Meptazinol

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Meptazinol
Meptazinol racemate2DCSD.svg
Clinical data
AHFS/Drugs.com International Drug Names
Dependence
liability
Low
Routes of
administration
Oral, IM, IV
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
Pharmacokinetic data
Metabolism The peak analgesic effect is seen within 30–60 minutes and lasts about 3–4 hours.
Biological half-life Half-Life (1.4–4 hours).
Excretion The drug is rapidly metabolised to the glucuronide, and mostly excreted in the urine.
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.053.718
Chemical and physical data
Formula C15H23NO
Molar mass 233.34922 g/mol
3D model (Jmol)
Chirality Racemic mixture
 NYesY (what is this?)  (verify)

Meptazinol (trade name Meptid) is an opioid analgesic developed by Wyeth in the 1970s.[1] Indications for use in moderate to severe pain, most commonly used to treat pain in obstetrics (childbirth).

Meptazinol is a 3-phenylazpane derivative, whereas the other phenazepanes like ethoheptazine and proheptazine are 4-phenylazepanes.

A partial µ-opioid receptor agonist, its mixed agonist/antagonist activity affords it a lower risk of dependence and abuse than full µ agonists like morphine. Meptazinol exhibits not only a short onset of action, but also a shorter duration of action relative to other opioids such as morphine, pentazocine, or buprenorphine.[2]

References[edit]

  1. ^ US patent 4197239, Cavalla JF, Shepherd RG, White AC, "Hexahydroazepine, Piperidine and Pyrrolidine Derivatives", issued 1980-04-08, assigned to Wyeth 
  2. ^ Holmes B, Ward A (1985). "Meptazinol. A Review of its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Efficacy". Drugs. 30 (4): 285–312. doi:10.2165/00003495-198530040-00001. PMID 2998723. 

External links[edit]