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Namespace Prefixes

PrefixIRI
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n4http://linked.opendata.cz/resource/drugbank/dosage/
n11http://linked.opendata.cz/resource/drugbank/drug/DB06228/identifier/wikipedia/
n21http://www.rxlist.com/
n20http://bio2rdf.org/drugbank:
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n6http://linked.opendata.cz/resource/drugbank/patent/
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n5http://linked.opendata.cz/resource/drugbank/property/
n13http://linked.opendata.cz/resource/drugbank/drug/DB06228/identifier/national-drug-code-directory/
xsdhhttp://www.w3.org/2001/XMLSchema#
n15http://linked.opendata.cz/resource/atc/
n14http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06228
rdf:type
n3:Drug
n3:description
Rivaroxaban is an anticoagulant and the first orally active direct factor Xa inhibitor. Unlike warfarin, routine lab monitoring of INR is not necessary. However there is no antidote available in the event of a major bleed. Only the 10 mg tablet can be taken without regard to food. The 15 mg and 20 mg tablet should be taken with food. FDA approved on July 1, 2011.
n3:dosage
n4:271B4AF2-363D-11E5-9242-09173F13E4C5 n4:271B4AF3-363D-11E5-9242-09173F13E4C5 n4:271B4AEF-363D-11E5-9242-09173F13E4C5 n4:271B4AF4-363D-11E5-9242-09173F13E4C5 n4:271B4AEE-363D-11E5-9242-09173F13E4C5 n4:271B4AF0-363D-11E5-9242-09173F13E4C5 n4:271B4AF1-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Piccini JP, Patel MR, Mahaffey KW, Fox KA, Califf RM: Rivaroxaban, an oral direct factor Xa inhibitor. Expert Opin Investig Drugs. 2008 Jun;17(6):925-37. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18491993 # Alban S: Pharmacological strategies for inhibition of thrombin activity. Curr Pharm Des. 2008;14(12):1152-75. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18473863 # Stevenson M, Scope A, Holmes M, Rees A, Kaltenthaler E: Rivaroxaban for the prevention of venous thromboembolism: a single technology appraisal. Health Technol Assess. 2009 Oct;13 Suppl 3:43-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19846028 # Imberti D, Dall'Asta C, Pierfranceschi MG: Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review. Intern Emerg Med. 2009 Dec;4(6):471-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19696978 # Alexander D, Jeremias A: Rivaroxaban in the contemporary treatment of acute coronary syndromes. Expert Opin Investig Drugs. 2011 Jun;20(6):849-57. Epub 2011 May 10. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21554163 # Cabral KP: Pharmacology of the new target-specific oral anticoagulants. J Thromb Thrombolysis. 2013 May 5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23645472
n3:group
approved
n3:halfLife
The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly.
n3:indication
Rivaroxaban is indicated for the prevention of venous thromboembolic events (VTE) in patients who have undergone total hips replacements and total knee replacement surgery; prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE); to reduce risk of recurrent DVT and/or PE. Due to a lack of safety studies, it is not recommended for use in those under 18 years old. Its use is also not recommended in those with severe renal impairment (<30mL/min).
owl:sameAs
n17:DB06228 n20:DB06228
dcterms:title
Rivaroxaban
adms:identifier
n8:68579 n11:Rivaroxaban n12:D07086 n13:50458-579-10 n24:DB06228
n3:mechanismOfAction
Rivaroxaban competitively inhibits free and clot bound factor Xa. Factor Xa is needed to activate prothrombin (factor II) to thrombin (factor IIa). Thrombin is a serine protease that is required to activate fibrinogen to fibrin, which is the loose meshwork that completes the clotting process. Since one molecule of factor Xa can generate more than 1000 molecules of thrombin, selective inhibitors of factor Xa are profoundly useful in terminating the amplification of thrombin generation. The action of rivaroxaban is irreversible.
n3:patent
n6:2547113 n6:2396561
n3:routeOfElimination
Approximately two-thirds of rivaroxaban is excreted into urine (via active tubular secretion in which approximately 36% as unchanged drug and 30% as inactive metabolism). The remaining third of the administered dose is excreted via feces in which 7% is in the form of unchanged drug and 21% as inactive metabolites.
n3:synonym
BAY 59-7939 Xarelto BAY59-7939
n3:toxicity
Excessive bleeding. Overdosages should be treated using activated charcoal and supportive measures such as mechanical compression and hemodynamic support. If bleeding is not controlled, the following procoagulants can be administered: activated prothrombin complex concentrate, prothrombin complex concentrate and recombinant factor VIIa. There is also a higher chance of post procedural hemorrhage compared to enoxaparin (1.55% vs. 1.39% respectively).
n3:volumeOfDistribution
The steady state Vd is 50 L
n14:hasAHFSCode
n22:20-12-04-14
n3:foodInteraction
St. John's Wort is a CYP3A4 inducer and will decrease levels of rivaroxaban Foods with antiplatelet/anticoagulants properties such as horseradish, gingko, ginger, garlic, feverfew Food should be taken with the 15 mg and 20 mg tablet. Food increases the bioavailability of the 20 mg dose.
n3:proteinBinding
Plasma protein binding is about 92% to 95%
n3:synthesisReference
Prabhudas BODHURI, Gamini Weeratunga, "PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF." U.S. Patent US20100273790, issued October 28, 2010.
n18:hasConcept
n19:M0501463
foaf:page
n10:rivaroxaban.html n21:xarelto-drug.htm
n3:IUPAC-Name
n5:271B4AF9-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4AFF-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4AFE-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4AFB-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4AFC-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4AFD-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4AF7-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4AF8-363D-11E5-9242-09173F13E4C5 n5:271B4AF5-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4AF6-363D-11E5-9242-09173F13E4C5
n14:hasATCCode
n15:B01AF01
n3:H-Bond-Acceptor-Count
n5:271B4B05-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4B06-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B4B00-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B4B01-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B4B03-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B4B02-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B4B04-363D-11E5-9242-09173F13E4C5
n3:absorption
Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. However, the 15-20 mg dose have a lower bioavailability if taken in the fasted state and consequently should be taken with food.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
366789-02-8
n3:clearance
Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h.
n3:Bioavailability
n5:271B4B0B-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4B0D-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4B0E-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4B0A-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4B09-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4B0C-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4AFA-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4B07-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4B08-363D-11E5-9242-09173F13E4C5