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Flumazenil (also known as flumazepil, code name Ro 15-1788 [3]) is a selective GABA A receptor antagonist [4] administered via injection, otic insertion, or intranasally. Therapeutically, it acts as both an antagonist and antidote to benzodiazepines (particularly in cases of overdose), through competitive inhibition .
Flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. [48] One study found that only 10% of the patient population presenting with a benzodiazepine overdose are suitable candidates for flumazenil. [ 48 ]
Flumazenil functions as a competitive antagonist at the GABA-A receptor complex's benzodiazepine site. By doing this, the CNS and respiratory depression would reverse and the inward chloride current would reduce. Flumazenil is useful in treating and preventing benzodiazepine-induced coma from recurring. [40]
Flumazenil is a benzodiazepine antagonist and blocks the binding of benzodiazepines to gamma-aminobutyric acid receptors. Similarly to naloxone, flumazenil has a short half-life, and this needs to be taken into account because the patient may exhibit central nervous depression after the antidote has been cleared.
Flumazenil was found to be more effective than placebo in reducing feelings of hostility and aggression in patients who had been free of benzodiazepines for 4–266 weeks. [92] This may suggest a role for flumazenil in treating protracted benzodiazepine withdrawal symptoms.
While flumazenil, a GABA A –receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose. [ 20 ] Zolpidem is a nonbenzodiazepine , or Z-drug , which acts as a sedative and hypnotic [ 11 ] [ 20 ] as a positive allosteric modulator at the GABA A receptor.
Flumazenil is an imidazobenzodiazepine that can help mediate and antagonize the effects of benzodiazepines. It can be used in anaesthesia as well as intensive care. [6] Flumazenil raises concerns with its tendency to induce benzodiazepine withdrawal, and symptoms include seizures and agitation.
Zopiclone overdosage can be treated with the GABA A receptor benzodiazepine site antagonist flumazenil, which displaces zopiclone from its binding site, thereby rapidly reversing its effects. [ 41 ] [ 42 ] Serious effects on the heart may also occur from a zopiclone overdose [ 43 ] [ 44 ] when combined with piperazine .
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