Lijnen H R, Stassen J M, Vanlinthout I, Fukao H, Okada K, Matsuo O, Collen D
Center for Thrombosis and Vascular Research, University of Leuven, Belgium.
Thromb Haemost. 1991 Oct 1;66(4):468-73.
The thrombolytic and pharmacokinetic properties of staphylokinase were compared with those of streptokinase in hamsters with a pulmonary embolus produced from human plasma or from hamster plasma, and in rabbits with a jugular vein blood clot produced from rabbit blood. In both models, a continuous intravenous infusion of staphylokinase and streptokinase over 60 min in hamsters or over 4 h in rabbits, induced dose-dependent progressive clot lysis in the absence of significant systemic activation of the fibrinolytic system. The results of thrombolytic potency (clot lysis at 30 min after the end of the infusion, in percent, versus dose administered, in mg/kg) were fitted with an exponentially transformed sigmoidal function (formula: see text) and the maximal percent clot lysis (c), the maximal rate of lysis (z = 1/4 ac.eb) and the dose at which the maximal rate of lysis is achieved (b) were determined. In hamsters with a pulmonary embolus produced from human plasma, streptokinase had a somewhat higher thrombolytic potency than staphylokinase, as revealed by a higher z value (2,100 +/- 1,100% lysis per mg/kg streptokinase administered versus 1,100 +/- 330% lysis per mg/kg for staphylokinase). In hamsters with a pulmonary embolus produced from hamster plasma, staphylokinase had a somewhat higher thrombolytic potency than streptokinase (z = 1,600 +/- 440 versus 1,200 +/- 370% lysis per mg/kg). Staphylokinase had a higher thrombolytic potency than streptokinase in rabbits,as revealed by a higher z-value (950 +/- 350% lysis per mg/kg staphylokinase administered versus 330 +/- 39% lysis per mg/kg for streptokinase) and a lower b-value (0.035 +/- 0.010 mg/kg staphylokinase versus 0.091 +/- 0.008 mg/kg for streptokinase.(ABSTRACT TRUNCATED AT 250 WORDS)
在由人血浆或仓鼠血浆产生肺栓塞的仓鼠以及由兔血产生颈静脉血栓的兔子中,对葡萄球菌激酶和链激酶的溶栓特性及药代动力学特性进行了比较。在这两种模型中,仓鼠连续60分钟或兔子连续4小时静脉输注葡萄球菌激酶和链激酶,在纤溶系统无显著全身激活的情况下,诱导剂量依赖性的渐进性血栓溶解。溶栓效力结果(输注结束后30分钟时的血栓溶解率,以百分比计,与给药剂量,以mg/kg计)用指数变换的S形函数拟合(公式:见正文),并确定最大血栓溶解百分比(c)、最大溶解速率(z = 1/4 ac·eb)以及达到最大溶解速率时的剂量(b)。在由人血浆产生肺栓塞的仓鼠中,链激酶的溶栓效力略高于葡萄球菌激酶,z值更高表明了这一点(每mg/kg链激酶给药的溶解率为2100±1100%,而每mg/kg葡萄球菌激酶给药的溶解率为1100±330%)。在由仓鼠血浆产生肺栓塞的仓鼠中,葡萄球菌激酶的溶栓效力略高于链激酶(每mg/kg的溶解率分别为1600±440%和1200±370%)。在兔子中,葡萄球菌激酶的溶栓效力高于链激酶,z值更高(每mg/kg葡萄球菌激酶给药的溶解率为950±350%,而每mg/kg链激酶给药的溶解率为330±39%)以及b值更低(葡萄球菌激酶为0.035±0.010 mg/kg,链激酶为0.091±0.008 mg/kg)表明了这一点。(摘要截断于250字)