PMID: 8946470Oct 1, 1996Paper

Formation of meprobamate from carisoprodol is catalysed by CYP2C19

Pharmacogenetics
P DalénH Olsen

Abstract

Carisoprodol is a muscle relaxant analgesic, which has an active metabolite i.e. meprobamate. We conducted an open three-panel single-dose administration study with 15 healthy volunteers: five poor metabolizers of mephenytoin, five poor metabolizers of debrisoquine and five extensive metabolizers of both substrates. The aim was to investigate if the elimination of carisoprodol and meprobamate is dependent on the two metabolic polymorphisms of mephenytoin and debrisoquine. The subjects were given single oral doses of 700 mg carisoprodol and 400 mg meprobamate on separate occasions. The disposition of carisoprodol was clearly correlated to the mephenytoin hydroxylation phenotype. The mean serum clearance of carisoprodol was four times lower in poor metabolizers of mephenytoin than in extensive metabolizers, which confirms the hypothesis from our previous study that N-dealkylation of carisoprodol cosegregates with the mephenytoin hydroxylation polymorphism. However, mean serum clearance of meprobamate did not differ between the two groups. Also, polymorphic debrisoquine hydroxylation did not influence the elimination of carisoprodol or meprobamate. Poor metabolizers of mephenytoin thus have a lower capacity to metabolize carisopro...Continue Reading

Citations

Feb 4, 2014·Journal of Analytical Toxicology·Stephanie A TseBrookie M Best
Nov 23, 2006·International Journal of Legal Medicine·Gudrun HøisethJørg Mørland
Aug 13, 2008·Analytical and Bioanalytical Chemistry·Ulrich M ZangerMatthias Schwab
Jul 16, 2005·European Journal of Clinical Pharmacology·Jørgen G BramnessJørg Mørland
Mar 1, 2005·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Jørgen G BramnessDag Jacobsen
Jun 15, 2004·Drug and Alcohol Dependence·Jørgen G BramnessJørg Mørland
Mar 6, 2018·Basic & Clinical Pharmacology & Toxicology·David E MoodyWenfang B Fang
Sep 27, 2005·Journal of Psychiatric Practice·Gautam RohatgiJack M Gorman
Sep 12, 2002·Clinical Pharmacokinetics·Zeruesenay DestaDavid A Flockhart
Jul 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Judy L RaucyJerome M Lasker
Feb 27, 2009·The Journal of Pharmacology and Experimental Therapeutics·Lorie A GonzalezGlenn H Dillon
Oct 18, 2016·Journal of Mass Spectrometry : JMS·Laszlo ProkaiMichael J Forster
Sep 3, 2011·Pharmacology, Biochemistry, and Behavior·James P ZacnyDennis W Coalson
Jun 26, 2010·Environmental Science & Technology·Gretchen M BruceShane A Snyder
Jun 9, 2006·Medicina clínica·Hortensia Alonso-NavarroJosé A García-Agúndez

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