Administration of the drug requires careful monitoring by an anesthesiologist due to potential side effects and serious risks associated with over-administeration. This is similar to naloxone's application to reverse the effect of opiates and opioids following surgery. Because of the potential risks of withdrawal symptoms and the drug's short half-life, patients must be carefully monitored to prevent recurrence of overdose symptoms or adverse side effects.įlumazenil is also sometimes used after surgery to reverse the sedative effects of benzodiazepines. Flumazenil's short half-life requires multiple doses. These include lowered seizure threshold, agitation, and anxiousness. There are many complications that must be taken into consideration when used in the acute care setting. It reverses the effects of benzodiazepines by competitive inhibition at the benzodiazepine (BZ) recognition site on the GABA/benzodiazepine receptor complex. The drug has been used as an antidote in the treatment of benzodiazepine overdoses.

Medical uses įlumazenil benefits patients who become excessively drowsy after use of benzodiazepines for either diagnostic or therapeutic procedures.

Administration of flumazenil by sublingual lozenge and topical cream has also been tested. Intravenous flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. The developer lost its exclusive patent rights in 2008 so at present, generic formulations of this drug are available. However, it did not receive FDA approval until December 20, 1991. It was first characterized in 1981, and was first marketed in 1987 by Hoffmann-La Roche under the trade name Anexate. Therapeutically, it acts as both an antagonist and antidote to benzodiazepines (particularly in cases of overdose), through competitive inhibition. A vial of flumazenil solution for injectionįlumazenil (also known as flumazepil, code name Ro 15-1788 ) is a selective GABA A receptor antagonist administered via injection, otic insertion, or intranasally.

Antidote of benzodiazepines