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

Abstract

OBJECTIVES:

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.

METHODS:

Forty-two subjects were assigned to receive intravenous administration of oxycodone hydrochloride of 2.5, 5 or 10 mg. Plasma and urine samples were collected for up to 24 h after intravenous administration of oxycodone hydrochloride.

RESULTS:

Pharmacokinetic parameters showed that mean values of C(max), AUC(0-t) and AUC(0-∞) of oxycodone were dose dependent, whereas Tmax and t(1/2) were not. The mean AUC(0-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 24 h. 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.

CONCLUSION:

Our pharmacokinetics of oxycodone injection in Chinese patients with pain strongly support continued development of oxycodone as an effective analgesic drug in China.

• Authors: Guang-Tao Hao, Hai-Yan Zhou, Hong-Zhi Gao, Heng-Yan Qu, Yu-Guang Liang, Yuan-Yuan Li, Rui-Hua Dong, Li-Juan Zhang, Xiao-Fang Wang, Ze-Yuan Liu
• Journal: Pharmacological reports : PR (Pharmacol Rep) Vol. 66 Issue 1 Pg. 153-8 (Feb 2014) ISSN: 2299-5684 [Electronic] Switzerland
• PMID: 24905321 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

Chemical References

• Analgesics, Opioid
• Morphinans
• noroxycodone
• noroxymorphone
• Oxymorphone
• Oxycodone

Topics

• Adult
• Analgesics, Opioid (pharmacokinetics)
• Area Under Curve
• Female
• Humans
• Injections, Intravenous
• Male
• Middle Aged
• Morphinans (pharmacokinetics)
• Oxycodone (adverse effects, pharmacokinetics)
• Oxymorphone (pharmacokinetics)
• Pain (drug therapy)