Loma Linda University, Loma Linda, CA 92354, USA.
Expert Rev Respir Med. 2010 Jun;4(3):291-9. doi: 10.1586/ers.10.27.
Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, is the newest drug in the armamentarium of tobacco-addiction treatment. Improved smoking quit rates with varenicline are seen in comparison with other pharmacotherapies or behavioral treatments alone. Efficacy, tolerability and safety have been demonstrated in healthy smokers and in smokers with cardiovascular or pulmonary comorbidity, as well as in smokeless tobacco users. Varenicline is started 1 week before a target quit date, uptitrated to 1 mg twice daily, and continued for 12-24 weeks. Post-marketing reports have led to labeling changes to monitor patients for change in behavior, hostility, agitation, depressed mood and suicide-related events. Varenicline's pharmacological profile does not clearly explain an association with these adverse events. A review of placebo-controlled studies found that varenicline was not associated with self-reported neuropsychiatric symptoms, with the exception of sleep disorders. Data in smokers with psychiatric problems are limited.
伐伦克林，一种α4β2 烟碱型乙酰胆碱受体部分激动剂，是烟草依赖治疗手段中的最新药物。与其他药物治疗或行为治疗单独相比，伐伦克林可提高戒烟率。在健康吸烟者、有心血管或肺部合并症的吸烟者以及使用无烟烟草的人群中，已证实其具有疗效、耐受性和安全性。伐伦克林在目标戒烟日期前 1 周开始服用，逐渐增至每日 2 次 1 毫克，并持续 12-24 周。上市后报告导致标签变更，以监测患者的行为、敌意、激越、抑郁情绪和与自杀相关事件的变化。伐伦克林的药理学特征并不能清楚地解释与这些不良事件的关联。对安慰剂对照研究的回顾发现，伐伦克林与自我报告的神经精神症状无关，除了睡眠障碍。在有精神问题的吸烟者中的数据有限。
