Imaging studies in drug-dependent subjects show reduced striatal dopamine D(2/3) receptor (DRD2/3) availability, and it is hypothesized that increasing DRD2/3 availability is a promising strategy to treat drug dependence. We recently showed that rats treated for two weeks with 2mg/kg/day varenicline (a partial agonist at α4β2 nicotinic acetylcholine receptors) showed higher striatal DRD2/3 avai...

BACKGROUND Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). Varenicline was developed as a nicotine receptor partial agonist from cytisine, a drug widely used in central and eastern Europe for smoking ...

Varenicline tartrate (Chantix®/Champix®) is a selective partial agonist of the α(4)β(2) nicotinic acetylcholine receptor and is approved as an aid to smoking cessation. The usual oral dosage in adults is 1 mg twice daily for 12 weeks, with an initial titration week. Several clinical pharmacology studies have characterized the pharmacokinetics of varenicline in adult smokers aged 18-55 years, el...

OBJECTIVE Effective smoking cessation treatments are needed for patients with schizophrenia, who, compared with the general population, have high rates of cigarette smoking and more difficulty quitting. We evaluated the safety and efficacy of varenicline for smoking cessation in outpatients with stable schizophrenia or schizoaffective disorder. METHOD In this 12-week, randomized, double-blind...

BACKGROUND Varenicline is an efficacious medicine for smoking cessation (SC) but little is known about the characteristics of varenicline users. This study examined the characteristics of first-time (naïve) varenicline users in Finland and compared those who had previously used SC pharmacotherapy to those who were trying SC pharmacotherapy for the first time. METHODS A cross-sectional survey ...

BACKGROUND Varenicline was designed to relieve symptoms of nicotine withdrawal, including cigarette craving, and to block the reinforcing effects of continued nicotine use. The cost-effectiveness of varenicline in some countries has not been studied. OBJECTIVE The aim of this study was to compare the cost-effectiveness of varenicline to that of bupropion, nicotine-replacement therapy (NRT), a...

INTRODUCTION Telephone counseling through quitlines combined with cessation medication is an effective strategy to support tobacco cessation. This study assessed the characteristics of quitline enrollees selecting varenicline (Chantix) compared with nicotine replacement therapy (NRT) medication and evaluated the cessation outcomes (7-day point prevalence) among these enrollees at 3 and 6 months...

UNLABELLED Schizophrenic patients have a high rate of smoking and cognitive deficits which may be related to a decreased number or responsiveness of nicotinic receptors in their brains. Varenicline is a partial nicotinic agonist which is effective as an antismoking drug in cigarette smokers, although concerns have been raised about potential psychiatric side-effects. We conducted a double-blind...

The efficacy and safety of retreatment with varenicline in smokers attempting to quit were evaluated in this randomized, double-blind, placebo-controlled, multicenter trial (Australia, Belgium, Canada, the Czech Republic, France, Germany, the United Kingdom, and the United States). Participants were generally healthy adult smokers (≥ 10 cigarettes/day) with ≥ 1 prior quit attempt (≥ 2 weeks) us...

Varenicline, a partial agonist of alpha(4)beta(2) nicotinic acetylcholine receptors, is the most recently approved drug for smoking cessation. This paper reviews the outcomes of Phase 2 and Phase 3 clinical trials that assess the efficacy of varenicline in comparison to placebo and other smoking cessation pharmacotherapies, ie, sustained-release bupropion (bupropion SR) and nicotine transdermal...