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关于乙酰水杨酸的血小板聚集抑制及镇痛活性(作者译)

[On the platelet aggregation inhibiting and analgesic activities of acetylsalicylic acid (author's transl)].

作者信息

Schnell O, Lang E, Bertholdt H

出版信息

Arzneimittelforschung. 1980;30(11):1917-22.

PMID:7193003
Abstract

Acetylsalicylic acid (ASA)--now the most potent platelet-aggregation inhibitor--is being investigated in combination with glycine (Godamed; text preparation A) and microencapsulated (test preparation B) in view of the plasma total salicylate level and platelet aggregation inhibiting effect. The examination is conducted on 20 patients by the cross-over method. An increase of the plasma total salicylate level of test preparation A compared with test preparation B is highly significant up to 60 min after application of 1000 mg ASA respectively. As in shorter time a higher plasma total salicylate level is reached a significantly higher analgesic effect of the test preparation A may be expected. In certain indications, occurring with pain, as for instance arterial occlusive disease, thrombophlebitis, etc., this is absolutely desired. Additional application of analgetics is then often unnecessary. A differentiated use of ASA preparations as platelet-aggregation inhibitors is therefore required. To investigate the disaggregating effect of both ASA preparations the PAT-III test by Breddin was used. 2 h after the oral application of 1000 mg ASA a complete normalisation by both ASA preparations was reached, whereas before a significant higher platelet aggregation had been recognized. The somewhat faster reached effect of test preparation A is not significant and clinically not relevant. When in the acute phase as well as in the long-term treatment of the above mentioned indications an ASA-containing platelet-aggregation inhibitor is used, that preparation should get preference which is well tolerable and has the same platelet-disaggregating effect but with the higher analgesic effect.

摘要

乙酰水杨酸(ASA)——目前最强效的血小板聚集抑制剂——正与甘氨酸(戈达美;制剂A)联合以及微囊化形式(制剂B)进行研究,观察其血浆总水杨酸水平和血小板聚集抑制效果。采用交叉法对20名患者进行检测。分别服用1000毫克ASA后,制剂A的血浆总水杨酸水平在60分钟内相比制剂B显著升高。由于在更短时间内就能达到更高的血浆总水杨酸水平,因此可以预期制剂A具有显著更高的镇痛效果。在某些伴有疼痛的病症中,如动脉闭塞性疾病、血栓性静脉炎等,这是非常理想的。这样通常就无需额外使用镇痛药。因此,需要对作为血小板聚集抑制剂的ASA制剂进行差异化使用。为研究两种ASA制剂的解聚作用,采用了布雷丁的PAT-III试验。口服1000毫克ASA 2小时后,两种ASA制剂均使血小板聚集完全恢复正常,而在此之前血小板聚集明显更高。制剂A起效稍快但差异不显著,临床上也无相关性。当在上述病症的急性期以及长期治疗中使用含ASA的血小板聚集抑制剂时,应优先选用耐受性良好、具有相同血小板解聚效果但镇痛效果更佳的制剂。

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