What are the recommended medications for smoking cessation?

Recommended Medications for Smoking Cessation

The preferred primary therapies for smoking cessation are combination nicotine replacement therapy (NRT) or varenicline, with varenicline showing superior efficacy for maintaining long-term abstinence. 1, 2

First-Line Pharmacotherapy Options

Preferred Primary Therapies

• Combination NRT: Nicotine patch (long-acting) plus a short-acting NRT (lozenge, gum, inhaler, or nasal spray) for breakthrough cravings 1

  • Standard dosing: 21 mg patch plus short-acting NRT for 12 weeks
  • For inadequate response, consider increasing to 35 or 42 mg patch 1
  • Blood nicotine levels from NRT are significantly lower than from cigarettes, making toxicity rare even when used with occasional smoking 1

• Varenicline: A partial agonist at α4β2 nicotinic acetylcholine receptors 3, 4

  • Initiate 1-2 weeks before quit date with dose titration:
    • 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
  • Mechanism: Reduces withdrawal symptoms while blocking rewarding effects of nicotine if smoking occurs 3, 5
  • Superior efficacy compared to bupropion and NRT in clinical trials 2, 6

Subsequent Therapy Options

• Bupropion (with or without NRT): An atypical antidepressant that inhibits norepinephrine and dopamine reuptake 6
  • Initiate 1-2 weeks before quit date:
    • Days 1-3: 150 mg once daily
    • Day 4-12 weeks: 150 mg twice daily if tolerated (maximum 300 mg daily) 1
  • Consider for patients who failed or cannot use the preferred therapies 1
  • May be particularly beneficial for patients with history of depression 1

Comparative Efficacy

• Varenicline demonstrates significantly higher continuous abstinence rates compared to bupropion (OR = 1.60,95% CI: 1.22-2.12) at 52 weeks 2
• In clinical trials, varenicline showed abstinence rates of 21.9-34.6% at 52 weeks compared to lower rates with placebo 5
• Combination NRT approaches show comparable efficacy to varenicline in some studies but generally lower long-term abstinence rates 1

Important Safety Considerations

Varenicline

• Common side effect: Nausea (may need management especially during cancer chemotherapy) 1
• Contraindicated in patients with brain metastases due to seizure risk 1
• Monitor for neuropsychiatric symptoms, though recent large trials show no significant increase in these events compared to nicotine patch or placebo 1

Bupropion

• Contraindicated in patients with:
  • Seizure risks (stroke, brain metastases)
  • Those taking MAO inhibitors (risk of hypertensive reactions)
  • Patients taking tamoxifen
  • Closed-angle glaucoma 1
• Side effects include disturbed sleep, dry mouth, headaches, and nausea 1

NRT

• Generally well-tolerated with minimal side effects 1
• Can be safely used even with occasional smoking during quit attempts 1

Treatment Duration and Follow-up

• Minimum recommended duration: 12 weeks for combination NRT or varenicline 1
• May extend therapy to 6 months-1 year to promote continued cessation 1
• Follow-up recommended within 2-3 weeks of starting therapy to assess efficacy and manage side effects 1
• Additional follow-up at minimum 12-week intervals during therapy 1

Practical Implementation Tips

• Pharmacotherapy should always be combined with behavioral counseling for optimal results 1
• If initial therapy fails, switch to the other primary therapy option before trying subsequent options 1
• Dose adjustments may be necessary based on side effects and efficacy 1
• Nicotine withdrawal symptoms typically peak within 1-2 weeks of quitting and then subside 1
• Encourage continued therapy through brief slips; patients who don't quit immediately may quit later 1

Special Considerations

• For patients with psychiatric disorders, both varenicline and bupropion have been shown to be safe in large clinical trials 1
• For perioperative patients, smoking cessation should occur as far in advance as feasible, though cancer surgery should not be delayed based on smoking status 1
• Higher-dose nicotine patch therapy (>25 mg/day) may provide incremental benefit for heavy smokers 1