|Systematic (IUPAC) name|
|Trade names||Anexate, Lanexat, Mazicon, Romazicon|
|Pregnancy cat.||B3 (AU) C|
|Legal status||℞ Prescription only|
|Half-life||7-15 min (initial)
20-30 min (brain)
40-80 min (terminal)
|Synonyms||ethyl 8-fluoro- 5,6-dihydro- 5-methyl- 6-oxo- 4H- imidazo [1,5-a] [1,4] benzodiazepine- 3-carboxylate|
|Mol. mass||303.288 g/mol|
|(what is this?)|
Flumazenil (also known as flumazepil, code name Ro 15-1788) is a GABAA receptor antagonist primarily available by injection only, and the only GABAA receptor antagonist on the market today.
It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by the FDA on December 20, 1991. Flumazenil went off patent in 2008 so at present generic formulations of this drug are available. Daily administration of flumazenil by sublingual lozenge and topical cream has been tested positively at Emory University. To date the use of this medicine was in rare cases of benzodiazepine overdoses but due to recent studies suggesting the successful treatment of idiopathic hypersomnia with this medicine, the demand of this medicine is estimated to increase drastically. Researchers have recently suggested that the prevalence of idiopathic hypersomnia is higher, at least 1 in 800, which translates to about 400,000 in the U.S. alone thus suggesting a potential market for this drug.