Mexazolam

Mexazolam[1] (marketed under the trade names Melex and Sedoxil)[2] is a drug which is a benzodiazepine derivative.[3] Mexazolam has been trialed for anxiety and was found to be effective in alleviating anxiety at one week follow-up, however, after three weeks of therapy mexazolam had lost its therapeutic anxiolytic properties becoming no more effective than placebo, presumably due to benzodiazepine tolerance.[4] Mexazolam is metabolised via the CYP3A4 pathway. HMG-CoA reductase inhibitors including simvastatin, simvastatin acid, lovastatin, fluvastatin, atorvastatin and cerivastatin inhibit the metabolism of mexazolam,[5] but not the HMG-CoA reductase inhibitor pravastatin.[6][7]

Mexazolam
Clinical data
Trade namesMelex, Sedoxil
Other names13-chloro- 2-(2-chlorophenyl)- 5-methyl- 3-oxa- 6,9-diazatricyclo[8.4.0.02,6] tetradeca- 1(10),11,13-trien- 8-one
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic (CYP3A4)
ExcretionRenal
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H16Cl2N2O2
Molar mass363.237 g/mol g·mol−1
3D model (JSmol)
  (verify)

See also

References
  1. DE Patent 1954065
  2. "Benzodiazepine Names". non-benzodiazepines.org.uk. Archived from the original on 2008-12-08. Retrieved 2009-04-05.
  3. Kurono, Y; Kamiya, K; Kuwayama, T; Jinno, Y; Yashiro, T; Ikeda, K (1987). "Kinetics and mechanism of the acid-base equilibrium of mexazolam and comparison with those of other commercial benzodiazepinooxazole drugs". Chemical & Pharmaceutical Bulletin. 35 (9): 3831–7. doi:10.1248/cpb.35.3831. PMID 2893667.
  4. Ferreira, L; Figueira, ML; Bessa-Peixoto, A; Marieiro, A; Albuquerque, R; Paz, C; Cerqueira, A; Damião, P; et al. (2003). "Psychomotor and anxiolytic effects of mexazolam in patients with generalised anxiety disorder". Clinical Drug Investigation. 23 (4): 235–43. doi:10.2165/00044011-200323040-00003. PMID 17535036.
  5. Mc Donnell, CG; Harte, S; O'driscoll, J; O'loughlin, C; Van Pelt, FN; Shorten, GD (2003). "The effects of concurrent atorvastatin therapy on the pharmacokinetics of intravenous midazolam". Anaesthesia. 58 (9): 899–904. doi:10.1046/j.1365-2044.2003.03339.x. PMID 12911366.
  6. Ishigami, M; Takasaki, W; Ikeda, T; Komai, T; Ito, K; Sugiyama, Y (2002). "Sex difference in inhibition of in vitro mexazolam metabolism by various 3-hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors in rat liver microsomes". Drug Metabolism and Disposition. 30 (8): 904–10. doi:10.1124/dmd.30.8.904. PMID 12124308.
  7. Ishigami, Michi; Honda, Tomoyo; Takasaki, Wataru; Ikeda, Toshihiko; Komai, Toru; Ito, Kiyomi; Sugiyama, Yuichi (2001). "A Comparison of the Effects of 3-Hydroxy-3-Methylglutaryl-Coenzyme A (HMG-CoA) Reductase Inhibitors on the CYP3A4-Dependent Oxidation of Mexazolam in Vitro". Drug Metabolism and Disposition. 29 (3): 282–8. PMID 11181496.


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.