Wittner M, Di Stefano A, Wangemann P, Greger R
Institut de Recherche Fondamentale, Centre d'Etudes Nucléaires de Saclay, Gif-sur-Yvette, France.
Drugs. 1991;41 Suppl 3:1-13. doi: 10.2165/00003495-199100413-00003.
In the thick ascending limb of the loop of Henle, NaCl reabsorption is mediated by a Na+/2Cl-/K+ cotransport system, present in the luminal membrane of this nephron segment. Loop diuretics such as furosemide (frusemide), piretanide, bumetanide and torasemide bind reversibly to this carrier protein, thus reducing or abolishing NaCl reabsorption. This leads to a decrease in interstitial hypertonicity and thus to a reduced water reabsorption. In nephron segments other than the thick ascending limb, loop diuretics have no quantitative importance with respect to their saluretic and diuretic activities. Loop diuretics also reduce Ca++ and Mg++ reabsorption in the thick ascending limb in a way which is still not clear. Furthermore, these drugs increase the urinary K+ excretion by enhancing distal tubular K+ secretion and reducing K+ reabsorption in the loop of Henle. Finally, by reduction of active NaCl transport, loop diuretics drastically reduce the substrate requirement and oxygen dependence of the thick ascending limb cells. This renders these cells, which are characterised by high transport rates and only limited substrate reserves, less vulnerable in acute renal failure.
在髓袢升支粗段,氯化钠的重吸收由存在于该肾单位节段管腔膜中的Na⁺/2Cl⁻/K⁺共转运系统介导。袢利尿剂如呋塞米、吡咯他尼、布美他尼和托拉塞米可与该载体蛋白可逆性结合,从而减少或消除氯化钠的重吸收。这导致间质高渗性降低,进而使水的重吸收减少。在髓袢升支粗段以外的肾单位节段,袢利尿剂就其利钠和利尿活性而言没有定量重要性。袢利尿剂还以一种尚不清楚的方式减少髓袢升支粗段的Ca²⁺和Mg²⁺重吸收。此外,这些药物通过增强远曲小管钾分泌和减少髓袢钾重吸收来增加尿钾排泄。最后,通过减少主动的氯化钠转运,袢利尿剂极大地降低了髓袢升支粗段细胞对底物的需求和对氧的依赖性。这使得这些以高转运率和有限底物储备为特征的细胞在急性肾衰竭中更不易受损。