title: Pharmacokinetics of oxycodone hydrochloride and three of its metabolites after intravenous administration in Chinese patients with pain.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  Our pharmacokinetics of oxycodone injection in Chinese patients with pain strongly support continued development of oxycodone as an effective analgesic drug in China.
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Guang-Tao
authors.initials: GT
authors.lastname: Hao
authors.affiliation: Department of Pharmacy, Cancer Institute and Hospital, Chinese Academy of Medical Sciences, Beijing, China.
authors.forename: Hai-Yan
authors.initials: HY
authors.lastname: Zhou
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Hong-Zhi
authors.initials: HZ
authors.lastname: Gao
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Heng-Yan
authors.initials: HY
authors.lastname: Qu
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Yu-Guang
authors.initials: YG
authors.lastname: Liang
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Yuan-Yuan
authors.initials: YY
authors.lastname: Li
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Rui-Hua
authors.initials: RH
authors.lastname: Dong
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Li-Juan
authors.initials: LJ
authors.lastname: Zhang
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
authors.forename: Xiao-Fang
authors.initials: XF
authors.lastname: Wang
authors.affiliation: Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China. Electronic address: YLS307@126.com.
authors.forename: Ze-Yuan
authors.initials: ZY
authors.lastname: Liu
mesh_terms: D000328:Adult; D000701:Analgesics, Opioid / Q000493:pharmacokinetics*; D019540:Area Under Curve; D005260:Female; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D009019:Morphinans / Q000493:pharmacokinetics; D010098:Oxycodone / Q000009:adverse effects / Q000493:pharmacokinetics*; D010111:Oxymorphone / Q000493:pharmacokinetics; D010146:Pain / Q000188:drug therapy*
chemical_list: D000701:Analgesics, Opioid; D009019:Morphinans; C077256:noroxycodone; C526569:noroxymorphone; D010111:Oxymorphone; D010098:Oxycodone
keywords: Chinese patients with pain; Metabolites; Oxycodone; Pharmacokinetics