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Bupropion

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Critical Care Toxicology

Abstract

Bupropion is an atypical antidepressant primarily used for the treatment of depression and as an adjunct for smoking cessation. The United Sates Food and Drug Administration approved bupropion for the treatment of depression in 1985, but the drug was withdrawn prior to marketing after seizures were reported in four of 55 nondepressed bulimic patients who received it [1]. It was later reported that the risk of seizures with bupropion was comparable to that of other antidepressants, provided the daily dose did not exceed 450 mg, and the drug was reintroduced in 1989 [2, 3]. Today, bupropion is available as immediate-release, sustained-release, and extended-release formulations [4]. It is generally well tolerated at therapeutic doses, with common side effects including insomnia, agitation, dry mouth, and nausea [5]. Given its unique pharmacologic properties, adverse effects frequently encountered with other antidepressants (such as sexual dysfunction, weight gain, and sedation) are rarely seen with bupropion [5]. In overdose, however, bupropion can exhibit significant toxicity, and bupropion abuse is increasingly recognized as an evolving concern. This chapter focuses on the pharmacological and toxicological properties of bupropion, with particular attention to its pharmacokinetics, the clinical manifestations of overdose, and recommendations for management.

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References

  1. Home RL, Ferguson JM, Pope Jr HG, Hudson JI, Lineberry CG, Ascher J, Cato A. Treatment of bulimia with bupropion: a multicenter controlled trial. J Clin Psychiatry. 1988;49(7):262–6.

    Google Scholar 

  2. Davidson J. Seizures and bupropion: a review. J Clin Psychiatry. 1989;50(7):256–61.

    CAS  PubMed  Google Scholar 

  3. Johnston JA, Lineberry CG, Ascher JA, Davidson J, Khayrallah MA, Feighner JP, Stark P. A 102-center prospective study of seizure in association with bupropion. J Clin Psychiatry. 1991;52:450–6.

    CAS  PubMed  Google Scholar 

  4. Belson MG, Kelley TR. Bupropion exposures: clinical manifestations and medical outcome. J Emerg Med. 2002;23:223–30.

    Article  PubMed  Google Scholar 

  5. Stahl SM, Pradko JF, Haight BR, Modell JG, Rockett CB, Learned-Coughlin S. A review of the neuropharmacology of bupropion, a dual norepinephrine and dopamine reuptake inhibitor. Prim Care Comp J Clin Psychiatry. 2004;6(4):159–66.

    Article  Google Scholar 

  6. Dwoskin LP, Rauhut AS, King-Pospisil KA, Bardo MT. Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent. CNS Drug Rev. 2006;12:178–207.

    Article  PubMed  Google Scholar 

  7. Caillier B, Pilote S, Castonguay A, Patoine D, Ménard-Desrosiers V, Vigneault P, Hreiche R, Turgeon J, Daleau P, De Koninck Y, Simard C, Drolet B. QRS widening and QT prolongation under bupropion: a unique cardiac electrophysiological profile. Fundam Clin Pharmacol. 2012;26:599–608.

    Article  CAS  PubMed  Google Scholar 

  8. Jasiak NM, Bostwick JR. Risk of QT/QTc prolongation among newer non-SSRI antidepressants. Ann Pharmacother. 2014;48:1620–8.

    Article  CAS  PubMed  Google Scholar 

  9. Jefferson JW, Pradko JF, Muir KT. Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations. Clin Ther. 2005;27(11):1685–95.

    Article  CAS  PubMed  Google Scholar 

  10. Donnelly K, Walkowiak HB, Donnelly C, Jenkinson E, Rizkalla J, Langford N. Bupropion toxicokinetic: a case report. Clin Toxicol. 2010;48:385–7.

    Article  CAS  Google Scholar 

  11. Al-abri SA, Orengo JP, Hayashi S, Thoren KL, Benowitz NL, Olson KR. Delayed bupropion cardiotoxicity associated with elevated serum concentrations of bupropion but not hydroxybupropion. Clin Toxicol. 2013;51:1230–4.

    Article  CAS  Google Scholar 

  12. White RS, Langford JR. Sustained release bupropion overdose and treatment. Am J Emerg Med. 2002;20:388–9.

    Article  PubMed  Google Scholar 

  13. Silverstone PH, Williams R, McMahon L, Fleming R, Fogarty S. Convulsive liability of bupropion hydrochloride metabolites in Swiss albino mice. Ann Gen Psychiatry. 2008;7:19.

    Article  PubMed  PubMed Central  Google Scholar 

  14. DeVane CL, Laizure SC, Stewart JT, Kolts BE, Ryerson EG, Miller RL, Lai AA. Disposition of bupropion in healthy volunteers and subjects with alcoholic liver disease. J Clin Psychopharmacol. 1990;10:328–32.

    Article  CAS  PubMed  Google Scholar 

  15. Worrall SP, Almond MK, Dhillon S. Pharmacokinetics of bupropion and its metabolites in hemodialysis patients who smoke: a single dose study. Nephron Clin Pract. 2004;97:83–9.

    Article  CAS  Google Scholar 

  16. Spiller HA, Ramoska EA, Krenzelok EP, Sheen SR, Borys DJ, Villalobos D, Muir S, Jones-Easom L. Bupropion overdose: a 3-year multi-center retrospective analysis. Am J Emerg Med. 1994;12:43–5.

    Article  CAS  PubMed  Google Scholar 

  17. Shepherd G, Velez LI, Keyes DC. Intentional Bupropion overdoses. J Emerg Med. 2004;27:147–51.

    Article  PubMed  Google Scholar 

  18. Starr P, Klein-Schwartz W, Spiller H, Kern P, Ekleberry SE, Kunkel S. Incidence and onset of delayed seizures after overdoses of extended-release bupropion. Am J Emerg Med. 2009;27:911–5.

    Article  PubMed  Google Scholar 

  19. Curry SC, Kashani JS, LoVecchio F, Houbek W. Intraventricular conduction delay after bupropion overdose. J Emerg Med. 2005;29:299–305.

    Article  PubMed  Google Scholar 

  20. Morazin F, Lumbroso A, Harry P, Blaise M, Turcant A, Montravers P, Gauzit R. Cardiogenic shock and status epilepticus after massive bupropion overdose. Clin Toxicol. 2007;45:794–7.

    Article  Google Scholar 

  21. Sirianni AJ, Osterhoudt KC, Calello DP, Muller AA, Waterhouse MR, Goodkin MB, Gl W, Henretig FM. Use of lipid emulsion in the resuscitation of a patient with prolonged cardiovascular collapse after overdose of bupropion and lamotrigine. Ann Emerg Med. 2008;51:412–5.

    Article  PubMed  Google Scholar 

  22. Druteika D, Zed PJ. Cardiotoxicity following bupropion overdose. Ann Pharmacother. 2002;36:1791–5.

    Article  CAS  PubMed  Google Scholar 

  23. Isbister GK, Balit CR. Bupropion overdose: QTc prolongation and its clinical significance. Ann Pharmacother. 2003;37:999–1002.

    Article  PubMed  Google Scholar 

  24. Mundi JP, Betancourt J, Ezziddin O, Tremayne B, Majic T, Mosenifar Z. Dilated and unreactive pupils and burst-suppression on electroencephalography due to bupropion overdose. J Intensive Care Med. 2012;27:384–8.

    Article  PubMed  Google Scholar 

  25. Davoudian V. Bupropion overdose mimicking brain death. American College of Physicians Colorado, Chapter Annual Meeting, Colorado Springs, CO, Broadmoor Hotel; 2008.

    Google Scholar 

  26. Spiller HA, Bottei E, Kalin L. Fata bupropion overdose with post mortem blood concentrations. Forensic Sci Med Pathol. 2008;4:47–50.

    Article  CAS  PubMed  Google Scholar 

  27. Strike M, Hatcher S. Bupropion injection resulting in tissue necrosis and psychosis. J Addict Med. 2015;9:246–50.

    Article  CAS  PubMed  Google Scholar 

  28. Baribeau D, Araki KF. Intravenous bupropion: a previously undocumented method of abuse of a commonly prescribed antidepressant agent. J Addict Med. 2013;7:216–7.

    Article  PubMed  Google Scholar 

  29. Yoon G, Westermeyer J. Intranasal bupropion abuse: case report. Am J Addict. 2013;22:180.

    Article  PubMed  Google Scholar 

  30. McCormick J. Recreational bupropion abuse in a teenager. J Clin Pharmacol. 2002;53:211–4.

    Article  Google Scholar 

  31. Oppek K, Koller G, Zwergal A, Pogarell O. Intravenous administration and abuse of bupropion: a case report and a review of the literature. J Addict Med. 2014;8:290–3.

    Article  PubMed  Google Scholar 

  32. Reeves RR, Ladner ME. Additional evidence of the abuse potential of bupropion. J Clin Psychopharmacol. 2013;33:584–5.

    Article  PubMed  Google Scholar 

  33. Kim D, Steinhart B. Seizures induced by recreational abuse of bupropion tablets via nasal insufflation. Can J Emerg Med. 2010;12:158–61.

    Google Scholar 

  34. Langguth B, Hajak G, Landgrebe M, Unglaub W. Abuse potential of bupropion nasal insufflation: a case report. J Clin Psychopharmacol. 2009;29:618–9.

    Article  PubMed  Google Scholar 

  35. Hill S, Sikand H, Lee J. A case report of seizure induced by bupropion nasal insufflation. Prim Care Companion J Clin Psychiatry. 2007;9(1):67–9.

    Article  PubMed  PubMed Central  Google Scholar 

  36. Khurshid K, Decker D. Bupropion insufflation in a teenager. J Child Adol Psychop. 2004;14:157–8.

    Article  Google Scholar 

  37. Welsh C, Doyon S. Seizure induced by insufflation of bupropion. N Engl J Med. 2002;347:951.

    Article  PubMed  Google Scholar 

  38. Lewis JC, Sutter ME, Albertson TE, Owen KP, Ford JB. An 11-year review of bupropion insufflation exposures in adults reported to the California Poison Control System. Clin Toxicol. 2014;52:969–72.

    Article  CAS  Google Scholar 

  39. Hilliard WT, Barloon L, Farley P, Penn JV, Koranek A. Bupropion diversion and misuse in the correctional facility. J Correct Health Care. 2013;19:211–7.

    PubMed  Google Scholar 

  40. Casey ER, Scott MG, Tang S, Mullins ME. Frequency of false positive amphetamine screens due to bupropion using the Syva EMIT II immunoassay. J Med Toxicol. 2011;7:105–8.

    Article  PubMed  Google Scholar 

  41. Juurlink DN. Activated charcoal for acute overdose: a reappraisal. Br J Clin Pharmacol. 2016;81(3):482–7.

    Article  PubMed  Google Scholar 

  42. Thanacoody R, Caravati EM, Troutman B, Höjer J, Benson B, Hoppu K, Erdman A, Bedry R, Mégarbane B. Position paper update: whole bowel irrigation for gastrointestinal decontamination of overdose patients. Clin Toxicol. 2015;53(1):5–12.

    Article  Google Scholar 

  43. Tutka P, Mróz T, Klucha K, Piekarczyk M, Wielosz M. Bupropion-induced convulsions: preclinical evaluation of antiepileptic drugs. Epilepsy Res. 2005;64:13–22.

    Article  CAS  PubMed  Google Scholar 

  44. Shah AS, Eddleston M. Should phenytoin or barbiturates be used as second-line anticonvulsant therapy for toxicological seizures? Clin Toxicol. 2010;48:800–5.

    Article  CAS  Google Scholar 

  45. Shenoi AN, Gertz SJ, Mikkilineni S, Kalyanaraman M. Refractory hypotension from massive bupropion overdose successfully treated with extracorporeal membrane oxygenation. Pediatr Emerg Care. 2011;27(1):43–5.

    Article  PubMed  Google Scholar 

  46. Heise CW, Skolnik AB, Raschke RA, Owen-Reece H, Graeme KA. Two cases of refractory cardiogenic shock secondary to bupropion successfully treated with veno-arterial extracorporeal membrane oxygenation. J Med Toxicol. 2016;12(3):301–4.

    Article  CAS  PubMed  Google Scholar 

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Author information

Authors and Affiliations

  1. Department of Medicine, University Health Network, University of Toronto, Toronto, ON, Canada

    Peter Wu

  2. Departments of Medicine and Pediatrics, University of Toronto, Toronto, ON, Canada

    David Juurlink

Authors
  1. Peter Wu
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Corresponding author

Correspondence to Peter Wu .

Editor information

Editors and Affiliations

  1. University of Colorado School of Medicine, Toxicology Associates, Denver, Colorado, USA

    Jeffrey Brent

  2. Office of New Drugs Drug Evaluation and Research, FDA, Silver Spring, Maryland, USA

    Keith Burkhart

  3. Clinical Toxicology, St Thomas' Hospital, London, United Kingdom

    Paul Dargan

  4. University of Colorado School of Medicine, Toxicology Associates, Denver, Colorado, USA

    Benjamin Hatten

  5. Med & Toxicological Intensive Care Unit, Lariboisière Hospital Paris-Diderot University, Paris, France

    Bruno Megarbane

  6. University of Colorado School of Medicine, Toxicology Associates, Denver, Colorado, USA

    Robert Palmer

Grading System for Levels of Evidence Supporting Recommendations in Critical Care Toxicology, 2nd Edition

Grading System for Levels of Evidence Supporting Recommendations in Critical Care Toxicology, 2nd Edition

  1. I

    Evidence obtained from at least one properly randomized controlled trial.

  2. II-1

    Evidence obtained from well-designed controlled trials without randomization.

  3. II-2

    Evidence obtained from well-designed cohort or case–control analytic studies, preferably from more than one center or research group.

  4. II-3

    Evidence obtained from multiple time series with or without the intervention. Dramatic results in uncontrolled experiments (such as the results of the introduction of penicillin treatment in the 1940s) could also be regarded as this type of evidence.

  5. III

    Opinions of respected authorities, based on clinical experience, descriptive studies, and case reports, or reports of expert committees.

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Wu, P., Juurlink, D. (2016). Bupropion. In: Brent, J., Burkhart, K., Dargan, P., Hatten, B., Megarbane, B., Palmer, R. (eds) Critical Care Toxicology. Springer, Cham. https://doi.org/10.1007/978-3-319-20790-2_135-1

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  • DOI: https://doi.org/10.1007/978-3-319-20790-2_135-1

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  • Publisher Name: Springer, Cham

  • Online ISBN: 978-3-319-20790-2

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