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伐尼克兰:作为戒烟治疗辅助药物的应用综述

Varenicline: a review of its use as an aid to smoking cessation therapy.

作者信息

Keating Gillian M, Siddiqui M Asif A

机构信息

Wolters Kluwer Health, Adis, Auckland, New Zealand.

出版信息

CNS Drugs. 2006;20(11):945-60. doi: 10.2165/00023210-200620110-00007.

DOI:10.2165/00023210-200620110-00007
PMID:17044731
Abstract

Varenicline is an orally administered alpha4beta2 nicotinic acetylcholine (ACh) receptor partial agonist. It has been approved by the US FDA (Chantix) and the European Commission (Champix) for use as an aid to smoking cessation therapy. Varenicline is an effective and generally well tolerated treatment for use in smokers who want to quit. In two well designed, phase III trials, 12 weeks' treatment with varenicline was associated with significantly higher continuous abstinence rates at weeks 9-12 than placebo or bupropion sustained-release (SR). In the longer term, continuous abstinence rates for weeks 9 through 52 demonstrated that the odds of remaining abstinent were 2.7 to 3.1 times higher with 12 weeks of varenicline treatment than with placebo; the significant difference between varenicline and bupropion SR was also maintained in the longer term in one trial. Moreover, varenicline appeared to attenuate the urge to smoke, negative affect withdrawal symptoms and the reinforcing effects of smoking. Among those achieving abstinence, an additional 12 weeks of varenicline therapy helped increase the likelihood of long-term abstinence. Thus, varenicline is a valuable new agent for use as an aid to smoking cessation treatment.

摘要

伐尼克兰是一种口服的α4β2烟碱型乙酰胆碱(ACh)受体部分激动剂。它已获美国食品药品监督管理局(商品名畅沛)和欧盟委员会(商品名 Champix)批准,用作戒烟治疗的辅助药物。伐尼克兰对于想要戒烟的吸烟者来说是一种有效的、耐受性普遍良好的治疗方法。在两项精心设计的 III 期试验中,与安慰剂或安非他酮缓释片相比,接受 12 周伐尼克兰治疗的患者在第 9 - 12 周的持续戒烟率显著更高。从长期来看,第 9 周至第 52 周的持续戒烟率表明,接受 12 周伐尼克兰治疗的患者保持戒烟状态的几率比接受安慰剂治疗的患者高 2.7 至 3.1 倍;在一项试验中,伐尼克兰与安非他酮缓释片之间的显著差异在长期内也得以维持。此外,伐尼克兰似乎能减轻吸烟欲望、负面情绪戒断症状以及吸烟的强化作用。在成功戒烟的人群中,额外接受 12 周伐尼克兰治疗有助于提高长期戒烟的可能性。因此,伐尼克兰是一种用于辅助戒烟治疗的有价值的新型药物。

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本文引用的文献

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Single-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healthy smokers and nonsmokers.伐尼克兰(一种选择性烟碱受体部分激动剂)在健康吸烟者和非吸烟者中的单剂量药代动力学。
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Efficacy and safety of the novel selective nicotinic acetylcholine receptor partial agonist, varenicline, for smoking cessation.新型选择性烟碱型乙酰胆碱受体部分激动剂伐尼克兰用于戒烟的疗效和安全性。
Arch Intern Med. 2006;166(15):1571-7. doi: 10.1001/archinte.166.15.1571.
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Smoking cessation with varenicline, a selective alpha4beta2 nicotinic receptor partial agonist: results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up.
量化药物与自杀行为之间关系的策略:有哪些经验教训?
Drug Saf. 2011 May 1;34(5):375-95. doi: 10.2165/11589350-000000000-00000.
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Varenicline: a pharmacoeconomic review of its use as an aid to smoking cessation.伐仑克林:作为戒烟辅助药物的药物经济学评价。
Pharmacoeconomics. 2010;28(3):231-54. doi: 10.2165/11204380-000000000-00000.
5
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-(substituted phenyl)epibatidine analogues. Nicotinic partial agonists.3'-(取代苯基)埃巴替啶类似物的合成、烟碱型乙酰胆碱受体结合和抗伤害感受特性。烟碱部分激动剂。
J Nat Prod. 2010 Mar 26;73(3):306-12. doi: 10.1021/np9006124.
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Drug Alcohol Depend. 2008 Dec 1;98(3):169-78. doi: 10.1016/j.drugalcdep.2008.06.003. Epub 2008 Aug 3.
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JAMA. 2006 Jul 5;296(1):56-63. doi: 10.1001/jama.296.1.56.
7
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JAMA. 2006 Jul 5;296(1):47-55. doi: 10.1001/jama.296.1.47.
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Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.伐尼克兰是α4β2的部分激动剂和α7神经元烟碱受体的完全激动剂。
Mol Pharmacol. 2006 Sep;70(3):801-5. doi: 10.1124/mol.106.025130. Epub 2006 Jun 9.
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The neurobiological basis for partial agonist treatment of nicotine dependence: varenicline.尼古丁依赖部分激动剂治疗的神经生物学基础:伐尼克兰
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