Medazepam

Medazepam

Clinical data
Trade names	Rudotel
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral
ATC code	N05BA03 (WHO)
Legal status
Legal status	CA: Schedule IV DE: Anlage III (Prescription only) US: Schedule IV
Pharmacokinetic data
Bioavailability	50–75% (Сmax = 1–2 hours)
Protein binding	>99%
Metabolism	Hepatic
Biological 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 Y
KEGG	D01292 Y
ChEMBL	CHEMBL28333 Y
ECHA InfoCard	100.018.895
Chemical and physical data
Formula	C16H15ClN2
Molar mass	270.8 g/mol
3D model (Jmol)	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?)

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.

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.