Abstract
Argatroban, a direct thrombin inhibitor, is used clinically because of its safe and
effective antithrombotic action. This drug of low molecular weight shows reversible
inhibition of thrombin irrespective of whether thrombin is fibrin-bound or soluble.
Optimal anticoagulant effects can easily be attained by monitoring with the activated
partial thromboplastin time or whole-blood activated clotting time when a therapeutic
range of argatroban equivalent to that of heparin is used. The antithrombotic action
is simply detected with a chromogenic substrate assay. The clinical use of the drug
in Japan was approved for the treatment of chronic peripheral arterial obstructive
disease and acute ischemic stroke. For coronary artery disease in patients with deficiency
of antithrombin activities attributable to either antithrombin III or heparin cofactor
II deficiency, argatroban is effective as an anticoagulant. Acute coronary occlusion
during and after percutaneous transluminal coronary angioplasty can be treated by
argatroban as an alternative to heparin. The presence of platelets activated by a
trace amount of thrombin is evidenced by modified methods of platelet aggregometry
in acute ischemic stroke. Therefore, argatroban can render the platelets insensitive
against the platelet hyperaggregation enhanced by thrombin.
Keywords:
Argatroban - thrombin inhibitor - monitoring - cardiovascular disease - acute ischemic
stroke
