Skip to main content
PMC home page
Primary Care Companion to The Journal of Clinical Psychiatry logoLink to Primary Care Companion to The Journal of Clinical Psychiatry
. 2002;4(1):30–32. doi: 10.4088/pcc.v04n0110a

The Many Uses of Bupropion and Bupropion Sustained Release (SR) in Adults

Timothy R Berigan 1
PMCID: PMC314381  PMID: 15014734

Sir: Bupropion is an antidepressant originally approved by the U.S. Food and Drug Administration (FDA) in 1989 for the treatment of depression.1 Its unique mechanism of action among antidepressants is thought to be due to reuptake of dopamine and norepinephrine.2 In 1997, the FDA approved bupropion sustained release (SR) for the treatment of smoking cessation.3 Bupropion has been used to treat a number of conditions, and the following discussion will review those off-label uses.

It appears that bupropion may be an effective antidepressant across a wide spectrum of depressive conditions. Weihs et al.4 found bupropion to be a safe and effective agent in the treatment of depression in the elderly. In addition to having a favorable side effect profile, bupropion has been shown to have positive results in treating anxiety associated with depression compared with sertraline and fluoxetine.5–7 The most common side effects of bupropion described in a series of studies include headache, dry mouth, and nausea when compared with placebo.8 Two important clinical issues noted in the studies were that sexual dysfunction was reported by less than 1% of patients and that a dose-associated weight loss was found in all 3 studies.8 Bupropion has also been associated with weight loss in overweight and obese women in a recently published study.9

Dysthymic disorder, a chronic low-grade depression, is often treated with antidepressants.10 In an open-label study of 21 adults diagnosed with dysthymia, 71.4% responded to bupropion SR treatment with no dropouts due to side effects.11

Bipolar depression can be a debilitating phase of the illness with associated morbidity and increased risk of suicide.12 Mood stabilizer monotherapy is insufficient for the majority of bipolar patients.13 In the Expert Consensus Guideline Series for the medication treatment of bipolar disorder, bupropion is the treatment of choice for mild-to-moderate depression.14 It is also a preferred agent in the treatment of severe melancholic and atypical depression associated with bipolar disorder.14 Bupropion was associated with lower rates of inducing mania than desipramine in a prospective, double-blind trial.15 It may also be associated with milder manic states than other antidepressants.16 Bupropion may also be a promising adjunct to lithium in rapid-cycling bipolar patients.17

Up to 46% of patients do not adequately respond to treatment with antidepressants.18 Clinicians are left with either switching or augmenting options. Bupropion appears to be a safe and effective agent when added to selective serotonin reuptake inhibitors (SSRIs).19 Mischoulon et al.20 reported that bupropion was the most widely chosen augmentation agent in a survey of 801 clinicians in the United States and Canada.

Sexual dysfunction may occur in up to 75% of patients taking antidepressants.21 In head-to-head trials, bupropion SR has also been shown to have a significantly lower rate of sexual dysfunction than sertraline and fluoxetine.22–24 Bupropion has been used successfully to treat antidepressant-induced sexual dysfunction in a number of studies.25–30 Bupropion SR may also be a useful agent in treating orgasmic dysfunction in nondepressed patients.31 It has been reported to be a treatment option for women diagnosed with hypoactive sexual desire disorder.32

Initial results of an open-label study involving bupropion in the treatment of social phobia appear to be promising.33 Canive et al.34 looked at bupropion's efficacy in treating posttraumatic stress disorder (PTSD). They found bupropion decreased depressive symptoms, but no significant changes in symptoms of intrusion and avoidance were noted. Almai et al.,35 in an open trial evaluating bupropion SR in the treatment of PTSD, noted that 89% of the patients completing the study reported a marked improvement in reexperiencing, avoidance, numbing, and hyperarousal symptoms.

Bupropion may offer a valuable treatment option in adults with attention-deficit/hyperactivity disorder (ADHD), which may occur in as many as 4.7% of adults.36 As early as 1990 in an open-label trial, Wender and Reimherr37 reported that bupropion treatment was beneficial in adults with ADHD. Wilens et al.38 conducted a double-blind, placebo-controlled, randomized, parallel 6-week trial comparing bupropion SR with placebo in adults with ADHD. The results showed that bupropion SR was associated with significant changes in ADHD symptoms, with 76% reporting improvement compared with 37% taking placebo. Based on Clinical Global Impressions scale screens, 52% of patients taking bupropion reported being much improved compared with 11% treated with placebo. Kuperman et al.39 in a randomized, double-blind, parallel study compared bupropion, methylphenidate, and placebo. The group treated with bupropion reported a 64% response rate based on the Clinical Global Impressions scale versus a 50% response rate in the methylphenidate group and a 25% response rate in the placebo-treated group. There are at least 2 other double-blind, placebo-controlled studies and 1 open-label study in adults demonstrating bupropion SR to be effective in reducing ADHD symptoms.40–42

To date there is 1 double-blind, placebo-controlled crossover study evaluating the efficacy of bupropion in the treatment of neuropathic pain, which showed promising results with 73% of patients experiencing pain relief on bupropion SR.43

In a case report, bupropion SR has been shown to be of value when combined with behavior modification in treating smokeless tobacco use.44 Bupropion has been helpful in reducing cravings associated with cocaine use in an active-controlled study, an open-label trial, and a case report,45–47 but showed no advantage in 2 other reports.48,49 In another case report, bupropion SR therapy and participation in a 12-step program showed positive results in reducing cravings associated with methamphetamine use.50

Bupropion appeared to be superior to placebo in a double-blind, controlled study of patients with bulimia.51 However, 4 patients suffered grand mal seizures during treatment, and it is recommended that bupropion not be used in patients with any history of seizures, anorexia nervosa, bulimia, or major head injury.1 It is also recommended that when physicians are prescribing medications in an off-label use that informed consent be obtained acknowledging the off-label use.

Bupropion appears to have a number of uses in a variety of conditions, in addition to its FDA indications. It is recommended that physicians using bupropion in an off-label condition document the patient.

Footnotes

Dr. Berigan reports no financial affiliation or other relationship relevant to the subject matter of this letter.

REFERENCES

  1. Schatzberg AF, Cole JO, and De Battista C. Antidepressants. In: Schatzberg AF, Cole JO, De Battista C, eds. Manual of Clinical Psychopharmacology. 3rd ed. Washington, DC: American Psychiatric Press. 1997 31–112. [Google Scholar]
  2. Stahl SM. Antidepressants and mood stabilizers. In: Stahl SM, ed. Essential Psychopharmacology: Neuroscientific Basis and Practical Applications. Cambridge, Mass: Cambridge University Press. 1996 131–166. [Google Scholar]
  3. Franklin JE, Frances RJ. Alcohol and other psychoactive substance use disorders. In: Hales RE, Yudofsky SC, Talbott JA, eds. The American Psychiatric Press Textbook of Psychiatry. 3rd ed. Washington, DC: American Psychiatric Press. 1999 363–423. [Google Scholar]
  4. Weihs KL, Settle EC Jr, Batey SR, et al. Bupropion sustained release versus paroxetine for the treatment of depression in the elderly. J Clin Psychiatry. 2000;61:196–202. doi: 10.4088/jcp.v61n0309. [DOI] [PubMed] [Google Scholar]
  5. Rush AJ, Batey S, Donahue R, et al. Does pretreatment anxiety predict response to either bupropion SR or sertraline? J Affect Disord. 2001;64:81–87. doi: 10.1016/s0165-0327(00)00250-0. [DOI] [PubMed] [Google Scholar]
  6. Trivedi MH, Rush AJ, Carmody TJ, et al. Do bupropion SR and sertraline differ in their effects on anxiety in depressed patients? J Clin Psychiatry. 2001;62:776–781. doi: 10.4088/jcp.v62n1005. [DOI] [PubMed] [Google Scholar]
  7. Feighner JP, Gardner EA, Johnston JA, et al. Double-blind comparison of bupropion and fluoxetine in depressed outpatients. J Clin Psychiatry. 1991;52:329–335. [PubMed] [Google Scholar]
  8. Settle EC, Stahl SM, Batey SR, et al. Safety profile of sustained-release bupropion in depression: results of three clinical trials. Clin Ther. 1999;21:454–463. doi: 10.1016/s0149-2918(00)88301-0. [DOI] [PubMed] [Google Scholar]
  9. Gadde KM, Parker CB, Maner LG, et al. Bupropion for weight loss: an investigation of efficacy and tolerability in overweight and obese women. Obes Res. 2001;9:544–551. doi: 10.1038/oby.2001.71. [DOI] [PubMed] [Google Scholar]
  10. Gorman JM. Drugs used to treat depression. In: Gorman JM, ed. The Essential Guide to Psychiatric Drugs. 3rd ed. New York, NY: St Martin's Griffin. 1997 47–119. [Google Scholar]
  11. Hellerstein DJ, Batchelder S, Kreditor D, et al. Bupropion sustained release for the treatment of dysthymic disorder: an open-label study. J Clin Psychopharmacol. 2001;21:325–329. doi: 10.1097/00004714-200106000-00012. [DOI] [PubMed] [Google Scholar]
  12. Kalin NH. Management of the depressive component of bipolar disorder. Depress Anxiety. 1996–97;4:190–198. doi: 10.1002/(SICI)1520-6394(1996)4:4<190::AID-DA5>3.0.CO;2-J. [DOI] [PubMed] [Google Scholar]
  13. Post RM, Ketter TA, Pazzaglia PJ, et al. Rational polypharmacy in the bipolar affective disorders. Epilepsy Res Suppl. 1996;11:153–180. [PubMed] [Google Scholar]
  14. The Expert Consensus Guideline Series: Medication Treatment of Bipolar Disorder 2000. Postgrad Med. 2000 Spec. 1–104. [PubMed] [Google Scholar]
  15. Sachs GS, Lafer B, Stoll AL, et al. A double-blind trial of bupropion versus desipramine for bipolar depression. J Clin Psychiatry. 1994;55:391–393. [PubMed] [Google Scholar]
  16. Stoll AL, Mayer PV, Kolbrener M, et al. Antidepressant-associated mania: a controlled comparison with spontaneous mania. Am J Psychiatry. 1994;151:1642–1645. doi: 10.1176/ajp.151.11.1642. [DOI] [PubMed] [Google Scholar]
  17. Haykal RF, Akiskal HS. Bupropion as a promising approach to rapid cycling bipolar II patients. J Clin Psychiatry. 1990;51:450–455. [PubMed] [Google Scholar]
  18. Joffe RT. Refractory depression treatment strategies with particular reference to the thyroid axis. J Psychiatry Neurosci. 1997;22:327–331. [PMC free article] [PubMed] [Google Scholar]
  19. Bodkin JA, Lasser RA, Wines JD, et al. Combining serotonin reuptake inhibitors and bupropion in partial responders to antidepressant monotherapy. J Clin Psychiatry. 1997;58:137–145. doi: 10.4088/jcp.v58n0401. [DOI] [PubMed] [Google Scholar]
  20. Mischoulon D, Nierenberg AA, Kizilbash L, et al. Strategies for managing depression refractory to selective serotonin reuptake inhibitor treatment: a survey of clinicians. Can J Psychiatry. 2000;45:476–481. doi: 10.1177/070674370004500509. [DOI] [PubMed] [Google Scholar]
  21. Segraves RT. Antidepressant-induced sexual dysfunction. J Clin Psychiatry. 1998;59(suppl 4):48–54. [PubMed] [Google Scholar]
  22. Coleman CC, Cunningham LA, Foster VJ, et al. Sexual dysfunction associated with the treatment of depression: a placebo-controlled comparison of bupropion sustained release and sertraline treatment. Ann Clin Psychiatry. 1999;11:205–215. doi: 10.1023/a:1022309428886. [DOI] [PubMed] [Google Scholar]
  23. Croft H, Settle E Jr, Houser T, et al. A placebo-controlled comparison of the antidepressant efficacy and effects on sexual functioning of sustained-release bupropion and sertraline. Clin Ther. 1999;21:643–658. doi: 10.1016/S0149-2918(00)88317-4. [DOI] [PubMed] [Google Scholar]
  24. Coleman CC, King BR, Bolden-Watson C, et al. A placebo-controlled comparison of the effects on sexual functioning of bupropion sustained release and fluoxetine. Clin Ther. 2001;23:1040–1058. doi: 10.1016/s0149-2918(01)80090-4. [DOI] [PubMed] [Google Scholar]
  25. Ashton AK, Rosen RC. Bupropion as an antidote for serotonin reuptake inhibitor–induced sexual dysfunction. J Clin Psychiatry. 1998;59:112–115. doi: 10.4088/jcp.v59n0304. [DOI] [PubMed] [Google Scholar]
  26. Labbate LA, Grimes JB, Hines A, et al. Bupropion treatment of serotonin reuptake antidepressant-associated sexual dysfunction. Ann Clin Psychiatry. 1997;9:241–245. doi: 10.1023/a:1022356427242. [DOI] [PubMed] [Google Scholar]
  27. Walker PW, Cole JO, Gardner EA, et al. Improvement in fluoxetine-associated sexual dysfunction in patients switched to bupropion. J Clin Psychiatry. 1993;54:459–465. [PubMed] [Google Scholar]
  28. Clayton AH, McGarvey ED, Warnock J, and et al. Bupropion as an antidote to SSRI-induced sexual dysfunction [poster]. Presented at the 40th annual meeting of the New Clinical Drug Evaluation Unit. May 30–June 2, 2000 Boca Raton, Fla. [Google Scholar]
  29. Solvason HB, DeBattista C, Kendrick E, and et al. Bupropion SR in the treatment of SSRI-induced sexual dysfunction [poster]. Presented at the 40th annual meeting of the New Clinical Drug Evaluation Unit. May 30–June 2, 2000 Boca Raton, Fla. [Google Scholar]
  30. Gitlin MJ, Suri RA, Altshuler LL, and et al. Bupropion as a treatment for SSRI-induced sexual side effects. In: New Research Abstracts of the 153rd Annual Meeting of the American Psychiatric Association; May 17, 2000; Chicago, Ill. Abstract NR617:224. [Google Scholar]
  31. Modell JG, May RS, Kathol CR. Effect of bupropion SR on orgasmic dysfunction in nondepressed subjects: a pilot study. J Sex Marital Ther. 2000;26:231–240. doi: 10.1080/00926230050084623. [DOI] [PubMed] [Google Scholar]
  32. Segraves RT, Croft H, Kavousis R, et al. Bupropion sustained release (SR) for the treatment of hypoactive sexual desire disorder (HSDD) in nondepressed women. J Sex Marital Ther. 2001;27:303–316. doi: 10.1080/009262301750257155. [DOI] [PubMed] [Google Scholar]
  33. Emmanuel NP, Brawman-Mintzer O, Morton WA. Bupropion SR in treatment of social phobia. Depress Anxiety. 2000;12:111–113. doi: 10.1002/1520-6394(2000)12:2<111::AID-DA9>3.0.CO;2-3. [DOI] [PubMed] [Google Scholar]
  34. Canive JM, Clark RD, Calais LA, et al. Bupropion treatment in veterans with posttraumatic stress disorder: an open study. J Clin Psychopharmacol. 1998;18:379–383. doi: 10.1097/00004714-199810000-00005. [DOI] [PubMed] [Google Scholar]
  35. Almai AM, Brouette TE, and Goddard AW. Bupropion treatment of civilian PTSD. In: New Research Abstracts of the 153rd Annual Meeting of the American Psychiatric Association; May 15, 2000; Chicago, Ill. Abstract NR17:61. [Google Scholar]
  36. Murphy K, Barkley RA. Prevalence of DSM-IV symptoms of ADHD in adult licensed drivers: implications for clinical diagnosis. J Atten Disord. 1996;1:147–161. [Google Scholar]
  37. Wender PH, Reimherr FW. Bupropion treatment of attention-deficit hyperactivity disorder in adults. Am J Psychiatry. 1990;147:1018–1020. doi: 10.1176/ajp.147.8.1018. [DOI] [PubMed] [Google Scholar]
  38. Wilens TE, Spencer TJ, Bierderman J, et al. A controlled clinical trial of bupropion for attention deficit hyperactivity disorder in adults. Am J Psychiatry. 2001;158:282–288. doi: 10.1176/appi.ajp.158.2.282. [DOI] [PubMed] [Google Scholar]
  39. Kuperman S, Perry PJ, Gaffney GR, et al. Bupropion SR versus methylphenidate versus placebo for attention deficit hyperactivity in adults. Ann Clin Psychiatry. 2001;13:129–134. doi: 10.1023/a:1012239823148. [DOI] [PubMed] [Google Scholar]
  40. Perry PJ, Kuperman S, Gaffney GR, and et al. Bupropion sustained release versus methylphenidate versus placebo in the treatment of adult ADHD. In: New Research Abstracts of the 153rd Annual Meeting of the American Psychiatric Association; May 17, 2000; Chicago, Ill. Abstract NR568:211. [Google Scholar]
  41. Reimherr FW, Strong RE, Marchant B, and et al. Six-week, double-blind, placebo-controlled trial of bupropion sustained release in the treatment of adults with ADHD. In: New Research Abstracts of the 153rd Annual Meeting of the American Psychiatric Association; May 18, 2000; Chicago, Ill. Abstract NR718:252. [Google Scholar]
  42. Wilens TE, Prince JD, Spencer T, and et al. Bupropion SR for attention deficit hyperactivity (ADHD) in adults with bipolar disorder (BPD) and ADHD [poster]. Presented at the 40th annual meeting of the New Clinical Drug Evaluation Unit; May 30–June 2, 2000; Boca Raton, Fla. [Google Scholar]
  43. Semenchuk MR, Sherman S, Davis B. Double-blind randomized trial of bupropion SR for the treatment of neuropathic pain. Neurology. 2001;57:1583–1588. doi: 10.1212/wnl.57.9.1583. [DOI] [PubMed] [Google Scholar]
  44. Berigan TR, Deagle EA III. Treatment of smokeless tobacco addiction with bupropion and behavior modification [letter] JAMA. 1999;281:233. doi: 10.1001/jama.281.3.233-b. [DOI] [PubMed] [Google Scholar]
  45. Avants SK, Margolin A, DePhilippis D, et al. A comprehensive pharmacologic-psychosocial treatment program for HIV-seropositive cocaine- and opioid-dependent patients: preliminary findings. J Subst Abuse Treat. 1998;15:261–265. doi: 10.1016/s0740-5472(97)00226-2. [DOI] [PubMed] [Google Scholar]
  46. Margolin A, Kosten T, Petrakis I, et al. Bupropion reduces cocaine abuse in methadone-maintained patients [letter] Arch Gen Psychiatry. 1991;48:87. doi: 10.1001/archpsyc.1991.01810250089015. [DOI] [PubMed] [Google Scholar]
  47. Harazin JS, Berigan TR. The use of bupropion in reducing cravings after cessation of cocaine [letter] Subst Abuse. 1995;16:181–182. [Google Scholar]
  48. Hollister LE, Krajewski K, Rustin T, et al. Drugs for cocaine dependency: not easy [letter with reply] Arch Gen Psychiatry. 1992;49:905. doi: 10.1001/archpsyc.1992.01820110069011. [DOI] [PubMed] [Google Scholar]
  49. Margolin A, Kosten TR, Avants SK, et al. A multicenter trial of bupropion for cocaine dependence in methadone-maintained patients. Drug Alcohol Depend. 1995;40:125–131. doi: 10.1016/0376-8716(95)01198-6. [DOI] [PubMed] [Google Scholar]
  50. Berigan TR, Russell ML. Treatment of methamphetamine cravings with bupropion: a case report. Primary Care Companion J Clin Psychiatry. 2001;3:267–268. doi: 10.4088/pcc.v03n0603b. [DOI] [PMC free article] [PubMed] [Google Scholar]
  51. Spiller HA, Ramoska EA, Krenzelok EP, et al. Bupropion overdose: a 3-year multi-center retrospective analysis. Am J Emerg Med. 1994;12:43–45. doi: 10.1016/0735-6757(94)90195-3. [DOI] [PubMed] [Google Scholar]

Articles from Primary Care Companion to The Journal of Clinical Psychiatry are provided here courtesy of Physicians Postgraduate Press, Inc.

RESOURCES