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Namespace Prefixes

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Statements

Subject Item
n2:DB00889
rdf:type
n3:Drug
n3:description
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients. [PubChem]
n3:dosage
n9:271B58F4-363D-11E5-9242-09173F13E4C5 n9:271B58F5-363D-11E5-9242-09173F13E4C5 n9:271B58F6-363D-11E5-9242-09173F13E4C5 n9:271B58F7-363D-11E5-9242-09173F13E4C5 n9:271B58F8-363D-11E5-9242-09173F13E4C5 n9:271B58F9-363D-11E5-9242-09173F13E4C5 n9:271B58FA-363D-11E5-9242-09173F13E4C5 n9:271B58FB-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# "Link":http://www.medsafe.govt.nz/Profs/Datasheet/k/Kytriltabinj.htm # Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15740177 # Tan M: Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2003 Sep;4(9):1563-71. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12943486 # Feyer P, Seegenschmiedt MH, Steingraeber M: Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer. 2005 Sep;13(9):671-8. Epub 2005 Jul 26. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16044252
n3:group
approved investigational
n3:halfLife
4-6 hours in healthy patients, 9-12 hours in cancer patients
n3:indication
For the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).
n3:manufacturer
n4:271B58E3-363D-11E5-9242-09173F13E4C5 n4:271B58E4-363D-11E5-9242-09173F13E4C5 n4:271B58E1-363D-11E5-9242-09173F13E4C5 n4:271B58E2-363D-11E5-9242-09173F13E4C5 n4:271B58DF-363D-11E5-9242-09173F13E4C5 n4:271B58E0-363D-11E5-9242-09173F13E4C5 n4:271B58DD-363D-11E5-9242-09173F13E4C5 n4:271B58DE-363D-11E5-9242-09173F13E4C5 n4:271B58E9-363D-11E5-9242-09173F13E4C5 n4:271B58EA-363D-11E5-9242-09173F13E4C5 n4:271B58E7-363D-11E5-9242-09173F13E4C5 n4:271B58E8-363D-11E5-9242-09173F13E4C5 n4:271B58E5-363D-11E5-9242-09173F13E4C5 n4:271B58E6-363D-11E5-9242-09173F13E4C5 n4:271B58DB-363D-11E5-9242-09173F13E4C5 n4:271B58D9-363D-11E5-9242-09173F13E4C5 n4:271B58DA-363D-11E5-9242-09173F13E4C5 n4:271B58D7-363D-11E5-9242-09173F13E4C5 n4:271B58D8-363D-11E5-9242-09173F13E4C5 n4:271B58D5-363D-11E5-9242-09173F13E4C5 n4:271B58D6-363D-11E5-9242-09173F13E4C5 n4:271B58D3-363D-11E5-9242-09173F13E4C5 n4:271B58D4-363D-11E5-9242-09173F13E4C5 n4:271B58D1-363D-11E5-9242-09173F13E4C5 n4:271B58D2-363D-11E5-9242-09173F13E4C5 n4:271B58CF-363D-11E5-9242-09173F13E4C5 n4:271B58D0-363D-11E5-9242-09173F13E4C5 n4:271B58DC-363D-11E5-9242-09173F13E4C5
owl:sameAs
n32:DB00889 n33:DB00889
dcterms:title
Granisetron
adms:identifier
n13:Granisetron n19:3510 n20:46505137 n21:0378-1003-94 n22:PA449809 n23:C07023 n24:D04370 n25:2300 n26:2300 n27:DB00889 n28:50000483 n29:3390
n3:mechanismOfAction
Granisetron is a potent, selective antagonist of 5-HT<sub>3</sub> receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
n3:packager
n4:271B58C9-363D-11E5-9242-09173F13E4C5 n4:271B58CA-363D-11E5-9242-09173F13E4C5 n4:271B58C7-363D-11E5-9242-09173F13E4C5 n4:271B58C8-363D-11E5-9242-09173F13E4C5 n4:271B58CD-363D-11E5-9242-09173F13E4C5 n4:271B58CE-363D-11E5-9242-09173F13E4C5 n4:271B58CB-363D-11E5-9242-09173F13E4C5 n4:271B58CC-363D-11E5-9242-09173F13E4C5 n4:271B58B1-363D-11E5-9242-09173F13E4C5 n4:271B58B2-363D-11E5-9242-09173F13E4C5 n4:271B58AF-363D-11E5-9242-09173F13E4C5 n4:271B58B0-363D-11E5-9242-09173F13E4C5 n4:271B58B5-363D-11E5-9242-09173F13E4C5 n4:271B58B6-363D-11E5-9242-09173F13E4C5 n4:271B58B3-363D-11E5-9242-09173F13E4C5 n4:271B58B4-363D-11E5-9242-09173F13E4C5 n4:271B58C1-363D-11E5-9242-09173F13E4C5 n4:271B58C2-363D-11E5-9242-09173F13E4C5 n4:271B58BF-363D-11E5-9242-09173F13E4C5 n4:271B58C0-363D-11E5-9242-09173F13E4C5 n4:271B58C5-363D-11E5-9242-09173F13E4C5 n4:271B58C6-363D-11E5-9242-09173F13E4C5 n4:271B58C3-363D-11E5-9242-09173F13E4C5 n4:271B58C4-363D-11E5-9242-09173F13E4C5 n4:271B58B9-363D-11E5-9242-09173F13E4C5 n4:271B58BA-363D-11E5-9242-09173F13E4C5 n4:271B58B7-363D-11E5-9242-09173F13E4C5 n4:271B58B8-363D-11E5-9242-09173F13E4C5 n4:271B58BD-363D-11E5-9242-09173F13E4C5 n4:271B58BE-363D-11E5-9242-09173F13E4C5 n4:271B58BB-363D-11E5-9242-09173F13E4C5 n4:271B58BC-363D-11E5-9242-09173F13E4C5
n3:patent
n6:2158354 n6:2100777 n6:5952340 n6:7608282
n3:routeOfElimination
The remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces.
n3:synonym
Granisetronum BRL-43694 SID90340785 Sancuso Granisetron
n3:toxicity
LD<sub>50</sub>&gt;2000 mg/kg (rat, oral)
n7:hasAHFSCode
n8:56-22-20
n3:foodInteraction
Take without regard to meals.
n3:proteinBinding
65%
n3:salt
n3:synthesisReference
Neal Ward, David Alan Jones, Victor Witold Jacewicz, "Process for the preparation of granisetron." U.S. Patent US6268498, issued April, 1986.
n16:hasConcept
n17:M0026935
foaf:page
n11:granisetron.htm n30:granisetron.html
n3:IUPAC-Name
n5:271B5900-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B5906-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B5905-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B5902-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B5903-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B5904-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B58FE-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B58FC-363D-11E5-9242-09173F13E4C5 n5:271B58FF-363D-11E5-9242-09173F13E4C5 n5:271B5917-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B58FD-363D-11E5-9242-09173F13E4C5
n7:hasATCCode
n18:A04AA02
n3:H-Bond-Acceptor-Count
n5:271B590C-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B590D-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B5907-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B5908-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B590A-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B5909-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B590B-363D-11E5-9242-09173F13E4C5
n3:absorption
Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
109889-09-0
n3:category
n3:clearance
* 0.52 L/h/kg [Cancer Patients with 1 mg bid for 7 days] * 0.41 L/h/kg [Healthy subject with a single 1 mg dose]
n3:containedIn
n15:271B58ED-363D-11E5-9242-09173F13E4C5 n15:271B58EE-363D-11E5-9242-09173F13E4C5 n15:271B58EB-363D-11E5-9242-09173F13E4C5 n15:271B58EC-363D-11E5-9242-09173F13E4C5 n15:271B58F1-363D-11E5-9242-09173F13E4C5 n15:271B58F2-363D-11E5-9242-09173F13E4C5 n15:271B58EF-363D-11E5-9242-09173F13E4C5 n15:271B58F0-363D-11E5-9242-09173F13E4C5 n15:271B58F3-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B5912-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B5914-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B5915-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n5:271B5916-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B5911-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B5910-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B5913-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B5901-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B590E-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B590F-363D-11E5-9242-09173F13E4C5