Medazepam

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]

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)[1] 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 N
PubChem CID	4041
DrugBank	none N
ChemSpider	3901 Y
UNII	P0J3387W3S
KEGG	D01292 Y
ChEMBL	ChEMBL28333 Y
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 Y Key:YLCXGBZIZBEVPZ-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

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]

See also

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