Medazepam
Benzodiazepine drug
From Wikipedia, the free encyclopedia
Medazepam is a drug that is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam.[2] Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.[3]
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| Trade names | Rudotel |
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| Routes of administration | Oral |
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| Bioavailability | 50–75% (Сmax = 1–2 hours) |
| Protein binding | >99% |
| Metabolism | Hepatic |
| Elimination half-life | 2 hours, 36–150 hours (terminal) |
| Excretion | Renal (63–85%), Biliary 15–37% |
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| ECHA InfoCard | 100.018.895 |
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| Formula | C16H15ClN2 |
| Molar mass | 270.76 g·mol−1 |
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Pharmacology
Medazepam acts as a prodrug to nordazepam. Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor.[4] Benzodiazepines may also act via micromolar benzodiazepine-binding sites as Ca2+ channel blockers and significantly inhibited depolarization-sensitive calcium uptake in experiments with cell components from rat brains. This has been conjectured as a mechanism for high dose effects against seizures in a study.[5] It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effect after administration.[6]