Varenicline
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| Trade names | Chantix |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a606024 |
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Oral |
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| Pharmacokinetic data | |
| Protein binding | <20% |
| Metabolism | Limited (<10%) |
| Biological half-life | 24 hours |
| Excretion | Renal (81–92%) |
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| Formula | C13H13N3 |
| Molar mass | 211.267 g/mol |
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Varenicline (trade name Chantix and Champix usually in the form of varenicline tartrate), is a prescription medication used to treat nicotine addiction. Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. 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. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms it can assist some patients to quit smoking.
Varenicline is used for smoking cessation. In a 2009 meta-analysis varenicline was found to be more effective than bupropion (odds ratio 1.40) and NRTs (odds ratio 1.56).
A 2013 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 on varenicline than with placebo treatment. Varenicline was more efficacious than bupropion or NRT and as effective as combination NRT for tobacco smoking cessation.
The United States' Food and Drug Administration (US FDA) has approved the use of varenicline for up to twelve weeks. If smoking cessation has been achieved it may be continued for another twelve weeks.
Varenicline has not been tested in those under 18 years old or pregnant women and therefore is not recommended for use by these groups. Varenicline is considered a class C pregnancy drug, as animal studies have shown no increased risk of congenital anomalies, however, no data from human studies is available. An observational study is currently being conducted assessing for malformations related to varenicline exposure, but has no results yet. An alternate drug is preferred for smoking cessation during breastfeeding due to lack of information and based on the animal studies on nicotine.
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