BACKGROUND Varenicline, a new treatment for smoking cessation, has demonstrated significantly greater efficacy over placebo and sustained release bupropion (bupropion SR). A study was undertaken to compare a 12-week standard regimen of varenicline with a 10-week standard regimen of transdermal nicotine replacement therapy (NRT) for smoking cessation. METHODS In this 52-week, open-label, rando...

Background: Cocaine use, abuse and dependence remains a pressing public health problem. Based on its mechanism of action, varenicline, an alpha4beta2 partial agonist seemed to be a likely candidate for treating cocaine dependence. Methods: Cocaine dependent participants (n = 37) were enrolled in a 9-week double-blind placebo controlled clinical trial. Varenicline was titrated up to a target dos...

INTRODUCTION This study evaluated the effect of varenicline in combination with counseling to assist long-term nicotine replacement therapy (NRT) users to quit NRT. METHODS This was a double-blind, placebo-controlled, randomized trial of varenicline or placebo for 12 weeks, with 52-week follow-up, performed in 1 hospital-based smoking cessation specialist clinic. At the first visit, 139 ex-sm...

AIMS The FDA approved smoking cessation aid varenicline can effectively attenuate nicotine-stimulated dopamine release. Varenicline may also exert important actions on other transmitter systems that also influence nicotine reinforcement or contribute to the drug's cognitive and affective side effects. In this study, we determined if varenicline, like nicotine, can stimulate presynaptic GABA rel...

We evaluated the effects of the smoking cessation aid varenicline and nicotine on brain activation, locomotor sensitization and cognitive functioning in rats. Blood oxygenation level dependent (BOLD) activation on fMRI was measured in awake adult male Sprague-Dawley rats in response to their first dose of varenicline 0.04 mg/kg administered intravenously and compared to saline controls. Other g...

PURPOSE The effects of varenicline treatment for smoking cessation on mental health (MH) stability in veterans with posttraumatic stress disorder (PTSD) was studied. METHODS Data were collected by retrospective chart review at a Veterans Affairs medical center. Patients with PTSD who were prescribed varenicline for smoking cessation between May 2006 and July 2008 were included; all patients h...

BACKGROUND AND PURPOSE Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. The proposed mechanism of action for varenicline to reduce ethanol consumption has been through modulation of dopamine (DA) release in the nucleus accumbens (NAc) via α4*-containing nAChRs in the ventral tegmental area (VTA). However, presynapti...

IMPORTANCE Standard varenicline tartrate dosing was formulated to avoid adverse effects (primarily nausea), but some patients may be underdosed. To our knowledge, no evidence-based guidance exists for physicians considering increasing varenicline dose if there is no response to the standard dosage. OBJECTIVE To determine whether increasing varenicline dose in patients showing no response to t...

OBJECTIVE To assess the cost effectiveness of varenicline compared with bupropion or unaided cessation for smoking cessation in Finnish adult smokers. RESEARCH DESIGN AND METHODS The BENESCO (BENEfits of Smoking Cessation on Outcomes) Markov model was used to follow a hypothetical cohort of smokers making a single quit attempt over a lifetime. Gender and age-specific data on the incidence and...

Varenicline, a widely used and successful smoking cessation agent, acts as a partial agonist at nicotinic acetylcholine receptors. Here, we explore the effects of varenicline at human and mouse 5-Hydroxytryptamine(3) (5-HT(3)) receptors. Application of varenicline to human 5-HT(3) receptors expressed in Xenopus laevis oocytes reveal it is almost a full agonist (R(max) = 80%) with an EC(50) (5.9...