About: Alosetron

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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)

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	Alosetron is a 5-HT3 antagonist used only for the management of severe diarrhoea-predominant irritable bowel syndrome (IBS) in women. Alosetron has an antagonist action on the 5-HT3 receptors and thus may modulate serotonin-sensitive gastrointestinal (GI) processes. Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or ruptured bowel, and death. In June 2002, the FDA approved a supplemental new drug application allowing the remarketing of the drug under restricted conditions of use. (en)
http://linked.open...y/drugbank/dosage	http://linked.opendata.cz/resource/drugbank/dosage/271B45F5-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B45F6-363D-11E5-9242-09173F13E4C5
http://linked.open...generalReferences	# Andresen V, Hollerbach S: Reassessing the benefits and risks of alosetron: what is its place in the treatment of irritable bowel syndrome? Drug Saf. 2004;27(5):283-92. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15061683 # Camilleri M: Pharmacology and clinical experience with alosetron. Expert Opin Investig Drugs. 2000 Jan;9(1):147-59. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11060667 # Mayer EA, Bradesi S: Alosetron and irritable bowel syndrome. Expert Opin Pharmacother. 2003 Nov;4(11):2089-98. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14596662 # Rahimi R, Nikfar S, Abdollahi M: Efficacy and tolerability of alosetron for the treatment of irritable bowel syndrome in women and men: a meta-analysis of eight randomized, placebo-controlled, 12-week trials. Clin Ther. 2008 May;30(5):884-901. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18555935 # Lewis JH: Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective. Expert Rev Gastroenterol Hepatol. 2010 Feb;4(1):13-29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20136586 (en)
http://linked.open...gy/drugbank/group	approved (en) withdrawn (en)
http://linked.open...drugbank/halfLife	1.5 hours (en)
http://linked.open...ugbank/indication	Only for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and have not responded to conventional therapy. (en)
http://linked.open...bank/manufacturer	Pharmacia Inc.
sameAs	Alosetron
Title	Alosetron (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/bindingdb/50131429 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/chebi/253342 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/chemspider/2015 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/drugbank/DB00969 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/guide-to-pharmacology/2296 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/iuphar/2296 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/national-drug-code-directory/0173-0738-00 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/pubchem-compound/2099 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/pubchem-substance/46506274 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/pharmgkb/PA164745502 http://linked.opendata.cz/resource/drugbank/drug/DB00969/identifier/wikipedia/Alosetron
http://linked.open...mechanismOfAction	Alosetron is a potent and selective 5-HT<sub>3</sub> receptor antagonist. 5-HT<sub>3</sub> receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT<sub>3</sub> receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of serotonin-sensitive GI motor and sensory processes. (en)
http://linked.open...drugbank/packager	F Hoffmann-La Roche Ltd. Gilead Sciences Inc.
http://linked.open...y/drugbank/patent	http://linked.opendata.cz/resource/drugbank/patent/5360800
http://linked.open...outeOfElimination	Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans. (en)
http://linked.open.../drugbank/synonym	2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one (en)
http://linked.open...umeOfDistribution	* 65 to 95 L (en)
http://linked.open...k/foodInteraction	Take without regard to meals. (en) Absorption is decreased by about 25% when taken with meals. (en)
http://linked.open...nk/proteinBinding	82% (en)
http://linked.open...ogy/drugbank/salt	(en)
http://linked.open...ynthesisReference	Buchi Reddy REGURI, Sampathkumar UPPARAPALLI, Nilam SAHU, Karunakara Rao JAVVAJI, Brahma Reddy GADE, "PROCESS FOR THE PREPARATION OF ALOSETRON." U.S. Patent US20120178937, issued July 12, 2012. (en)
foaf:page	http://www.drugs.com/cdi/alosetron.html http://www.rxlist.com/cgi/generic3/alosetron.htm
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http://linked.open...ugbank/absorption	50-60 % (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	122852-42-0 (en)
http://linked.open...rugbank/clearance	* 600 mL/min (en)
http://linked.open...gbank/containedIn	Fuzeon convenience kit Lotronex 0.5 mg tablet
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