Flumazenil (also known as flumazepil, code name Ro 15-1788[3]) is a selective GABAA 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.
It was first characterized in 1981,[5] and was first marketed in 1987 by Hoffmann-La Roche under the trade name Anexate. However, it did not receive FDA approval until December 20, 1991. The developer lost its exclusive patent rights in 2008; so at present, generic formulations of this drug are available. Intravenous flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual lozenge and topical cream has also been tested.[6][7]
^"FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
^Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
Flumazenil (also known as flumazepil, code name Ro 15-1788) is a selective GABAA receptor antagonist administered via injection, otic insertion, or intranasally...
improve sleepiness. These currently include clarithromycin and flumazenil. Flumazenil is the only GABAA receptor antagonist on the market as of January...
mainstay of treatment of benzodiazepine overdose. There is an antidote, flumazenil, but its use is controversial. Deaths from single-drug benzodiazepine...
involved, the flumazenil detoxification method is controversial and can only be done as an inpatient procedure under medical supervision. Flumazenil was found...
severe side effects include memory problems and hallucinations. While flumazenil, a GABAA–receptor antagonist, can reverse zolpidem's effects, usually...
thienotriazolodiazepine, but produces very similar effects as benzodiazepines. Flumazenil is an imidazobenzodiazepine derivative, and in layman's terms, it is a...
subsequently, the administration of flumazenil may result in seizures. Therefore, slow administration of flumazenil is necessary to prevent the occurrence...
improve sleepiness. These currently include clarithromycin and flumazenil. Flumazenil, a GABAA receptor antagonist is approved by the FDA for use in anesthesia...
D50W IV), flumazenil (0.2 mg IV), naloxone (2 mg IV), and thiamine (100 mg IV). It has been suggested that the use of naloxone and flumazenil be administered...
securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other agents which may have GABAA receptor antagonism include the antibiotic...
3% of patients discontinuing benzodiazepines completely within a year. Flumazenil delivered via slow subcutaneous infusion represents a safe procedure for...
benzodiazepine) is flumazenil (Anexate). This drug is only used in cases with severe respiratory depression or cardiovascular complications. Because flumazenil is a...
an overdose of chlordiazepoxide (or any other benzodiazepine) is flumazenil. Flumazenil should be given with caution as it may precipitate severe withdrawal...
help combat any belief or fear that they were "awake" during anesthesia. Flumazenil, reverses the effects of benzodiazepines Naloxone, reverses the effects...
effects including convulsions, neurotoxicity, and anxiety, among others. Flumazenil is a competitive antagonist of the benzodiazepine site of the GABAA receptor...
if necessary, considering the hazards of doing so, giving intravenous flumazenil. People are ideally nursed in a kind, frustration-free environment, since...
1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as a high-potency...
MZ; Stoller KB; Griffiths RR (November 1999). "A controlled study of flumazenil-precipitated withdrawal in chronic low-dose benzodiazepine users". Psychopharmacology...
combination of hydroxyzine and two other medications (gabapentin and flumazenil) as well as therapy, is an ineffective treatment promoted for methamphetamine...
can be treated with the GABAA receptor benzodiazepine site antagonist flumazenil, which displaces zopiclone from its binding site, thereby rapidly reversing...
contrast, most benzodiazepine overdose does not benefit from its antidote, flumazenil. Respiratory therapy/respiratory physiotherapy may be beneficial in some...
the amnesia-producing properties of the drug. In extreme situations, flumazenil can be administered to inhibit or reverse the effects of midazolam. Antipsychotic...
most closely related to other imidazobenzodiazepines such as midazolam, flumazenil, and bretazenil. Imidazenil is a highly potent benzodiazepine receptor...
benzodiazepine receptor inverse agonists. The benzodiazepine antagonist flumazenil, however, fails to alter the anticonvulsant activity of loreclezole, indicating...
benzodiazepines, the LD50 is still far beyond the prescribed or recommended dose. Flumazenil, a GABA antagonist agent used to reverse benzodiazepine overdoses, inhibits...
PMID 15214628. S2CID 39966201. "Treatment of benzodiazepine overdose with flumazenil. The Flumazenil in Benzodiazepine Intoxication Multicenter Study Group". Clinical...
Fertonani G, Chittolini B, Avanzini P, et al. (June 1996). "Intravenous flumazenil following prolonged exposure to lormetazepam in humans: lack of precipitated...
Global Information
