Medazepam

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Medazepam
Clinical data
Trade namesRudotel
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability50–75% (Сmax = 1–2 hours)
Protein binding>99%
MetabolismHepatic
Elimination half-life2 hours, 36–150 hours (terminal)
ExcretionRenal (63–85%), Biliary 15–37%
Identifiers
  • 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1,4-benzodiazepine
JSmol)
  • ClC1=CC(C(C2=CC=CC=C2)=NCCN3C)=C3C=C1
  • 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 checkY
  • Key:YLCXGBZIZBEVPZ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Medazepam is a drug that is a

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.

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

References

  1. ^ 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.
  2. ^ "Benzodiazepines". Encyclopedia of Drugs.
  3. ^ 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.
  4. PMID 23084
    .
  5. PMID 6328498
    .
  6. PMID 6144464
    .

External links
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