Bupropion Dosing for Smoking Cessation
The recommended dosing of bupropion (Wellbutrin/Zyban) for smoking cessation is 150 mg once daily for the first 3 days, followed by 150 mg twice daily for 7-12 weeks, with treatment initiated 1-2 weeks prior to the target quit date. 1
Standard Dosing Protocol
The optimal dosing schedule for bupropion in smoking cessation follows this pattern:
- Initiation phase: Begin 1-2 weeks before the target quit date
- Days 1-3: 150 mg orally once daily (morning)
- Day 4 onward: 150 mg orally twice daily (maximum 300 mg per day)
- Duration: Continue for 7-12 weeks total 1
Administration Considerations
- Maximum daily dose should not exceed 300 mg
- Doses should be taken at least 8 hours apart to minimize the risk of seizures
- Morning and afternoon dosing is preferred (avoid evening doses to prevent insomnia)
- No dose adjustment is needed based on smoking status 2
Special Populations
- Hepatic impairment: For patients with mild to moderate hepatic cirrhosis, consider reducing the dose or frequency. For severe hepatic cirrhosis, the maximum dose should be significantly reduced due to substantially increased bupropion exposure (approximately 70% higher Cmax and 3-fold higher AUC) 2
- Elderly patients: No specific dose adjustment is required based on age alone, though some studies suggest elderly patients may be at increased risk for accumulation of bupropion and its metabolites 2
Contraindications
Bupropion is contraindicated in patients with:
- Seizure disorders
- Current or prior diagnosis of bulimia or anorexia nervosa
- Use of MAO inhibitors within the past 14 days
- Abrupt discontinuation of alcohol, benzodiazepines, or antiepileptic drugs
- Severe hepatic cirrhosis (use with extreme caution if necessary)
- History of bipolar disorder 1
Efficacy and Comparison with Other Treatments
Bupropion has demonstrated effectiveness for smoking cessation with:
- 12-month abstinence rates of approximately 30.3% compared to 15.6% with placebo 3
- Similar efficacy to single-form nicotine replacement therapy (NRT)
- Less effectiveness than combination NRT or varenicline 4
- Potential benefit when combined with NRT, though evidence is mixed 1, 4
Common Adverse Effects
- Insomnia (most common)
- Dry mouth
- Headache
- Nausea
- Anxiety 5
Serious Adverse Effects
- Seizures (risk approximately 0.1% at recommended doses)
- Hypersensitivity reactions (approximately 0.1%)
- Neuropsychiatric symptoms including depression and suicidal ideation (uncommon but requires monitoring) 1, 5
Clinical Pearls
- For patients who fail to quit in the first 3 weeks of treatment, continuing bupropion therapy may still result in successful late-term smoking cessation 6
- The efficacy of bupropion appears to be independent of its antidepressant effect 1
- Combining bupropion with behavioral support significantly increases cessation success rates
- Cost-effectiveness analyses suggest bupropion is a cost-effective intervention for smoking cessation 7
Remember that bupropion's effectiveness for smoking cessation is well-established, with high-certainty evidence supporting its use as a first-line pharmacotherapy option alongside NRT and varenicline 4.