Bupropion

Bupropion is a medication that is primarily used as an antidepressant and smoking cessation aid. It works by increasing the levels of the neurotransmitters norepinephrine and dopamine in the brain, which can help improve mood and reduce cravings for nicotine. Bupropion is also sometimes used to treat attention deficit hyperactivity disorder (ADHD) and as an aid for weight loss. It is sold under several brand names, including Wellbutrin, Zyban, and Aplenzin. Bupropion is available in different forms, including tablets, extended-release tablets, and extended-release capsules. It is typically taken by mouth, with or without food, as directed by a doctor or healthcare provider.

Active Ingredient
  • Bupropion (as hydrochloride; hydrobromide for Aplenzin)
Brand Names
  • Wellbutrin (IR)
  • Wellbutrin SR
  • Wellbutrin XL
  • Zyban
  • Aplenzin (bupropion HBr)
  • Forfivo XL
Forms & Strengths
  • Immediate-release tablets (HCl): 75 mg, 100 mg
  • Sustained-release (SR) tablets: 100 mg, 150 mg, 200 mg
  • Extended-release (XL) tablets: 150 mg, 300 mg, 450 mg (e.g., Forfivo XL 450 mg QD)
  • Aplenzin ER (HBr): 174 mg, 348 mg, 522 mg (≈ HCl 150/300/450 mg)
  • Zyban SR: 150 mg
Onset / Half-life
  • Tmax (peak): IR ~2 h; SR ~3 h; XL ~5 h
  • Elimination half-life: bupropion ~21 h; active metabolite hydroxybupropion ~20 h (others up to ~37 h)
  • Antidepressant response typically noted after 1–2 weeks; fuller effect by 4–6 weeks

Warnings

  • Antidepressants: ↑ risk of suicidality in young patients—monitor mood/behavior
  • Seizure risk is dose-related; contraindicated in seizure disorder and in current/prior bulimia or anorexia nervosa
  • Avoid abrupt withdrawal of alcohol/benzodiazepines/sedatives (seizure risk)
  • Do not use with MAOIs or within 14 days of stopping an MAOI
  • Hypertension/↑ BP (risk ↑ with nicotine patch)
  • Possible activation: insomnia, agitation, anxiety—dose early in the day
  • Mania/hypomania activation in bipolar disorder
  • Hypersensitivity reactions (rare)

Monitoring

  • Blood pressure (baseline and periodically)
  • Mood/suicidality—especially early in treatment or dose changes
  • Sleep/activation (insomnia, agitation); dose timing adherence
  • Weight/appetite changes
  • Seizure risk factors (history, alcohol/sedative use)
  • Concomitant drugs metabolized by CYP2D6 (bupropion is a CYP2D6 inhibitor)

Indications

  • Approved: Major depressive disorder (MDD)
  • Approved: Seasonal affective disorder (SAD) — XL/Aplenzin
  • Approved: Smoking cessation aid — Zyban
  • Off-label: Attention-deficit/hyperactivity disorder (ADHD) in adults
  • Off-label: SSRI-induced sexual dysfunction (adjunct)
  • Off-label: Bipolar depression (adjunct with mood stabilizer)

Guides & Questions