Refereed review article in scientific journal (A2)
Does the pharmacology of oxycodone justify its increasing use as an analgesic?
List of Authors: Olkkola KT, Kontinen VK, Saari TI, Kalso EA
Publisher: ELSEVIER SCIENCE LONDON
Publication year: 2013
Journal: Trends in Pharmacological Sciences
Journal name in source: TRENDS IN PHARMACOLOGICAL SCIENCES
Journal acronym: TRENDS PHARMACOL SCI
Number in series: 4
Volume number: 34
Issue number: 4
Start page: 206
End page: 214
Number of pages: 9
ISSN: 0165-6147
DOI: http://dx.doi.org/10.1016/j.tips.2013.02.001
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 mu-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.
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 mu-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.
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