The Medical Letter on Drugs and Therapeutics
Varenicline (Chantix) for Tobacco Dependence
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Varenicline tartrate (Chantix – Pfizer) is now available for oral treatment of tobacco dependence. Some other drugs for this indication1 are listed in the table on page 67.

MECHANISM OF ACTION — Varenicline is a partial agonist that binds selectively to α4β2 nicotinic acetylcholine receptors with a greater affinity than nicotine; it blocks nicotine from binding and stimulates receptormediated activity, but to a lesser degree than nicotine. Stimulation of this receptor leads to release of dopamine, which is thought to be a component of the “reward” that reinforces smoking and relieves craving and withdrawal symptoms.2

PHARMACOKINETICS — Varenicline is rapidly absorbed across the gastric mucosa, reaching a peak plasma concentration (Cmax) in about 4 hours.3 With daily dosing, plasma concentrations reach a steady state ... more      

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