Common Smoking Cessation Medications
The most effective first-line smoking cessation medications include nicotine replacement therapy (NRT), bupropion SR, and varenicline, with combination NRT and varenicline showing the highest cessation rates. 1
First-Line Pharmacotherapies
Nicotine Replacement Therapy (NRT)
- Available in multiple forms: patches, gum, lozenges, inhalers, and nasal spray 1
- Works by providing nicotine to reduce withdrawal symptoms while eliminating exposure to other harmful chemicals in tobacco 1
- Using combination NRT (particularly a nicotine patch plus a rapid-delivery form like gum or lozenge) is more effective than single NRT products 1
- Long-term nicotine patch therapy (>14 weeks) appears superior to shorter-term treatment 1
- Common side effect: Local irritation at application site; epistaxis with nasal spray 1
Varenicline (Chantix)
- Partial agonist at α4β2 nicotinic acetylcholine receptors that reduces cravings and blocks rewarding effects of smoking 1, 2
- Recommended dosing: Start 1-2 weeks before quit date, titrate from 0.5 mg once daily (days 1-3), to 0.5 mg twice daily (days 4-7), to target dose of 1 mg twice daily for 12 weeks 1, 2
- Most effective single agent with cessation rates of approximately 28% compared to 12% with placebo 1, 3
- Common side effect: Nausea (most common adverse effect) 1
- Requires monitoring for neuropsychiatric symptoms, though recent evidence suggests these risks may be lower than previously thought 1
Bupropion SR (Zyban)
- Atypical antidepressant that inhibits norepinephrine and dopamine reuptake 4
- Recommended dosing: Start 1-2 weeks before quit date, 150 mg once daily for 3 days, then 150 mg twice daily for 7-12 weeks 1
- Increases cessation rates to approximately 19% compared to 11% with placebo 3
- Common side effects: Insomnia, dry mouth; rare but serious risk of seizures (contraindicated in patients with seizure disorders) 1
- Contraindicated in patients with seizure risk, those taking MAO inhibitors, or those with closed-angle glaucoma 1
Second-Line Medications
- Nortriptyline: Tricyclic antidepressant shown to be effective for smoking cessation (25-50 mg/day) 1, 5
- Clonidine: Antihypertensive medication that can aid smoking cessation but has more side effects 1
- Cytisine: A partial nicotine receptor agonist available in some European countries 1
Combination Therapies
- Combination NRT (patch plus short-acting form) has shown the highest cessation rates of approximately 31.5% 3
- Bupropion plus nicotine patch appears superior to bupropion alone 1
- Adding behavioral support to pharmacotherapy significantly increases cessation rates from 18% to 21% 1
Comparative Effectiveness
- Varenicline appears more effective than bupropion or NRT monotherapy 3, 4
- Combination NRT shows comparable effectiveness to varenicline 3
- Both varenicline and combination NRT are more effective than single NRT products or bupropion alone 3
Common Pitfalls and Caveats
- Inadequate duration of therapy: Most pharmacotherapies should be used for at least 8-12 weeks 1
- Insufficient dosing: Higher-dose NRT may be needed for heavy smokers 1
- Failure to combine behavioral counseling with pharmacotherapy: Combined approaches significantly increase success rates 1, 6
- Premature discontinuation due to side effects: Most side effects are mild and diminish over time 1
- Not considering combination therapy for patients who fail monotherapy 1
- Overlooking the need for extended treatment in some patients to prevent relapse 1
Selection Algorithm
- For most patients: Start with varenicline or combination NRT (patch plus short-acting form) as these have the highest success rates 3, 4
- For patients with psychiatric history or concerns about varenicline: Consider combination NRT or bupropion 1
- For patients with seizure risk: Avoid bupropion; use NRT or varenicline 1
- For patients who failed previous quit attempts with one medication: Try an alternative first-line medication or combination therapy 1
- For patients with high nicotine dependence: Consider combination therapy from the start 1
Remember that the success rate of smoking cessation increases significantly when pharmacotherapy is combined with behavioral counseling interventions 1, 6.