Omosu M, Fujimoto K, Sakaguchi T, Yamamoto K, Iwao H, Abe Y
Arzneimittelforschung. 1983;33(9):1277-80.
Effects of 4-phenoxy-3-(1-pyrrolidinyl)-5-sulfamoyl benzoic acid (piretanide, Arelix) on renal function and hemodynamics were investigated in anesthetized dogs by clearance, stop-flow and radioactive microsphere methods. Marked diuresis occurred within 10 min after intravenous injection of piretanide (0.01, 0.05 and 0.25 mg/kg) and it was accompanied b natriuresis. Piretanide (0.25 mg/kg) clearly inhibited the reabsorption of solute-free water during saline diuresis, suggesting that the drug acts in the ascending limb of Henle's loop. Stop-flow experiments revealed that sodium reabsorption was reduced by piretanide (0.25 mg/kg) at the distal tubule including the ascending limb of Henle's loop. Piretanide (0.25 mg/kg) caused a maximum increase of about 30% in renal blood flow at 10-15 min after the injection; within the renal cortex the increase in blood flow was greater in the juxtamedullary area than in the superficial area. The increased blood flow in the inner cortex conceivably resulted in a washout of the osmotic substances in the medulla and inhibited the concentrating mechanisms of the kidney. The effect of piretanide on intrarenal hemodynamics may also contribute to its diuretic action.
采用清除率、停流及放射性微球法,在麻醉犬身上研究了4-苯氧基-3-(1-吡咯烷基)-5-氨磺酰苯甲酸(吡咯他尼,阿瑞利克斯)对肾功能和血流动力学的影响。静脉注射吡咯他尼(0.01、0.05和0.25mg/kg)后10分钟内出现明显利尿,并伴有排钠。吡咯他尼(0.25mg/kg)在盐水利尿期间明显抑制无溶质水的重吸收,提示该药作用于亨利袢升支。停流实验显示,吡咯他尼(0.25mg/kg)可降低包括亨利袢升支在内的远曲小管的钠重吸收。注射后10 - 15分钟,吡咯他尼(0.25mg/kg)使肾血流量最大增加约30%;在肾皮质内,近髓区的血流增加比浅表区更大。肾内皮质血流增加可能导致髓质中渗透物质的清除,并抑制肾脏的浓缩机制。吡咯他尼对肾内血流动力学的影响也可能有助于其利尿作用。