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
First attempt: Start with either:
If first attempt fails: Try the other first-line option before proceeding to second-line therapy 2
If both first-line options fail: Consider bupropion SR (150 mg twice daily after titration) 1, 5
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