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Medazepam
Clinical data
Trade names	Rudotel
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	N05BA03 (WHO) ;
Legal status
Legal status	BR: Class B1 (Psychoactive drugs); CA: Schedule IV; DE: Prescription only (Anlage III for higher doses); US: Schedule IV;
Pharmacokinetic data
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%
Identifiers
	IUPAC name 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepine;
CAS Number	2898-12-6 ;
PubChem CID	4041;
DrugBank	none ;
ChemSpider	3901 ;
UNII	P0J3387W3S;
KEGG	D01292 ;
ChEMBL	ChEMBL28333 ;
CompTox Dashboard (EPA)	DTXSID1048708 ;
ECHA InfoCard	100.018.895
Chemical and physical data
Formula	C16H15ClN2
Molar mass	270.76 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES ClC1=CC(C(C2=CC=CC=C2)=NCCN3C)=C3C=C1;
	InChI InChI=1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3 ; Key:YLCXGBZIZBEVPZ-UHFFFAOYSA-N ;
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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]

References

^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
^ "Benzodiazepines". Encyclopedia of Drugs.
^ 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. PMID 23084.
^ Taft WC, DeLorenzo RJ (May 1984). "Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations" (PDF). Proceedings of the National Academy of Sciences of the United States of America (PDF). 81 (10): 3118–22. Bibcode:1984PNAS...81.3118T. 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". Current Medical Research and Opinion. 8 Suppl 4: 60–79. doi:10.1185/03007998409109545. PMID 6144464.