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.

journal_name

Trends Pharmacol Sci

authors

Olkkola KT,Kontinen VK,Saari TI,Kalso EA

doi

10.1016/j.tips.2013.02.001

subject

Has Abstract

pub_date

2013-04-01 00:00:00

pages

206-14

issue

4

eissn

0165-6147

issn

1873-3735

pii

S0165-6147(13)00025-4

journal_volume

34

pub_type

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