Bupropion


Description

Bupropion (also known as the brand name product Wellbutrin®) is a norepinephrine/dopamine-reuptake inhibitor (NDRI) used most commonly for the management of Major Depressive Disorder (MDD), Seasonal Affective Disorder (SAD), and as an aid for smoking...

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Pharmacology

Indication

Bupropion is indicated for the treatment of major depressive disorder (MDD), seasonal affective diso... Read more

Pharmacodynamic

Bupropion is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitor... Read more

Mechanism of action

Bupropion is a norepinephrine/dopamine-reuptake inhibitor (NDRI) that exerts its pharmacological eff... Read more

Absorption

Bupropion is currently available in 3 distinct, but bioequivalent formulations: immediate release (I... Read more

Protein binding

In vitro tests show that bupropion is 84% bound to human plasma proteins at concentrations up to 200... Read more

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

24 hours

Route of elimination

Bupropion is extensively metabolized in humans. Oxidation of the bupropion side chain results in the... Read more

Toxicity

Symptoms of overdose include seizures, hallucinations, loss of consciousness, tachycardia, and cardi... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Insomnia US
  • Kind: experimental
    • Percent: 40%
  • Kind: placebo
    • Percent: 18%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 32%
  • Kind: placebo
    • Percent: 22%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 31%
  • Kind: placebo
    • Percent: 21%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 28%
  • Kind: placebo
    • Percent: 18%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 17%
  • Clinical Trial
    Migraine US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 22%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 22%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 19%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 19%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 16%
  • Clinical Trial
    Excessive sweating US
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 15%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Sedation US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 20%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 19%
  • Kind: placebo
    • Percent: 16%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Application site reaction US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Disturbed concentration US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Hostility US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dream abnormality US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Cardiac Arrhythmias US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Menstrual complaints US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Auditory disturbance US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Appetite increased US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Impaired sleep quality US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Sensory disturbance US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial

    Contraindications

    • Regions: Canada
    • With Drugs:
        • Name: Thioridazine
        • Drugbank Id: DB00679
    • Regions: US
    • Patient Conditions:
        • Name: Uncontrolled Hypertension
        • Drugbank Id: DBCOND0043537
    • Regions: US
    • Patient Conditions:
        • Name: History of bulimia nervosa
        • Drugbank Id: DBCOND0108221
    • Regions: US
    • Patient Conditions:
        • Name: Anorexia Nervosa
        • Drugbank Id: DBCOND0006073
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Regions: US
    • Patient Conditions:
        • Name: History of anorexia nervosa
        • Drugbank Id: DBCOND0108222
    • Regions: US
    • Patient Conditions:
        • Name: Bulimia Nervosa
        • Drugbank Id: DBCOND0006074
    • Regions: US
    • Patient Conditions:
        • Name: Seizure Disorder
        • Drugbank Id: DBCOND0032405
    • Regions: US
    • Patient Conditions:
        • Name: Abrupt cessation of benzodiazepines
        • Drugbank Id: DBCOND0108224
    • Regions: US
    • Patient Conditions:
        • Name: Abrupt cessation of barbiturates
        • Drugbank Id: DBCOND0108225
    • Time Period: within 14 days
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Regions: US
    • Patient Conditions:
        • Name: Abrupt cessation of alcohol
        • Drugbank Id: DBCOND0108223
    • Regions: US
    • With Drugs Coadmin:
        • Name: Methylene blue
        • Drugbank Id: DB09241
    • Regions: US
    • Patient Conditions:
        • Name: Abrupt cessation of antiepileptic drugs
        • Drugbank Id: DBCOND0108226
    • Regions: US
    • With Drugs Coadmin:
        • Name: Linezolid
        • Drugbank Id: DB00601

    Food Interactions

    • Avoid alcohol.
    • Avoid St.John's Wort.
    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Bupropion

    The metabolism of (R)-warfarin can be decreased when combined with Bupropion.
    The metabolism of (S)-Warfarin can be decreased when combined with Bupropion.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 3,5-Dinitrocatechol.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 4-hydroxycoumarin.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 4-Methoxyamphetamine.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 5-methoxy-N,N-dimethyltryptamine.
    The risk or severity of adverse effects can be increased when Bupropion is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Bupropion.
    Abacavir may decrease the excretion rate of Bupropion which could result in a higher serum level.
    The metabolism of Bupropion can be increased when combined with Abatacept.
    The metabolism of Bupropion can be decreased when combined with Abiraterone.
    Acarbose may decrease the excretion rate of Bupropion which could result in a higher serum level.
    The metabolism of Acebutolol can be decreased when combined with Bupropion.
    Aceclofenac may decrease the excretion rate of Bupropion which could result in a higher serum level.
    Acemetacin may decrease the excretion rate of Bupropion which could result in a higher serum level.
    The metabolism of Acenocoumarol can be decreased when combined with Bupropion.
    The risk or severity of adverse effects can be increased when Bupropion is combined with Acepromazine.
    The risk or severity of adverse effects can be increased when Bupropion is combined with Aceprometazine.

    References

    • 1 . Fryer JD, Lukas RJ: Noncompetitive functional inhibition at diverse, human nicotinic acetylcholine receptor subtypes by bupropion, phencyclidine, and ibogaine. J Pharmacol Exp Ther. 1999 Jan;288(1):88-92. [PubMed: 9862757]
    • 2 . Fava M, Rush AJ, Thase ME, Clayton A, Stahl SM, Pradko JF, Johnston JA: 15 years of clinical experience with bupropion HCl: from bupropion to bupropion SR to bupropion XL. Prim Care Companion J Clin Psychiatry. 2005;7(3):106-13. [PubMed: 16027765]
    • 3 . Thase ME, Haight BR, Richard N, Rockett CB, Mitton M, Modell JG, VanMeter S, Harriett AE, Wang Y: Remission rates following antidepressant therapy with bupropion or selective serotonin reuptake inhibitors: a meta-analysis of original data from 7 randomized controlled trials. J Clin Psychiatry. 2005 Aug;66(8):974-81. [PubMed: 16086611]
    • 4 . Authors unspecified: Annual report on the results of treatment in gynecological cancer. Twenty-first volume. Statements of results obtained in patients treated in 1982 to 1986, inclusive 3 and 5-year survival up to 1990. Int J Gynaecol Obstet. 1991 Sep;36 Suppl:1-315. [PubMed: 1684162]
    • 5 . Thase ME, Clayton AH, Haight BR, Thompson AH, Modell JG, Johnston JA: A double-blind comparison between bupropion XL and venlafaxine XR: sexual functioning, antidepressant efficacy, and tolerability. J Clin Psychopharmacol. 2006 Oct;26(5):482-8. [PubMed: 16974189]
    • 6 . Richter T, Schwab M, Eichelbaum M, Zanger UM: Inhibition of human CYP2B6 by N,N',N''-triethylenethiophosphoramide is irreversible and mechanism-based. Biochem Pharmacol. 2005 Feb 1;69(3):517-24. doi: 10.1016/j.bcp.2004.10.008. Epub 2004 Dec 15. [PubMed: 15652242]
    • 7 . Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ: Medication augmentation after the failure of SSRIs for depression. N Engl J Med. 2006 Mar 23;354(12):1243-52. doi: 10.1056/NEJMoa052964. [PubMed: 16554526]
    • 8 . 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 Companion J Clin Psychiatry. 2004;6(4):159-166. [PubMed: 15361919]
    • 9 . John Rush A, Jain SB: Clinical Implications of the STAR*D Trial. Handb Exp Pharmacol. 2018 Sep 11. doi: 10.1007/164_2018_153. [PubMed: 30203327]
    • 10 . Patel K, Allen S, Haque MN, Angelescu I, Baumeister D, Tracy DK: Bupropion: a systematic review and meta-analysis of effectiveness as an antidepressant. Ther Adv Psychopharmacol. 2016 Apr;6(2):99-144. doi: 10.1177/2045125316629071. Epub 2016 Feb 18. [PubMed: 27141292]
    • 11 . Ashton AK, Rosen RC: Bupropion as an antidote for serotonin reuptake inhibitor-induced sexual dysfunction. J Clin Psychiatry. 1998 Mar;59(3):112-5. [PubMed: 9541153]
    • 12 . Shalabi AR, Walther D, Baumann MH, Glennon RA: Deconstructed Analogues of Bupropion Reveal Structural Requirements for Transporter Inhibition versus Substrate-Induced Neurotransmitter Release. ACS Chem Neurosci. 2017 Jun 21;8(6):1397-1403. doi: 10.1021/acschemneuro.7b00055. Epub 2017 Feb 27. [PubMed: 28220701]
    • 13 . Cahill K, Stevens S, Perera R, Lancaster T: Pharmacological interventions for smoking cessation: an overview and network meta-analysis. Cochrane Database Syst Rev. 2013 May 31;(5):CD009329. doi: 10.1002/14651858.CD009329.pub2. [PubMed: 23728690]
    • 14 . Slemmer JE, Martin BR, Damaj MI: Bupropion is a nicotinic antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):321-7. [PubMed: 10991997]
    • 15 . Johnston AJ, Ascher J, Leadbetter R, Schmith VD, Patel DK, Durcan M, Bentley B: Pharmacokinetic optimisation of sustained-release bupropion for smoking cessation. Drugs. 2002;62 Suppl 2:11-24. doi: 10.2165/00003495-200262002-00002. [PubMed: 12109932]
    • 16 . Pandhare A, Pappu AS, Wilms H, Blanton MP, Jansen M: The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors. Neuropharmacology. 2017 Feb;113(Pt A):89-99. doi: 10.1016/j.neuropharm.2016.09.021. Epub 2016 Sep 24. [PubMed: 27671323]
    • 17 . Ahern TH, Javors MA, Eagles DA, Martillotti J, Mitchell HA, Liles LC, Weinshenker D: The effects of chronic norepinephrine transporter inactivation on seizure susceptibility in mice. Neuropsychopharmacology. 2006 Apr;31(4):730-8. doi: 10.1038/sj.npp.1300847. [PubMed: 16052243]
    • 18 . Roose SP, Dalack GW, Glassman AH, Woodring S, Walsh BT, Giardina EG: Cardiovascular effects of bupropion in depressed patients with heart disease. Am J Psychiatry. 1991 Apr;148(4):512-6. doi: 10.1176/ajp.148.4.512. [PubMed: 1900980]
    • 19 . Benowitz NL, Pipe A, West R, Hays JT, Tonstad S, McRae T, Lawrence D, St Aubin L, Anthenelli RM: Cardiovascular Safety of Varenicline, Bupropion, and Nicotine Patch in Smokers: A Randomized Clinical Trial. JAMA Intern Med. 2018 May 1;178(5):622-631. doi: 10.1001/jamainternmed.2018.0397. [PubMed: 29630702]
    • 20 . Wang GJ, Tomasi D, Volkow ND, Wang R, Telang F, Caparelli EC, Dunayevich E: Effect of combined naltrexone and bupropion therapy on the brain's reactivity to food cues. Int J Obes (Lond). 2014 May;38(5):682-8. doi: 10.1038/ijo.2013.145. Epub 2013 Aug 8. [PubMed: 23924756]
    • 21 . Greenway FL, Fujioka K, Plodkowski RA, Mudaliar S, Guttadauria M, Erickson J, Kim DD, Dunayevich E: Effect of naltrexone plus bupropion on weight loss in overweight and obese adults (COR-I): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial. Lancet. 2010 Aug 21;376(9741):595-605. doi: 10.1016/S0140-6736(10)60888-4. Epub 2010 Jul 29. [PubMed: 20673995]
    • 22 . Reece AS: Hypothalamic opioid-melanocortin appetitive balance and addictive craving. Med Hypotheses. 2011 Jan;76(1):132-7. doi: 10.1016/j.mehy.2010.09.002. [PubMed: 20926200]
    • 23 . Arias HR: Is the inhibition of nicotinic acetylcholine receptors by bupropion involved in its clinical actions? Int J Biochem Cell Biol. 2009 Nov;41(11):2098-108. doi: 10.1016/j.biocel.2009.05.015. Epub 2009 Jun 2. [PubMed: 19497387]
    • 24 . Dailymed: Contrave (bupropion + naltrexone) [Link]
    • 25 . The Canadian Network for Mood and Anxiety Treatments (CANMAT) task force recommendations for the management of patients with mood disorders and comorbid attention-deficit/hyperactivity disorder [File]

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