About: Varenicline

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An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors. On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced. (en)
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http://linked.open...generalReferences	# Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR: Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006 Jul 5;296(1):56-63. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16820547 # Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16766716 # 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 Jan;34(1):121-30. Epub 2005 Oct 12. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16221753 # 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 May 19;48(10):3474-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15887955 # Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16467225 (en)
http://linked.open...gy/drugbank/group	approved (en) investigational (en)
http://linked.open...drugbank/halfLife	The elimination half-life of varenicline is approximately 24 hours (en)
http://linked.open...ugbank/indication	For use as an aid in smoking cessation. (en)
sameAs	Varenicline Varenicline
Title	Varenicline (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/chemspider/4470510 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/drugbank/DB01273 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/national-drug-code-directory/0069-0471-97 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/pubchem-compound/5310966 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/pubchem-substance/46505502 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/pharmgkb/PA164781343 http://linked.opendata.cz/resource/drugbank/drug/DB01273/identifier/wikipedia/Varenicline
http://linked.open...mechanismOfAction	Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectiviyty for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms. (en)
http://linked.open...drugbank/packager	Hoffmann la roche inc Alphapharm Party Ltd. Cardinal Health Diversified Healthcare Services Inc. Lake Erie Medical and Surgical Supply Pfizer Inc. Physicians Total Care Inc.
http://linked.open...y/drugbank/patent	http://linked.opendata.cz/resource/drugbank/patent/2316921 http://linked.opendata.cz/resource/drugbank/patent/2525874 http://linked.opendata.cz/resource/drugbank/patent/6410550 http://linked.opendata.cz/resource/drugbank/patent/7265119
http://linked.open...outeOfElimination	Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2. (en)
http://linked.open.../drugbank/synonym	CP-526,555 (en)
http://linked.open...nk/proteinBinding	Less than 20%. (en)
http://linked.open...ogy/drugbank/salt	(en)
http://linked.open...ynthesisReference	Vinod Kumar Kansal, Suhail Ahmad, Amit Gupta, "PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF." U.S. Patent US20090318695, issued December 24, 2009. (en)
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foaf:page	http://www.drugs.com/cdi/varenicline.html http://www.rxlist.com/cgi/generic/chantix.htm
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http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	249296-44-4 (en)
http://linked.open...drugbank/category	(en)
http://linked.open...gbank/containedIn	Chantix 0.5 mg tablet Chantix 1 mg cont month pak Chantix 1 mg tablet Cyclobenzaprine HCl 5 mg tablet Flexeril 10 mg tablet
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