Department of Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China.
Department of Pharmacy, Cancer Institute and Hospital, Chinese Academy of Medical Sciences, Beijing, China.
Pharmacol Rep. 2014 Feb;66(1):153-8. doi: 10.1016/j.pharep.2013.08.012. Epub 2014 Feb 1.
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 10 mg. Plasma and urine samples were collected for up to 24 h after intravenous administration of oxycodone hydrochloride.
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.
Our pharmacokinetics of oxycodone injection in Chinese patients with pain strongly support continued development of oxycodone as an effective analgesic drug in China.
本研究旨在评估羟考酮及其三种代谢物（去甲羟考酮、羟吗啡酮和去甲羟吗啡酮）在中国疼痛患者静脉给药后的药代动力学特征。
42 名受试者被分配接受盐酸羟考酮 2.5、5 或 10 mg 的静脉给药。在静脉给予盐酸羟考酮后，采集长达 24 小时的血浆和尿液样本。
药代动力学参数显示，羟考酮的 C(max)、AUC(0-t)和 AUC(0-∞)的平均值呈剂量依赖性，而 Tmax 和 t(1/2)则不是。去甲羟考酮与羟考酮的 AUC(0-t)比值在三个剂量范围内的平均值为 0.35 至 0.42，而去甲羟吗啡酮和羟吗啡酮与羟考酮的比值分别为 0.06-0.08 和 0.007-0.008。羟考酮及其三种代谢物从尿液中排泄。在 24 小时内，约有 10%的未改变的羟考酮被回收。报告的大多数不良事件（AE）为轻度至中度。常见的 AE 有头晕、恶心、呕吐、嗜睡和疲劳。未发现与剂量相关的 AE。
我们在中国疼痛患者中进行的羟考酮注射液的药代动力学研究强烈支持将羟考酮作为一种有效的镇痛药物在中国继续开发。
