Summary: A benzazepine derivative that functions as an ALPHA4/BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.

Top Publications

  1. Hays J, Ebbert J. Varenicline for tobacco dependence. N Engl J Med. 2008;359:2018-24 pubmed publisher
  2. Gibbons R, Mann J. Varenicline, smoking cessation, and neuropsychiatric adverse events. Am J Psychiatry. 2013;170:1460-7 pubmed publisher
    In 2009, the U.S. Food and Drug Administration issued a black box warning for varenicline regarding neuropsychiatric events...
  3. Fiore M, Baker T. Clinical practice. Treating smokers in the health care setting. N Engl J Med. 2011;365:1222-31 pubmed publisher
  4. Fatemi S, Yousefi M, Kneeland R, Liesch S, Folsom T, Thuras P. Antismoking and potential antipsychotic effects of varenicline in subjects with schizophrenia or schizoaffective disorder: a double-blind placebo and bupropion-controlled study. Schizophr Res. 2013;146:376-8 pubmed publisher
  5. Harrison Woolrych M. Mental health effects of varenicline. BMJ. 2015;350:h1168 pubmed publisher
  6. Davies N, Taylor G, Taylor A, Martin R, Munafo M, Thomas K. Cardiovascular and neuropsychiatric risks of varenicline: too good to be true?. Lancet Respir Med. 2015;3:e39-40 pubmed publisher
  7. Kotz D, Viechtbauer W, Simpson C, van Schayck O, West R, Sheikh A. Cardiovascular and neuropsychiatric risks of varenicline and bupropion in smokers with chronic obstructive pulmonary disease. Thorax. 2017;72:905-911 pubmed publisher
    b>Varenicline and bupropion are effective smoking cessation treatments, but there are concerns about their safety in smokers with COPD...
  8. Frye M, Ebbert J, Prince C, Lineberry T, Geske J, Patten C. A feasibility study of varenicline for smoking cessation in bipolar patients with subsyndromal depression. J Clin Psychopharmacol. 2013;33:821-3 pubmed publisher
  9. Anthenelli R, Morris C, Ramey T, Dubrava S, Tsilkos K, Russ C, et al. Effects of varenicline on smoking cessation in adults with stably treated current or past major depression: a randomized trial. Ann Intern Med. 2013;159:390-400 pubmed publisher
    ..To evaluate smoking abstinence and changes in mood and anxiety levels in smokers with depression treated with varenicline versus placebo. Phase 4, multicenter, parallel, 1:1 allocation, double-blind, randomization trial...

More Information


  1. Siu A. Behavioral and Pharmacotherapy Interventions for Tobacco Smoking Cessation in Adults, Including Pregnant Women: U.S. Preventive Services Task Force Recommendation Statement. Ann Intern Med. 2015;163:622-34 pubmed publisher
    ..The USPSTF recommends that clinicians direct patients who smoke tobacco to other cessation interventions with established effectiveness and safety (previously stated). (I statement). ..
  2. Koga M, Kanaoka Y, Sugiyama K, Ohishi K, Ejima Y, Hisanaga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated ?7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017;390:1-9 pubmed publisher
    b>Varenicline is a widely used and effective drug for smoking cessation. Despite its efficacy, varenicline increases the risk of cardiovascular disease...
  3. Shen Z, Huang P, Wang C, Qian W, Yang Y, Zhang M. Increased network centrality as markers of relapse risk in nicotine-dependent individuals treated with varenicline. Prog Neuropsychopharmacol Biol Psychiatry. 2017;75:142-147 pubmed publisher
    ..After 12-week treatment with varenicline, smokers were divided into relapsers (n=36) and quitters (n=21) (quitter: continuously abstinent for weeks 9-12)..
  4. Tervonen H, Turunen J, Baker C, Laine J, Linden K. Characteristics of first-time varenicline users - A cross-sectional study in Finnish quitters. BMC Public Health. 2017;17:331 pubmed publisher
    b>Varenicline is an efficacious medicine for smoking cessation (SC) but little is known about the characteristics of varenicline users...
  5. Zhou C, Wu L, Liu Q, An H, Jiang B, Zuo F, et al. Evaluation of smoking cessation intervention in patients with chronic diseases in smoking cessation clinics. Medicine (Baltimore). 2017;96:e7459 pubmed publisher mental intervention, patients in psychological plus drug group also received bupropion hydrochloride or varenicline tartrate to quit smoking...
  6. Dehghani P, Habib B, Windle S, Roy N, Old W, Grondin F, et al. Smokers and Postcessation Weight Gain After Acute Coronary Syndrome. J Am Heart Assoc. 2017;6: pubmed publisher
    ..Data were prospectively collected from the EVITA (Evaluation of Varenicline in Smoking Cessation for Patients Post-Acute Coronary Syndrome) trial...
  7. Lesage E, Aronson S, Sutherland M, Ross T, Salmeron B, Stein E. Neural Signatures of Cognitive Flexibility and Reward Sensitivity Following Nicotinic Receptor Stimulation in Dependent Smokers: A Randomized Trial. JAMA Psychiatry. 2017;74:632-640 pubmed publisher
    ..decision making is affected by abstinence and by pharmacotherapies such as nicotine replacement therapy and varenicline tartrate may aid cessation treatment...
  8. Reid R, Pritchard G, Walker K, Aitken D, Mullen K, Pipe A. Managing smoking cessation. CMAJ. 2016;188:E484-E492 pubmed
  9. Weiner E, Buchholz A, Coffay A, Liu F, McMahon R, Buchanan R, et al. Varenicline for smoking cessation in people with schizophrenia: a double blind randomized pilot study. Schizophr Res. 2011;129:94-5 pubmed publisher