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Benzodiazepam
Mexazolam
Trade names Melex, Sedoxil Other names 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
AHFS /
Drugs.com
International Drug Names
Routes of administration Oral
ATC code
Legal status
Metabolism
Liver (
CYP3A4 )
Excretion
Kidney
10-chloro-11b -(2-chlorophenyl)-3-methyl-2,3,5,7-tetrahydro-[1,3]oxazolo[3,2-d ][1,4]benzodiazepin-6-one
CAS Number
PubChem
CID
ChemSpider
UNII
KEGG
CompTox Dashboard (
EPA )
Formula C 18 H 16 Cl 2 N 2 O 2
Molar mass 363.24 g·mol−1 3D model (
JSmol )
Clc1ccccc1C42OCC(N2CC(=O)Nc3c4cc(Cl)cc3)C
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
(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. 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,
[4] but not the HMG-CoA reductase inhibitor
pravastatin .
[5]
[6] Its principal active metabolites are chlorodesmethyldiazepam (also known as chloronordiazepam or
delorazepam , trade name Dadumir) and chloroxazepam (also known as
lorazepam , trade name Ativan).
[7]
See also
References
^ DE Patent 1954065
^
"Benzodiazepine Names" . non-benzodiazepines.org.uk. Archived from
the original on 2008-12-08. Retrieved 2009-04-05 .
^ Kurono Y, Kamiya K, Kuwayama T, Jinno Y, Yashiro T, Ikeda K (September 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): 3831–3837.
doi :
10.1248/cpb.35.3831 .
PMID
2893667 .
^ Mc Donnell CG, Harte S, O'Driscoll J, O'Loughlin C, Van Pelt FN, Shorten GD (September 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 .
S2CID
25382546 .
^ Ishigami M, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y (August 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): 904–910.
doi :
10.1124/dmd.30.8.904 .
PMID
12124308 .
S2CID
2620104 .
^ Ishigami M, Honda T, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y (March 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): 282–288.
PMID
11181496 .
^ Fernandes H, Moreira R (June 2014).
"Mexazolam: clinical efficacy and tolerability in the treatment of anxiety" . Neurology and Therapy . 3 (1): 1–14.
doi :
10.1007/s40120-014-0016-7 .
PMC
4381915 .
PMID
26000220 .
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