The American Journal of Medicine
Volume 121, Issue 4, Supplement , Pages S32-S42 , April 2008

Efficacy and Safety of Varenicline for Smoking Cessation

  • J. Taylor Hays, MD

      Affiliations

    • Corresponding Author InformationRequests for reprints should be addressed to J. Taylor Hays, MD, Nicotine Dependence Center, Mayo Clinic, 200 First Street SW, Rochester, Minnesota 55905.
  • ,
  • Jon O. Ebbert, MD
  • ,
  • Amit Sood, MD

References 

  1. Thun MJ, Luiza da Costa e Silva V. Introduction and overview of global tobacco surveillance. In:  Shafey O,  Dolwick S,  Guindon GE editor. Tobacco Control Country Profiles. 2nd ed. Atlanta, GA: American Cancer Society; 2003;p. 7–12
  2. Peto R, Lopez AD, Boreham J, Thun M, Heath C. Mortality from smoking in developed countries 1950–2000. In: Indirect Estimates from National Vital Statistics. New York: Oxford University Press; 1994;
  3. Cigarette smoking among adults–United States, 2000. MMWR Morb Mortal Wkly Rep. 2001;52:953–956
  4. Annual smoking-attributable mortality, years of potential life lost, and economic costs–United States, 1995–1999. MMWR Morb Mortal Wkly Rep. 2002;51:300–303
  5. Mokdad AH, Marks JS, Stroup DF, Gerberding JL. Actual causes of death in the United States, 2000. JAMA. 2004;291:1238–1245
  6. The Health Benefits of Smoking Cessation: US Dept of Health and Human Services, Public Health Service, Centers for Disease Control, Center for Chronic Disease Prevention and Health Promotion, Office of Smoking and Health, 1990.
  7. Doll R, Peto R, Boreham J, Sutherland I. Mortality in relation to smoking: 50 years’ observations on male British doctors. BMJ. 2004;328:1519;e-pub
  8. Benowitz NL. Neurobiology of nicotine addiction: implications for smoking cessation treatment. Am J Med. 2008; 121(4A):S3–S10.
  9. Corringer PJ, Le Novere N, Changeux JP. Nicotinic receptors at the amino acid level. Annu Rev Pharmacol Toxicol. 2000;40:431–458
  10. Wonnacott S, Sidhpura N, Balfour DJ. Nicotine: from molecular mechanisms to behaviour. Curr Opin Pharmacol. 2005;5:53–59
  11. Léna C, Changeux JP. The role of β2-subunit-containing nicotinic acetylcholine receptors in the brain explored with a mutant mouse. Ann N Y Acad Sci. 1999;868:611–616
  12. Tapper AR, McKinney SL, Nashmi R, et al. Nicotine activation of α4* receptors: sufficient for reward, tolerance, and sensitization. Science. 2004;306:1029–1032
  13. Picciotto MR, Corrigall WA. Neuronal systems underlying behaviors related to nicotine addiction: neural circuits and molecular genetics. J Neurosci. 2002;22:3338–3341
  14. Koob GF. Neural mechanisms of drug reinforcement. Ann N Y Acad Sci. 1992;654:171–191
  15. Tzschentke TM. Pharmacology and behavioral pharmacology of the mesocortical dopamine system. Prog Neurobiol. 2001;63:241–320
  16. Maskos U, Molles BE, Pons S, et al. Nicotine reinforcement and cognition restored by targeted expression of nicotinic receptors. Nature. 2005;436:103–107
  17. Papke RL, Heinemann SF. Partial agonist properties of cytisine on neuronal nicotinic receptors containing the β2 subunit. Mol Pharmacol. 1994;45:142–149
  18. Slater YE, Houlihan LM, Maskell PD, et al. Halogenated cytisine derivatives as agonists at human neuronal nicotinic acetylcholine receptor subtypes. Neuropharmacology. 2003;44:503–515
  19. Etter JF. Cytisine for smoking cessation: a literature review and a meta-analysis. Arch Intern Med. 2006;166:1553–1559
  20. Coe JW, Brooks PR, Vetelino MG, et al. Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005;48:3474–3477
  21. Rollema H, Chambers LK, Coe JW, et al. Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology. 2007;52:985–994
  22. Nides M, Oncken C, Gonzales D, et al. Smoking cessation with varenicline, a selective α4β2 nicotinic receptor partial agonist: results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up. Arch Intern Med. 2006;166:1561–1568
  23. Oncken C, Gonzales D, Nides M, et al. Efficacy and safety of the novel selective nicotinic acetylcholine receptor partial agonist, varenicline, for smoking cessation. Arch Intern Med. 2006;166:1571–1577
  24. Gonzales D, Rennard SI, Nides M, et al. Varenicline Phase 3 Study Group Varenicline, an α4β2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trial. JAMA. 2006;296:47–55
  25. Jorenby DE, Hays JT, Rigotti NA, et al. Varenicline Phase 3 Study Group Efficacy of varenicline, an α4β2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006;296:56–63
  26. Tonstad S, Tonnesen P, Hajek P, Williams KE, Billing CB, Reeves KR. Effect of maintenance therapy with varenicline on smoking cessation: a randomized controlled trial. JAMA. 2006;296:64–71
  27. Hajek P, Stead LF, West R, Jarvis M. Relapse prevention interventions for smoking cessation. Cochrane Database Syst Rev. 2005;(1):CD003999
  28. Hays JT, Hurt RD, Rigotti NA, et al. Sustained-release bupropion for pharmacologic relapse prevention after smoking cessation: a randomized, controlled trial. Ann Intern Med. 2001;135:423–433
  29. Killen JD, Fortmann SP, Murphy GM, et al. Extended treatment with bupropion SR for cigarette smoking cessation. J Consult Clin Psychol. 2006;74:286–294
  30. Sprecht M. New stop-smoking drug shows promise, but so did others (Health and Behavior [USA Today Web site]). http://www.usatoday.com/news/health/2006-07-31-stop-smoking-drug_x.htmAccessed October 24, 2007
  31. Stapleton J. Is varenicline cost-effective enough to be funded by the NHS now? (Action on Smoking and Health Web site). http://newash.org.uk/files/documents/ASH_446/ASH=446.htmlAccessed January 21, 2008
  32. Food and Drug Administration. Information for Healthcare Professions: Varenicline (marketed as Chantix). http://www.fda.gov/cder/drug/infosheets/hcp/vareniclinehcp.htmAccessed February 15, 2008

 Statement of conflict of interest: Please see Author Disclosures section at the end of this article.

PII: S0002-9343(08)00106-X

doi: 10.1016/j.amjmed.2008.01.017

The American Journal of Medicine
Volume 121, Issue 4, Supplement , Pages S32-S42 , April 2008