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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 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.
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. [39]
Flurazepam [2] (marketed under the brand names Dalmane and Dalmadorm) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.
Flumazenil, an imidazobenzodiazepine, is an antidote for some benzodiazepine overdoses. [202] The structual scaffold can even be used to target receptors other than GABA A . [ 203 ]
Flumazenil raises concerns with its tendency to induce benzodiazepine withdrawal, and symptoms include seizures and agitation. When a patient overdoses intentionally, benzodiazepines can actually mediate the effects of other lethal drugs in the system, so flumazenil's action to reverse its effects can actually be harmful.
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 ]
IC 50 / pIC 50 values represent binding affinity only and do not reflect efficacy or pharmacokinetics, and some compounds listed are GABA A antagonists rather than agonists (e.g. flumazenil). Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.)