Varenicline
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| Image:Varenicline.png | |
| Varenicline
| |
| Systematic (IUPAC) name | |
| 7,8,9,10-tetrahydro-6,10-methano- 6H-pyrazino(2,3-h)(3)benzazepine | |
| Identifiers | |
| CAS number | 375815-87-5 |
| ATC code | N07 |
| PubChem | |
| Chemical data | |
| Formula | C13H13N3 |
| Mol. mass | 211.267 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | <20% |
| Metabolism | Limited (<10%) |
| Half life | 24 hours |
| Excretion | Renal (81–92%) |
| Therapeutic considerations | |
| Licence data |
|
| Pregnancy cat. |
C(US) |
| Legal status |
℞ Prescription only |
| Routes | Oral |
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 pharmacokinetically different from other smoking cessation aids, such as the antagonist, bupropion (trade name Zyban), and nicotine replacement therapys (NRTs) like 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.
Use and dosing
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.[1]
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.[1]
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.
Mechanism of action
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.[1]
Pharmacokinetics
Most of the active compound is excreted renally (81%). A small proportion is glucuronidated, oxidated, N-formylated or conjugated to a hexose.[1]
Side-effects
Side-effects, none common, include:[1]
History
Varenicline was selected by Pfizer from a large number of compounds evaluated that showed affinity to the α 4β2 nicotinic receptor.[1] 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 trials and perceived lack of safety issues.[1] The agency's approval of the drug came on May 11, 2006.[1]
References
External links
de:Vareniclinit:Vareniclina nl:Varenicline
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
