Mexazolam

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
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	?
Legal status	Schedule IV(US)
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half-life	?
Excretion	Renal
Identifiers
ATC code	None
PubChem	CID 4177
ChemSpider	4033 Y
UNII	S5969B6237 Y
KEGG	D01316 Y
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
Chemical data
Formula	C18H16Cl2N2O2
Mol. mass	363.237 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C18H16Cl2N2O2/c1-11-10-24-18(13-4-2-3-5-15(13)20)14-8-12(19)6-7-16(14)21-17(23)9-22(11)18/h2-8,11H,9-10H2,1H3,(H,21,23) Y Key:ANUCDXCTICZJRH-UHFFFAOYSA-N Y
Y(what is this?)  (verify)

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]

See also

• Benzodiazepine

References

1. ^ DE Patent 1954065
2. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html. 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. 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: 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. 
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. http://dmd.aspetjournals.org/cgi/content/full/29/3/282. 

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