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

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
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Bupropion is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-Dinitrocatechol
The risk or severity of adverse effects can be increased when Bupropion is combined with 3,5-Dinitrocatechol.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Bupropion is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Bupropion is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Bupropion is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Bupropion.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Bupropion is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Bupropion.
Abacavir
Abacavir may decrease the excretion rate of Bupropion which could result in a higher serum level.
Abatacept
The metabolism of Bupropion can be increased when combined with Abatacept.
Abiraterone
The metabolism of Bupropion can be decreased when combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Bupropion which could result in a higher serum level.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Bupropion.
Aceclofenac
Aceclofenac may decrease the excretion rate of Bupropion which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Bupropion which could result in a higher serum level.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Bupropion.
Acepromazine
The risk or severity of adverse effects can be increased when Bupropion is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Bupropion is combined with Aceprometazine.
Acetaminophen
The metabolism of Acetaminophen can be decreased when combined with Bupropion.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Bupropion.
27 References
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  24. 24 . Dailymed: Contrave (bupropion + naltrexone) Link
  25. 25 . FDA Approved Drug Products: Wellbutrin XL® extended-release tablets Link
  26. 26 . FDA Approved Drug Products: Wellbutrin immediate-release tablets Link
  27. 27 . 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