Bupropion Formulations for Smoking Cessation
Bupropion for smoking cessation is available exclusively as a sustained-release (SR) formulation, dosed at 150 mg twice daily for a total of 300 mg per day. 1
Formulation Specifics
Bupropion comes in sustained release tablets when used for smoking cessation. 1 This is the only formulation that has been studied and approved for this indication, distinguishing it from the extended-release (XL) formulation used primarily for depression. 2
Dosing Algorithm for Smoking Cessation
Standard Dosing Protocol
- Start with 150 mg once daily for 3 days, then increase to 150 mg twice daily (300 mg total daily dose). 2, 3
- Begin treatment 1-2 weeks before the target quit date to allow therapeutic drug levels to establish before the cessation attempt. 2, 3
- Continue treatment for 7-12 weeks, with formal efficacy assessment at the end of this period. 1, 2, 3
- Maximum dose must not exceed 300 mg per day for smoking cessation to minimize seizure risk. 2, 3
Why Sustained-Release Matters
The SR formulation requires twice-daily dosing, which differs from the XL formulation (used for depression) that can be given once daily. 2 For smoking cessation specifically, the evidence base exclusively supports the SR formulation at 150 mg twice daily. 1, 4, 5, 6
Dose Adjustments for Special Populations
Hepatic Impairment
- For moderate to severe hepatic impairment: maximum 150 mg daily (one tablet total), not the standard 300 mg. 2, 3
Renal Impairment
- For moderate to severe renal impairment: reduce total daily dose by half (75 mg twice daily instead of 150 mg twice daily). 2, 3
Older Adults
- Start with 37.5 mg every morning, increase by 37.5 mg every 3 days as tolerated, with a maximum of 150 mg twice daily. 2
- Administer the second dose before 3 p.m. to minimize insomnia risk. 2
Critical Safety Considerations
Absolute Contraindications
- Seizure disorders (risk approximately 1 in 1,000, similar to other antidepressants). 1, 3
- Current MAOI use or within 14 days of discontinuing MAOIs. 2, 3
- Eating disorders (anorexia nervosa or bulimia). 7
- Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs. 7
Monitoring Requirements
- Monitor for neuropsychiatric adverse effects, especially in patients younger than 24 years. 2, 3
- Monitor blood pressure, as bupropion should be avoided in uncontrolled hypertension. 2, 3
- Watch for allergic reactions (risk approximately 1 in 1,000 to 1 in 10,000). 1, 3
Clinical Efficacy and Behavioral Support
Bupropion SR improves 12-month sustained abstinence rates by approximately 9-10 percentage points and reduces withdrawal symptom severity. 1, 3, 4 The efficacy appears independent of its antidepressant effect. 1, 3
Evidence for bupropion effectiveness comes primarily from studies that included behavioral support, specifically medium to heavy smokers (≥15 cigarettes per day) receiving frequent counseling sessions. 1, 3 While the medication is effective, combining it with structured behavioral support optimizes outcomes. 4
Common Pitfalls to Avoid
- Do not use the XL formulation for smoking cessation—the evidence base and dosing regimen are specific to the SR formulation. 1, 2
- Do not exceed 300 mg daily for smoking cessation, as this increases seizure risk without improving efficacy for this indication. 2, 3
- Do not prescribe the full course upfront—provide 4 weeks initially, then repeat only if the quit attempt is continuing, as many patients fail or relapse within the first few weeks. 1
- Do not forget to start 1-2 weeks before the quit date—this timing is essential for therapeutic levels. 2, 3
Special Clinical Scenarios
Bupropion may be particularly beneficial for patients with comorbid depression who want to quit smoking, addressing both conditions simultaneously. 2, 3 It has also shown promise in patients with anxiety disorders like PTSD, though this requires careful monitoring when combined with other psychotropic medications. 8
If no significant progress toward abstinence occurs by weeks 7-12, reassess the treatment plan rather than continuing indefinitely. 3