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低分子肝素及肝素类似物抗凝作用的体内研究。II. 肝素类似物的作用

In vivo studies on the inhibition of coagulation by fractionated heparin and by a heparin analogue. II. Effects of a heparin analogue.

作者信息

Schmitz-Huebner U, Asbeck F, van de Loo J

出版信息

Thromb Haemost. 1981 Oct;46(3):617-20.

PMID:6797091
Abstract

SSHA, a semi-synthetic heparin analogue, and sodium heparin from porcine intestinal mucosa were injected subcutaneously into six healthy volunteers over a period of three days in a cross-over trial. Before injection and 2, 4, 6, 8 hrs afterwards, the heparin-like activity was measured with the APTT, the anti-Xa clotting test and two chromogenic substrate assays. The results show that SSHA mediates both anti-Xa and antithrombin activities in vivo. A comparison between the effects of SSHA and heparin is problematical due to the heterogeneity of different heparin preparations. Low doses of the analogue (45 mg s.c.) induced proportionally higher and longer lasting anti-Xa activities than higher doses (90 mg s.c.). Repeated injections of SSHA twice daily led to increasing effects on two tests for heparin-like activity, whereas two other tests remained unchanged. Both drugs were tolerated equally well, side effects were not detected. Clinical studies are required to demonstrate whether SSHA is similar or superior to low-dose heparin for use in thrombosis prophylaxis.

摘要

在一项交叉试验中,将半合成肝素类似物SSHA和来自猪肠黏膜的肝素钠在三天时间内皮下注射给六名健康志愿者。注射前以及注射后2、4、6、8小时,用活化部分凝血活酶时间(APTT)、抗Xa凝血试验和两种显色底物测定法测量肝素样活性。结果表明,SSHA在体内介导抗Xa和抗凝血酶活性。由于不同肝素制剂的异质性,比较SSHA和肝素的效果存在问题。低剂量的类似物(皮下注射45毫克)比高剂量(皮下注射90毫克)诱导出成比例更高且持续时间更长的抗Xa活性。每天两次重复注射SSHA对两种肝素样活性检测产生递增效应,而另外两种检测保持不变。两种药物的耐受性相同,未检测到副作用。需要进行临床研究以证明SSHA在预防血栓形成方面是否与低剂量肝素相似或更优。

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