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Bupropion is generally well tolerated by smokers.



Bupropion is an atypical antidepressant which increases dopamine and noradrenaline and blocks nicotinic receptors (Hughes et al., 2007). It appears to be of equal efficacy to NRT. In smoking cessation studies, the most common adverse events were headache, dry mouth, nausea, and insomnia. The rates of premature discontinuation due to an adverse event for bupropion-treated patients typically ranged from 7-12% (compared to 5-10% for NRT) and were dose-related. Serious adverse events are very rare. 

Bupropion has sympathomimetic effects and in overdose is associated with tachycardia, hypertension and seizures. It is not associated with cardiac conduction abnormalities or orthostatic hypotension. Clinical trials of bupropion in smokers with cardiovascular disease, including hypertension, found efficacy for smoking cessation but no significant adverse cardiovascular side effects (Joseph & Fu, 2003; Tonstad et al., 2003; Rigotti et al., 2006). The combination of bupropion and nicotine replacement therapy may be associated with the emergence of hypertension in some smokers, so monitoring of blood pressure is recommended when initiating combination therapy (see also Key Finding #11).

The risk of seizures occurring with the use of bupropion is dose-dependent. At 300 mg/day (the dose used for smoking cessation) the risk is about 1:1000, is dose-dependent and is associated with predisposing risk factors of head injury, current alcoholism, eating disorders, a history of seizures and medications that lower the seizure threshold (e.g., antipsychotics, antidepressants and theophylline). Caution should be used in those clinical circumstances associated with an increased risk of seizures. These also include alcohol abuse, abrupt withdrawal from alcohol or benzodiazepines, diabetes treated with hypoglycemic or insulin, and use of stimulants or anorectic products. Because bupropion has stimulant-like effects in animals, theoretically it could make mania or psychoses worse; however, this has not been observed in clinical settings.

Some deaths have been associated with bupropion; however, a review by the EU regulatory agency concluded this association may not be causal (Hughes et al., 2007).  Regulatory agencies have added a warning statement to all antidepressants that they may increase suicidal ideation. Such a warning has been added to bupropion; however, no increase in suicide has been seen in studies or post-marketing when bupropion is used for smoking cessation.

Bupropion shares some characteristics of stimulant drugs, such as amphetamine. It can produce pleasant subjective effects and is self-administered in animals. Nevertheless, despite widespread use to treat depression, reports of dependence on bupropion are rare and it is not regulated as a controlled substance under the International Conventions that regulate drugs with significant abuse potential, by the European Medicines Agency or by national regulatory agencies such as the US Drug Enforcement Administration. Sustained-release bupropion (Zyban) has been judged by the United States Food & Drug Administration to have low abuse potential. This is likely, in part, because the slow-release formulation would be expected to produce milder subjective effects than an immediate-release formulation.

Several clinical trials, over nine years of surveillance data in an estimated 6 million patients, and five years of epidemiological data, have demonstrated the lack of abuse potential of bupropion. Early in development, the theoretical concern of abuse was directly tested in humans, since bupropion is structurally similar to diethylpropion and is related to phenylethylamines. However, clinical studies in healthy subjects and drug addicts suggest low abuse potential (Peck et al., 1979; Miller & Griffith, 1983; Margolin et al., 1995; Rush et al., 1998).



Hughes JR, Stead LF, Lancaster T. Antidepressants for smoking cessation. Cochrane Database of Systematic Reviews 2007; 1.

Joseph AM, Fu SS. Safety issues in pharmacotherapy for smoking in patients with cardiovascular disease. Prog Cardiovasc Dis. 2003; 45: 429-441.

Tonstad S, Farsang C, Klaene G, Lewis K, Manolis A, Perruchoud AP, Silagy C, van Spiegel PI, Astbury C, Hider A, Sweet R. Bupropion SR for smoking cessation in smokers with cardiovascular disease: a multicentre, randomised study. Eur Heart J. 2003; 24: 946-955.

Rigotti NA, Thorndike AN, Regan S, McKool K, Pasternak RC, Chang Y, Swartz S, Torres-Finnerty N, Emmons KM, Singer DE. Bupropion for smokers hospitalized with acute cardiovascular disease. Am J Med. 2006; 119(12): 1080-1087.

Wenger TL, Cohn JB, Bustrack J. Comparison of the effects of bupropion and amitriptyline on cardiac conduction in depressed patients. J Clin Psychiatry. 1983; 44: 174-175.

Wenger TL, Stern WC. The cardiovascular profile of bupropion. J Clin Psychiatry. 1983; 44: 176-182.

Kiev A, Masco HL, Wenger TL, Johnston JA, Batey SR, Holloman LC. The cardiovascular effects of bupropion and nortriptyline in depressed outpatients. Ann Clin Psychiatry. 1994; 6: 107-115.

Roose SP, Glassman AH, Giardina EG, Johnson LL, Walsh BT, Bigger JT Jr
. Cardiovascular effects of imipramine and bupropion in depressed patients with congestive heart failure. J Clin Psychopharmacol. 1987; 7: 247-251.

Peck AW, Bye CE, Clubley M, Henson T, Riddington C
. A comparison of bupropion hydrochloride with dexamphetamine and amitriptyline in healthy subjects. Br J Clin Pharmac. 1979; 7: 469-478.

Miller L, Griffith J. A comparison of bupropion, dextroamphetamine, and placebo in mixed-substance abusers. Psychopharmacology. 1983; 80: 199-205.

Margolin A, Kosten TR, Avants SK, Wilkins J, Ling W, Beckson M, Arndt IO, Cornish J, Ascher JA, Li SH, et al. A multicenter trial of bupropion for cocaine dependence in methadone-maintained patients. Drug Alcohol Depend. 1995; 40: 125-131.

Rush CR, Kollins SH, Pazzaglia PJ. Discriminative-stimulus and participant-rated effects of methylphenidate, bupropion, and triazolam in d-amphetamine-trained humans. Exp Clin Psychopharmacol. 1998; 6: 32-44.

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