About: Tolvaptan

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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	Tolvaptan is used to treat low blood sodium levels (hyponatremia) associated with various conditions like congestive heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormones (SIADH). FDA approved on May 19, 2009. (en)
http://linked.open...y/drugbank/dosage	http://linked.opendata.cz/resource/drugbank/dosage/271B4A75-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B4A76-363D-11E5-9242-09173F13E4C5
http://linked.open...generalReferences	# Gheorghiade M, Teerlink JR, Mebazaa A: Pharmacology of new agents for acute heart failure syndromes. Am J Cardiol. 2005 Sep 19;96(6A):68G-73G. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16181825 # Ambrosy A, Goldsmith SR, Gheorghiade M: Tolvaptan for the treatment of heart failure: a review of the literature. Expert Opin Pharmacother. 2011 Apr;12(6):961-76. doi: 10.1517/14656566.2011.567267. Epub 2011 Mar 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21401442 # Yi S, Jeon H, Yoon SH, Cho JY, Shin SG, Jang IJ, Yu KS: Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men. J Cardiovasc Pharmacol. 2012 Apr;59(4):315-22. doi: 10.1097/FJC.0b013e318241e89c. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22130104 # Nemerovski C, Hutchinson DJ: Treatment of hypervolemic or euvolemic hyponatremia associated with heart failure, cirrhosis, or the syndrome of inappropriate antidiuretic hormone with tolvaptan: a clinical review. Clin Ther. 2010 Jun;32(6):1015-32. doi: 10.1016/j.clinthera.2010.06.015. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20637957 # FDA label (en)
http://linked.open...gy/drugbank/group	approved (en)
http://linked.open...drugbank/halfLife	Terminal half life, oral dose = 12 hours. (en)
http://linked.open...ugbank/indication	Treatment of symptomatic and resistant to fluid restriction euvolemic or hypervolemic hyponatremia associated with congestive heart failure, SIADH, and cirrhosis. (en)
sameAs	Tolvaptan
Title	Tolvaptan (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/chemspider/391976 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/drugbank/DB06212 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/kegg-drug/D01213 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/national-drug-code-directory/59148-021-50 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/pubchem-compound/443894 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/pubchem-substance/7848276 http://linked.opendata.cz/resource/drugbank/drug/DB06212/identifier/wikipedia/Tolvaptan
http://linked.open...mechanismOfAction	Tolvaptan is a selective and competitive arginine vasopressin receptor 2 antagonist. Vasopressin acts on the V2 receptors found in the walls of the vasculature and luminal membranes of renal collecting ducts. By blocking V2 receptors in the renal collecting ducts, aquaporins do not insert themselves into the walls thus preventing water absorption. This action ultimately results in an increase in urine volume, decrease urine osmolality, and increase electrolyte-free water clearance to reduce intravascular volume and an increase serum sodium levels. Tolvaptan is especially useful for heart failure patients as they have higher serum levels of vasopressin. (en)
http://linked.open...y/drugbank/patent	http://linked.opendata.cz/resource/drugbank/patent/5258510 http://linked.opendata.cz/resource/drugbank/patent/5753677
http://linked.open...outeOfElimination	Fecal- very little renal elimination (<1% is excreted unchanged in the urine) (en)
http://linked.open.../drugbank/synonym	Samsca (en)
http://linked.open...drugbank/toxicity	The oral LD50 of tolvaptan in rats and dogs is >2000 mg/kg. Most common adverse reactions (≥5% placebo) are thirst, dry mouth, asthenia, constipation, pollakiuria or polyuria, and hyperglycemia. (en)
http://linked.open...umeOfDistribution	Healthy subjects: 3L/kg; slightly higher in heart failure patients. (en)
http://linked.open.../drug/hasAHFSCode	http://linked.opendata.cz/resource/AHFS/40-28-28
http://linked.open...nk/proteinBinding	99% bound (en)
http://linked.open...ynthesisReference	Bandi Parthasaradhi Reddy, "PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES." U.S. Patent US20130190490, issued July 25, 2013. (en)
foaf:page	http://www.drugs.com/monograph/tolvaptan.html http://www.rxlist.com/samsca-drug.htm
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http://linked.open...l/drug/hasATCCode	Tolvaptan
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http://linked.open...ugbank/absorption	Tmax, Healthy subjects: 2 - 4 hours; Cmax, Healthy subjects, 30 mg: 374 ng/mL; Cmax, Healthy subjects, 90 mg: 418 ng/mL; Cmax, heart failure patients, 30 mg: 460 ng/mL; Cmax, heart failure patients, 90 mg: 723 ng/mL; AUC(0-24 hours), 60 mg: 3.71 μg·h/mL; AUC(∞), 60 mg: 4.55 μg·h/mL; The pharmacokinetic properties of tolvaptan are stereospecific, with a steady-state ratio of the S-(-) to the R-(+) enantiomer of about 3. The absolute bioavailability of tolvaptan is unknown. At least 40% of the dose is absorbed as tolvaptan or metabolites. Food does not impact the bioavailability of tolvaptan. (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	150683-30-0 (en)
http://linked.open...drugbank/category	(en)
http://linked.open...rugbank/clearance	4 mL/min/kg (post-oral dosing). (en)
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