PMID- 24905321 OWN - NLM STAT- MEDLINE DCOM- 20150205 LR - 20220408 IS - 2299-5684 (Electronic) IS - 1734-1140 (Linking) VI - 66 IP - 1 DP - 2014 Feb TI - Pharmacokinetics of oxycodone hydrochloride and three of its metabolites after intravenous administration in Chinese patients with pain. PG - 153-8 LID - S1734-1140(14)00024-3 [pii] LID - 10.1016/j.pharep.2013.08.012 [doi] AB - 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-infinity) 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. CI - Copyright (c) 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved. FAU - Hao, Guang-Tao AU - Hao GT AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Zhou, Hai-Yan AU - Zhou HY AD - Department of Pharmacy, Cancer Institute and Hospital, Chinese Academy of Medical Sciences, Beijing, China. FAU - Gao, Hong-Zhi AU - Gao HZ AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Qu, Heng-Yan AU - Qu HY AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Liang, Yu-Guang AU - Liang YG AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Li, Yuan-Yuan AU - Li YY AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Dong, Rui-Hua AU - Dong RH AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Zhang, Li-Juan AU - Zhang LJ AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Wang, Xiao-Fang AU - Wang XF AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. FAU - Liu, Ze-Yuan AU - Liu ZY AD - Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. Electronic address: YLS307@126.com. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20140201 PL - Switzerland TA - Pharmacol Rep JT - Pharmacological reports : PR JID - 101234999 RN - 0 (Analgesics, Opioid) RN - 0 (Morphinans) RN - 95Q949779D (noroxycodone) RN - 9NZ7111A9O (noroxymorphone) RN - 9VXA968E0C (Oxymorphone) RN - CD35PMG570 (Oxycodone) SB - IM MH - Adult MH - Analgesics, Opioid/*pharmacokinetics MH - Area Under Curve MH - Female MH - Humans MH - Injections, Intravenous MH - Male MH - Middle Aged MH - Morphinans/pharmacokinetics MH - Oxycodone/adverse effects/*pharmacokinetics MH - Oxymorphone/pharmacokinetics MH - Pain/*drug therapy OTO - NOTNLM OT - Chinese patients with pain OT - Metabolites OT - Oxycodone OT - Pharmacokinetics EDAT- 2014/06/07 06:00 MHDA- 2015/02/06 06:00 CRDT- 2014/06/07 06:00 PHST- 2012/10/23 00:00 [received] PHST- 2013/07/29 00:00 [revised] PHST- 2013/08/13 00:00 [accepted] PHST- 2014/06/07 06:00 [entrez] PHST- 2014/06/07 06:00 [pubmed] PHST- 2015/02/06 06:00 [medline] AID - S1734-1140(14)00024-3 [pii] AID - 10.1016/j.pharep.2013.08.012 [doi] PST - ppublish SO - Pharmacol Rep. 2014 Feb;66(1):153-8. doi: 10.1016/j.pharep.2013.08.012. Epub 2014 Feb 1.