The neurobiological basis for partial agonist treatment of nicotine dependence: varenicline: Varenicline For Treatment Of Nicotine Dependence
Open accessAbstract
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 alpha4beta2 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 alpha4beta2 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.
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After chronic nicotine use, abnormally low levels of dopamine are released when central nervous system nicotine concentrations are depleted.
“Thus while nicotine acutely increases the release of dopamine in the nucleus accumbens, after chronic use there appears to be abnormally low levels of dopamine released when central nervous system (CNS) nicotine concentrations are depleted (16).”
From The Multiple Facets of Cigarette Addiction and What They Mean for Encouraging and Helping Smokers to Stop (2009) · cites this paper as [16]
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- Authors
- Foulds, J.
- Affiliations
- Rutgers, The State University of New Jersey (US)
- Corresponding author
- Foulds, J.
- ORCID
- Foulds, J.
- Venue
- International Journal of Clinical Practice
- Publisher
- Hindawi Limited
- Published
- 2006-05-02
- Volume
- 60
- Issue
- 5
- Pages
- 571-576
- ISSN
- 1368-5031 (ISSN-L)
- OpenAlex
- W2106950438
- Cited by
- 136
- References
- 33
- Citations by year
- 2026: 1 · 2024: 1 · 2023: 1 · 2022: 4 · 2020: 2 · 2019: 1 · 2018: 1 · 2017: 6 · 2016: 5 · 2015: 5 · 2014: 11 · 2013: 10 · 2012: 8
- FWCI
- 2.32
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- International Journal of Clinical Practice (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Epidemiology › Substance Abuse Treatment and Outcomes
- Keywords
- varenicline, nicotine dependence, smoking cessation, α4β2 nicotinic acetylcholine receptor, partial agonists, dopamine release, mesolimbic system, nicotine withdrawal symptoms, nicotine craving, pharmacotherapy, bupropion, clonidine, nicotine replacement therapy
- MeSH terms
- Varenicline, Benzazepines, Brain, Humans, Quinoxalines, Tobacco Use Disorder, Smoking Cessation, Treatment Outcome, Nicotinic Agonists
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