PHARMACOKINETIC-PHARMACODYNAMIC RELATIONSHIPS OF CONTROLLED-RELEASE OXYCODONE

Plasma concentrations of oxycodone, oxymorphone, and noroxycodone were determined after administration of 20 mg oral controlled-release oxyc odone tablets to four subject groups: young (aged 21 to 45 years) men, elderly (aged 65 to 79 years) men, young women, and elderly women. Ar ea under the oxycodone and noroxycodone concentration-time curve (AUG) values were comparable among the four groups. Compared with oxycodone , the oxymorphone AUC values were small, with significant differences between subject groups, AUC values were also calculated for the pharma codynamic variable ''drug effect,'' scored on a 100 mm visual analog s cale. The two groups with the highest oxycodone AUC values (young and elderly women) had the lowest oxymorphone AUC values and the greatest drug effect AUC values. The two groups with the lowest oxycodone AUC v alues (young and elderly men) had the highest oxymorphone AUC values a nd the lowest drug effect AUC values. These results support oxycodone, and not oxymorphone, as bring primarily responsible for pharmacodynam ic and analgesic effects.