|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%|
|Chemical and physical data|
|Molar mass||270.8 g/mol g·mol−1|
|3D model (JSmol)|
|(what is this?)|
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.
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.
- Benzodiazepine dependence
- Benzodiazepine withdrawal syndrome
- Long-term effects of benzodiazepines
- Encyclopedia of Drugs: Benzodiazepines
- Professor heather Ashton (April 2007). “BENZODIAZEPINE EQUIVALENCY TABLE”. Retrieved September 23, 2007.
- Zakusov VV; Ostrovskaya RU; Kozhechkin SN; Markovich VV; Molodavkin GM; Voronina TA. (October 1977). “Further evidence for GABA-ergic mechanisms in the action of benzodiazepines”. Archives Internationales de Pharmacodynamie et de Thérapie. 229 (2): 313–26. PMID 23084.
- Taft WC; DeLorenzo RJ (May 1984). “Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations” (PDF). Proc Natl Acad Sci USA (PDF). 81 (10): 3118–22. doi:10.1073/pnas.81.10.3118. PMC 345232. PMID 6328498.
- Jochemsen R, Breimer DD (1984). “Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles”. Curr Med Res Opin. 8 Suppl 4: 60–79. doi:10.1185/03007998409109545. PMID 6144464.