Efficacy and Safety of Varenicline for Smoking Cessation

Nicotine Dependence Center, Mayo Clinic College of Medicine, Mayo Clinic, Rochester, Minnesota 55905, USA.
The American journal of medicine (Impact Factor: 5). 05/2008; 121(4 Suppl 1):S32-42. DOI: 10.1016/j.amjmed.2008.01.017
Source: PubMed


Effective treatment of nicotine addiction is essential for reducing the substantial current and predicted morbidity and mortality associated with tobacco smoking. Despite the availability of effective treatments for smoking cessation, such as nicotine replacement therapy and bupropion sustained-release (SR), abstinence rates remain less than optimal. Varenicline is the first in a new class of agents for smoking cessation, the alpha(4)beta(2) nicotinic acetylcholine receptor (nAChR) partial agonists. Nicotine addiction is mediated by stimulation of central alpha(4)beta(2) nAChRs by nicotine, which causes the release of dopamine, ultimately leading to the pleasurable effects of smoking. As a nAChR partial agonist, varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Thus, varenicline offers a new therapeutic option for the treatment of nicotine addiction. Clinical trials have demonstrated superior efficacy of this agent over placebo and bupropion-SR for achieving abstinence from smoking, and varenicline has also been shown to significantly delay smoking relapse. As the newest agent approved for smoking cessation, the mechanism of action, efficacy, and safety of varenicline.

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Available from: J. Taylor Hays, Oct 02, 2015
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    • "Surprisingly, bupropion increases tobacco use in non-treatment seeking smokers (Cousins et al., 2001) and decreases seizure threshold, which is a limiting side-effect (Kuate et al, 2004). Varenicline, a partial agonist at α4β2 and full agonist at α7 nicotinic receptors (Coe et al., 2005; Mihalak et al, 2006), reduces nicotine reinforcement and craving (Gonzales et al., 2006; Oncken et al, 2006; West et al, 2008), but with sideeffects including agitation, depression and suicidal ideation (Hays et al., 2008). Clearly, there is a need for more efficacious smoking cessation therapeutics. "
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    • "They mediate acetylcholine (Ach) neurotransmission and adjust the activities of neurotransmitters such as dopamine, serotonin, glutamate, and GABA (Girod et al, 2000; Kenny et al, 2000; Dehkordi et al, 2007; Grady et al, 2007). These receptors are associated with diseases such as epilepsy, cognition disorders, Alzheimer's diseases, Parkinson's diseases, and nicotine addiction (Dougherty et al, 2003; Vincler & McIntosh, 2007; Hays et al, 2008; Kuryatov et al, 2008; Owen et al, 2008; O'Leary et al, 2008; Pons et al, 2008). The nAChRs can be classified according to several subunits. "
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