title: Does the pharmacology of oxycodone justify its increasing use as an analgesic?
abstract: Oxycodone is a semisynthetic opioid analgesic that is increasingly used for the treatment of acute, cancer, and chronic non-malignant pain. Oxycodone was synthesized in 1917 but its pharmacological properties were not thoroughly studied until recently. Oxycodone is a fairly selective μ-opioid receptor agonist, but there is a striking discrepancy between the relatively low binding potential and G protein activation by oxycodone and its analgesic efficacy. It has been claimed that this is because of active metabolites and enhanced passage to the central nervous system by active transport. We critically review studies on the basic pharmacology of oxycodone and on its pharmacokinetics and pharmacodynamics in humans. In particular, the role of pharmacogenomics and population pharmacokinetics in understanding the properties of oxycodone is discussed in detail. We compare oxycodone with morphine, the standard opioid in clinical use.
authors: Department of Anaesthesiology, Intensive Care, Emergency Care, and Pain Medicine, University of Turku and Turku University Hospital, P.O. Box 52 (Kiinamyllynkatu 4-8), FI-20520 Turku, Finland. klaus.olkkola@utu.fi
authors: Klaus T
authors: KT
authors: Olkkola
authors: Vesa K
authors: VK
authors: Kontinen
authors: Teijo I
authors: TI
authors: Saari
authors: Eija A
authors: EA
authors: Kalso
mesh_terms: D000701:Analgesics, Opioid / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D006801:Humans; D010098:Oxycodone / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D017450:Receptors, Opioid, mu / Q000819:agonists
chemical_list: D000701:Analgesics, Opioid; D017450:Receptors, Opioid, mu; D010098:Oxycodone