OBJECTIVES:  Approximately 4.5 million Canadians, or 18.6% of the total population, smoke. Although the prevalence of smoking has shown a significantly decreasing trend, nicotine dependence remains a major public health issue. A number of pharmacological treatments are available to help smokers quit such as nicotine replacement therapies, bupropion and varenicline. The objective of this study was to evaluate the incremental cost-utility ratio of pharmacological anti-smoking treatments. METHODS:  A Markov model based on the Benesco Simulation model (the Benefits of Smoking Cessation on Outcomes) was developed to determine the costs and QALYs associated with the nicotine replacement therapies, bupropion and varenicline. This cost-utility analysis was performed over a lifetime horizon and from a health care system perspective. The model considers the health status of smokers, recent non-smokers and long-term non-smokers; the adverse health outcomes of smoking (asthma, chronic obstructive pulmonary disease [COPD], coronary heart disease, stroke and lung cancer); and deaths from all causes and from smoking. The model also considers smoking cessation probabilities associated with anti-smoking treatments, probabilities of resuming, probabilities of complications attributable to smoking, and probabilities of death. The costs considered are the costs of anti-smoking treatments according to recommended doses and amounts reimbursed by the Régie de l'assurance maladie du Québec. RESULTS:  Nicotine patches, with higher costs and less QALYs, are dominated by both bupropion and varenicline. Nicotine gum is also dominated by bupropion. Varenicline is the most effective of the anti-smoking treatments studied, albeit more costly than nicotine gum and bupropion. The incremental cost-utility ratios for varenicline versus nicotine gum and bupropion are respectively $825 and $1,235 per QALY. CONCLUSIONS:  Results show that varenicline is the most effective option of the currently available pharmacological anti-smoking treatments, with a very acceptable cost-utility ratio.