How Does Varenicline Work?
Varenicline works by binding to α4β2 subtype of nicotinic acetylcholine receptors, where it acts as a partial agonist.
This means that it has agonist activity with a lower intrinsic efficacy than nicotine, and also has antagonist activity when nicotine is present.
Varenicline therefore produces an effect that helps alleviate cravings and withdrawal symptoms when qutting smoking (agonist activity), while simultaneously reducing the reward and positive reinforcement effects of smoking.
This makes it easier for the smoker to quit. Varenicline has been shown to significantly increase the chances of quitting and may be more effective than some forms of NRT.
