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普萘洛尔、心得宁和阿替洛尔对人血小板血栓素生成及血浆中前列腺素6-酮-F1α和E2水平的影响。

Effect of propranolol, practolol and atenolol on human platelet thromboxane formation and plasma levels of prostaglandins 6-keto-F1 alpha and E2.

作者信息

Brandt R, Seppälä E, Nowak J, Vapaatalo H

出版信息

Prostaglandins Leukot Med. 1984 Nov;16(2):191-203. doi: 10.1016/0262-1746(84)90071-4.

Abstract

The effects of three different beta-adrenergic blocking drugs, propranolol, practolol and atenolol on platelet thromboxane production and the release of prostacyclin and prostaglandin E2 into the circulation were investigated in healthy volunteers. The beta-adrenergic antagonists were administered intravenously at equipotent doses. The serum TxB2 levels after whole blood clotting and the arterial and venous plasma concentrations of 6-keto-PGF1 alpha and PGE2 were measured before and during a 60 min period after the administration of the drugs, using radioimmunoassay. Practolol and atenolol elicited a significant decrease in platelet thromboxane formation but remained without effect on plasma 6-keto-PGF1 alpha and PGE2 levels. In contrast, propranolol did not influence serum TxB2 concentrations but induced a significant increase in plasma content of 6-keto-PGF1 alpha and PGE2. The results indicate that beta-adrenergic antagonists alter the balance between the proaggregatory, vasoconstricting and antiaggregatory, vasodilating prostanoids in the human cardiovascular system. Although the direction of the action of these drugs seems to differ depending on the selectivity of the beta-adrenoceptor blocking properties the net effect of this action should be beneficial.

摘要

在健康志愿者中研究了三种不同的β-肾上腺素能阻滞剂(普萘洛尔、心得宁和阿替洛尔)对血小板血栓素生成以及前列环素和前列腺素E2释放进入循环的影响。以等效剂量静脉注射β-肾上腺素能拮抗剂。使用放射免疫分析法在给药前和给药后60分钟内测量全血凝固后的血清TxB2水平以及动脉和静脉血浆中6-酮-PGF1α和PGE2的浓度。心得宁和阿替洛尔可使血小板血栓素形成显著减少,但对血浆6-酮-PGF1α和PGE2水平无影响。相比之下,普萘洛尔不影响血清TxB2浓度,但可使血浆6-酮-PGF1α和PGE2含量显著增加。结果表明,β-肾上腺素能拮抗剂改变了人类心血管系统中促聚集、血管收缩和抗聚集、血管舒张的前列腺素之间的平衡。尽管这些药物的作用方向似乎因β-肾上腺素受体阻断特性的选择性而异,但这种作用的净效应应该是有益的。

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