Sustained-release bupropion as a pharmacological aid to smoking cessation

Tobacco use, primarily from cigarette smoking, is the most common cause of preventable morbidity and mortality in the United States. The expected morbidity and mortality from smoking-attributable diseases will not decline substantially without effective nicotine dependence treatment. Treatment for nicotine dependence requires the combination of behavioral and pharmacological treatment, including nicotine replacement therapy and non-nicotine medications. The non-nicotine medication with the best evidence for efficacy in the treatment of nicotine dependence is bupropion. Bupropion in the sustained-release form (bupropion SR; Wellbutrin SR™ and Zyban™) is the only non-nicotine medication approved for the treatment of tobacco dependence. The efficacy of bupropion SR for the treatment of nicotine dependence is presumed to be due to the blockade of dopamine reuptake in the mesolimbic dopamine system. Randomized, controlled clinical trials in general populations have shown that bupropion SR approximately doubles abstinence rates compared with placebo. In addition, long-term treatment with bupropion SR may reduce or delay smoking relapse. Bupropion SR is also effective for the treatment of special populations of smokers, including those who have recently relapsed, those with comorbid psychiatric conditions, African-Americans, women, and those with medical comorbidity, such as chronic obstructive lung disease and cardiovascular disease. Bupropion SR has a favorable side-effect profile, but the risk exists for serious drug adverse effects such as seizures. Postmarketing surveillance reports have raised safety concerns, although clinical trial evidence and large effectiveness studies have indicated no important issues with the safety of bupropion SR. In this chapter, evidence for the efficacy and safety of bupropion SR in the treatment of tobacco dependence are reviewed. Recommendations for the appropriate clinical use of bupropion SR are summarized.