Open AccessThe neurobiological basis for partial agonist treatment of nicotine dependence: varenicline
Author(s) -
Foulds J.
Publication year - 2006
Publication title -
international journal of clinical practice
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.756
H-Index - 98
eISSN - 1742-1241
pISSN - 1368-5031
DOI - 10.1111/j.1368-5031.2006.00955.x
Subject(s) - varenicline , medicine , nicotine , partial agonist , smoking cessation , bupropion , pharmacology , nicotinic agonist , nicotine withdrawal , agonist , receptor , pathology
Summary Smoking cessation has major health benefits for men and women of all ages. However, most smokers are addicted to nicotine and fail repeatedly in their attempts to quit. Stimulation of nicotinic receptors in the brain, particularly α 4 β 2 receptors, releases dopamine in the meso‐limbic area of the brain and is reinforcing. Nicotine abstinence reduces dopamine release, and this is associated with withdrawal symptoms and craving for nicotine. Eight current pharmacotherapies – bupropion, nortriptyline, clonidine and nicotine patch, gum, inhaler, lozenge and nasal spray – are moderately effective aids to smoking cessation. Each is significantly better than placebo, but approximately 80% of patients using one of these medications return to smoking within the first year. Varenicline, a specific α 4 β 2 nicotinic receptor partial agonist, is a new pharmacotherapy that stimulates dopamine and simultaneously blocks nicotine receptors. Phase II and III trials have yielded promising results suggesting that varenicline could be an important advance in the treatment of nicotine dependence.