Indications for Varenicline
Varenicline is indicated as an aid to smoking cessation treatment. 1
Primary Indication
- Smoking cessation: Varenicline is FDA-approved specifically for use as an aid to smoking cessation treatment in adults who want to quit smoking 1
Mechanism and Clinical Context
Varenicline functions as a selective partial agonist at the α4β2 nicotinic acetylcholine receptor, which helps reduce cravings, withdrawal symptoms, and the rewarding effects of smoking 2, 3
The National Comprehensive Cancer Network recommends varenicline as the most effective single pharmacotherapy option for smoking cessation, increasing the odds of cessation by almost 3-fold compared with placebo (OR 2.88; 95% CI, 2.40–3.47) 4, 5
Alternative Cessation Approaches
Gradual smoking reduction: Varenicline is effective for patients unwilling to quit abruptly but willing to gradually reduce cigarette consumption over time 5
The FDA label specifically mentions that patients can begin varenicline dosing and then quit smoking between days 8 and 35 of treatment, allowing flexibility in quit timing 1
For gradual reduction, patients should reduce smoking by 50% from baseline within the first 4 weeks, by an additional 50% in the next 4 weeks, with the goal of complete abstinence by 12 weeks 1
Comparative Effectiveness Context
Varenicline demonstrates superior efficacy compared to bupropion (OR 1.59; 95% CI, 1.29–1.96) and single forms of nicotine replacement therapy (OR 1.57; 95% CI, 1.29–1.91) 5
Varenicline appears equally effective as combined treatment with more than one form of nicotine replacement therapy 5
Important Caveat
- Varenicline is not approved for use in patients under 18 years of age, despite pharmacokinetic studies in adolescents 6