title: Pharmacology of argatroban.
abstract: Argatroban is a synthetic, small-molecule direct thrombin inhibitor that is approved in the USA, the EU and Japan for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT), and for anticoagulation of HIT patients undergoing PCI. Argatroban binds reversibly to, and inhibits both soluble and clot-bound thrombin. Argatroban does not generate antibodies, is not susceptible to degradation by proteases and is cleared hepatically. It has a predictable anticoagulant effect and there is a good correlation between dose, plasma concentration and pharmacodynamic effect. Initial clinical studies suggest that further investigations to establish the use of argatroban in ischemic stroke, acute coronary syndrome, hemodialysis, blood oxygenation, off-pump cardiac surgery and other clinical indications are warranted.
authors.affiliation: Cardiovascular Institute, Loyola University Medical Center, 2160 S. First Avenue, Maywood, IL 60153, USA. wjeske@lumc.edu
authors.forename: Walter P
authors.initials: WP
authors.lastname: Jeske
authors.forename: Jawed
authors.initials: J
authors.lastname: Fareed
authors.forename: Debra A
authors.initials: DA
authors.lastname: Hoppensteadt
authors.forename: Bruce
authors.initials: B
authors.lastname: Lewis
authors.forename: Jeanine M
authors.initials: JM
authors.lastname: Walenga
mesh_terms: D054058:Acute Coronary Syndrome / Q000188:drug therapy / Q000517:prevention & control; D000991:Antithrombins / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001120:Arginine / Q000031:analogs & derivatives; D005062:European Union; D005260:Female; D006493:Heparin / Q000009:adverse effects; D006801:Humans; D007536:Isomerism; D007564:Japan; D008297:Male; D057786:Peptidomimetics / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D010875:Pipecolic Acids / Q000494:pharmacology* / Q000627:therapeutic use; D020521:Stroke / Q000188:drug therapy / Q000517:prevention & control; D013449:Sulfonamides; D013917:Thrombin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013921:Thrombocytopenia / Q000139:chemically induced / Q000188:drug therapy / Q000517:prevention & control; D013927:Thrombosis / Q000188:drug therapy* / Q000517:prevention & control; D014481:United States
chemical_list: D000991:Antithrombins; D057786:Peptidomimetics; D010875:Pipecolic Acids; D013449:Sulfonamides; D006493:Heparin; D001120:Arginine; D013917:Thrombin; C031942:argatroban