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

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 cmax,auc0-t and auc0-1 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 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. © 2014 institute of pharmacology,polish academy of sciences. published by elsevier urban & partner sp. z o.o. all rights reserved.