Scandinavian Journal of Pain
Volume 1, Supplement 1 , Pages S18-S23, May 2009

Pharmacology of oxycodone: does it explain why oxycodone has become a bestselling strong opioid?

  • Kim K. Lemberg

      Affiliations

    • Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland
    • Corresponding Author InformationCorresponding author. Kim Lemberg, DDS, Institute of Biomedicine/Pharmacology, P.O. Box 63, FIN-00014 University of Helsinki, Finland. Tel.: +358 50 5950009; fax: +358 9 19125364
    • ,
  • Tarja E. Heiskanen

      Affiliations

    • Pain Clinic, Department of Anaesthesiology and Intensive Care Medicine, Helsinki University Central Hospital, Helsinki, Finland
    • ,
  • Vesa K. Kontinen

      Affiliations

    • Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland
    • Pain Clinic, Department of Anaesthesiology and Intensive Care Medicine, Helsinki University Central Hospital, Helsinki, Finland
    • ,
  • Eija A. Kalso

      Affiliations

    • Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland
    • Pain Clinic, Department of Anaesthesiology and Intensive Care Medicine, Helsinki University Central Hospital, Helsinki, Finland

Abstract 

As morphine, oxycodone is a m-opioid receptor agonist with a significantly different pharmacokinetic profile compared with morphine. It seems that oxycodone is able to compensate its lower binding affinity for the m-opioid receptor compared with that of morphine by active transport to the central nervous system. Although the analgesic properties of oxycodone are mainly due to its own activity, cytochrome (CYP) inhibitors and inductors may change oxycodone-induced analgesia as a result of higher or lower, respectively, oxycodone concentrations.

Keywords:  oxycodone , noroxycodone , oxymorphone , noroxymorphone

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PII: S1877-8860(09)70005-9

doi:10.1016/S1877-8860(09)70005-9

Scandinavian Journal of Pain
Volume 1, Supplement 1 , Pages S18-S23, May 2009

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