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曲帕胺的作用部位。

Sites of action of tripamide.

作者信息

Brater D C, Anderson S

出版信息

Clin Pharmacol Ther. 1983 Jul;34(1):79-85. doi: 10.1038/clpt.1983.133.

Abstract

Tripamide is a new diuretic derived from a sulfonamide nucleus that has both antihypertensive and natriuretic properties. We assessed its renal site of effect with standard clearance techniques. Studies during water loading indicated a 47% increase in fractional free water clearance (an effect opposite that of thiazide diuretics) and a simultaneous 75% increase in fractional delivery of solute to the diluting segment. Consequently, when free water clearance was assessed relative to delivery of solute, tripamide induced a decrease from 0.86 +/- 0.03 to 0.75 +/- 0.01. This indicated an inhibitory effect on solute reabsorption at the cortical segment of the thick ascending limb of Henle's loop. Studies during hydropenia indicated increased free water reabsorption. When factored for delivery of solute, however, free water reabsorption decreased from 0.66 +/- 0.02 to 0.61 +/- 0.02, indicating a site of effect of tripamide at the medullary segment of the thick ascending limb of Henle's loop. Tripamide also increased calcium excretion. No effects on renal hemodynamics or indices of effect at the proximal tubule were observed. The data indicate that tripamide is a loop diuretic that may also affect more proximal nephron sites.

摘要

曲帕胺是一种源自磺胺核的新型利尿剂,具有抗高血压和利钠特性。我们用标准清除技术评估了其肾脏作用部位。水负荷期间的研究表明,自由水清除率分数增加了47%(与噻嗪类利尿剂的作用相反),同时溶质向稀释段的输送分数增加了75%。因此,当相对于溶质输送评估自由水清除率时,曲帕胺使其从0.86±0.03降至0.75±0.01。这表明对髓袢升支粗段皮质部的溶质重吸收有抑制作用。缺水期间的研究表明自由水重吸收增加。然而,考虑到溶质输送时,自由水重吸收从0.66±0.02降至0.61±0.02,表明曲帕胺在髓袢升支粗段髓质部有作用部位。曲帕胺还增加了钙排泄。未观察到对肾血流动力学或近端小管作用指标的影响。数据表明曲帕胺是一种袢利尿剂,也可能影响更靠近近端的肾单位部位。

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