ObjectiveTo systematically review the effectiveness and safety of bupropion for smoking cessation in smokers with cardiovascular disease. MethodsDatabases including The Cochrane Library, PubMed, EMbase, Web of Science, CBM, CNKI, WanFang Data and VIP databases were electronically searched from inception to February 23rd, 2013. Randomized controlled trials (RCTs) on bupropion versus placebo for smoking cessation in smokers with cardiovascular disease were included. Two reviewers independently screened literature according to the inclusion and exclusion criteria, extracted the data, and assessed the methodological quality of included studies. Meta-analysis was performed by using RevMan 5.1 software. ResultsIn total, 4 studies involving 1 415 patients were finally included. The results of metaanalyses indicated that, compared with placebo, bupropion significantly increased the point prevalence abstinence rate at 3 months (RR=1.79, 95%CI 1.14 to 2.83, P=0.01). However, the point prevalence abstinence rates at 6 months (RR=1.81, 95%CI 0.77 to 4.24, P=0.18) and 12 months (RR=1.46, 95%CI 0.94 to 2.27, P=0.10), and the continuous abstinence rates at 3 months (RR=1.48, 95%CI 0.89 to 2.47, P=0.13), 6 months (RR=1.41, 95%CI 0.79 to 2.51, P=0.25), and 12 months (RR=1.43, 95%CI 0.93 to 2.17, P=0.10) were similar in the two groups. The use of bupropion did not increase all-cause mortality (RR=1.13, 95%CI 0.49 to 2.56, P=0.78) and the incidence of cardiovascular events (RR=1.25, 95%CI 0.95 to 1.64, P=0.11). ConclusionBupropion is safe to use in smokers with cardiovascular disease. Although bupropion could increase the point prevalence abstinence rate at 3 months, it is not effective for long-term smoking cessation. Due to the limited quantity and quality of the included studies, more large-scale high-quality RCTs are required to verify the aforementioned conclusion.