|Values are valid only on day of printing.|
Oxycodone hydrochloride is an opioid analgesic with several actions qualitatively similar to those of morphine. The clearance half-life of oxycodone is approximately 3 to 6 hours.(1)
Although its own strong analgesic activity precludes oxycodone from being considered a prodrug, it is also converted to a highly active metabolite, oxymorphone, through the activity of the cytochrome P450 enzyme CYP2D6.(2) This conversion appears to be less of a concern for CYP2D6 poor metabolizers, since oxycodone itself still provides analgesia, than for ultra-rapid metabolizers who could be at increased risk for adverse effects.(3)
Monitoring oxycodone therapy
Routine drug monitoring is not indicated in all patients. Because drug diversion (use of prescription drugs for recreational purposes) is a possibility, compliance monitoring is indicated in patients being treated for chronic pain requiring high doses (>40 mg twice a day)
The minimal effective peak serum concentration of oxycodone for analgesia is 10 ng/mL from a dose of 5 to 10 mg of regular release oxycodone (Percodan).(1,4) Patients develop tolerance to oxycodone and may require larger doses for effective management of chronic pain.
Monitor patients carefully if drugs inhibiting CYP2D6 are coadministered.
1. Baselt RC: Oxycodone. In Dispositition of Toxic Drugs and Chemical in Man. Eighth edition. Edited by RC Baselt. Foster City, CA, Biomedical Publications, 2008, pp1166-1168
2. Riley J, Eisenberg E, Muller-Schwefe G, et al: Oxycodone: a review of its use in the management of pain. Curr Med Res Opin 2008;24:175-192
3. de Leon J, Dinsmore L, Wedlund P: Adverse drug reactions to oxycodone and hydrocodone in CYP2D6 ultrarapid metabolizers. J Clin Psychopharmacol 2003;23:420-421
4. Gutstein HB, Akil H: Chapter 21: Opioid analgesics. In Goodman and Gilman's The Pharmacological Basis of Therapeutics. 11th edition. Edited by LL Brunton, JS Lazo, KL Parker. New York, McGraw-Hill Inc, 2006. Available at: http://www.accessmedicine.com/content.aspx?aID=940653