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]
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]
^Ashton H (April 2007).
"Benzodiazepine Equivalency Table". Benzodiazepines Co-operation Not Confrontation (BCNC). Archived from
the original on September 28, 2007. 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 Therapie. 229 (2): 313–26.
PMID23084.
^Jochemsen R, Breimer DD (1984). "Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles". Current Medical Research and Opinion. 8 Suppl 4: 60–79.
doi:
10.1185/03007998409109545.
PMID6144464.