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. Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.
|AHFS/Drugs.com||International Drug Names|
|Bioavailability||50–75% (Сmax = 1–2 hours)|
|Elimination half-life||2 hours, 36–150 hours (terminal)|
|Excretion||Renal (63–85%), Biliary 15–37%|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||270.8 g/mol g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Medazepam acts as a prodrug to diazepam, as well as nordazepam, temazepam and oxazepam. Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor. 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. It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effects after administration.
- Encyclopedia of Drugs: Benzodiazepines
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