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钠-葡萄糖协同转运蛋白2抑制剂对心血管和血压有显著影响:一类新型抗糖尿病药物。

Promising cardiovascular and blood pressure effects of the SGLT2 inhibitors: a new class of antidiabetic drugs.

作者信息

Chrysant S G

机构信息

University of Oklahoma College of Medicine, Oklahoma City, Oklahoma, USA.

出版信息

Drugs Today (Barc). 2017 Mar;53(3):191-202. doi: 10.1358/dot.2017.53.3.2555985.

Abstract

Patients with type 2 diabetes mellitus (T2DM) exhibit an increased risk of cardiovascular (CV) events. Treatment of these patients with traditional as well as newer glucose-lowering drugs has not demonstrated superiority in CV outcomes compared to placebo, despite effective control of diabetes. However, the recently FDA-approved sodium-glucose cotransporter 2 (SGLT2) inhibitors for the treatment of T2DM have demonstrated promising CV-protecting and blood pressure-lowering effects in addition to their effectiveness in glucose lowering, making them a novel class of drugs for the treatment of T2DM. So far, there are three SGLT2 inhibitors approved by the FDA and EMA for the treatment of T2DM: canagliflozin, dapagliflozin and empagliflozin. They exert their antihyperglycemic effect through inhibition of SGLT2 in the kidney and significantly reduce glucose reabsorption from the proximal renal tubule. By blocking glucose reabsorption, they lead to loss of calories, weight, abdominal and total body fat, blood pressure and CV complications. One CV outcomes randomized trial and several short-term studies have shown reductions in CV events and blood pressure in patients with T2DM. It is the hope that large ongoing long-term outcome studies will provide further much-needed information, when they are completed.

摘要

2型糖尿病(T2DM)患者发生心血管(CV)事件的风险增加。尽管这些患者的糖尿病得到了有效控制,但使用传统降糖药物以及新型降糖药物进行治疗,在CV结局方面并未显示出优于安慰剂的效果。然而,最近美国食品药品监督管理局(FDA)批准用于治疗T2DM的钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂,除了具有降糖效果外,还显示出了有前景的CV保护和降压作用,使其成为一类治疗T2DM的新型药物。到目前为止,有三种SGLT2抑制剂已获FDA和欧洲药品管理局(EMA)批准用于治疗T2DM:卡格列净、达格列净和恩格列净。它们通过抑制肾脏中的SGLT2发挥降糖作用,并显著减少近端肾小管对葡萄糖的重吸收。通过阻断葡萄糖重吸收,它们导致热量、体重、腹部和全身脂肪、血压及CV并发症的减少。一项CV结局随机试验和几项短期研究表明,T2DM患者的CV事件和血压有所降低。人们希望正在进行的大型长期结局研究完成后,将提供更多急需的信息。

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