Verbrugge Frederik H, Vangoitsenhoven Roman, Mullens Wilfried, Van der Schueren Bart, Mathieu Chantal, Tang W H Wilson
Department of Cardiovascular Medicine, Heart and Vascular Institute, Cleveland Clinic, 9500 Euclid Avenue, Desk J3-4, Cleveland, OH 44195, USA.
Department of Cardiology, Ziekenhuis Oost-Limburg, Genk, Belgium.
Curr Cardiovasc Risk Rep. 2015 Aug;9(8). doi: 10.1007/s12170-015-0467-0. Epub 2015 Jun 17.
Sodium-glucose transporter-2 (SGLT-2) inhibitors have emerged as novel oral glucose-lowering agents for type 2 diabetes. SGLT-2 inhibitors improve glycemic control by blocking sodium-glucose cotransport in the renal proximal tubules, thereby promoting glycosuria. In this review, it is discussed mechanistically how SGLT-2 inhibitors might be particularly relevant to use in patients with or at high risk for heart failure. On a daily base, SGLT-2 inhibitors block ~330-495 mEq sodium reabsorbed in the proximal tubules, although substantial amounts can be reabsorbed more distally in the nephron. Increased sodium offering to the distal nephron is sensed at the macula densa and may attenuate neurohumoral activation, thereby improving salt sensitivity, augmenting diuretic efficacy of loop and thiazide diuretics, and potentiating the native natriuretic peptide system. Whether the favorable profile offered by SGLT-2 inhibitors is renoprotective and whether SGLT-2 inhibition can relieve and/or prevent congestion beyond traditional diuretic drugs warrants further investigation.
钠-葡萄糖协同转运蛋白2(SGLT-2)抑制剂已成为用于2型糖尿病的新型口服降糖药。SGLT-2抑制剂通过阻断近端肾小管中的钠-葡萄糖协同转运来改善血糖控制,从而促进糖尿。在本综述中,将从机制上讨论SGLT-2抑制剂在心力衰竭患者或高危患者中使用可能具有的特殊意义。每天,SGLT-2抑制剂会阻断近端肾小管中约330-495 mEq的钠重吸收,尽管大量钠可在肾单位更远端被重吸收。致密斑可感知到向远端肾单位提供的钠增加,这可能会减弱神经体液激活,从而改善盐敏感性,增强襻利尿剂和噻嗪类利尿剂的利尿效果,并增强内源性利钠肽系统。SGLT-2抑制剂所具有的有利特性是否具有肾脏保护作用,以及SGLT-2抑制是否能在传统利尿药物之外缓解和/或预防充血,这值得进一步研究。