What are the recommended medications for smoking cessation?

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Recommended Medications for Smoking Cessation

The first-line recommended medications for smoking cessation are combination nicotine replacement therapy (NRT) or varenicline, with varenicline showing superior efficacy for maintaining long-term abstinence. 1

First-Line Pharmacotherapy Options

Combination Nicotine Replacement Therapy (NRT)

  • Combination NRT involves using both a long-acting form (patch) plus a short-acting form (gum, lozenge, inhaler, or nasal spray) to manage both baseline cravings and breakthrough cravings 2, 1
  • Standard dosing typically includes a 21 mg patch plus a short-acting NRT for 12 weeks 1
  • NRT at normal doses has not been shown to negatively affect acute wound healing, making it valuable for perioperative smoking cessation 2

Varenicline

  • Varenicline is a partial agonist/antagonist with affinity and selectivity for α4β2 nicotinic acetylcholine receptors 3
  • Dosing: Start 1-2 weeks before quit date with dose titration (0.5 mg once daily, increasing to 1 mg twice daily if tolerated) 1, 4
  • Varenicline demonstrates significantly higher continuous abstinence rates compared to bupropion, with an odds ratio of 1.60 (95% CI: 1.22-2.12) at 52 weeks 1, 5
  • Mechanism of action: Reduces cravings/withdrawal symptoms while simultaneously blocking the rewarding effects of nicotine if smoking occurs 6, 7

Second-Line Option

Bupropion

  • Bupropion, an atypical antidepressant that inhibits norepinephrine and dopamine reuptake, may be considered for patients who failed or cannot use the preferred therapies 1, 5
  • Dosing regimen: 150 mg once daily for days 1-3, then 150 mg twice daily for days 4-12 weeks 1
  • Less effective than varenicline for maintaining abstinence 5, 7

Implementation Considerations

Treatment Duration and Follow-up

  • Minimum recommended duration for combination NRT or varenicline is 12 weeks, with possible extension to 6 months-1 year to promote continued cessation 2, 1
  • Follow-up should occur within 2-3 weeks of initiating therapy to assess efficacy and toxicity of pharmacotherapy 2
  • Subsequent follow-up should occur at no more than 12-week intervals during treatment 2

Behavioral Support

  • All pharmacotherapy regimens should always be paired with behavioral counseling for optimal results 2, 1
  • Combining pharmacotherapy with behavioral therapy has been shown to enhance success rates 2

Safety Considerations

  • Varenicline: Common side effects include nausea (16.3%-41.9%) and should be avoided in patients with brain metastases due to seizure risk 2, 4, 3
  • Bupropion: Contraindicated in patients with seizure risks, those taking MAO inhibitors, and patients taking tamoxifen 1
  • Common side effects of bupropion include disturbed sleep, dry mouth, headaches, and nausea 1, 3

Treatment Algorithm

  1. First attempt: Start with either:

    • Combination NRT (patch + short-acting form) for 12 weeks 2, 1, OR
    • Varenicline (1 mg twice daily after titration) for 12 weeks 2, 1
  2. If first attempt fails: Try the other first-line option before proceeding to second-line therapy 2

  3. If both first-line options fail: Consider bupropion SR (150 mg twice daily after titration) 1, 5

  4. For all options: Provide concurrent behavioral counseling and follow-up within 2-3 weeks of initiation 2

Important Clinical Pearls

  • Recent evidence does not support combining varenicline with nicotine patch or extending treatment duration to 24 weeks, as these approaches did not significantly improve 7-day point prevalence abstinence at 52 weeks compared to varenicline monotherapy for 12 weeks 8
  • Nicotine withdrawal symptoms typically peak within 1-2 weeks of cessation before subsiding, making early follow-up crucial 2
  • For perioperative patients, smoking cessation should occur as far in advance as feasible, though cancer surgery should not be delayed based on smoking status 2
  • Dose adjustments may be necessary based on side effects and efficacy 2, 1

References

Guideline

Smoking Cessation Medications

Praxis Medical Insights: Practical Summaries of Clinical Guidelines, 2025

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Smoking cessation pharmacotherapy; varenicline or bupropion?

Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 2024

Research

Efficacy and safety of varenicline for smoking cessation.

The American journal of medicine, 2008

Research

Discovery and development of varenicline for smoking cessation.

Expert opinion on drug discovery, 2018

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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