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钠-葡萄糖协同转运蛋白2抑制剂

SGLT2 inhibitors.

作者信息

Dardi I, Kouvatsos T, Jabbour S A

机构信息

Division of Endocrinology, Diabetes & Metabolic Diseases, Sidney Kimmel Medical College at Thomas Jefferson University, 211 South Ninth Street, Ste 600, Philadelphia, PA 19107, USA.

出版信息

Biochem Pharmacol. 2016 Feb 1;101:27-39. doi: 10.1016/j.bcp.2015.09.005. Epub 2015 Sep 8.

Abstract

Diabetes mellitus is a serious health issue and an economic burden, rising in epidemic proportions over the last few decades worldwide. Although several treatment options are available, only half of the global diabetic population achieves the recommended or individualized glycemic targets. Sodium-glucose cotransporter 2 (SGLT2) inhibitors are a new class of antidiabetic agents with a novel insulin-independent action. SGLT2 is a transporter found in the proximal renal tubules, responsible for the reabsorption of most of the glucose filtered by the kidney. Inhibition of SGLT2 lowers the blood glucose level by promoting the urinary excretion of excess glucose. Due to their insulin-independent action, SGLT2 inhibitors can be used with any degree of beta-cell dysfunction or insulin resistance, related to a very low risk of hypoglycemia. In addition to improving glycemic control, SGLT2 inhibitors have been associated with a reduction in weight and blood pressure when used as monotherapy or in combination with other antidiabetic agents in patients with type 2 diabetes mellitus (T2DM). Treatment with SGLT2 inhibitors is usually well tolerated; however, they have been associated with an increased incidence of urinary tract and genital infections, although these infections are usually mild and easy to treat. SGLT2 inhibitors are a promising new option in the armamentarium of drugs for patients with T2DM.

摘要

糖尿病是一个严重的健康问题和经济负担,在过去几十年里在全球呈流行趋势上升。尽管有几种治疗选择,但全球只有一半的糖尿病患者达到推荐的或个体化的血糖目标。钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂是一类新型抗糖尿病药物,具有全新的非胰岛素依赖作用机制。SGLT2是一种存在于近端肾小管的转运蛋白,负责重吸收肾脏滤过的大部分葡萄糖。抑制SGLT2可通过促进尿中过量葡萄糖排泄来降低血糖水平。由于其非胰岛素依赖作用机制,SGLT2抑制剂可用于任何程度的β细胞功能障碍或胰岛素抵抗患者,且低血糖风险极低。除了改善血糖控制外,在2型糖尿病(T2DM)患者中,SGLT2抑制剂单药治疗或与其他抗糖尿病药物联合使用时,还与体重减轻和血压降低有关。SGLT2抑制剂治疗通常耐受性良好;然而,它们与泌尿道和生殖器感染的发生率增加有关,尽管这些感染通常较轻且易于治疗。对于T2DM患者,SGLT2抑制剂是药物治疗手段中一个很有前景的新选择。

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