Bupropion Dosage for Nicotine Detoxification
For smoking cessation, bupropion SR should be dosed at 150 mg once daily in the morning for the first 3 days, then increased to 150 mg twice daily (300 mg total daily dose) for 7-12 weeks, with treatment initiated 1-2 weeks before the target quit date. 1, 2
Standard Dosing Regimen
The titration schedule is critical for minimizing adverse effects while achieving therapeutic levels:
- Days 1-3: 150 mg once daily in the morning 1, 2
- Day 4 through Week 12: 150 mg twice daily (300 mg total daily dose) 1, 3, 2
- Maximum dose: 300 mg per day for smoking cessation (do not exceed to minimize seizure risk) 1, 2
The second daily dose should be administered before 3 PM to minimize insomnia risk. 2
Treatment Timeline and Duration
Begin bupropion 1-2 weeks prior to the target quit date to allow therapeutic drug levels to be established before cessation attempts. 1, 2, 4 This pre-quit initiation is essential for optimal efficacy.
Standard treatment duration is 7-12 weeks, with efficacy formally assessed after this period. 1, 3, 2 Consider extending treatment to 6 months-1 year for patients who achieve successful cessation to prevent relapse. 3
Efficacy and Clinical Context
Bupropion SR increases 12-month abstinence rates by approximately 9-10 percentage points compared to placebo, with long-term abstinence rates of 30.3% versus 15.6% for placebo. 5, 4 While effective, varenicline remains the preferred first-line agent due to superior efficacy (nearly 3-fold increase in quit rates versus placebo), with bupropion serving as an effective alternative when varenicline is contraindicated or not tolerated. 6, 3
Combination Therapy
Bupropion can be safely combined with nicotine replacement therapy (NRT) for enhanced efficacy. 1, 3 The combination of bupropion SR plus nicotine patch achieved 35.5% abstinence at 12 months versus 30.3% for bupropion alone, though this difference was not statistically significant. 4
Common Side Effects and Management
The most frequent adverse effects include:
- Insomnia (most common) - managed by ensuring second dose is before 3 PM 1, 2, 7
- Dry mouth - generally transient and resolves without intervention 1, 7
- Headache 7, 4
- Nausea 7
These side effects are typically mild to moderate and often resolve quickly without therapeutic intervention. 7 If necessary, they can be managed by dose reduction. 7
Critical Contraindications and Precautions
Absolute contraindications include:
- History or risk of seizure disorders (bupropion lowers seizure threshold) 1, 2
- Eating disorders (bulimia or anorexia nervosa - increased seizure risk) 1, 2
- Concurrent MAO inhibitor use or within 14 days of discontinuing MAOIs 1, 2
- Concurrent tamoxifen use (drug interaction) 2
- Severe hepatic cirrhosis 2
- Uncontrolled hypertension 2
Seizure risk is approximately 0.1% (1 in 1,000) when patients are properly screened and the maximum dose of 300 mg/day is not exceeded. 5, 7
Dose Adjustments for Special Populations
- Moderate to severe hepatic impairment: Maximum 150 mg daily (single dose) 2
- Moderate to severe renal impairment (GFR <90 mL/min): Reduce total daily dose by 50% 2
- Older adults: Consider starting at 37.5 mg daily and titrating by 37.5 mg every 3 days as tolerated 2
Monitoring and Follow-Up
- First follow-up: Within 2-3 weeks of starting medication to assess tolerability and smoking status 3
- Subsequent follow-up: At 12 weeks and at end of therapy 3
- Monitor for: Neuropsychiatric symptoms (depression, agitation, behavioral changes), blood pressure, and seizure activity 2
Clinical Pearls
Bupropion may be particularly beneficial for patients with comorbid depression who want to quit smoking, as it addresses both conditions simultaneously through noradrenergic/dopaminergic pathways. 2
Bupropion significantly reduces weight gain during smoking cessation compared to placebo (1.7 kg versus 2.1 kg at 7 weeks). 4
If treatment fails after 7-12 weeks, consider switching to varenicline or intensifying behavioral therapy rather than continuing ineffective treatment. 3