What are the recommended medications for smoking cessation?

Recommended Medications for Smoking Cessation

Varenicline and combination nicotine replacement therapy (NRT) are the most effective first-line medications for smoking cessation, with varenicline showing superior efficacy in clinical trials. 1

First-Line Medication Options

Preferred Primary Therapy Options:

1. Varenicline (Chantix)

   • Mechanism: Partial agonist at α4β2 nicotinic acetylcholine receptors
   • Reduces withdrawal symptoms and decreases satisfaction from smoking
   • Standard dosing:
     • Days 1-3: 0.5 mg once daily
     • Days 4-7: 0.5 mg twice daily
     • Weeks 2-12: 1 mg twice daily (if tolerated) 1
   • Efficacy: Doubles the chances of quitting at 6 months compared to placebo (RR 2.38) 2
   • Outperforms both bupropion (RR 1.52) and nicotine replacement therapy (RR 1.31) 2

2. Combination NRT

   • Nicotine patch (long-acting) + short-acting NRT (gum, lozenge, inhaler, or nasal spray)
   • Standard dosing: 21 mg patch + short-acting NRT for breakthrough cravings
   • For heavy smokers: Consider increasing to 35 or 42 mg patch if 21 mg is ineffective 1

Important Considerations for Medication Selection:

• Treatment duration: Minimum 12 weeks for initial quit attempt 1
• Follow-up: Within 2-3 weeks of starting therapy and periodically thereafter 1
• Varenicline contraindications: Brain metastases (seizure risk), use caution in patients with psychiatric disorders 1
• NRT safety: Blood nicotine levels from NRT are significantly lower than from cigarettes; nicotine toxicity is rare 1

Second-Line Medication Options

For patients who fail first-line therapy:

1. Bupropion SR (alone or with NRT)

   • Dosing:
     • Days 1-3: 150 mg once daily
     • Day 4-12 weeks: 150 mg twice daily (maximum 300 mg/day) 1
   • Contraindicated in patients with seizure risk, those taking MAO inhibitors, or those with closed-angle glaucoma 1

2. Extended treatment duration

   • Prolonged treatment with nicotine patch (>14 weeks) may be superior to standard duration 1
   • Therapy may be extended up to 6 months to 1 year to promote continued cessation 1

Common Side Effects and Management

• Varenicline: Nausea (30-40% of users), insomnia, abnormal dreams, headache 2

  • Nausea is typically mild to moderate and diminishes over time
  • Dose-dependent side effects may be reduced with lower doses 1
  • Flexible dosing strategy (average 1.3 mg/day) may maintain efficacy while reducing side effects 1

• NRT: Local irritation (patch site, mouth, throat), hiccups, dyspepsia 1

• Bupropion: Insomnia, dry mouth, headaches, nausea 1

Clinical Pearls and Pitfalls

• Neuropsychiatric concerns: Monitor for mood changes, agitation, or suicidal ideation with varenicline and bupropion, though recent evidence suggests these risks may be lower than initially thought 1, 2

• Withdrawal management: Nicotine withdrawal symptoms typically peak within 1-2 weeks of quitting; encourage continued therapy through brief slips 1

• Combination approach: Combining effective medications with counseling is superior to either treatment approach alone 1

• Treatment failures: If reduction efforts stall or abstinence seems unlikely, consider switching to a different pharmacotherapy 1

• Flexible dosing: For varenicline, lower doses (e.g., 0.5 mg daily to 1 mg twice daily) may reduce side effects while maintaining efficacy 1

• Extended therapy: Some patients may benefit from indefinite NRT to prevent relapse 1

By following these evidence-based recommendations and selecting appropriate pharmacotherapy based on patient factors, clinicians can significantly improve smoking cessation outcomes and reduce the substantial morbidity and mortality associated with tobacco use.