Bupropion, Wellbutrin®, Zyban®

Brand name

  • Wellbutrin®
  • Zyban®
  • Aplenzin®

Drug Class

  • Antidepressant

Preparations

  • Tablets: 75 mg, 100 mg, 300 mg
  • Wellbutrin
  • Wellbutrin SR
  • Wellbutrin XL

Indications

  • Antidepressant
  • ADHD
  • ADD
  • Smoking cessation

Pharmacology

  • The exact mechanism of the antidepressant action of bupropion is not known, but is presumed to be related to noradrenergic and/or dopaminergic mechanisms

Metabolism

  • Bupropion is metabolized in liver and the following enzymes are involved:
    • CYP-2D6 (inhibitor)
    • CYP-2B6

Dosing

  • Tablets: 100 mg, 150 mg
  • The usual recommended dose is 100 mg to 150 mg once daily.
  • Maximum daily dose: 300 mg, divided 150 mg BID
  • Do not exceed the maximum dose of 300 mg per day, and do not take a single dose greater than 150 mg.

Drug Interactions

  • Alcohol
  • Amantadine
  • Antihistamines (e.g,. doxylamine, diphenhydramine, hydroxyzine)
  • Anti-malarial medications (e.g., chloroquine, mefloquine)
  • Antipsychotics (e.g., chlorpromazine, haloperidol, risperidone, thioridazine)
  • Aripiprazole
  • Atomoxetine
  • Beta-blockers (e.g., metoprolol, propranolol, timolol)
  • Captopril
  • Carbamazepine
  • Clopidogrel
  • Codeine
  • Corticosteroids (e.g., prednisone)
  • Cyclophosphamide
  • Doxorubicin
  • Dextromethorphan
  • Droperidol
  • Fosphenytoin
  • HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delaviridine, efavirenz, etravirine, nevirapine)
  • irinotecan
  • Ketamine
  • Levodopa
  • Linezolid
  • Lithium
  • Lopinavir
  • Methadone
  • Methamphetamine
  • Methotrimeprazine
  • Mexiletine
  • Mirtazapine
  • Monoamine oxidase inhibitors (MAO inhibitors; e.g., phenelzine, tranylcypromine, moclobemide, selegilene) – bupropion should not be started until at least 14 days after MAO inhibitors are stopped
  • Nicotine replacement therapy (e.g., nicotine patch)
  • Orphenadrine
  • Nefazodone
  • Phenobarbital
  • Phenytoin
  • Pimozide
  • Primidone
  • Procainamide
  • Promethazine
  • Propafenone
  • Quinolone antibiotics (e.g., ciprofloxacin, moxifloxacin)
  • Rifampin
  • Ritonavir
  • Selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
  • Sorafenib
  • Tamoxifen
  • Tetrabenazine
  • Theophylline
  • Thioridazine – bupropion should not be started until at least 14 days after thioridazine is stopped
  • Ticlopidine
  • Tramadol
  • Tricyclic antidepressants (e.g., nortriptyline, imipramine, desipramine)
  • Venlafaxine

Adverse Effects

HEENT:

  • blurred vision
  • change in sense of taste
  • dizziness
  • drowsiness
  • dryness of mouth

Cardiovascular:

  • feeling of fast or irregular heartbeat

Gastrointestinal:

  • abdominal pain
  • constipation
  • decrease in appetite
  • nausea or vomiting
  • Dysphagia
  • Thirst disturbance
  • Liver damage/jaundice

Urogenital:

  • frequent need to urinate
  • increased sweating
  • decrease in sexual function

MSK:

  • muscle pain

Neurological/Psychiatry:

  • trembling or shaking
  • trouble sleeping
  • unusual feeling of well-being

Endocrine:

  • SIADH

 

If you experience any of the following symptoms, stop taking bupropion and call your doctor immediately or get emergency medical treatment:

  • fever
  • rash or blisters
  • itching
  • hives
  • swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  • hoarseness
  • difficulty breathing or swallowing
  • chest pain

Contraindications

  • Known hypersensitivity to bupropion or other ingredients of WELLBUTRIN
  • Seizure disorder
  • Current or prior diagnosis of bulimia or anorexia nervosa
  • Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, antiepileptic drugs
  • Monoamine Oxidase Inhibitors (MAOIs): Do not use MAOIs with WELLBUTRIN or within 14 days of stopping treatment with WELLBUTRIN.
  • Do not use WELLBUTRIN within 14 days of stopping an MAOI

Pregnancy and Breastfeeding

  • The safety of bupropion during pregnancy has not been established.
  • Bupropion passes into breast milk. Because this medication presents risks to breast-feeding infants, a decision should be made whether to discontinue breast-feeding or to discontinue bupropion

Precautions

  • This medication may increase the risk of seizures
  • Increased risk of suicide or suicidal ideation
  • Increased risk of agitated behaviour
  • Treatment with Bupropion can result in elevated blood pressure and hypertension
  • Treatment with bupropion could cause a variety of neuropsychiatric signs and symptoms, including delusions, hallucinations, psychosis, concentration disturbance, paranoia, and confusion. In such cases, does reduction is suggested.

Symptoms of overdose may include the following:

  • seizure
  • hallucinating (seeing things or hearing voices that do not exist)
  • loss of consciousness
  • rapid or pounding heartbeat

Warning

  • Some people have reported symptoms such as changes in behavior, hostility, agitation, depressed mood, and suicidal thoughts while taking bupropion to stop smoking. The role of bupropion in causing these mood changes is unclear since people who quit smoking with or without medication may experience changes in their mental health due to nicotine withdrawal. However, some of these symptoms occurred in people who were taking bupropion and continued to smoke. Some people had these symptoms when they began taking bupropion, and others developed them after several weeks of treatment or after stopping bupropion.
  • These symptoms have occurred in people without a history of mental illness and have worsened in people who already had a mental illness. Tell your doctor if you have or have ever had depression, bipolar disorder (mood that changes from depressed to abnormally excited), schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions), or other mental illnesses.

Section

This document is prepared by the “Mental Health for All” team. This document is provided for information purposes only and does not necessarily represent endorsement by or an official position of the Essentials of Medicine. Advice on the treatment or care of an individual patient should be obtained through consultation with a physician who has examined that patient or is familiar with that patient’s medical history.

error: Content is protected !!