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[尿激酶给药后,用合成发色底物S-2444测定血液中α2-纤溶酶抑制剂,尤其是尿激酶活性的变化]

[The changes of alpha 2-plasmin inhibitor, and notably urokinase activities in blood measured by synthetic chromogenic substrates S-2444 after urokinase administration].

作者信息

Itoh Y, Tsuji K, Tanaka N, Yamada M, Nakanishi M, Ishihara M, Kobayashi M

出版信息

Nihon Sanka Fujinka Gakkai Zasshi. 1983 Jan;35(1):68-76.

PMID:6338134
Abstract

Thrombolytic therapy with Urokinase (UK) has often been successful but it is very difficult to determine the effective dosage of UK. It is reported that after UK administration, plasmin fibrinolytic activity was immediately inhibited by alpha 2-Plasmin inhibitor (alpha 2-PI). In this study, we used UK on patients with myoma to prevent the occurrence of thrombosis after operation and the initial decrease in alpha 2-PI activities following UK administration was investigated to determine the minimum effective dosage of UK required to suppress alpha 2-PI. An attempt was also made to measure UK activity in blood by means of chromogenic substrate S-2444, and in some cases by administering 60,000 I.U. UK, alpha 1-Antitrypsin (alpha 1-AT), alpha 2-Macroglobulin (alpha 2-M), Antithrombin III (AT III) and Plasminogen (Plg) were measured at the same time. The results were as follows: 1) By the drip infusion method. In all doses, alpha 2-PI and UK activity showed no remarkable change. 2) By the one shot method. a) A decrease in alpha 2-PI was observed following both 48,000 and 60,000 I.U. UK administration. It was noted that in the case of 48,000 I.U. UK, alpha 2-PI showed the lowest level, 60% of the pre-administration level. b) UK activity showed a gradual increase in the case of 60,000 I.U. UK only and large changes in the other cases. c) alpha 1-AT, alpha 2-M, AT III and Plg produced no remarkable changes. This indicated that the effective dosage of UK for suppressing alpha 2-PI was at least 48,000 I.U. UK with the one shot method, and alpha 2-PI is a reliable indicator of the effectiveness of UK therapy.

摘要

用尿激酶(UK)进行溶栓治疗常常是成功的,但很难确定UK的有效剂量。据报道,UK给药后,纤溶酶纤维蛋白溶解活性立即被α2 -纤溶酶抑制剂(α2 - PI)抑制。在本研究中,我们将UK用于子宫肌瘤患者以预防术后血栓形成,并研究UK给药后α2 - PI活性的初始下降情况,以确定抑制α2 - PI所需的UK最小有效剂量。还尝试通过发色底物S - 2444测定血液中的UK活性,在某些情况下,通过给予60,000国际单位的UK,同时测定α1 -抗胰蛋白酶(α1 - AT)、α2 -巨球蛋白(α2 - M)、抗凝血酶III(AT III)和纤溶酶原(Plg)。结果如下:1)通过滴注法。在所有剂量下,α2 - PI和UK活性均无明显变化。2)通过单次注射法。a)在给予48,000和60,000国际单位的UK后均观察到α2 - PI下降。注意到在给予48,000国际单位UK的情况下,α2 - PI显示出最低水平,为给药前水平的60%。b)仅在给予60,000国际单位UK的情况下,UK活性逐渐增加,在其他情况下变化较大。c)α1 - AT、α2 - M、AT III和Plg无明显变化。这表明采用单次注射法时,抑制α2 - PI的UK有效剂量至少为48,000国际单位,并且α2 - PI是UK治疗有效性的可靠指标。

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1
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