| Attributes | Values |
|---|
| rdf:type
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| http://linked.open...gbank/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. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...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 (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly. (en)
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| http://linked.open...ugbank/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). (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...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. (en)
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| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - 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. (en)
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| http://linked.open.../drugbank/synonym
| - Xarelto (en)
- BAY 59-7939 (en)
- BAY59-7939 (en)
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| http://linked.open...drugbank/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). (en)
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| http://linked.open...umeOfDistribution
| - The steady state Vd is 50 L (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Foods with antiplatelet/anticoagulants properties such as horseradish, gingko, ginger, garlic, feverfew (en)
- St. John's Wort is a CYP3A4 inducer and will decrease levels of rivaroxaban (en)
- Food should be taken with the 15 mg and 20 mg tablet. Food increases the bioavailability of the 20 mg dose. (en)
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| http://linked.open...nk/proteinBinding
| - Plasma protein binding is about 92% to 95% (en)
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| http://linked.open...ynthesisReference
| - Prabhudas BODHURI, Gamini Weeratunga, "PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF." U.S. Patent US20100273790, issued October 28, 2010. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/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. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...rugbank/clearance
| - Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h. (en)
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
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