What is the dosing regimen for bupropion (Wellbutrin) for smoking cessation?

Bupropion (Wellbutrin) Dosing for Smoking Cessation

The standard dosing regimen for bupropion in smoking cessation is 150 mg twice daily (300 mg total daily dose) of the sustained-release formulation, starting 1-2 weeks before the target quit date and continuing for 7-12 weeks. 1

Titration Schedule

• Start with 150 mg once daily for the first 3 days, then increase to 150 mg twice daily if tolerated 2, 1
• This gradual titration minimizes seizure risk while achieving therapeutic drug levels 1
• Begin treatment 1-2 weeks prior to the target quit date to allow therapeutic levels to establish before the cessation attempt 1, 3

Timing of Doses

• Administer the first dose in the morning and the second dose before 3 PM to minimize insomnia risk 1
• This timing is critical as bupropion has activating properties that can interfere with sleep if taken late in the day 1

Treatment Duration and Efficacy Assessment

• Continue treatment for 7-12 weeks after the quit date 1, 3
• Assess efficacy formally after this 7-12 week treatment period 4, 1
• Bupropion improves 12-month sustained abstinence rates by approximately 9-10 percentage points compared to placebo 3, 5
• When combined with intensive behavioral support, bupropion achieves abstinence rates of 9% above baseline 4

Critical Safety Considerations

Absolute contraindications include: 3, 6

• Any seizure disorder (seizure risk is approximately 1 in 1,000) 4
• Current or recent use of MAOIs (within 14 days) 1
• Eating disorders (bulimia or anorexia nervosa) 3
• Abrupt discontinuation of alcohol, benzodiazepines, or antiepileptic drugs 1
• Severe hepatic cirrhosis 3

Maximum dose must not exceed 300 mg per day for smoking cessation to maintain seizure risk at 0.1% 6, 1

Dose Adjustments for Special Populations

• Moderate to severe hepatic impairment: Maximum 150 mg daily (single dose) 1
• Moderate to severe renal impairment: Reduce total daily dose by 50% 1
• Older adults: Consider starting at 37.5 mg daily and titrating more gradually 1

Monitoring Requirements

• Monitor blood pressure and heart rate, especially during the first 12 weeks, as bupropion can cause elevations in both 1
• Screen for neuropsychiatric adverse effects, particularly in patients under 24 years old who have increased risk of suicidal thoughts (black box warning) 1
• Assess for uncontrolled hypertension before initiating, as this is a relative contraindication 1

Common Side Effects

• Insomnia and dry mouth are the most common adverse events, occurring significantly more frequently than placebo 6, 5
• These effects are generally transient and often resolve without intervention 6
• Headache, nausea, and anxiety may also occur, though anxiety can be difficult to distinguish from nicotine withdrawal symptoms 6

Clinical Pearls

• Bupropion may be particularly beneficial for patients with comorbid depression who want to quit smoking, addressing both conditions simultaneously 1
• Combination therapy with nicotine replacement therapy (NRT) can be used safely and may provide slightly higher abstinence rates than bupropion alone, though differences are not always statistically significant 2, 5
• Weight gain is typically less with bupropion compared to placebo during smoking cessation 2, 5
• The medication should always be combined with behavioral support for optimal outcomes, as published trials included smokers receiving frequent counseling sessions 4