Varenicline: Difference between revisions
imported>David E. Volk (new page for WAT) |
imported>Anthony.Sebastian (elaborate on 'Properties' in chem infobox) |
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|molmass= 361.37 (tartrate) | |molmass= 361.37 (tartrate) | ||
|uses=smoking cessation | |uses=smoking cessation | ||
|properties=nicotine receptor agonist | |properties=nicotine receptor partial agonist | ||
|hazards=suicide, hostility, heart problems | |hazards=suicide, hostility, heart problems | ||
|iupac= 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate | |iupac= 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate | ||
Revision as of 20:34, 5 July 2011
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| varenicline | |||||||
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| Uses: | smoking cessation | ||||||
| Properties: | nicotine receptor partial agonist | ||||||
| Hazards: | suicide, hostility, heart problems | ||||||
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‘’’Varenicline’’’, sold under the brand names Chantix and Champix, is a medication which helps with smoking cessation by blocking nicotine receptors. Some concerns have been raised about possible side effects of the medication, prompting the FDA to add a Boxed Warning for Chantix’s label listing depressed mood, suicidal thoughts, and hostility, similar to warnings associated with Zyban (bupropion), a similar drug. More recently, a meta-analysis of 14 studies reported possible 72% increased risk of heart problems when taking varenicline.[1]
Mechanism of Action
Varenicline binds to neuronal nicotinic acetylcholine receptors, especially to the alpha-4/beta-2 receptor,[2],[3],[4] and stops nicotine from binding to these same receptors, thus removing satisfaction typically caused by smoke inhalation. In addition, varenicline is a weak agonist of these receptors, leading to a feeling of relaxation which lessens withdrawal symptoms of smoking cessation.
References
- ↑ Canadian Medical Association Journal, 2011
- ↑ Coe et al (2005) Varenicline: an a4b2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474.
- ↑ Rollema et al (2007) Pharmacological profile of the a4b2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985
- ↑ Rollema et al (2009) Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813.