FLUMAZENIL
Chemistry - A benzodiazepine antagonist, flumazenil is a 1, 4-imidazobenzodiazepine derivative.
Uses, Indications - Flumazenil may be useful for the reversal of benzodiazepine effects after eithertherapeutic use or overdoses. Flumazenil may be of benefit in the treatment of encephalopathy inpatients with chronic intractable portosystemic encephalopathy. More studies are required for thispotential indication however.
Flumazenil should not be used, or used with extreme caution, in patients with mixed overdoseswhere benzodiazepine reversal may lead to seizures or other complications.
Flumazenil has caused some teratogenic effects in lab animals after very high dosages. Use duringpregnancy only when necessary.
Overdosage, Acute Toxicity - Large IV overdoses have rarely caused symptoms in otherwisehealthy humans. Seizures, if precipitated have been treated with barbiturates benzodiazepines andphenytoin, usually with prompt responses.
Storage, Stability, Compatibility
Flumazenil is compatible with lactated Ringer's, D5W, or normal saline solutions. Once drawn into a syringe or mixed with the above solutions, discard after 24 hours.Pharmacology - FLUMAZENIL
Flumazenil is a competitive blocker of benzodiazepines at benzodiazepine receptors in the CNS. It antagonizes the sedative and amnestic qualities of benzodiazepines.Uses, Indications - Flumazenil may be useful for the reversal of benzodiazepine effects after eithertherapeutic use or overdoses. Flumazenil may be of benefit in the treatment of encephalopathy inpatients with chronic intractable portosystemic encephalopathy. More studies are required for thispotential indication however.
Pharmacokinetics - FLUMAZENIL
Flumazenil is administered by rapid IV injection. It is rapidly distributed andalso rapidly metabolized in the liver. In humans, the average half life is about one hour.Contraindications, Precautions, Reproductive Safety
Flumazenil is contraindicated in patientshypersensitive to it or other benzodiazepines or in patients with where benzodiazepines are beingused to treat a potentially life-threatening condition (e.g., status epilepticus, increased CSFpressure). It should also not be used in patients with a serious tricyclic antidepressant overdose.Flumazenil should not be used, or used with extreme caution, in patients with mixed overdoseswhere benzodiazepine reversal may lead to seizures or other complications.
Flumazenil has caused some teratogenic effects in lab animals after very high dosages. Use duringpregnancy only when necessary.
Adverse Effects, Warnings
In some human patients, flumazenil use has been associated withseizures. These patients usually have a long history of benzodiazepine use or are showing signs ofserious tricyclic antidepressant toxicity. Adverse effects reported in humans include injection sitereactions, vomiting, cutaneus vasodilatation, vertigo, ataxia and blurred vision. Deaths have beenassociated with its use in humans having serious underlying diseases.Overdosage, Acute Toxicity - Large IV overdoses have rarely caused symptoms in otherwisehealthy humans. Seizures, if precipitated have been treated with barbiturates benzodiazepines andphenytoin, usually with prompt responses.