Medazepam Explained

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.^[1] Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.^[2]

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.^[3] 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.^[4] It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effect after administration.^[5]

See also

• Benzodiazepine dependence
• Benzodiazepine withdrawal syndrome
• Long-term effects of benzodiazepines

External links

• Inchem - Medazepam

Notes and References

1. Encyclopedia: Benzodiazepines . Encyclopedia of Drugs .
2. Web site: Benzodiazepine Equivalency Table . April 2007 . September 23, 2007 . Heather . Ashton . vanc . Benzodiazepines Co-operation Not Confrontation (BCNC) . September 28, 2007 . https://web.archive.org/web/20070928121055/http://www.bcnc.org.uk/equivalence.html . dead .
3. Zakusov VV, Ostrovskaya RU, Kozhechkin SN, Markovich VV, Molodavkin GM, Voronina TA . Further evidence for GABA-ergic mechanisms in the action of benzodiazepines . Archives Internationales de Pharmacodynamie et de Therapie . 229 . 2 . 313–26 . October 1977 . 23084 .
4. Taft WC, DeLorenzo RJ . Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations . Proceedings of the National Academy of Sciences of the United States of America . 81 . 10 . 3118–22 . May 1984 . 6328498 . 345232 . 10.1073/pnas.81.10.3118 . PDF . 1984PNAS...81.3118T . free .
5. Jochemsen R, Breimer DD . Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles . Current Medical Research and Opinion . 8 Suppl 4 . 60–79 . 1984 . 6144464 . 10.1185/03007998409109545 .