Meyer B H, Luus H G, Müller F O, Badenhorst P N, Röthig H J
Department of Pharmacology, University of the Orange Free State, Bloemfontein.
S Afr Med J. 1990 Sep 1;78(5):268-70.
A new anticoagulant, recombinant hirudin, was given to healthy volunteers (5 per test dose) in single intravenous doses of 0.01, 0.02, 0.04, 0.07 and 0.1 mg/kg to study its anticoagulant effects, how it was tolerated and its pharmacokinetics. Hirudin proved to be a potent anticoagulant with important effects on thrombin (increase in thrombin time and partial thromboplastin time). The maximum pharmacodynamic effect was achieved with the 0.07 mg/kg dose, and upwards. All doses of the compound were tolerated without side-effects. The mean elimination half-life is about 1 hour. Mean total clearance and volume of distribution are approximately 190 ml/min and 14 l, respectively. Hirudin obeys first-order pharmacokinetics.
一种新型抗凝剂重组水蛭素，以0.01、0.02、0.04、0.07和0.1毫克/千克的单次静脉注射剂量给予健康志愿者（每个测试剂量5人），以研究其抗凝作用、耐受性及药代动力学。水蛭素被证明是一种强效抗凝剂，对凝血酶有重要影响（凝血酶时间和部分凝血活酶时间增加）。0.07毫克/千克及以上剂量可达到最大药效学效应。该化合物的所有剂量耐受性良好，无副作用。平均消除半衰期约为1小时。平均总清除率和分布容积分别约为190毫升/分钟和14升。水蛭素符合一级药代动力学。
