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钠-葡萄糖协同转运蛋白2抑制剂的肾脏效应及文献综述

The renal effects of SGLT2 inhibitors and a mini-review of the literature.

作者信息

Andrianesis Vasileios, Glykofridi Spyridoula, Doupis John

机构信息

Athens Naval Hospital, Athens, Greece.

Metaxa General Hospital, Athens, Greece.

出版信息

Ther Adv Endocrinol Metab. 2016 Dec;7(5-6):212-228. doi: 10.1177/2042018816676239. Epub 2016 Nov 11.

Abstract

Sodium-glucose linked transporter 2 (SGLT2) inhibitors are a new and promising class of antidiabetic agents which target renal tubular glucose reabsorption. Their action is based on the blockage of SGLT2 sodium-glucose cotransporters that are located at the luminal membrane of tubular cells of the proximal convoluted tubule, inducing glucosuria. It has been proven that they significantly reduce glycated hemoglobin (HbA1c), along with fasting and postprandial plasma glucose in patients with type 2 diabetes mellitus (T2DM). The glucosuria-induced caloric loss as well as the osmotic diuresis significantly decrease body weight and blood pressure, respectively. Given that SGLT2 inhibitors do not interfere with insulin action and secretion, their efficacy is sustained despite the progressive β-cell failure in T2DM. They are well tolerated, with a low risk of hypoglycemia. Their most frequent adverse events are minor: genital and urinal tract infections. Recently, it was demonstrated that empagliflozin presents a significant cardioprotective effect. Although the SGLT2 inhibitors' efficacy is affected by renal function, new data have been presented that some SGLT2 inhibitors, even in mild and moderate renal impairment, induce significant HbA1c reduction. Moreover, recent data indicate that SGLT2 inhibition has a beneficial renoprotective effect. The role of this review paper is to explore the current evidence on the renal effects of SGLT2 inhibitors.

摘要

钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂是一类新型且有前景的抗糖尿病药物,其作用靶点为肾小管葡萄糖重吸收。它们的作用基于对位于近端曲管肾小管细胞腔膜上的SGLT2钠-葡萄糖协同转运蛋白的阻断,从而诱导糖尿。已证实,它们能显著降低2型糖尿病(T2DM)患者的糖化血红蛋白(HbA1c)以及空腹和餐后血糖。糖尿引起的热量损失以及渗透性利尿分别显著降低体重和血压。鉴于SGLT2抑制剂不干扰胰岛素作用和分泌,尽管T2DM患者存在进行性β细胞功能衰竭,但其疗效仍能持续。它们耐受性良好,低血糖风险低。其最常见的不良事件较为轻微:生殖器和泌尿道感染。最近,已证明恩格列净具有显著的心脏保护作用。尽管SGLT2抑制剂的疗效受肾功能影响,但已有新数据表明,一些SGLT2抑制剂即使在轻度和中度肾功能损害的情况下,也能显著降低HbA1c。此外,最近的数据表明SGLT2抑制具有有益的肾脏保护作用。本综述文章的作用是探讨关于SGLT2抑制剂肾脏效应的现有证据。

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The renal effects of SGLT2 inhibitors and a mini-review of the literature.钠-葡萄糖协同转运蛋白2抑制剂的肾脏效应及文献综述
Ther Adv Endocrinol Metab. 2016 Dec;7(5-6):212-228. doi: 10.1177/2042018816676239. Epub 2016 Nov 11.

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