Bupropion
Norepinephrine-dopamine reuptake inhibitor (NDRI) atypical antidepressant. Indications: MDD, seasonal affective disorder, smoking cessation (Zyban). No sexual dysfunction, minimally sedating.
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WHAT IS BUPROPION?
Detailed overview
Bupropion is an atypical antidepressant developed by GlaxoSmithKline (Wellbutrin, FDA 1989). Its NDRI (norepinephrine-dopamine reuptake inhibitor) and nicotinic receptor antagonist mechanism distinguishes from SSRI/SNRI: no sexual dysfunction or weight gain, not sedating, supports smoking cessation (Zyban brand FDA 1997). FDA-approved indications: MDD, seasonal affective disorder (SAD), smoking cessation. Jorenby 1999 (NEJM PMID 10080847) trial showed 1-year abstinence 30.3% on bupropion+nicotine patch, vs 16.4% placebo. Hewett 2010 meta-analysis of 6 MDD trials demonstrated SSRI-comparable efficacy with better tolerability.
ATC code
N06AX12
Prescription
Prescription only (Rx)
Mechanism
NDRI + nicotinic receptor antagonist
Half-life
~21 h (hydroxybupropion metabolite 20-37 h)
Onset
1-2 weeks (motivation, focus), 4-6 weeks (full AD effect)
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 8
- BOXED WARNING: increased risk of suicidal thoughts and behavior in children, adolescents and young adults (<25 yrs) at treatment start or dose change; close monitoring required.
- Dose-dependent seizures: ~0.1% at standard dose (≤300 mg/day), ~0.4% at 450 mg/day, exponential above; the hallmark serious risk. Respect max dose (SR 400, XL 450 mg/day); do not crush tablets.
- Insomnia (15-20%), dry mouth (10-15%) and headache (~10%); to limit insomnia, take the last dose by early afternoon (around 5 pm).
- Agitation, anxiety, restlessness and tremor, especially in the first weeks; an activating, non-sedating profile with a narrow therapeutic window.
- Blood pressure elevation (dose-dependent NDRI effect); monitor BP at initiation, especially when combined with nicotine replacement or other sympathomimetics.
- Weight loss / reduced appetite (5-8%); weight-neutral or weight-reducing unlike SSRIs (often a benefit, but a concern in eating disorders).
- Neuropsychiatric events: may trigger mania/hypomania in bipolar patients (NDRI activation); rarely psychotic symptoms, hallucinations or paranoia, mainly at high doses.
- Hypersensitivity reactions: rash, urticaria, pruritus; rarely serum-sickness-like reaction or Stevens-Johnson syndrome; discontinue if rash persists or worsens.
Contraindications · 4
- Seizure disorder (epilepsy) history or known predisposition
- Eating disorders (bulimia, anorexia nervosa) – elevated seizure risk
- Acute alcohol or benzodiazepine withdrawal (seizure risk)
- Concurrent or within-14-days MAOi use (hypertensive crisis)
Related Pharmaceuticals
Same therapeutic category
Studies
Related research and clinical findings
A randomized placebo-controlled clinical trial of 5 smoking cessation pharmacotherapies.
Piper ME, Smith SS, Schlam TR, Fiore MC, Jorenby DE, Fraser D, Baker TB
Bupropion versus paroxetine for the treatment of major depressive disorder
Weihs KL, Settle EC Jr, Batey SR et al.
Comparative efficacy and acceptability of 21 antidepressant drugs for major depressive disorder
Cipriani A, Furukawa TA, Salanti G et al.
Bupropion for the treatment of seasonal affective disorder.
Niemegeers P, Dumont GJ, Patteet L, Neels H, Sabbe BG
Effects of naltrexone-bupropion on weight loss (COR-I trial)
Greenway FL, Fujioka K, Plodkowski RA et al.
Bupropion and seizure risk: a systematic review
Davidson J.
The effects of the adjunctive bupropion on male sexual dysfunction induced by a selective serotonin reuptake inhibitor: a double-blind placebo-controlled and randomized study.
Safarinejad MR
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Educational drug info from official sources (PubMed, FDA, EMA). Does NOT replace medical consultation or the SmPC. Talk to your doctor!
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The information here is for educational and scientific purposes only. Medication use requires medical consultation and a prescription. The indications, dose ranges, and side effects listed here do NOT replace the official Summary of Product Characteristics (SmPC) or consultation with a physician. Do not start or stop any medication on your own. In an emergency, call your local emergency number.