Pharmacokinetics of oxycodone hydrochloride and three of its metabolites after intravenous administration in Chinese patients with pain

• Published in: Pharmacological reports Vol. 66; no. 1; pp. 153 - 158
• Main Authors: Hao, Guang-Tao, Zhou, Hai-Yan, Gao, Hong-Zhi, Qu, Heng-Yan, Liang, Yu-Guang, Li, Yuan-Yuan, Dong, Rui-Hua, Zhang, Li-Juan, Wang, Xiao-Fang, Liu, Ze-Yuan
• Format: Journal Article
• Language: English
• Published: Cham Elsevier Urban & Partner Sp. z o.o 01.02.2014; Springer International Publishing
• Subjects: Adult; Analgesics, Opioid - pharmacokinetics; Area Under Curve; Chinese patients with pain; Drug Safety and Pharmacovigilance; Female; Humans; Injections, Intravenous; Male; Metabolites; Middle Aged; Morphinans - pharmacokinetics; Original Research Article; Oxycodone; Oxycodone - adverse effects; Oxycodone - pharmacokinetics; Oxymorphone - pharmacokinetics; Pain - drug therapy; Pharmacokinetics; Pharmacotherapy; Pharmacy; Metabolites; Pharmacokinetics; Chinese patients with pain; Oxycodone
• ISSN: 1734-1140; 2299-5684
• DOI: 10.1016/j.pharep.2013.08.012

The aim of this study is to evaluate the pharmacokinetic profile of oxycodone and three of its metabolites, noroxycodone, oxymorphone and noroxymorphone after intravenous administration in Chinese patients with pain. Forty-two subjects were assigned to receive intravenous administration of oxycodone hydrochloride of 2.5, 5 or 10mg. Plasma and urine samples were collected for up to 24h after intravenous administration of oxycodone hydrochloride. Pharmacokinetic parameters showed that mean values of Cmax, AUC0–t and AUC0–∞ of oxycodone were dose dependent, whereas Tmax and t1/2 were not. The mean AUC0–t ratio of noroxycodone to oxycodone ranged from 0.35 to 0.42 over three doses, and those of noroxymorphone, or oxymorphone, to oxycodone were ranging of 0.06–0.08 and 0.007–0.008, respectively. Oxycodone and its three metabolites were excreted from urine. Approximately 10% of unchanged oxycodone was recovered in 24h. Most adverse events (AEs) reported were mild to moderate. The frequently occurred AEs were dizziness, nausea, vomiting, drowsiness and fatigue. No dose-related AEs were found. Our pharmacokinetics of oxycodone injection in Chinese patients with pain strongly support continued development of oxycodone as an effective analgesic drug in China.