Varenicline is "indicated" for suggested for use in smoking cessation. It is an alternative to Zyban and nicotine replacement therapy (NRT), such as nicotine patches.

Varenicline or Champix in the USA is sold as 0.5 mg and 1 mg tablets. Standard dosing is 1 mg twice daily, with variations as permitted by the FDA. The FDA has approved it use in for twelve weeks; if smoking cessation has been achieved it may be continued for another twelve weeks.

Varenicline or Champix in the USA has not been tested in sub-adults (those under 18) or pregnant women yet, and therefore is not recommended for use by these groups.Women currently breastfeeding should also avoid this product, since varenicline may pass into the breast milk, leading to unknown effects to the child. Varenicline is a partial agonist of the α4β2 subtype of the nicotinic acetylcholine receptor. In addition it acts on α3β4 and weakly on α3β2 and α6-containing receptors. A full agonism was displayed on α7-receptors.

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