Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites

• Published in: Clinical pharmacology and therapeutics Vol. 79; no. 5; p. 461
• Main Authors: Lalovic, Bojan, Kharasch, Evan, Hoffer, Christine, Risler, Linda, Liu-Chen, Lee-Yuan, Shen, Danny D
• Format: Journal Article
• Language: English
• Published: United States 01.05.2006
• Subjects: Administration, Oral; Adult; Analgesics, Opioid - administration & dosage; Analgesics, Opioid - pharmacokinetics; Analgesics, Opioid - pharmacology; Animals; Brain - metabolism; CHO Cells; Cricetinae; Cricetulus; Female; Half-Life; Humans; Male; Oxidation-Reduction; Oxycodone - administration & dosage; Oxycodone - pharmacokinetics; Oxycodone - pharmacology; Pilot Projects; Pupil - drug effects; Radioligand Assay; Rats; Receptors, Opioid - metabolism; Tissue Distribution

In vitro experiments suggest that circulating metabolites of oxycodone are opioid receptor agonists. Clinical and animal studies to date have failed to demonstrate a significant contribution of the O-demethylated metabolite oxymorphone toward the clinical effects of the parent drug, but the role of...