Mexazolam Explained

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

• Benzodiazepine
• Delorazepam
• Lorazepam

Notes and References

1. DE Patent 1954065
2. Web site: Benzodiazepine Names . 2009-04-05 . non-benzodiazepines.org.uk . dead . https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html . 2008-12-08 .
3. Kurono Y, Kamiya K, Kuwayama T, Jinno Y, Yashiro T, Ikeda K . 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 . September 1987 . 2893667 . 10.1248/cpb.35.3831 . free .
4. Mc Donnell CG, Harte S, O'Driscoll J, O'Loughlin C, Van Pelt FN, Shorten GD . The effects of concurrent atorvastatin therapy on the pharmacokinetics of intravenous midazolam . Anaesthesia . 58 . 9 . 899–904 . September 2003 . 12911366 . 10.1046/j.1365-2044.2003.03339.x . 25382546 . free .
5. Ishigami M, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y . 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 . August 2002 . 12124308 . 10.1124/dmd.30.8.904 . 2620104 .
6. Ishigami M, Honda T, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y . 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 . March 2001 . 11181496 .
7. Fernandes H, Moreira R . Mexazolam: clinical efficacy and tolerability in the treatment of anxiety . Neurology and Therapy . 3 . 1 . 1–14 . June 2014 . 26000220 . 4381915 . 10.1007/s40120-014-0016-7 .