, Volume 62, Supplement 2, pp 45–52 | Cite as

Tolerability and Safety of Sustained-Release Bupropion in the Management of Smoking Cessation

Review Article


Sustained-release bupropion (bupropion SR) was first launched in the US in 1997 as an aid to smoking cessation and has since been launched in many other countries. Adverse events associated with the use of bupropion SR at the recommended dosage of 150mg twice daily in clinical trials most commonly included insomnia, headache, dry mouth, nausea and anxiety; insomnia and anxiety are also recognised as symptoms of nicotine withdrawal. Only insomnia and dry mouth occurred significantly more frequently with bupropion SR than with placebo. Relative to placebo, no significant changes in mean values for heart rate, blood pressure or routine laboratory parameters have been reported in smokers using bupropion SR alone in clinical trials. When bupropion SR was compared with a nicotine transdermal patch in a clinical trial, insomnia predominated in the bupropion SR group, while dream abnormalities were more common in smokers using the nicotine patch. Bupropion SR and the nicotine transdermal patch in combination can be used safely (with appropriate monitoring) as an aid to smoking cessation.

Infrequent but clinically important adverse reactions to bupropion SR include seizures and hypersensitivity reactions: in controlled clinical trials of bupropion SR (300 mg/day), where smokers were carefully screened for risk factors for seizure, the incidence of both seizures and severe hypersensitivity reactions was ≈0.1% for each event. In order to avoid a risk of seizure of greater than 0.1%, smokers should be screened for predisposing risk factors and adhere to the manufacturer’s dosage recommendations (maximum daily dose of 300mg).

Thus, bupropion SR is generally well tolerated, as seen by the low discontinuation rate due to an adverse event in clinical trials (6 to 12%). The most common adverse events (insomnia and dry mouth) are generally transient and often resolve quickly without therapeutic intervention; they can be managed if necessary by a reduction in bupropion dose.



The author is acting as a consultant for GlaxoSmithKline France.


  1. 1.
    Ferry L, Johnston JA. Efficacy and safety of bupropion SR for smoking cessation: data from clinical trials and 5 years of postmarketing experience [abstract]. Accepted by the Third European Conference on Tobacco OR Health; 2002 Jun 20–22; Warsaw, PolandGoogle Scholar
  2. 2.
    Hurt RD, Sachs DP, Glover ED, et al. A comparison of sustained-release bupropion and placebo for smoking cessation. N Engl J Med 1997; 337: 1195–202PubMedCrossRefGoogle Scholar
  3. 3.
    Jorenby DE, Leischow SJ, Nides MA, et al. A controlled trial of sustained-release bupropion, a nicotine patch, or both for smoking cessation. N Engl J Med 1999; 340: 685–91PubMedCrossRefGoogle Scholar
  4. 4.
    Bolliger C, van Spiegel P, Gilljam H, et al. Buproprion hydrochloride is effective and well tolerated aid to smoking cessation: a multi-centre study [abstract]. Eur Respir J 2001; 18 Suppl. 33: USGoogle Scholar
  5. 5.
    Gonzales DH, Nides MA, Ferry LH, et al. Bupropion SR as an aid to smoking cessation in smokers treated previously with bupropion: a randomized placebo-controlled study. Clin Pharmacol Ther 2001; 69: 438–44PubMedCrossRefGoogle Scholar
  6. 6.
    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: 423–33PubMedGoogle Scholar
  7. 7.
    Puska PMJ, Brath H, Astbury C, et al. Zyban® is an effective and well-tolerated aid to smoking cessation in a health care professionals population: a multicountry study [poster no.22]. Third Annual Conference of the European Society for Research on Nicotine and Tobacco; 2001 Sep 202–22; Paris, France: Part IIGoogle Scholar
  8. 8.
    Perruchoud AP, Klane G, Krause H, et al. Bupropion sustained release (Zyban®) is an effective and well tolerated aid to smoking cessation in smokers with cardiovascular disease. Presented at the American Heart Association; 2001 Nov 11–14; Anaheim (CA)Google Scholar
  9. 9.
    Tashkin D, Kanner R, Bailey W, et al. Smoking cessation in patients with chronic obstructive pulmonary disease: a double-blind, placebo-controlled, randomised trial. Lancet 2001; 357: 1571–5PubMedCrossRefGoogle Scholar
  10. 10.
    GlaxoSmithKline. Product information: Zyban® (bupropion hydrochloride) sustained release tablets, 2002. Available from URL: http://us.gsk.com/products/assets/us_zyban.pdf [Accessed 2002 Apr 18]
  11. 11.
    GlaxoSmithline. Summary of product characteristics. Last updated 5th April 2002. Available from URL: http://emc.vhn.net/eMC/assets/c/html/DisplayDoc.asp?.DocumentID=2948 [Accessed 2002 Apr 18]
  12. 12.
    Tripathi A, Greenberger PA. Bupropion hydrochloride induced serum sickness-like reaction. Ann Allergy Asthma Immunol 1999; 83: 165–6PubMedCrossRefGoogle Scholar
  13. 13.
    Peloso PM, Baillie C. Serum sickness-like reaction with bupropion [letter]. JAMA 1999; 282: 1817PubMedCrossRefGoogle Scholar
  14. 14.
    Benson E. Bupropion-induced hypersensitivity reactions. Med J Aust 2001; 174:650–1PubMedGoogle Scholar
  15. 15.
    Davis JS, Boyle MJ, Hannaford R, et al. Bupropion and serum sickness-like reaction. Med J Aust 2001; 174: 479–80PubMedGoogle Scholar
  16. 16.
    Dunner DL, Zisook S, Billow AA, et al. A prospective safety surveillance study for bupropion sustained-release in the treatment of depression. J Clin Psychiatry 1998; 59: 366–73PubMedCrossRefGoogle Scholar
  17. 17.
    Jordan WP. Clinical evaluation of the contact sensitization potential of a transdermal nicotine system (Nicoderm). J Fam Pract 1992; 34: 709–12PubMedGoogle Scholar
  18. 18.
    Russell MA, Stapleton JA, Feyerabend C, et al. Targeting heavy smokers in general practice: randomised controlled trial of transdermal nicotine patches. BMJ 1993; 306: 1308–12PubMedCrossRefGoogle Scholar
  19. 19.
    Martin PD, Robinson GM. The safety, tolerability and efficacy of transdermal nicotine (Nicotinell TTS) in initially hospitalised patients. N Z Med J 1995; 108: 6–8PubMedGoogle Scholar
  20. 20.
    Roose SP, Glassman AH, Giardina EG, et al. Cardiovascular effects of imipramine and bupropion in depressed patients with congestive heart failure. J Clin Psychopharmacol 1987; 7:247–51PubMedCrossRefGoogle Scholar
  21. 21.
    Roose SP, Dalack GW, Glassman AH, et al. Cardiovascular effects of bupropion in depressed patients with heart disease. Am J Psychiatry 1991; 148: 512–6PubMedGoogle Scholar
  22. 22.
    Branconnier RJ, Cole JO, Ghazvinian S, et al. Clinical pharmacology of bupropion and imipramine in elderly depressives. J Clin Psychiatry 1983; 44: 130–3PubMedGoogle Scholar
  23. 23.
    Medicines Control Agency. Zyban® (bupropion hydrochloride): safety update, 2002. Available from URL: http://www.mca.gov.uk [Accessed 2002 Mar 22]
  24. 24.
    Australian Drug Reactions Advisory Committee, Australian Government. Update on bupropion (Zyban® SR): 31 August 2001. Available from URL: http://www.health.gov.au/tga/docs/html/zyban.htm [Accessed 2002 Mar 22]
  25. 25.
    World Health Organization (WHO). Bupropion safety information. WHO Drug Information 2001; 15: 76Google Scholar
  26. 26.
    Patten CA, Rummans TA, Croghan IT, et al. Development of depression during placebo-controlled trials of bupropion for smoking cessation: case reports. J Clin Psychiatry 1999; 60: 436–41PubMedCrossRefGoogle Scholar
  27. 27.
    Aubin HJ, Tilikete S, Barrucand D. Depression and smoking. Encéphale 1996; 22: 17–22PubMedGoogle Scholar

Copyright information

© Adis International Limited 2002

Authors and Affiliations

  1. 1.Centre de Traitement des AddictionsHôpital Emile RouxLimeil-BrévannesFrance

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