Nakajima K, Yamamoto S, Tsukamoto M, Nagakura M
J Pharmacobiodyn. 1982 May;5(5):356-62. doi: 10.1248/bpb1978.5.356.
The effects of dilazep on blood fibrinolytic system were studied in ex vivo experiment. Fibrinolytic activity in plasma was determined by the fibrin plate method at designed times after the administration of dilazep in guinea pigs, rabbits and mongrel dogs. In guinea pigs, fibrinolytic activity of euglobulin (plasminogen activator level, 1.10+/-0.08 CU/ml in control animals) rose to 1.53+/-0.24, 1.92+/-0.13 and 2.35+/-0.15 CU/ml 2 h after the p.o. administration of 30, 100 and 300 mg/kg of dilazep, respectively. Plasminogen levels in euglobulin were unchanged, however, plasmin inhibitory activities were lowered following the increase of plasminogen activator levels. About 2-fold increase of plasminogen activator level was also observed in rabbits 60 min after the p.o. administration of 300 mg/kg dilazep and returned to the initial level (0.054 CU/ml) within 3 h after the administration. A rapid increase of plasminogen activator level was observed in a case of the i.v. administration of dilazep into rabbits and mongrel dogs. In in vitro experiment, dilazep added to whole blood or plasma of guinea pigs ranging 0.1 to 1000 microgram/ml did not reveal any effects on plasminogen activator level or plasmin inhibitory activity in plasma.
在离体实验中研究了地拉卓对血液纤溶系统的影响。在豚鼠、兔和杂种犬给予地拉卓后的特定时间，采用纤维蛋白平板法测定血浆中的纤溶活性。在豚鼠中，口服30、100和300mg/kg地拉卓后2小时，优球蛋白的纤溶活性（对照动物的纤溶酶原激活物水平为1.10±0.08 CU/ml）分别升至1.53±0.24、1.92±0.13和2.35±0.15 CU/ml。优球蛋白中的纤溶酶原水平未改变，然而，随着纤溶酶原激活物水平的升高，纤溶酶抑制活性降低。在兔口服300mg/kg地拉卓60分钟后，纤溶酶原激活物水平也观察到约2倍的升高，并在给药后3小时内恢复到初始水平（0.054 CU/ml）。在兔和杂种犬静脉注射地拉卓的情况下，观察到纤溶酶原激活物水平迅速升高。在体外实验中，向豚鼠全血或血浆中添加0.1至1000μg/ml的地拉卓，未发现对血浆中的纤溶酶原激活物水平或纤溶酶抑制活性有任何影响。
