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Mexazolam: Wikis


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Mexazolam
Systematic (IUPAC) name
10-chloro- 11b-(2-chlorophenyl)- 3-methyl- 2,3,7,11b-tetrahydro [1,3]oxazolo [3,2-d] [1,4]benzodiazepin- 6(5H)-one
Identifiers
CAS number  ?
ATC code none
PubChem 4177
Chemical data
Formula C 18H16Cl2N2O2  
Mol. mass 363.237 g/mol
Synonyms 13-chloro- 2-(2-chlorophenyl)- 5-methyl- 3-oxa- 6,9-diazatricyclo[8.4.0.02,6] tetradeca- 1(10),11,13-trien- 8-one
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life  ?
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status Schedule IV(US)
Routes Oral

Mexazolam (marketed under brand name Melex and Sedoxil)[1] is a drug which is a benzodiazepine derivative.[2] Atorvastatin administration along with mexazolam results in a reduced elimination rate of mexazolam.[3] Mexazolam has been trialed for anxiety and was found to be effective in alleviating anxiety at one week follow-up, however, after 3 weeks of therapy mexazolam had lost it's therapeutic anxiolytic properties becoming no more effective than placebo, presumably due to benzodiazepine tolerance.[4] Mexazolam is metabolised via thee CYP3A4 pathway. HMG-CoA reductase inhibitors including simvastatin, simvastatin acid, lovastatin, fluvastatin, atorvastatin and cerivastatin inhibit the metabolism of mexazolam. Pravastatin, an HMG-CoA reductase inhibitor however, does not inhibit mexazolam metabolism.[5][6]

See also

References

  1. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html. Retrieved 2009-04-05.  
  2. ^ Kurono, Y; Kamiya; Kuwayama; Jinno; Yashiro; Ikeda (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. PMID 2893667.  
  3. ^ Mc Donnell, CG; Harte; O'driscoll; O'loughlin; Van Pelt; Shorten (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.  
  4. ^ Ferreira, L; Figueira; Bessa-Peixoto; Marieiro; Albuquerque; Paz; Cerqueira; Damião 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. ^ Ishigami, M; Takasaki; Ikeda; Komai; Ito; Sugiyama (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: the biological fate of chemicals 30 (8): 904–10. doi:10.1124/dmd.30.8.904. PMID 12124308. http://dmd.aspetjournals.org/cgi/content/full/30/8/904.  
  6. ^ 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. PMID 11181496. http://dmd.aspetjournals.org/cgi/content/full/29/3/282.  







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