期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 34, 期 4, 页码 206-214出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2013.02.001
关键词
morphine; opiate; nociception; mu-opioid receptor
资金
- Mundipharma Finland Inc.
- Grunenthal Inc.
- MSD Inc.
- Janssen-Cilag Oy, MSD Inc.
- Mundipharma Inc.
- Orion Oy
- Pfizer Inc.
- Steripolar Oy
- Janssen-Cilag Oy
- Napp Laboratories Ltd
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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