The hypoalgesic effect of tramadol in relation to CYP2D6

Clinical Pharmacology and Therapeutics
L PoulsenS H Sindrup

Abstract

Tramadol inhibits norepinephrine reuptake, stimulates serotonin release, and acts with mu-opioid receptors by way of its metabolite (+)-M1. Formation of M1 seems to depend on the genetic polymorphic CYP2D6. The analgesic effect of 2 mg/kg tramadol was evaluated in 15 extensive and 12 poor metabolizers of sparteine in two parallel, randomized, double-blind, placebo-controlled crossover studies that used experimental pain models. In extensive metabolizers, tramadol increased pressure pain detection (p = 0.03) and tolerance (p = 0.06) thresholds, as well as thresholds for eliciting nociceptive reflexes, after single (p = 0.0002) and repeated (p = 0.06) stimulation of the sural nerve. Peak pain and pain area in the cold pressor test were reduced (p = 0.0006 and 0.0009). In poor metabolizers, only thresholds to pressure pain tolerance (p = 0.02) and nociceptive reflexes after single stimulation (p = 0.04) were increased and the reflex threshold was less increased in poor metabolizers than in extensive metabolizers (p = 0.02). The serum concentration of (+)-M1 2 to 10 hours after tramadol ranged from 10 to 100 ng/L in extensive metabolizers, whereas in poor metabolizers serum concentrations of (+)-M1 were below or around the detectio...Continue Reading

References

Apr 1, 1992·Anaesthesia·M D VickersJ Yoshizumi
Jan 1, 1991·Drug and Alcohol Dependence·K L PrestonM Testa
Jan 27, 1990·BMJ : British Medical Journal·J N MatthewsP Royston
Jan 1, 1990·European Journal of Clinical Pharmacology·G AlvánU Gundert-Remy
Dec 1, 1989·British Journal of Clinical Pharmacology·Q Y YueJ Säwe
Oct 15, 1988·Lancet·Z R ChenF Bochner
Dec 1, 1986·Pain·Mark J Millan
May 21, 1988·British Medical Journal·M J Campbell, M J Gardner
Sep 1, 1994·British Journal of Anaesthesia·S Petersen-FelixA M Zbinden
Jan 1, 1996·British Journal of Clinical Pharmacology·J A DesmeulesP Dayer

❮ Previous
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Citations

Dec 18, 2012·European Journal of Clinical Pharmacology·Tuukka SaarikoskiKari Laine
Nov 5, 2010·International Journal of Clinical Pharmacy·Bob WilffertUNKNOWN KNMP working group Pharmacogenetics
Apr 17, 2013·Molecular Diagnosis & Therapy·C F SamerJ A Desmeules
Dec 22, 2007·Journal of Palliative Medicine·James F Cleary
May 27, 2003·British Journal of Anaesthesia·B P Sweeney
Feb 28, 2008·British Journal of Anaesthesia·K AllegaertB J Anderson
Jun 2, 2009·British Journal of Anaesthesia·R Searle, P M Hopkins
Aug 13, 2011·The Journal of Veterinary Medical Science·Takaharu ItamiKazuto Yamashita
Jul 4, 2008·Pharmacogenomics·Victoria RollasonJules Desmeules
Oct 22, 2009·Pharmacogenomics·Ibrahim A Abdel-Hamid, Karl-Erik Andersson
Dec 19, 2009·Pharmacogenomics·Ana AlfirevicMunir Pirmohamed
Nov 29, 2007·Vojnosanitetski pregled. Military-medical and pharmaceutical review·Leposava GrbovićGordana J Dragović
Feb 2, 2011·American Journal of Veterinary Research·Butch Kukanich, Mark G Papich
Jul 7, 2011·American Journal of Veterinary Research·Allison J StewartJenny Springfield
Jun 4, 2010·Expert Review of Neurotherapeutics·Craig T Hartrick
May 19, 2011·Expert Opinion on Drug Metabolism & Toxicology·Paul J Jannetto, Nancy C Bratanow
Aug 24, 2006·Expert Opinion on Pharmacotherapy·Consalvo Mattia, Flaminia Coluzzi
Jun 12, 2009·Drug Metabolism Reviews·Shu-Feng ZhouBalram Chowbay
Mar 29, 2008·Expert Opinion on Drug Metabolism & Toxicology·Esin KadievSwati Nagar
Oct 12, 2007·Expert Opinion on Pharmacotherapy·Ulrike M Stamer, Frank Stüber
Oct 3, 2009·Expert Opinion on Pharmacotherapy·Craig T Hartrick
Dec 14, 2011·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Robert G Hendrickson, Nathanael J McKeown
Oct 10, 2003·Cancer Investigation·Howard L McLeod, Jinsheng Yu
Jan 30, 2007·Current Medical Research and Opinion·Roy FreemanUNKNOWN CAPSS-237 Study Group
May 20, 2015·Pain Medicine : the Official Journal of the American Academy of Pain Medicine·Davide SeripaAlberto Pilotto
Jan 25, 2006·Anaesthesia·B P Sweeney, J Bromilow
Jan 8, 2008·Journal of Veterinary Pharmacology and Therapeutics·B H Pypendop, J E Ilkiw
Mar 5, 2008·Journal of Clinical Pharmacy and Therapeutics·R B Raffa
Apr 26, 2015·Clinical Pharmacokinetics·Dorte LassenKim Brøsen
Jan 7, 2015·European Journal of Clinical Pharmacology·Tuukka SaarikoskiKari Laine
Jan 25, 2014·Clinical Pharmacology and Therapeutics·K R CrewsUNKNOWN Clinical Pharmacogenetics Implementation Consortium
Mar 10, 2017·The Journal of Pain : Official Journal of the American Pain Society·Marion A CoeSharon L Walsh
Jul 19, 2005·European Journal of Clinical Pharmacology·Jónrit HallingKim Brøsen
Sep 6, 2007·European Journal of Clinical Pharmacology·Helmut Schmidt, Jörn Lötsch
Jun 10, 2006·European Journal of Clinical Pharmacology·Rasmus Steen PedersenKim Brøsen
Jun 2, 2009·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Lukás ChytilOndrej Slanar
Jan 14, 2009·The Veterinary Journal·Enzo VettoratoPetra Cagnardi
Sep 29, 2005·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Caroline F SamerJules A Desmeules
Apr 21, 2006·Der Anaesthesist·U StamerF Stüber
Apr 24, 2012·Journal of Psychopharmacology·David R OwenDavid J Nutt
Jul 8, 2017·Paediatric Anaesthesia·Brian J AndersonGeorge A Chalkiadis

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