Varenicline is a partial agonist of nicotinic acetylcholine receptors in the brain. It reduces the rewarding effects of nicotine while simultaneously decreasing withdrawal symptoms.
The drug binds to α4β2 nicotinic receptors, partially stimulating them and blocking nicotine from activating them fully. This dual mechanism helps reduce cravings and makes smoking less satisfying.
Varenicline is one of the most extensively studied medications for smoking cessation. Large international clinical trials demonstrated that quit rates with varenicline are two to three times higher compared with placebo.
Multiple multicenter studies have confirmed its effectiveness in reducing nicotine cravings and withdrawal symptoms. Varenicline is recommended in international clinical guidelines and by the World Health Organization for tobacco dependence treatment.
The medication works by targeting brain receptors involved in nicotine addiction, making smoking less rewarding and helping patients stop smoking.
The tablets are taken orally with water. Treatment typically begins several days before the planned quit date. The dose is gradually increased during the first week of therapy. The duration of treatment is usually several weeks and should be determined by a healthcare professional.
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