Varenicline

Varenicline is an active substance from the group of smoking cessation aids, used for smoking cessation in adults. On one hand, it reduces cravings and withdrawal symptoms, and on the other hand, it prevents the rewarding and reinforcing effects of smoking. Treatment is initiated one to two weeks before the quit date, with gradual dose escalation using a starter pack. Subsequently, one tablet is taken twice daily regardless of meals. The effects are based on selective partial agonism at the nicotinic acetylcholine receptor α4β2. The most common possible adverse effects include headache, dizziness, fatigue, somnolence, insomnia, abnormal dreams, nausea, dyspepsia, dysgeusia, and increased appetite. These side effects may also be associated with smoking cessation itself. Varenicline has a low potential for drug interactions. Varenicline (ATC N07BA03) has smoking cessation properties. The effects are based on selective partial agonism at the nicotinic acetylcholine receptor α4β2. This prevents the binding of nicotine and the associated reward and reinforcement. Partial agonism means that varenicline acts as both an agonist and an antagonist at the receptor. The agonism reduces the craving for smoking and withdrawal symptoms, while the antagonism prevents the rewarding and reinforcing effects of smoking. Varenicline has a long half-life of up to 24 hours.