Trade names, Mazicon, Romazicon
Route of administration is IV.
Metabolism is hepatic
Biological half-life is 7-15 min.
Half life 20-30 min in brain.
Excretion is by urine 90-95%, and 5-10% in feces.
A GABAA receptor antagonist primarily available by injection only, and the only GABAA receptor antagonist available.
Primarily used to treat benzodiazepine overdoses and to help reverse anesthesia.
Treatment for benzodiazepine dependence and tolerance.
Benefits patients who become excessively drowsy after benzodiazepines given for either diagnostic or therapeutic procedures.
An antidote in the treatment of benzodiazepine overdoses.
Reverses benzodiazepines by competitive inhibition at the benzodiazepine binding site on the GABAA receptor.
Has a short half-life and requires multiple doses and careful patient monitoring to prevent recurrence of overdose symptoms.
Has been effectively used to treat overdoses of non-benzodiazepine hypnotics, such as zolpidem, zaleplon and zopiclone, and in reducing excessive daytime sleepiness of hypersomnias.
Has variable results in hepatic encephalopathy.
This agent’s onset of action is rapid and usually within one to two minutes, with a peak effect at six to ten minutes.
The recommended dose is 200 μg every 1–2 minutes until the effect is seen, to a maximum of 3 mg per hour.
It is available for intravenous injection, containing 500 μg in 5 mL.
Many benzodiazepines, including midazolam, have longer half-lives than flumazenil, and repeat doses of flumazenil may be required to prevent recurrent symptoms of overdosage.
Patients physically dependent on benzodiazepines may suffer benzodiazepine withdrawal symptoms, including seizure, upon rapid administration of flumazenil.
Has a role in treating protracted benzodiazepine withdrawal symptoms.
An imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system.
Competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex.
Only creates behavioral effects when administered concurrently with a benzodiazepine receptor agonist or inverse agonist.
Flumazenil does not antagonize all of the central nervous system effects of drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor.
Does not reverse the effects of opioids.
Antagonizes sedation, impairment of recall, psychomotor impairment and ventilatory depression produced by benzodiazepines.
A benzodiazepine antagonist.
An imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system.
Competitively inhibits the activity at the benzodiazepine recognition site on the GABA / benzodiazepine receptor complex.
Used as an antidote in the treatment of benzodiazepine overdoses.
Effective in overdoses of non-benzodiazepine sleep enhancers, namely zolpidem and zaleplon.
Onset of action is rapid and usually effects are seen within one to two minutes, with a peak effect is seen at six to ten minutes.
The recommended dose for adults is 200 μg every 1–2 minutes until the effect is seen, to a maximum of 3 mg per hour by intravenous injection.
Because many benzodiazepines have longer half-lives than flumazenil repeat doses may be required to prevent recurrent symptoms of overdosage once the initial dose of flumazenil wears off.
Metabolized in the liver to inactive compounds which are excreted in the urine.
Patients dependent on benzodiazepines may suffer withdrawal symptoms, including seizure, upon administration of flumazenil.
Intravenous drug antagonizes sedation, impairment of recall, psychomotor impairment and ventilatory depression produced by benzodiazapines.