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CONTEXT Varenicline, a partial agonist at the alpha4beta2 nicotinic acetylcholine receptor, has the potential to aid smoking cessation by relieving nicotine withdrawal symptoms and reducing the rewarding properties of nicotine. OBJECTIVE To determine the efficacy and safety of varenicline for smoking cessation compared with placebo or sustained-release(More)
CONTEXT The majority of cigarette smokers who achieve abstinence relapse within the first year and require many attempts before achieving permanent abstinence. Evidence to support pharmacological treatment for relapse prevention is insufficient. OBJECTIVE To determine whether smokers who quit after 12 weeks of treatment with varenicline, a selective(More)
CONTEXT The alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are linked to the reinforcing effects of nicotine and maintaining smoking behavior. Varenicline, a novel alpha4beta2 nAChR partial agonist, may be beneficial for smoking cessation. OBJECTIVE To assess efficacy and safety of varenicline for smoking cessation compared with sustained-release(More)
Most smokers repeatedly fail in their attempts to stop smoking because of the addictive nature of the nicotine in tobacco products. Nicotine dependence is probably mediated through the activation of multiple subtypes of neuronal nicotinic acetylcholine receptor (nAChR), among which the mesolimbic alpha(4)beta(2) subtype has a pivotal role. Here, we discuss(More)
The pharmacological properties and pharmacokinetic profile of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target receptor that for a large part explain its efficacy as a smoking cessation aid. Since alpha4beta2 and other nAChR(More)
OBJECTIVES To evaluate varenicline's efficacy for smoking cessation versus bupropion SR and placebo and to explore whether factors typically predictive of abstinence influence varenicline's efficacy versus placebo, as measured by the week 9-12 continuous abstinence rate (CAR9-12). METHODS Smokers in 2 randomized, placebo-controlled trials received(More)
OBJECTIVE To determine whether self-regulated flexible dosing with varenicline tartrate is safe and effective for smoking cessation. RESEARCH DESIGN AND METHODS 320 healthy, motivated-to-quit smokers (> or =10 cigarettes/day) aged 18-65 years, entered a multicenter, randomized, double-blind, placebo-controlled study - conducted between December 26, 2001(More)
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. (More)
OBJECTIVE We assessed the safety of long-term varenicline administration for smoking cessation. METHODS In this randomized, double-blind, multicenter trial, eligible adult smokers (18-75 years) who smoked an average of > or =10 cigarettes/day were randomized to either varenicline 1 mg twice daily (BID) or placebo for 52 weeks. Subjects made weekly clinic(More)
BACKGROUND Rates of smoking in East Asian men range from >35% to >60%, and are increasing in women and the young. OBJECTIVE This study evaluated the efficacy and tolerability of 1 mg BID varenicline, a novel alpha4beta2 nicotinic acetylcholine receptor partial agonist, for smoking cessation in smokers in Taiwan and Korea. METHODS A randomized,(More)