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| Clinical data | |
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| 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 |
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| Pharmacokinetic data | |
| Metabolism | Liver (CYP3A4) |
| Excretion | Kidney |
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| Chemical and physical data | |
| Formula | C18H16Cl2N2O2 |
| Molar mass | 363.24 g·mol−1 |
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Mexazolam[1] (marketed under the trade namesMelex andSedoxil)[2] is a drug which is abenzodiazepine 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 theCYP3A4 pathway.HMG-CoA reductase inhibitors includingsimvastatin,simvastatin acid,lovastatin,fluvastatin,atorvastatin andcerivastatin inhibit the metabolism of mexazolam,[4] but not the HMG-CoA reductase inhibitorpravastatin.[5][6] Its principal active metabolites are chlorodesmethyldiazepam (also known as chloronordiazepam ordelorazepam, trade name Dadumir) and chloroxazepam (also known aslorazepam, trade name Ativan).[7] Researchers have found a dose of 1.67 mg mexazolam equals 5 mgdiazepam.[8] Clinical studies suggest that 3 mg of mexazolam has a comparable effect to 1.5 mg of alprazolam.[9]
Mexazolam is a long-acting benzodiazepine that undergoes extensive hepatic metabolism. In humans, the parent drug is primarily oxidized by cytochrome P450 3A isoforms, yielding two active benzodiazepine metabolites:chloronordiazepam andchloroxazepam. Mexazolam follows biphasic elimination profile: the initial distribution phase has a half-life of approximately 1.4 hours, reflecting rapid tissue uptake and first-pass metabolism, following by a terminal phase with a half-life of about 76 hours. The long duration of the terminal phase driven by high plasma protein binding (over 90 percent) and gradual release from peripheral compartments.[10] The active metabolites further extend duration of action of the drug.[10][11] The elimination half-lives of the active metabolites is130–200 h, which supports once-daily dosing but also calls for caution regarding accumulation and residual sedative effects during prolonged therapy.[10]
Mexazolam's primary target isGABAA receptor, benzodiazepine site, via the active metabolitechloronordiazepam.[11] Mexazolam potentiates GABA currents at α2/α3 (anxiolytic) subunit‑containing receptors. The drug has minimal effect on α1 (sedative) amplitude;[12][11] as such, mexazolam has lower sedative load compared to classical benzodiazepines[11] such aschlordiazepoxide.[13]
