Description

Simple

A medication used treat mood disorders, such as depression, and nicotine addiction.

Clinical

A norepinephrine and dopamine reuptake inhibitor used in the treatment of major depressive disorder (MDD), seasonal affective disorder (SAD), and as an aid to smoking cessation.

Overview

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 cessation. Bupropion exerts its pharmacological effects by weakly inhibiting the enzymes involved in the uptake of the neurotransmitters norepinephrine and dopamine from the synaptic cleft, therefore prolonging their duration of action within the neuronal synapse and the downstream effects of these neurotransmitters. More specifically, bupropion binds to the norepinephrine transporter (NET) and the dopamine transporter (DAT).[8,12]

Bupropion was originally classified as an "atypical" antidepressant because it does not exert the same effects as the classical antidepressants such as Monoa... Read more

Pharmacology

Indication

Bupropion is indicated for the treatment of major depressive disorder (MDD), seasonal affective disorder (SAD), and as an aid to smoking cessation.

When used in combination with [naltrexone] as the marketed product ContraveⓇ, bupropion is indicated as an adjunct to a reduced-calorie diet and inc... Read more

Pharmacodynamic

Bupropion is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitors, or other known antidepressant agents. Compared to classical tricyclic antidepressants, Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine. In addition, B... Read more

Mechanism of action

Bupropion is a norepinephrine/dopamine-reuptake inhibitor (NDRI) that exerts its pharmacological effects by weakly inhibiting the enzymes involved in the uptake of the neurotransmitters norepinephrine and dopamine from the synaptic cleft, therefore prolonging their duration of action within the neur... Read more

Absorption

Bupropion is currently available in 3 distinct, but bioequivalent formulations: immediate release (IR), sustained-release (SR), and extended-release (XL).

**Immediate Release Formulation**
In humans, following oral administration of bupropion hydrochloride tablets, peak plasma bupropion concent... Read more

Protein binding

In vitro tests show that bupropion is 84% bound to human plasma proteins at concentrations up to 200 mcg per mL. The extent of protein binding of the hydroxybupropion metabolite is similar to that for bupropion, whereas the extent of protein binding of the threohydrobupropion metabolite is about hal... 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 formation of a glycine conjugate of metachlorobenzoic acid, which is then excreted as the major urinary metabolite. Following oral administration of 200 mg of 14C-bupropion in humans, 87% and 10% of... Read more

Toxicity

Symptoms of overdose include seizures, hallucinations, loss of consciousness, tachycardia, and cardiac arrest.

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 34%
  • Kind: placebo
    • Percent: 26%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 31.9
  • Kind: placebo
    • Percent: 22.2
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 27.6
  • Kind: placebo
    • Percent: 18.4
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 26
  • Kind: placebo
    • Percent: 17.3
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 15%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 23%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 25.7
  • Kind: placebo
    • Percent: 22.2
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 25%
  • Kind: placebo
    • Percent: 23%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 23%
  • Kind: experimental
    • Percent: 11%
  • Clinical Trial
    Nausea and vomiting US
  • Kind: experimental
    • Percent: 22.9
  • Kind: placebo
    • Percent: 18.9
  • Clinical Trial
    Excessive sweating US
  • Kind: experimental
    • Percent: 22.3
  • Kind: placebo
    • Percent: 14.6
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 22.3
  • Kind: placebo
    • Percent: 16.2
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 21.1
  • Kind: placebo
    • Percent: 7.6
  • Clinical Trial
    Weight Gain US
  • Kind: experimental
    • Percent: 21%
  • Kind: experimental
    • Percent: 11%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 13%
  • Clinical Trial
    Sedation US
  • Kind: experimental
    • Percent: 19.8
  • Kind: placebo
    • Percent: 19.5
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 19%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 18.6
  • Kind: placebo
    • Percent: 15.7
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 17%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 16%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 14.6
  • Kind: placebo
    • Percent: 10.3
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Nasopharyngitis US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 12%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: 10.8
  • Kind: placebo
    • Percent: 8.6
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Upper Respiratory Tract Infection US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 8.4
  • Kind: placebo
    • Percent: 4.9
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 6.5
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Hostility US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • 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. Co-administration with alcohol may result in neuropsychiatric adverse effects and potentiation of CNS depressant effects.

    Take with or without food. Co-administration with food does not significantly affect pharmacokinetics.