Argatroban.
Argatroban is a direct thrombin inhibitor synthesised to bind to the catalytic site of the thrombin molecule. It binds rapidly and reversibly to both clot-bound and soluble thrombin. The relatively short elimination half-life of argatroban (39 to 51 minutes) and its reversible binding allow rapid achievement of therapeutic effect on initiation of therapy and rapid restoration of normal haemostasis upon cessation of therapy. Argatroban produces a predictable dose response that is well correlated with changes in anticoagulant parameters. Argatroban, given to patients with heparin-induced thrombocytopenia (HIT) and heparin-induced thrombocytopenia with thrombosis (HITTS) in a large scale, nonrandomised, prospective trial, reduced a combined end-point of morbidity and mortality when compared with historical controls. Argatroban was well tolerated in clinical trials of patients with HIT and caused no increase in bleeding risk compared with historical controls.
McKeage
K
K
Adis International Limited, Auckland, New Zealand. demail@adis.co.nz
Plosker
G L
GL
D000818:Animals; D000991:Antithrombins / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001120:Arginine / Q000031:analogs & derivatives; D002986:Clinical Trials as Topic; D006207:Half-Life; D006801:Humans; D010875:Pipecolic Acids / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D013449:Sulfonamides; D013921:Thrombocytopenia / Q000188:drug therapy*
D000991:Antithrombins; D010875:Pipecolic Acids; D013449:Sulfonamides; D001120:Arginine; C031942:argatroban