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Argatroban
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Argatroban
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| Systematic (IUPAC) name |
(2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-
[[(3R)-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]
sulfonylamino]pentanoyl]-4-methyl-piperidine-2-
carboxylic acid |
| Identifiers |
| CAS number |
74863-84-6 |
| ATC code |
B01AE03 |
| PubChem |
152951 |
| DrugBank |
APRD00105 |
| Chemical data |
| Formula |
C23H36N6O5S |
| Mol. mass |
508.635 g/mol |
| Pharmacokinetic data |
| Bioavailability |
100% (intravenous) |
| Protein binding |
54% |
| Metabolism |
hepatic |
| Half life |
39 and 51 minutes |
| Excretion |
? |
| Therapeutic considerations |
| Pregnancy cat. |
?
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| Legal status |
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| Routes |
intravenous |
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.[1] In 2000, argatroban was licensed by the Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). In 2002, it was approved for use during percutaneous coronary interventions in patients who have HIT or are at risk for developing it.
Argatroban is given intravenously. Argatroban is metabolized in the liver and has a half life of about 50 minutes. It is monitored by PTT. Because of its hepatic metabolism, it may be used in patients with renal dysfunction. (This is in contrast to lepirudin, a direct thrombin inhibitor that is primarily renally cleared).
It is manufactured by GlaxoSmithKline.
References
- ^ Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288
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Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01) |
| Vitamin K antagonists |
Acenocoumarol • Clorindione • Coumatetralyl • Dicumarol (Dicoumarol) • Diphenadione • Ethyl biscoumacetate • Phenprocoumon • Phenindione • Tioclomarol • Warfarin |
| Heparin group |
Antithrombin III • Danaparoid • Heparin • Sulodexide • low molecular weight heparin (Bemiparin, Dalteparin, Enoxaparin, Nadroparin, Parnaparin, Reviparin, Tinzaparin) |
| Glycoprotein IIb/IIIa inhibitors |
Abciximab • Eptifibatide • Tirofiban |
Other platelet
aggregation inhibitors |
Acetylsalicylic acid/Aspirin • Aloxiprin • Ditazole • Carbasalate calcium • Cloricromen • Dipyridamole • Indobufen • Picotamide • Triflusal • ADP receptor inhibitors (Clopidogrel, Ticlopidine, Prasugrel) • prostaglandin analogue (Beraprost, Prostacyclin, Iloprost, Treprostinil) |
| Enzymes |
plasminogen activators (Alteplase/Reteplase/Tenecteplase, Streptokinase, Urokinase/Saruplase, Anistreplase) • other serine endopeptidases (Ancrod, Drotrecogin alfa/Protein C, Fibrinolysin) • Brinase |
| Direct thrombin inhibitors |
Argatroban • Bivalirudin • Dabigatran • Desirudin • Hirudin • Lepirudin • Melagatran • Ximelagatran |
| Other antithrombotics |
Defibrotide • Dermatan sulfate • Fondaparinux • Rivaroxaban |
| Non-medicinal |
Citrate • EDTA • Oxalate |
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Argatroban". A list of authors is available in Wikipedia.
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