Keating Gillian M, Siddiqui M Asif A
Wolters Kluwer Health, Adis, Auckland, New Zealand.
CNS Drugs. 2006;20(11):945-60. doi: 10.2165/00023210-200620110-00007.
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.
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。