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学科主题: 临床医学
题名:
The pharmacokinetic and tolerability profile of varenicline in healthy Chinese volunteers
作者: Xiao, Y.1; Lv, Y.1; Zhang, X.2; Guo, Y.2; Bergstrom, T.3
关键词: varenicline ; smoking cessation ; pharmacokinetics ; tolerability ; Chinese
刊名: INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS
发表日期: 2009-04-01
卷: 47, 期:4, 页:246-254
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: RECEPTOR PARTIAL AGONIST ; SMOKING-CESSATION ; DOSE PHARMACOKINETICS ; GLOBAL MORTALITY ; IN-VITRO ; SMOKERS ; NICOTINE ; SINGLE ; VIVO
英文摘要:

Objective: Varenicline is a selective, nicotinic alpha(4)beta(2) acetylcholine receptor partial agonist that has been licensed as a smoking cessation drug in more than 70 countries worldwide. The current study was conducted in order to evaluate its pharmacokinetic (PK) properties and tolerability in healthy volunteer Chinese smokers. Methods: This was an open-label, non-randomized study conducted over 17 days at a single center in China. Male and female subjects (18 45 years old) received a single, 1 mg dose of varenicline on days 1 and 10 as well as 1 mg varenicline twice daily (12-h dosing interval) on Days 4 - 9. Results: A total of 14 subjects (50% male) received varenicline as per study protocol for 8 days. The mean maximum plasma concentration of varenicline (C(max)) was 1.93-fold larger at steady state (reached on Day 8, after 4 days of repeat dosing) than following a single dose, showing accumulation of varenicline on repeat administration. Median values of t(max) (time of occurrence of C(max)) were similar for both dosing regimens (3.0 and 2.5 h following single and multiple dosing, respectively). The mean elimination half-life following single and multiple dosing was 15.2 and 18.3 h, respectively. There was no evidence of time- or concentration-dependence in the PK of varenicline upon repeat dosing as the ratio of the area under the plasma concentration vs time curve (AUC) from time 0 - 12 h at steady state to the AUC from time 0 - 8 on Day I was nearly 1. The 2-sided 95% confidence intervals for this comparison included 1, demonstrating the linearity of the PK of varenicline for the single and multiple doses. Varenicline was safe and well-tolerated, adverse events were mild in severity and there were no abnormal laboratory tests. Conclusions: Varenicline I mg twice daily was safe and well-tolerated in a cohort of healthy male and female, 18- to 45-year-old Chinese smokers and demonstrated PK properties that were stable and reproducible and similar to those observed previously in Western subjects.

语种: 英语
WOS记录号: WOS:000265163000004
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64347
Appears in Collections:北京大学第一临床医学院_临床药理研究所_期刊论文

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作者单位: 1.Pfizer Pharmaceut Ltd, Beijing, Peoples R China
2.Pfizer Inc, New York, NY USA
3.Peking Univ, Hosp 1, Inst Clin Pharmacol, Beijing 100083, Peoples R China

Recommended Citation:
Xiao, Y.,Lv, Y.,Zhang, X.,et al. The pharmacokinetic and tolerability profile of varenicline in healthy Chinese volunteers[J]. INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS,2009,47(4):246-254.
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