Flumazenil

Chemical

Imidazo-benzodiazepine derivative

Benzodiazepine overdose

Clear, colourless solution 100mcg/ml

200mcg –> 60sec –> 100mcg (dose ranges 300-600mcg)

1-2min, peaks in 6-10min

Half life 4-11mins. t1/2b 40-80mins

Competitive antagonism of GABA_A receptor – inhibits the BZD binding site

Vd 1L/kg

PPB 50%

Hepatic. Fully metabolised to carboxylic acid metabolites predominantely

Metabolites renally eliminated

CNS: Hallucinations, aggression, convulsions

CVS: Arrythmias, myocardial infarction

GI: N+V

Resp: Dyspnoea, hyperventilation

Diaphoresis