Flumazenil

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Flumazenil
Systematic (IUPAC) name
ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo- 4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Identifiers
CAS number	78755-81-4
ATC code	V03AB25
PubChem	3373
DrugBank	APRD00974
Chemical data
Formula	C15H14FN3O3
Mol. weight	303.288 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half life	7-15 min (initial) 20-30 min (brain) 40-80 min (terminal)
Excretion	Urine 90-95% Feces 5-10%
Therapeutic considerations
Pregnancy cat.	C
Legal status
Routes	Intravenous

Flumazenil (flumazepil, Ro 15-1788, Anexate®, Lanexat®, Mazicon®, Romazicon®) is a benzodiazepine antagonist, used as an antidote in the treatment of benzodiazepine overdose. It reverses the effects of benzodiazepines by competitive inhibition at the benzodiazepine binding site on the GABA_A receptor. It was introduced in 1987 by Hoffmann-La Roche under the trade name Anexate.

The onset of action is rapid and usually effects are seen within one to two minutes. The peak effect is seen at six to ten minutes. The recommended dose for adults is 200mcg every 1-2 minutes until the effect is seen, to a maximum of 3mg per hour. It is available as a clear, colourless solution for i.v. injection, containing 500mcg in 5 mls.

Many benzodiazepines have longer half-lives than flumazenil. Therefore, repeat doses of flumazenil may be required to prevent recurrent symptoms of overdosage once the initial dose of flumazenil wears off. It is hepatically metabolised to inactive compounds which are excreted in the urine. Subjects who are physically dependent on benzodiazepines may suffer benzodiazepine withdrawal symptoms, including seizure, upon administration of flumazenil.

[edit] References

Romazicon® product information, Roche USA