What is the role of Wellbutrin (bupropion) in smoking cessation?

Bupropion (Wellbutrin) for Smoking Cessation

Bupropion is an effective first-line pharmacotherapy for smoking cessation, with clinical trials showing it helps approximately one in five smokers successfully quit smoking. 1

Mechanism and Efficacy

• Bupropion works primarily through inhibition of dopamine reuptake into neuronal synaptic vesicles and is also a weak noradrenaline reuptake inhibitor 1
• The sustained-release (SR) formulation is specifically approved for smoking cessation under the brand name Zyban 2
• Unique features of bupropion for smoking cessation:
  • Requires prescription, bringing smoking cessation treatment back to medical settings
  • Treatment begins 1-2 weeks before the target quit date 3
  • Non-nicotine based option for those who cannot or prefer not to use nicotine replacement therapy

Dosing and Administration

• Start with lower doses (150 mg once daily) for 3 days, then increase to 150 mg twice daily 4
• Maximum dose should not exceed 300 mg daily for smoking cessation
• Administer the second dose before 3 p.m. to minimize insomnia risk 4
• Continue treatment for 7-12 weeks after the quit date

Patient Selection

Good Candidates:

• Smokers motivated to quit
• Those who have failed nicotine replacement therapy
• Patients with depression history (bupropion has shown efficacy regardless of depression history) 5
• Those concerned about weight gain during smoking cessation 2

Contraindications:

• Seizure disorders or conditions that lower seizure threshold 6
• Current use of MAO inhibitors 4
• History of anorexia or bulimia 6
• Abrupt discontinuation of alcohol, benzodiazepines, or barbiturates 6
• Uncontrolled hypertension 4
• Severe hepatic impairment 4

Monitoring and Safety

• Regular blood pressure monitoring is essential, especially during the first 12 weeks of treatment 4, 6
• Higher incidence of treatment-emergent hypertension when combined with nicotine replacement therapy (6.1% vs. 2.5% with bupropion alone) 6
• Risk of seizures (approximately 0.1% or 1/1000 patients) 6, 2
• Monitor for neuropsychiatric symptoms, particularly in younger patients 4

Common Side Effects

• Insomnia (most common)
• Dry mouth
• Anxiety/jitteriness
• Decreased appetite
• Headache 4, 1

Special Populations

Patients with Depression:

• Bupropion is effective for smoking cessation regardless of depression history 5
• May be particularly beneficial for smokers with current or past depression 5
• Can be safely added to SSRI treatment for patients with depression who want to quit smoking 7

Patients with Medical Conditions:

• Effective in patients with chronic obstructive pulmonary disease (COPD) 2
• Use with caution in patients with cardiovascular disease; monitor blood pressure closely 6
• Reduce dose by 50% in patients with moderate to severe renal impairment 4

Comparative Effectiveness

• Bupropion has shown similar or superior efficacy compared to nicotine replacement therapy in some studies 2
• Can be used in combination with nicotine patches for potentially greater efficacy, though with increased risk of hypertension 6

Practical Considerations

• Gradual tapering is recommended when discontinuing bupropion to minimize withdrawal symptoms 4
• Treatment duration of 7-12 weeks is standard, with longer durations potentially preventing relapse
• Cost-effectiveness has been demonstrated in various healthcare settings 3, 2