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在正常人体中,特他洛尔进行β受体阻滞时,无论有无环氧化酶抑制,肾脏灌注均得以保留。

Preserved renal perfusion during beta blockade by tertatolol with and without cyclooxygenase inhibition in normal humans.

作者信息

Reuse C, Leeman M, Degaute J P, Abramowicz M, Prost J F, Naeije R

机构信息

Department of Intensive Care, Erasme University Hospital, Brussels, Belgium.

出版信息

J Clin Pharmacol. 1988 Apr;28(4):312-6. doi: 10.1002/j.1552-4604.1988.tb03149.x.

Abstract

The systemic and renal hemodynamic effects of tertatolol, a new noncardioselective beta blocker without partial agonist activity, given alone or in combination with cyclooxygenase inhibition by acetylsalicylic acid (aspirin), were investigated in eight healthy volunteers. Tertatolol 5 mg, aspirin 1 g, tertatolol 5 mg together with aspirin 1 g and placebo were administered at 1-week intervals in a random order and in a double-blind fashion. Cardiac output was measured by Doppler echography and renal blood flow and glomerular filtration rate (GFR) by constant infusion techniques using (123I) iodohippurate and (51Cr) EDTA, respectively. Measurements were performed before and then successively 2 and 4 hours after oral intake of drugs or placebo. Tertatolol decreased cardiac output by 22% (P less than .05) and heart rate by 17% (P less than .05) without change in blood pressure, renal blood flow, and GFR. The same effects occurred when tertatolol was given together with aspirin. Either placebo or aspirin alone had no effect on systemic and renal hemodynamics. These results suggest that cardiac output is redistributed to the kidneys after tertatolol intake in normal humans. This favorable effect on renal hemodynamics is probably not mediated by a local release of vasodilating prostaglandins.

摘要

在8名健康志愿者中,研究了新型无部分激动剂活性的非选择性β受体阻滞剂替他洛尔单独使用或与乙酰水杨酸(阿司匹林)联合抑制环氧化酶时对全身和肾脏血流动力学的影响。替他洛尔5毫克、阿司匹林1克、替他洛尔5毫克与阿司匹林1克以及安慰剂以随机顺序、双盲方式每隔1周给药一次。分别采用多普勒超声心动图测量心输出量,采用(123I)碘马尿酸盐和(51Cr)乙二胺四乙酸通过恒速输注技术测量肾血流量和肾小球滤过率(GFR)。在口服药物或安慰剂之前以及之后2小时和4小时依次进行测量。替他洛尔使心输出量降低22%(P<0.05),心率降低17%(P<0.05),而血压、肾血流量和GFR无变化。替他洛尔与阿司匹林合用时也出现同样的效果。单独使用安慰剂或阿司匹林对全身和肾脏血流动力学均无影响。这些结果表明,在正常人体内服用替他洛尔后心输出量重新分布到肾脏。这种对肾脏血流动力学的有利作用可能不是由局部释放血管舒张性前列腺素介导的。

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