Varenicline

varenicline
IUPAC name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate Synonyms: Chantix, Champix Formula: C17H19N3O6
Uses:	smoking cessation
Properties:	nicotine receptor partial agonist
Hazards:	suicide, hostility, heart problems
Mass (g/mol): CAS #: 361.37 (tartrate) 375815-87-5

‘’’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.

Mechanism of Action

Varenicline binds to neuronal nicotinic acetylcholine receptors, especially to the alpha-4/beta-2 receptor,,, 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.

Drug toxicity

There is "the potential for an increased risk of serious adverse cardiovascular events associated with the use of varenicline among tobacco users" according to a meta-analysis.