bupropion (Wellbutrin, Wellbutrin SR, Zyban, Aplenzin)

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Introduction

Tradename: Wellbutrin.

Indications

* avoid for smoking cessation[22]

Contraindications

Caution:

  • allow 8 hours between doses
  • avoid alcohol
  • safety of use in children < 18 years of age has NOT been established

pregnancy category = b

safety in lactation = -

Dosage

  • adults
  • elderly patients:
    • start: 50-100 mg/day
    • increase by 50-100 mg every 3-4 days as tolerated
    • usual effective dose: 150 mg QD

Tabs: 75 & 100 mg

Sustained release:

  • Wellbutrin SR: 75, 100 & 150 mg. (BID dosing)
  • Wellbutrin XL: 150, 300 mg (QD dosing)

Alpenzin is the hydrobromide salt of bupropion Dosage adjustment with renal impairment: (& hepatic impairment)

  • use reduced dose
  • use with caution

Pharmacokinetics

elimination via kidney

1/2life = 9.6-21 hours

protein binding = 80 %

elimination by hemodialysis = -

elimination by peritoneal dialysis = -

Adverse effects

* increased potential with daily doses of 450-600 mg/day limit single doses to < 150 mg & daily doses to < 300 mg[3]

# risk of serious side effects on mood, behavior, or thinking lower than previously suspected[21]

Drug interactions

Laboratory

Mechanism of action

More general terms

Component of

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. 3.0 3.1 Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  5. Prescriber's Letter 8(4):23 2001
  6. 6.0 6.1 Prescriber's Letter 8(6):34 2001
  7. UCLA Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
  8. Journal Watch 21(20):162, 2001 Hayes et al, Ann Intern Med 135:423, 2002
  9. 9.0 9.1 Journal Watch 22(1):10, 2002 Semenchunk et al, Neurology 57:1583, 2001
  10. Prescriber's Letter 9(3):13-14 2002
  11. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  12. Prescriber's Letter 10(10):57 2003 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=191003&pb=PRL (subscription needed) http://www.prescribersletter.com
  13. Prescriber's Letter 13(9): 2006 Drug Treatment of Seasonal Affective Disorder (SAD) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220904&pb=PRL (subscription needed) http://www.prescribersletter.com
  14. 14.0 14.1 FDA Safety Alert Varenicline (marketed as Chantix) and Bupropion (marketed as Zyban, Wellbutrin, and generics) http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm170090.htm
  15. Stahl SM et al A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor Prim Care Companion J Clin Psychiatry. 2004; 6(4):159-166 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC514842/ http://www.bmj.com/content/347/bmj.f5704http://www.bmj.com/content/347/bmj.f5704
  16. 16.0 16.1 Deprecated Reference
  17. 17.0 17.1 Thomas KH et al. Smoking cessation treatment and risk of depression, suicide, and self harm in the Clinical Practice Research Datalink: Prospective cohort study. BMJ 2013 Oct 11; 347:f5704. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24124105 <Internet> http://www.bmj.com/content/347/bmj.f5704
  18. 18.0 18.1 18.2 Mills EJ et al Cardiovascular Events Associated with Smoking Cessation Pharmacotherapies: A Network Meta-Analysis. Circulation. Dex 9, 2013 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24323793 <Internet> http://circ.ahajournals.org/content/early/2013/11/25/CIRCULATIONAHA.113.003961.abstract
    Samet J Smoking Cessation: Benefits versus Risks of Using Pharmacotherapy to Quit. Circulation. Dex 9, 2013 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24323794 <Internet> http://circ.ahajournals.org/content/early/2013/11/25/CIRCULATIONAHA.113.006928.abstract
  19. 19.0 19.1 Anthenelli RM et al Neuropsychiatric safety and efficacy of varenicline, bupropion, and nicotine patch in smokers with and without psychiatric disorders (EAGLES): a double-blind, randomised, placebo- controlled clinical trial. The Lancet. April 22, 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27116918 <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736%2816%2930272-0/abstract
  20. 20.0 20.1 Fossati R, Apolone G, Negri E et al A double-blind, placebo-controlled, randomized trial of bupropion for smoking cessation in primary care. Arch Intern Med. 2007 Sep 10;167(16):1791-7. PMID: https://www.ncbi.nlm.nih.gov/pubmed/17846399
  21. 21.0 21.1 FDA Safety Alert. Dec 16, 2016 Chantix (varenicline) and Zyban (bupropion): Drug Safety Communication - Mental Health Side Effects Revised. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm533517.htm
    FDA Safety Aommunication. Dec 16, 2016 FDA revises description of mental health side effects of the stop-smoking medicines Chantix (varenicline) and Zyban (bupropion) to reflect clinical trial findings. http://www.fda.gov/Drugs/DrugSafety/ucm532221.htm
  22. 22.0 22.1 Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/
  23. Clayton AH, Croft HA, Horrigan JP et al. Bupropion extended release compared with escitalopram: effects on sexual functioning and antidepressant efficacy in 2 randomized, double-blind, placebo-controlled studies. J Clin Psychiatry 2006 Jul 18; 67:736. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16841623
  24. Patel K, Allen S, Haque MN et al. Bupropion: a systematic review and meta-analysis of effectiveness as an antidepressant. Ther Adv Psychopharmacol 2016 Apr; 6:99. PMID: https://www.ncbi.nlm.nih.gov/pubmed/27141292 Free PMC Article
  25. 25.0 25.1 25.2 Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019

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