavailability: Oral: 90%
Distribution: 90% protein bound
Metabolism: Hepatic
Half-life of elimination: 14 hours
Excretion: Urine
Flumazenil - benzodiazepine antagonist
Dilute in water for injection or 0.9% sodium chloride
Tablet - 0.5mg, 1mg and 2.5mg
Solution for injection - 1 vial = 2mg in 1 ml or 4mg in 1 ml.
Oral solution
References