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Flumazenil is a GABAA receptor antagonist primarily used to treat excessive drowsiness and fatigue in post-surgery patients after sedation with GABA-based anesthesia, which are typically benzodiazepine sedatives. Flumazenil has also been used to treat benzodiazepine overdose and hypersomnia due to its effects on GABAA receptors in the brain.
How It Works
Benzodiazepine based anesthesia is often administered as a sedative for surgical procedures. Benzodiazepines bind to the GABAA receptor in the brain and works synergistically to amplify its effects. According to a study done by Erwin Sigel, the GABAA receptor is “the major inhibitory ion channel in the mammalian brain.” This means the GABA neurotransmitter is responsible for drowsiness, anti-anxiety effects, and anti-convulsive effects. Flumazenil, a GABAA antagonist, works by reversing these effects. The antagonistic effects work by blocking the GABAA “receptors in the brain and central nervous system that benzodiazepines need to reach to be active” (Drugs.com). This essentially cancels out the effect of the benzodiazepine.
The primary application of Flumazenil is to reverse the intense disorientation and drowsiness of benzodiazepine based sedatives and anesthetics following a surgical procedure. The antagonistic properties of the drug reverse the effect of the benzodiazepine, also reversing drowsiness, fatigue, and disorientation.
Flumazenil has been an effective antidote in treating benzodiazepine overdose and withdrawal in the case of substance abuse. A study by Spivey WH found that the victim of overdose may experience seizures when administered Flumazenil if they are physically dependent on benzodiazepines or if they have taken other drugs, such as cyclic antidepressants. However, the positive effects outweigh the negative effects. Flumazenil can save lives by preventing death by overdose.
Recent research by Lynn Marie Trotti has shown that Flumazenil may be effective for the treatment of hypersomnia, a sleep disorder that causes “excessive daytime sleepiness.” This only applies to hypersomnia patients who are affected due to GABA abnormalities. Theoretically, Flumazenil should return the GABA back to normal. Most of the patients in Trotti’s study reported that their symptoms improved with Flumazenil.
Possible Side Effects
Pain at injection site
Risk of seizures
Confusion, fear, panic attack
Increased heart rate
Bayer MJ, Bosse GM, Hoffman JR, Votey SR (1991).
Flumazenil: a new benzodiazepine antagonist.
Flaishon R, Rudick V, Sorkine P, Szold O, Weinbroum AA (1997).
A risk-benefit assessment of flumazenil in the management of benzodiazepine overdose.
Sigel, E., & Buhr, A. (1997). The benzodiazepine binding site of GABAA receptors. Trends in pharmacological sciences, 18(4), 425-429.
Spivey WH (1992).
Flumazenil and seizures: analysis of 43 cases.
Trotti, L. (2013).
Flumazenil for the Treatment of Primary Hypersomnia
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