Argatroban is a
direct antithrombin agent developed for the first time by Okamoto et al in 1978. Unlike
heparin, it manifests its
anticoagulant effect by binding directly to the active site of
thrombin. A phase II double-blind comparative study was conducted in 52 facilities with a placebo control. The
drug was administered by a slow
intravenous infusion at 60 mg/d for the first 2 days and then
at 10 mg twice daily for the subsequent 5 days.
Glycerol was used concomitantly as a basic
therapy for both the
argatroban and placebo groups. The results demonstrated superior improvements, particularly in neurological symptoms (motor
paralysis) and
daily living activities (walking, standing up, continuous sitting, and eating), in the
argatroban group compared with the placebo group. These improvements were observed from the early stage of administration. It was also found that administration of the
drug in the early stage of the disease gave better results. In the present study, although a hemorrhagic
cerebral infarct occurred in one case in the
argatroban group, this seemed to be no different from a spontaneous incidence, as it also occurred in two cases in the placebo group. Symptoms were not aggravated in any of the cases. These results indicate that
argatroban is an effective and safe
drug for the treatment of acute
cerebral thrombosis.