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前列环素衍生物伊洛前列素(ZK 36374)对稳定型心绞痛患者缺血运动后血小板功能的影响。

Effects of iloprost (ZK 36374), a prostacyclin derivative, on platelet function after ischaemic exercise in patients with stable angina pectoris.

作者信息

Grauso F, Biagi G, Puddu P, Bugiardini R, Capelli M, Coccheri S

机构信息

Department of Angiology and Blood Coagulation, University Hospital S. Orsola, Bologna, Italy.

出版信息

Thromb Res. 1987 Oct 15;48(2):131-43. doi: 10.1016/0049-3848(87)90409-9.

Abstract

The effect of a chemically stable prostacyclin analogue (Iloprost) on platelet function was investigated in a controlled study in patients with angiographically confirmed stable angina pectoris after ischaemic exercise. In placebo experiments, ADP platelet aggregation was increased after exercise only when measured in whole blood and not in PRP. While plasma thromboxane B2 levels were unchanged, those of 6-keto PGF1 alpha were significantly although transiently increased after exercise. Iloprost displayed a potent antiaggregating activity in PRP and also reversed platelet hyperaggregation occurring in whole blood determinations after exercise. Plasma thromboxane B2 levels were significantly reduced but occasionally a rebound increase occurred 30 min. after end of the infusion. In contrast plasma level of 6-keto PGF1 alpha did not change after Iloprost and its recorded post-exercise increase was counteracted, thus suggesting a negative feed-back mechanism between Iloprost and natural prostacyclin. The data also suggest that degradation of the analogue is probably accomplished through pathways different from those of PGI2.

摘要

在一项对照研究中,对血管造影证实患有缺血性运动后稳定型心绞痛的患者,研究了化学稳定的前列环素类似物(依洛前列素)对血小板功能的影响。在安慰剂实验中,仅在全血中测量时,运动后ADP诱导的血小板聚集增加,而在富血小板血浆(PRP)中则未增加。虽然血浆血栓素B2水平未变,但运动后6-酮-前列腺素F1α水平显著升高,不过是短暂性的。依洛前列素在PRP中显示出强大的抗聚集活性,并且还能逆转运动后全血测定中出现的血小板过度聚集。血浆血栓素B2水平显著降低,但在输注结束后30分钟偶尔会出现反跳性升高。相比之下,依洛前列素给药后6-酮-前列腺素F1α的血浆水平未改变,并且其运动后记录的升高被抵消,这表明依洛前列素与天然前列环素之间存在负反馈机制。数据还表明,该类似物的降解可能通过与前列环素(PGI2)不同的途径完成。

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