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?)  (verify)

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

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 effects after administration.^[5]

See also

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

References

1. ↑ Encyclopedia of Drugs: Benzodiazepines
2. ↑ Professor heather Ashton (April 2007). "BENZODIAZEPINE EQUIVALENCY TABLE". Retrieved September 23, 2007. 
3. ↑ 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 Thérapie. 229 (2): 313–26. PMID 23084. 
4. ↑ Taft WC; DeLorenzo RJ (May 1984). "Micromolar-affinity benzodiazepine receptors regulate voltage-sensitive calcium channels in nerve terminal preparations" (PDF). Proc Natl Acad Sci USA (PDF). 81 (10): 3118–22. doi:10.1073/pnas.81.10.3118. PMC 345232. PMID 6328498. 
5. ↑ Jochemsen R, Breimer DD (1984). "Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles". Curr Med Res Opin. 8 Suppl 4: 60–79. doi:10.1185/03007998409109545. PMID 6144464. 

External links

• Inchem - Medazepam