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Pharmacological Basis of the Clinical Efficacy of Varenicline Used to Facilitate Smoking Cessation

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Modern problems caused by the high prevalence of smoking, as well as pharmacological approaches that facilitate quitting smoking are discussed in the review. Data on the mechanisms of formation of nicotine addiction, which determine the choice of drug interventions aimed at increasing the probability of quitting smoking are presented. The pharmacological characteristics of the most commonly used drugs used to facilitate smoking cessation are given. Special attention is paid to data on the mechanisms of action of varenicline and evidence of its clinical efficacy and safety, including in patients with concomitant cardiovascular diseases, as well as in patients with a history of acute coronary syndrome. Evidence on the effectiveness of the combined use of varenicline and nicotine replacement therapy are presented.

About the Author

S. R. Gilyarevskiy
Russian Medical Academy of Continuing Professional Education
Russian Federation

MD, PhD, Professor, Chair of Clinical Pharmacology and Therapy,

Barrikadnaya ul. 2/1, Moscow, 125993


1. Eriksen M., Mackay J., Schluger N. et al. The tobacco atlas.5th ed. Atlanta, GA: American Cancer Society; 2015.

2. Giovino G.A., Mirza S.A., Samet J.M. et al. GATS Collaborative Group. Tobacco use in 3 billion individuals from 16 countries: an analysis of nationally representative cross-sectional household surveys. Lancet. 2012;380:668-79. doi:10.1016/S0140-6736(12)61085-Xpmid:22901888.

3. Jha P., Peto R. Global effects of smoking, of quitting, and of taxing tobacco. N Engl J Med. 2014;370:60-8. doi:10.1056/NEJMra1308383.

4. Jha P. Avoidable global cancer deaths and total deaths from smoking. Nat Rev Cancer. 2009;9: 655-64.

5. WHO report on the global tobacco epidemic, 2013: enforcing bans on tobacco advertising, promotion and sponsorship. Geneva: World Health Organization; 2013.

6. Peto R., Lopez A.D. The future world-wide health effects of current smoking patterns. In: Koop E, Pearson CE, Schwarz MR, eds. Critical issues in global health. San Francisco: Jossey-Bass; 2001:154-61.

7. Hackshaw A., Morris J.K., Boniface S. et al. Low cigarette consumption and risk of coronary heart disease and stroke: meta-analysis of 141 cohort studies in 55 study reports. BMJ. 2018;360:j5855. doi:10.1136/bmj.j5855.

8. World Health Organization. Tobacco fact sheet [cited by Feb 01, 2019]. Available from:

9. World Health Organization. Cancer fact sheet [cited by Feb 01, 2019]. Available from:

10. US Department of Health and Human Services. The Health Consequences of Smoking: 50 Years of Progress: A Report of the Surgeon General. Atlanta, GA: US Department of Health and Human Services, Centers for Disease Control and Prevention, National Center for Chronic Disease Prevention and Health Promotion, Office of Smoking and Health; 2014.

11. Pirie K., Peto R., Reeves G.K. et al. The 21st century hazards of smoking and benefits of stopping: a pro - spective study of one million women in the UK. Lancet. 2013;381:133-41.

12. Jha P., Ramasundarahettige C., Landsman V. et al. 21st Century hazards of smoking and benefits of cessation in the United States. N Engl J Med. 2013;368:341-50.

13. Thun M.J., Carter B.D., Feskanich D. et al. 50-Year trends in smoking-related mortality in the United States. N Engl J Med. 2013;368:351-64.

14. Gottlieb S., Zeller M.A. Nicotine-Focused Framework for Public Health. N Engl J Med. 2017;377:1111-1114. doi:10.1056/NEJMp1707409.

15. NHS Digital. Health Survey for England. [cited by Feb 01, 2019]. Available from:

16. Jamal A., Homa D.M., O’Connor E. et al. Current cigarette smoking among adults - United States, 2005-2014. MMWR Morb Mortal Wkly Rep2015;64:1233-40. doi:10.15585/mmwr.mm6444a2pmid:26562061.

17. Myers R.L. The 100 Most Important Chemical Compounds: A Reference Guide. Westport, CT: Greenwood Press; 2007.

18. Benowitz N.L. Pharmacology of nicotine: addiction, smoking-induced disease, and therapeutics. Annu Rev Pharmacol Toxicol. 2009;49:57-71. doi:10.1146/annurev.pharmtox.48.113006. 094742.

19. Gotti C., Zoli M. Clementi F. Brain nicotinic acetylcholine receptors: native subtypes and their relevance. Trends Pharmacol Sci. 2006;27:482-91. doi:10.1016/

20. Picciotto M.R., Zoli M., Rimondini R. et al. Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine. Nature. 1998;391:173-7. doi:10.1038/34413.

21. Maskos U., Molles B.E., Pons S. et al. Nicotine reinforcement and cognition restored by targeted expression of nicotinic receptors. Nature. 2005;436:103-7. doi:10.1038/nature03694.

22. Aberger K., Chitravanshi V.C., Sapru H.N. Cardiovascular responses to microinjections of nicotine into the caudal ventrolateral medulla of the rat. Brain Res. 2001;892:138-46. doi:10.1016/S0006-8993(00)03250-9.

23. Brody A.L. Functional brain imaging of tobacco use and dependence. J Psychiatr Res. 2006;40:404- 18. doi:10.1016/j.jpsychires.2005.04.012.

24. Dani J.A., De Biasi M. Cellular mechanisms of nicotine addiction. Pharmacol Biochem Behav. 2001;70:439-46. doi:10.1016/S0091-3057(01)00652-9.

25. Nestler E.J. Is there a common molecular pathway for addiction? Nat Neurosci. 2005;8:1445-9. doi:10.1038/nn1578.

26. Jarvis M.J. Why people smoke. BMJ. 2004;328:277-9. doi:10.1136/bmj.328.7434.277.

27. Cryan J.F., Bruijnzeel A.W., Skjei K.L., Markou A. Bupropion enhances brain reward function and reverses the affective and somatic aspects of nicotine withdrawal in the rat. Psychopharmacology 2003;168:347-58. doi:10.1007/s00213-003-1445-7.

28. Epping-Jordan M.P., Watkins S.S., Koob G.F., Markou A. Dramatic decreases in brain reward function during nicotine withdrawal. Nature. 1998;393:76-9. doi:10.1038/30001.

29. Hughes J.R., Hatsukami D. Signs and symptoms of tobacco withdrawal. Arch Gen Psychiatry. 1986;43:289-294.

30. Koob G.F., LeMoal M. Drug abuse: Hedonic homeostatic dysregulation. Science. 1997;278:52-58. doi:10.1126/science.278.5335.52.

31. Rose J.E., Behm F.M., Levin E.D. Role of nicotine dose and sensory cues in the regulation of smoke intake. Pharmacol Biochem Behav. 1993;44:891-900. doi:10.1016/0091-3057(93)90021-K.

32. Rose J.E., Behm F.M., Westman E.C. Johnson M. Dissociating nicotine and nonnicotine components of cigarette smoking. Pharmacol Biochem Behav. 2000;67:71-81. doi:10.1016/S0091-3057(00)00301-4.

33. A Clinical Practice Guideline for Treating Tobacco Use and Dependence: 2008. A U.S. Public Health Service Report. Am J Prev Med. 2008;35:158-76. doi:10.1016/j.amepre.2008.04.009.

34. Hartmann-Boyce J., Chepkin S.C., Ye W. et al. Nicotine replacement therapy versus control for smoking cessation. Cochrane Database Syst Rev. 2018;5:CD000146. doi:10.1002/14651858. CD000146.pub5.

35. Henningfield J.E. Nicotine medications for smoking cessation. N Engl J Med. 1995;333:1196-7.

For citation:

Gilyarevskiy S.R. Pharmacological Basis of the Clinical Efficacy of Varenicline Used to Facilitate Smoking Cessation. Rational Pharmacotherapy in Cardiology. 2019;15(1):95-104. (In Russ.)

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