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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 .
The ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...
[citation needed] Bemegride and flumazenil are used to treat drug overdoses (of barbiturates and benzodiazepines respectively), but may cause convulsions if the dose is too high. [8] [9] Convulsants are also widely used in scientific research, for instance in the testing of new anticonvulsant drugs. Convulsions are induced in captive animals ...
Flumazenil delivered via slow subcutaneous infusion represents a safe procedure for those withdrawing from long-term, high dose benzodiazepine dependency. [67] It has a low risk of seizures even amongst those who have experienced convulsions when previously attempting benzodiazepine withdrawal.
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. [6]
Due to these contraindications and the possibility of it causing severe adverse effects including seizures, adverse cardiac effects, and death, [50] [51] in the majority of cases there is no indication for the use of flumazenil in the management of benzodiazepine overdose as the risks in general outweigh any potential benefit of administration.
An action potential occurs when the membrane potential of a specific cell rapidly rises and falls. [1] This depolarization then causes adjacent locations to similarly depolarize. Action potentials occur in several types of excitable cells, which include animal cells like neurons and muscle cells, as well as some plant cells.
[4] [5] [6] In addition, the selective α 5 subunit-containing GABA A receptor NAMs L-655,708 and MRK-016 have been found to produce rapid-acting antidepressant effects in animals similar to those of the NMDA receptor antagonist ketamine, and are of interest for the potential treatment of depression.