Rao J, Shankar P K
Department of Pharmacology, Melaka Manipal Medical College, Manipal, India.
Kathmandu Univ Med J (KUMJ). 2009 Apr-Jun;7(26):162-4. doi: 10.3126/kumj.v7i2.2714.
Varenicline, a partial agonist of alpha4beta2 nicotinic acetylcholine receptor (nAChR), is the most recently approved drug for smoking cessation. Despite the availability of effective treatments for smoking cessation, such as nicotine replacement therapy and Bupropion sustained-release, abstinence rates remain less than optimal. As a nAChR partial agonist, Varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Clinical trials have demonstrated superior efficacy of this drug over Bupropion-SR for achieving abstinence from smoking, and Varenicline has also been shown to significantly delay smoking relapse. As the latest agent approved for smoking cessation, the mechanism of action, efficacy, and safety of Varenicline has been reviewed in this paper.
伐尼克兰是α4β2烟碱型乙酰胆碱受体（nAChR）的部分激动剂，是最近获批用于戒烟的药物。尽管有有效的戒烟治疗方法，如尼古丁替代疗法和安非他酮缓释剂，但戒烟率仍不尽人意。作为一种nAChR部分激动剂，伐尼克兰可减轻戒烟时出现的渴望和戒断症状，还可降低复吸患者从吸烟中获得的尼古丁的奖赏效应。临床试验已证明，该药物在实现戒烟方面比安非他酮缓释剂具有更高的疗效，并且伐尼克兰还被证明可显著延迟吸烟复发。作为最新获批用于戒烟的药物，本文对伐尼克兰的作用机制、疗效和安全性进行了综述。
