TY - JOUR
T1 - Efficacy and Safety of Varenicline for Smoking Cessation
AU - Hays, J. Taylor
AU - Ebbert, Jon O.
AU - Sood, Amit
N1 - Funding Information:
Editorial support was provided by Darlene Benson, BSPharm, of Medesta Publications Group, and funded by Pfizer Inc.
PY - 2008/4
Y1 - 2008/4
N2 - 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 α4β2 nicotinic acetylcholine receptor (nAChR) partial agonists. Nicotine addiction is mediated by stimulation of central α4β2 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.
AB - 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 α4β2 nicotinic acetylcholine receptor (nAChR) partial agonists. Nicotine addiction is mediated by stimulation of central α4β2 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.
KW - Partial agonist
KW - Smoking cessation
KW - Varenicline
KW - αβ nicotinic acetylcholine receptor
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UR - http://www.scopus.com/inward/citedby.url?scp=40749151926&partnerID=8YFLogxK
U2 - 10.1016/j.amjmed.2008.01.017
DO - 10.1016/j.amjmed.2008.01.017
M3 - Article
C2 - 18342165
AN - SCOPUS:40749151926
SN - 0002-9343
VL - 121
SP - S32-S42
JO - American Journal of Medicine
JF - American Journal of Medicine
IS - 4 SUPPL.
ER -