Varenicline
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| Pronunciation | /vəˈrɛnɪkliːn/ və-REN-i-kleen |
| Trade names | Champix, Chantix, Tyrvaya, others |
| Other names | OC-01 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a606024 |
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| Routes of administration | By mouth, intranasal |
| Drug class | Nicotinic agonist |
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| Pharmacokinetic data | |
| Protein binding | <20% |
| Metabolism | Primarily unchanged by OCT2. Insignificant CYP450 enzyme involved |
| Metabolites | N-Formylvarenicline, Glucuronidated, Hexose Conjugated, Oxidated metabolites |
| Elimination half-life | 24 hours |
| Excretion | Kidney (81–92%) |
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| Chemical and physical data | |
| Formula | C13H13N3 |
| Molar mass | 211.268 g·mol−1 |
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Varenicline, sold under the brand names Chantix and Champix among others, is a medication used for smoking cessation and for the treatment of dry eye syndrome. It is a nicotinic acetylcholine receptor partial agonist. When activated, this receptor leads to the release of dopamine in the nucleus accumbens, the brain's reward center, thereby reducing cravings and withdrawal symptoms with smoking cessation, although less pronounced than a full agonist (e.g. nicotine).
Common side effects include nausea, insomnia, abnormal dreams, headache, and nasopharyngitis (inflammation of the nose and throat). Despite these potential adverse effects, varenicline has proven efficacy in helping individuals quit smoking. It is estimated that approximately one in eleven smokers who use varenicline successfully remain abstinent from tobacco at six months.
It is on the World Health Organization's List of Essential Medicines. The medication is available as a generic medication. In the United States, varenicline was prescribed over 1 million times in 2020, ranking as the 275th most commonly prescribed medication.