Varenicline: a first-line treatment option for smoking cessation.

BACKGROUND: Varenicline acts as a partial agonist/antagonist with affinity and selectivity for alpha(4) beta(2) nicotinic acetylcholine receptors. This activity at the nicotine-receptor level may help patients achieve smoking cessation by reducing cravings/withdrawal symptoms and smoking satisfaction.

OBJECTIVE: This article reviews the literature on the pharmacologic properties, therapeutic efficacy, and tolerability of varenicline for smoking cessation.

METHODS: Pertinent controlled clinical trials, meta-analyses, meeting abstracts, case reports, and review articles published in English between 1966 and May 2008 were identified through searches of MEDLINE and OVID using the terms varenicline, smoking, tobacco cessation, and CP 526555.

RESULTS: Eight clinical trials were identified that compared
CONCLUSIONS: Varenicline has a unique mechanism of action compared with other first-line options for smoking cessation. Available clinical-trial data support its use as an effective and generally well-tolerated therapy for smoking cessation in healthy adult smokers, although there is a need for further efficacy and safety evaluation in the general population, particularly those with comorbid conditions.