Background: Bupropion has been available in the United States since 1989. Initially a thrice-daily immediate-release formulation, a twice-daily sustained-release formulation followed in 1996, and, in August 2003, a once-daily extended-release formulation was introduced. On the 15th anniversary of its introduction, we undertook a review of the background/history, mechanism of action, formulations, and clinical profile of bupropion.

Data sources: Major efficacy trials and other reports were obtained and reviewed from MEDLINE searches, review of abstracts from professional meetings, and the bupropion SR manufacturer's databases. Searches of English-language articles were conducted from June 2003 through August 2004. No time limit was specified in the searches, which were conducted using the search terms bupropion, bupropion SR, and bupropion XL.

Data synthesis: Bupropion inhibits the re-uptake of norepinephrine and dopamine neurotransmission without any significant direct effects on serotonin neurotransmission. Bupropion is an effective antidepressant with efficacy comparable to selective serotonin reuptake inhibitors and other antidepressants. It is well tolerated in short-and longer-term treatment. Headache, dry mouth, nausea, insomnia, constipation, and dizziness are the most common adverse events. Seizure and allergic reactions are medically important adverse events associated with bupropion and are reported rarely. Among all the newer antidepressants in the United States, bupropion appears to have among the lowest incidence of sexual dysfunction, weight gain, and somnolence. Although not U.S. Food and Drug Administration approved for these indications, bupropion has also been used as an adjunctive treatment to reverse antidepressant-induced sexual dysfunction and to augment anti-depressant efficacy in partial responders and non-responders to other agents.

Conclusion: Bupropion has played and will continue to play an important role as a treatment for major depressive disorder in adults, as well as for other related disorders.