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Varenicline


Mechanism of action:

Varenicline is a partial nicotinic acetylcholine receptor agonist. Varenicline partially activates the alpha4beta2 nicotinic acetylcholine receptor in the central nervous system, leading to a small release of dopamine and reducing irritability, restlessness, and impaired attention associated with nicotine withdrawal.

Reference(s):

1. Jorenby DE et al. (2006). Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 


2. Mihalak KB et al. (2006). Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 


3. Obach RS et al. (2006). Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos.

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