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Namespace Prefixes

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Statements

Subject Item
n2:DB00001
rdf:type
n3:Drug
n3:description
Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.
n3:generalReferences
# Smythe MA, Stephens JL, Koerber JM, Mattson JC: A comparison of lepirudin and argatroban outcomes. Clin Appl Thromb Hemost. 2005 Oct;11(4):371-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16244762 # Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16690967 # Lubenow N, Eichler P, Lietz T, Greinacher A: Lepirudin in patients with heparin-induced thrombocytopenia - results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3. J Thromb Haemost. 2005 Nov;3(11):2428-36. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16241940 # Askari AT, Lincoff AM: Antithrombotic Drug Therapy in Cardiovascular Disease. 2009 Oct; pp. 440–. ISBN 9781603272346. "Google books":http://books.google.com/books?id=iadLoXoQkWEC&pg=PA440.
n3:group
approved
n3:halfLife
Approximately 1.3 hours
n3:indication
For the treatment of heparin-induced thrombocytopenia
n3:manufacturer
n25:271B3E74-363D-11E5-9242-09173F13E4C5
owl:sameAs
n9:DB00001 n14:DB00001
dcterms:title
Lepirudin
adms:identifier
n16:50419-150-57 n18:DB00001 n21:D06880 n22:PA450195 n23:Lepirudin n24:P01050
n3:mechanismOfAction
Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
n3:packager
n25:271B3E72-363D-11E5-9242-09173F13E4C5 n25:271B3E73-363D-11E5-9242-09173F13E4C5
n3:patent
n11:1339104 n11:5180668
n3:routeOfElimination
Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
n3:synonym
Hirudin variant-1
n3:toxicity
In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
n3:volumeOfDistribution
* 12.2 L [Healthy young subjects (n = 18, age 18-60 years)] * 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)] * 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)] * 32.1 L [HIT patients (n = 73)]
n19:hasAHFSCode
n26:20-12-04-12
n5:hasConcept
n6:M0222237
foaf:page
n13:lepirudin.htm n17:lepirudin.html
n3:Molecular-Formula
n4:271B3E7A-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B3E79-363D-11E5-9242-09173F13E4C5
n19:hasATCCode
n20:B01AE02
n3:absorption
Bioavailability is 100% following injection.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
120993-53-5
n3:category
n3:clearance
* 164 ml/min [Healthy 18-60 yrs] * 139 ml/min [Healthy 65-80 yrs] * 61 ml/min [renal impaired] * 114 ml/min [HIT (Heparin-induced thrombocytopenia)]
n3:containedIn
n10:271B3E75-363D-11E5-9242-09173F13E4C5
n3:Hydrophobicity
n4:271B3E77-363D-11E5-9242-09173F13E4C5
n3:Isoelectric-Point
n4:271B3E78-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B3E76-363D-11E5-9242-09173F13E4C5