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Medazepam

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Medazepam
120px
120px
Systematic (IUPAC) name
9-Chloro-2-methyl-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraene
Clinical data
AHFS/Drugs.com International Drug Names
  •  ?
Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half-life 36-150 hours
Excretion Renal
Identifiers
2898-12-6 7pxN
N05BA03
PubChem CID 4041
DrugBank none 7pxN
ChemSpider 3901 7pxY
UNII P0J3387W3S 7pxY
KEGG D01292 7pxY
ChEMBL CHEMBL28333 7pxY
Chemical data
Formula C16H15ClN2
270.8
 14pxN (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

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. PMC 345232. PMID 6328498. doi:10.1073/pnas.81.10.3118. 
  5. ^ Jochemsen R, Breimer DD (1984). "Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles". Curr Med Res Opin. 8 Suppl 4: 60–79. PMID 6144464. doi:10.1185/03007998409109545. 

External links