摘要
瓦伦尼克林(varenicline)是一种α_4β_2烟碱乙酰胆碱受体选择性部分激动剂,对α_4β_2神经元烟碱乙酰胆碱受体具有高度亲和力,能够选择性与之结合,阻断烟碱激活α_4β_2受体的作用,从而阻断了反复吸烟后成瘾的中枢性机制,临床用于戒烟的治疗。现综述其作用机制、药动学、临床研究、药物相互作用及不良反应。
Varenicline is a partial agonist selective for α4β2 nicotinic acetylcholine receptor subtypes. Varenicline binds with high affinity and selectivity at α4β2 nicotinic acetylcholine receptors. Varenicline blocks the ability of nicotine to activate 0t462 receptors and thus blocks the nervous transmission underlying reinforcement and reward experienced upon smoking. Varenicline is used for smoking cessation. This paper introduces mechanism of action, pharmacokinetics, clinical study, drug-drug interactions and adverse effects of varenicline.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2008年第1期83-85,共3页
Chinese Journal of New Drugs
关键词
瓦伦尼克林
戒烟
烟碱乙酰胆碱受体激动剂
作用机制
临床研究
varenicline
smoking cessation
nicotinic acetylcholine receptors agonist
mechanism of action
clinical study
