Arfendazam Explained
Arfendazam (INN)[1] is a drug which is a benzodiazepine derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam.
Arfendazam has sedative and anxiolytic effects similar to those produced by other benzodiazepine derivatives, but is a partial agonist at GABAA receptors, so the sedative effects are relatively mild and it produces muscle relaxant effects only at very high doses.[2] [3]
Arfendazam produces an active metabolite lofendazam, which is thought to be responsible for part of its effects.[4]
See also
Notes and References
- Web site: International Nonproprietary Names for Pharmaceutical Substances. Proposed International Nonproprietary Names (Prop. INN): List 39. Supplement to WHO Chronicle . March 1978 . 32 . 3 . 3 . World Health Organization. 4 December 2015.
- Mueller E . Benzodiazepine receptor interactions of arfendazam, a novel 1, 5-benzodiazepine. . Pharmacopsychiatry . January 1985 . 18 . 1 . 10–1 . 10.1055/s-2007-1017288 . 144951247 .
- Müller WE, Groh B, Bub O . In vitro and in vivo studies of the mechanism of action of arfendazam, a novel 1, 5-benzodiazepine. . Pharmacopsychiatry . July 1986 . 19 . 4 . 314–315 . 10.1055/s-2007-1017251. 143919337 .
- Book: Adrien J, Albani F, Baruzzi A, Berger M, Bixler EO, Borbeley AA, Dikeos DG, Drucker-Colin R, Montero RF, Hishikawa Y, Inoue S . The Pharmacology of Sleep. . Springer Science & Business Media . December 2012 . 978-3-540-58961-7 .