Argatroban

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Argatroban
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.

?
Legal status
Routes intravenous

Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. In 2000, argatroban was licensed by the Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. In 2002, it was approved for use during percutaneous coronary interventions in patients who have or at risk for developing HIT.

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.

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Antithrombotics (thrombolytics, anticoagulants, and antiplatelet drugs) (B01)
Vitamin K antagonists Acenocoumarol, Clorindione, Dicumarol (Dicoumarol), Diphenadione, Ethyl biscoumacetate, Phenprocoumon, Phenindione, Tioclomarol, Warfarin
Heparin group
(Platelet aggregation inhibitors)		 Antithrombin III, Bemiparin, Dalteparin, Danaparoid, Enoxaparin, Heparin, Nadroparin, Parnaparin, Reviparin, Sulodexide, Tinzaparin
Other platelet
aggregation inhibitors		 Abciximab, Acetylsalicylic acid (Aspirin), Aloxiprin, Beraprost, Ditazole, Carbasalate calcium, Cloricromen, Clopidogrel, Dipyridamole,Eptifibatide, Indobufen, Iloprost, Picotamide, Prasugrel,Prostacyclin, Ticlopidine, Tirofiban, Treprostinil, Triflusal
Enzymes Alteplase, Ancrod, Anistreplase, Brinase, Drotrecogin alfa, Fibrinolysin, Protein C, Reteplase, Saruplase, Streptokinase, Tenecteplase, Urokinase
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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