Varenicline is a medication used for smoking cessation. It is also used for the treatment of dry eye disease.
It is a high-affinity partial agonist for the alfa4beta2 nicotinic acetylcholine receptor subtype (nACh) that leads to the release of the neurotransmitter dopamine in the nucleus accumbens reward center of the brain when activated, and therefore, has the capacity to reduce the feelings of craving and withdrawal caused by smoking cessation.
In this respect it is similar to cytisine and different from the nicotinic antagonist bupropion and nicotine replacement therapies (NRTs) like nicotine patches and nicotine gum.
A 2021 Cochrane overview and network meta-analysis concluded that varenicline is the most effective medication for tobacco cessation and that smokers were nearly three times more likely to quit tobacco use while on varenicline than with placebo treatment.
Varenicline was more efficacious than bupropion or NRT and as effective as combination NRT for tobacco smoking cessation.
