'''Varenicline''' (trade name '''Chantix''' in the USA and '''Champix''' in Europe, Mexico and Canada, manufactured by [[Pfizer]], usually in the form of '''varenicline tartrate''') is a prescription medication used to treat smoking addiction. This medication is the first approved [[nicotinic receptor]] [[partial agonist]]. In this respect, it is [[pharmacokinetics|pharmacokinetically]] different from other [[smoking cessation]] aids, such as the [[Receptor_antagonist|antagonist]], [[bupropion]] (trade name Zyban), and [[nicotine replacement therapy]]s (NRTs) like [[nicotine patch|nicotine patches]] (commonly, "the patch") and [[nicotine gum]]. As a partial agonist, it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products, and through these mechanisms, it can assist some patients in quitting smoking. In May 2006, it was approved for sale in the United States. On August 1, 2006, Pfizer announced that Chantix was available for sale in the United States, and on September 29, 2006, it was approved for sale in the [[European Union]].
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==Use and dosing==
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Varenicline is indicated for (suggested for use in) smoking cessation. It is an alternative to NRTs and agonist medication and has demonstrated greater efficacy than them in comparable studies.<ref>{{cite journal | author = Jorenby D E, Hays J T, Rigotti N A, Azoulay S, Watsky E J, Williams K E, Billing C B, Gong J, Reeves K R| title = Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial | journal = JAMA| volume = 296|issue = 1|pages = 56–63| year = 2006 |id=PMID 16820547}}</ref>
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Varenicline is sold as 0.5 mg and 1 mg tablets. Titrating the dose from 0.5 mg every day for 3 days to 0.5 mg twice daily for 4 days to 1 mg twice daily is recommended. In the United States the standard maintenance dose is 1 mg twice daily, with variations as permitted by the [[Food and Drug Administration]]. The FDA has approved its use for twelve weeks. If smoking cessation has been achieved it may be continued for another twelve weeks.<ref name=FDA>U.S. Food and Drug Administration. [http://www.fda.gov/bbs/topics/NEWS/2006/NEW01370.html ''FDA Approves Novel Medication for Smoking Cessation'']. Press release, 11 May 2006.</ref>
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Varenicline has not been tested in children, those under 18 years old 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 on the child.
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==Mechanism of action==
Varenicline is a [[partial agonist]] of the α<sub>4</sub>β<sub>2</sub> subtype of the [[nicotinic acetylcholine receptor]]. In addition it acts on α<sub>3</sub>β<sub>4</sub> and weakly on α<sub>3</sub>β<sub>2</sub> and α<sub>6</sub>-containing receptors. A full agonism was displayed on α<sub>7</sub>-receptors.<ref>Mihalak KB, Carroll FI, Luetje CW. Varenicline is a partial agonist at α4β2 and a full agonist at α7 neuronal nicotinic receptors. ''Mol Pharmacol'' 2006;70(3):801-5. PMID 16766716.</ref>
==Pharmacokinetics==
Most of the active compound is excreted renally (81%). A small proportion is [[glucuronidation|glucuronidated]], oxidated, ''N''-formylated or conjugated to a hexose.<ref>Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. ''Drug Metab Dispos'' 2006;34:121-30. PMID 16221753.</ref>
Varenicline was selected by Pfizer from a large number of compounds evaluated that showed affinity to the α <sub>4</sub>β<sub>2</sub> nicotinic receptor.<ref>Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT. Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. ''J Med Chem'' 2005;48:3474-7. PMID 15887955.</ref> It derives chemically from [[cytisine]].
Varenicline received a "priority review" by the U.S. [[Food and Drug Administration]] in February 2006, shortening the usual 10-month review period to 6 months because of its demonstrated effectiveness in [[clinical trial]]s and perceived lack of safety issues.<ref>Kuehn BM. FDA speeds smoking cessation drug review. ''JAMA'' 2006;295:614. PMID 16467225.</ref> The agency's approval of the drug came on May 11, 2006.<ref name=FDA/>
==References==
<references/>
==External links==
{{wikinews|New drug for smoking cessation is under investigation}}
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Black Box Warning
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Varenicline is a {{{drugClass}}} that is FDA approved for the {{{indicationType}}} of {{{indication}}}. There is a Black Box Warning for this drug as shown here. Common adverse reactions include .
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There is limited information regarding Clinical Trial Experience of Varenicline in the drug label.
Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Varenicline in the drug label.
