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Namespace Prefixes

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Statements

Subject Item
n2:DB06212
rdf:type
n3:Drug
n3: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.
n3:dosage
n4:271B4A75-363D-11E5-9242-09173F13E4C5 n4:271B4A76-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
approved
n3:halfLife
Terminal half life, oral dose = 12 hours.
n3:indication
Treatment of symptomatic and resistant to fluid restriction euvolemic or hypervolemic hyponatremia associated with congestive heart failure, SIADH, and cirrhosis.
owl:sameAs
n9:DB06212
dcterms:title
Tolvaptan
adms:identifier
n7:7848276 n10:Tolvaptan n11:59148-021-50 n16:443894 n17:DB06212 n18:D01213 n23:391976
n3: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.
n3:patent
n21:5258510 n21:5753677
n3:routeOfElimination
Fecal- very little renal elimination (<1% is excreted unchanged in the urine)
n3:synonym
Samsca
n3: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.
n3:volumeOfDistribution
Healthy subjects: 3L/kg; slightly higher in heart failure patients.
n14:hasAHFSCode
n22:40-28-28
n3:proteinBinding
99% bound
n3:synthesisReference
Bandi Parthasaradhi Reddy, "PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES." U.S. Patent US20130190490, issued July 25, 2013.
foaf:page
n13:samsca-drug.htm n19:tolvaptan.html
n3:IUPAC-Name
n5:271B4A7B-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4A81-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4A80-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4A7D-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4A7E-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4A7F-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4A79-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4A77-363D-11E5-9242-09173F13E4C5 n5:271B4A7A-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4A78-363D-11E5-9242-09173F13E4C5
n14:hasATCCode
n15:C03XA01
n3:H-Bond-Acceptor-Count
n5:271B4A87-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4A88-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B4A82-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B4A83-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B4A85-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B4A84-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B4A86-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
150683-30-0
n3:category
n3:clearance
4 mL/min/kg (post-oral dosing).
n3:Bioavailability
n5:271B4A8D-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4A8F-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4A90-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4A8C-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4A8B-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4A8E-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4A7C-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4A89-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4A8A-363D-11E5-9242-09173F13E4C5