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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2017/05/28 00:41:55」(JST)
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Lepirudin
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Clinical data |
Trade names |
Refludan |
AHFS/Drugs.com |
Monograph |
Pregnancy
category |
- US: B (No risk in non-human studies)
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Routes of
administration |
SQ or IV |
ATC code |
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Legal status |
Legal status |
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Pharmacokinetic data |
Bioavailability |
100 |
Biological half-life |
~1.3 hours |
Excretion |
Renal |
Identifiers |
IUPAC name
- [Leu1,Thr2]-63-desulfohirudin
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CAS Number |
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IUPHAR/BPS |
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DrugBank |
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ChemSpider |
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UNII |
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KEGG |
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ChEMBL |
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Chemical and physical data |
Formula |
C288H448N80O110S6 |
Molar mass |
6983.5 g/mol |
NY (what is this?) (verify) |
Lepirudin is an anticoagulant that functions as a direct thrombin inhibitor.
Brand name: Refludan, Generic: Lepirudin rDNA for injection.
Lepirudin is a recombinant hirudin[1] derived from yeast cells. It is almost identical to hirudin extracted from Hirudo medicinalis. It differs by the 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.
Lepirudin may be used as an anticoagulant when heparins (unfractionated or low-molecular-weight) are contraindicated because of heparin-induced thrombocytopenia.
Market withdrawal
Bayer announced that it ceased the production of lepirudin (Refludan) on May 31, 2012. At the time of the announcement, the company expected that supply from wholesalers was going to be depleted by mid-2013.[2]
References
- ^ Arman T. Askari; A. Michael Lincoff (October 2009). Antithrombotic Drug Therapy in Cardiovascular Disease. Springer. pp. 440–. ISBN 978-1-60327-234-6. Retrieved 30 October 2010.
- ^ http://www.ashp.org/menu/DrugShortages/DrugsNoLongerAvailable/Bulletin.aspx?id=924
External links
- Smythe M, Stephens J, Koerber J, Mattson J (2005). "A comparison of lepirudin and argatroban outcomes.". Clin Appl Thromb Hemost. 11 (4): 371–4. doi:10.1177/107602960501100403. PMID 16244762.
- Tardy, B; Lecompte, T; Boelhen, F; Tardy-Poncet, B; Elalamy, I; Morange, P; Gruel, Y; Wolf, M; François, D (2006). "Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin". Blood. 108 (5): 1492–6. doi:10.1182/blood-2006-02-001057. PMID 16690967.
- Lubenow N, Eichler P, Lietz T, Greinacher A (2005). "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. 3 (11): 2428–36. doi:10.1111/j.1538-7836.2005.01623.x. PMID 16241940.
Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)
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Antiplatelet drugs |
Glycoprotein IIb/IIIa inhibitors |
- Abciximab
- Eptifibatide
- Orbofiban
- Roxifiban
- Sibrafiban§
- Tirofiban
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ADP receptor/P2Y12 inhibitors |
- Thienopyridines
- Clopidogrel
- Prasugrel
- Ticlopidine
- Nucleotide/nucleoside analogs
- Cangrelor
- Elinogrel
- Ticagrelor
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Prostaglandin analogue (PGI2) |
- Beraprost
- Iloprost
- Prostacyclin
- Treprostinil
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COX inhibitors |
- Acetylsalicylic acid/Aspirin#
- Aloxiprin
- Carbasalate calcium
- Indobufen
- Triflusal
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Thromboxane inhibitors |
- Thromboxane synthase inhibitors
- Dipyridamole (+ aspirin)
- Picotamide
- Terbogrel
- Receptor antagonists
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Phosphodiesterase inhibitors |
- Cilostazol
- Dipyridamole
- Triflusal
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Other |
- Cloricromen
- Ditazole
- Vorapaxar
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Anticoagulants |
Vitamin K antagonists
(inhibit II, VII, IX, X) |
- Coumarins: Acenocoumarol
- Coumatetralyl
- Dicoumarol
- Ethyl biscoumacetate
- Phenprocoumon
- Warfarin#
- 1,3-Indandiones: Clorindione
- Diphenadione
- Phenindione
- Other: Tioclomarol
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Factor Xa inhibitors
(with some II inhibition) |
Heparin group/
glycosaminoglycans/
(bind antithrombin) |
- Low molecular weight heparin
- Bemiparin
- Certoparin
- Dalteparin
- Enoxaparin
- Nadroparin
- Parnaparin
- Reviparin
- Tinzaparin‡
- Oligosaccharides
- Fondaparinux
- Idraparinux§
- Heparinoids
- Danaparoid
- Dermatan sulfate
- Sulodexide
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Direct Xa inhibitors ("xabans") |
- Apixaban
- Betrixaban†
- Darexaban§
- Edoxaban
- Otamixaban§
- Rivaroxaban
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Direct thrombin (IIa) inhibitors |
- Bivalent: Hirudin
- Bivalirudin
- Desirudin
- Lepirudin
- Univalent: Argatroban
- Dabigatran
- Efegatran
- Inogatran§
- Melagatran‡
- Ximelagatran‡
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Other |
- Antithrombin III
- Defibrotide
- Protein C
- Ramatroban
- REG1
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Thrombolytic drugs/
fibrinolytics |
- Plasminogen activators: r-tPA
- Alteplase
- Reteplase
- Tenecteplase
- UPA
- Anistreplase
- Monteplase
- Streptokinase#
- Other serine endopeptidases: Ancrod
- Brinase
- Fibrinolysin
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Non-medicinal |
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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UpToDate Contents
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English Journal
- Reciprocal relationship between contact and complement system activation on artificial polymers exposed to whole human blood.
- Huang S1, Engberg AE2, Jonsson N3, Sandholm K1, Nicholls IA4, Mollnes TE5, Fromell K6, Nilsson B6, Ekdahl KN7.
- Biomaterials.Biomaterials.2016 Jan;77:111-9. doi: 10.1016/j.biomaterials.2015.10.067. Epub 2015 Nov 9.
- BACKGROUND: Inappropriate and uncontrolled activation of the cascade systems in the blood is a driving force in adverse inflammatory and thrombotic reactions elicited by biomaterials, but limited data are available on the activation of the contact system by polymers and the present study was underta
- PMID 26584351
- Successful use of a bivalirudin treatment protocol to prevent extracorporeal thrombosis in ambulatory hemodialysis patients with heparin-induced thrombocytopenia.
- Al-Ali FS1, Elsayed M1, Khalifa S2, Abdulla AE1, Tolba H1, Bouanane H1, Ibrahim R1, Hamad A1.
- Hemodialysis international. International Symposium on Home Hemodialysis.Hemodial Int.2015 Oct 26. doi: 10.1111/hdi.12379. [Epub ahead of print]
- Heparin-induced thrombocytopenia (HIT) is an uncommon problem in hemodialysis (HD) patients. There have been a few reports on the use of lepirudin, argatroban, or danaparoid in the management of extracorporeal thrombosis (ECT) during dialysis in these patients, because heparin is contraindicated. He
- PMID 26501237
- Platelets and protease-activated receptor-4 contribute to acetaminophen-induced liver injury in mice.
- Miyakawa K1, Joshi N2, Sullivan BP3, Albee R4, Brandenberger C3, Jaeschke H5, McGill MR5, Scott MA3, Ganey PE2, Luyendyk JP1, Roth RA2.
- Blood.Blood.2015 Oct 8;126(15):1835-43. doi: 10.1182/blood-2014-09-598656. Epub 2015 Jul 15.
- Acetaminophen (APAP)-induced liver injury in humans is associated with robust coagulation cascade activation and thrombocytopenia. However, it is not known whether coagulation-driven platelet activation participates in APAP hepatotoxicity. Here, we found that APAP overdose in mice caused liver damag
- PMID 26179083
Japanese Journal
- Deep vein and intracardiac thrombosis during the post-partum period in Behcet's disease
- HIWARKAR Prashant,STASI Roberto,SUTHERLAND George,SHANNON Muriel
- International journal of hematology 91(4), 679-686, 2010-05-21
- NAID 10026402175
Related Links
- Lepirudin is an anticoagulant that functions as a direct thrombin inhibitor. Brand name: Refludan, Generic: Lepirudin rDNA for injection. Lepirudin is a recombinant hirudin derived from yeast cells. It is almost identical to hirudin extracted from ...
- Lepirudin, a recombinant hirudin, is a direct irreversible thrombin inhibitor by binding to both free and clot-bound thrombin. It is approved for treatment of heparin-induced thrombocytopenia (HIT), which is a serious antibody-mediated drug ...
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