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一类用于治疗2型糖尿病的新型药物:钠-葡萄糖协同转运蛋白抑制剂:“糖利尿药”

A new class of drug for the management of type 2 diabetes: sodium glucose co-transporter inhibitors: 'glucuretics'.

作者信息

Chan H W Esther, Ashan B, Jayasekera P, Collier Andrew, Ghosh Sujoy

机构信息

Diabetes Day Centre, Ayr Hospital, Dalmellington Road, Ayr KA6 6DX, UK.

出版信息

Diabetes Metab Syndr. 2012 Oct-Dec;6(4):224-8. doi: 10.1016/j.dsx.2012.08.003. Epub 2012 Oct 16.

Abstract

BACKGROUND

Type 2 diabetes is a common, chronic disease with a prevalence that is increasing at epidemic proportions. Management involves advice on lifestyle changes, oral anti-hyperglycaemic agents and/or insulin. The kidneys play a major role in the regulation of glucose, re-absorbing 99% of the plasma glucose filtered through the renal glomeruli tubules. The glucose transporter, SGLT2, which is found primarily in the S1 segment of the proximal renal tubule accounts for 90% of glucose re-absorption. Competitive inhibition of SGLT2 induces glucosuria in a dose dependent manner and appears to have beneficial effects on glucose regulation in individuals with type 2 diabetes. O-glucoside phlorozin is the model substance for SGLT2 inhibitors: various O-, C-, N- and S-glucosides with varying affinity and specificity have been synthesised.

AIMS

The aim of this review is to describe the background, the mechanism of action and the possible role for sodium glucose co-transporter inhibitors in the treatment of diabetes.

MATERIALS AND METHODS

Databases, including MEDLINE, COCHRANE, EMBASE and EBM reviews were searched for literature relating to sodium glucose transport inhibitors and improvements in glycaemic control in patients with diabetes.

RESULTS

The data suggest that sodium glucose transport inhibitors significantly improve glycaemic control by increasing glucosuria. Some studies described significant reductions in weight and improvement in blood pressure. The most common side effect was infection involving the urinary and genital tracts.

CONCLUSIONS

Sodium glucose co-transport inhibitors appear to be an effective line of treatment, well tolerated and could be a further drug class in the armamentarium available for the management of type 2 diabetes.

摘要

背景

2型糖尿病是一种常见的慢性疾病,其患病率正以流行趋势上升。治疗包括生活方式改变的建议、口服降糖药和/或胰岛素。肾脏在葡萄糖调节中起主要作用,可重吸收经肾小球肾小管滤过的血浆葡萄糖的99%。葡萄糖转运蛋白SGLT2主要存在于近端肾小管的S1段,占葡萄糖重吸收的90%。对SGLT2的竞争性抑制以剂量依赖方式诱导糖尿,并且似乎对2型糖尿病患者的血糖调节具有有益作用。邻葡萄糖基根皮苷是SGLT2抑制剂的模型物质:已合成了具有不同亲和力和特异性的各种O-、C-、N-和S-糖苷。

目的

本综述的目的是描述钠-葡萄糖协同转运蛋白抑制剂在糖尿病治疗中的背景、作用机制和可能的作用。

材料与方法

检索包括MEDLINE、COCHRANE、EMBASE和循证医学综述在内的数据库,以查找与钠-葡萄糖转运抑制剂及糖尿病患者血糖控制改善相关的文献。

结果

数据表明,钠-葡萄糖转运抑制剂通过增加糖尿显著改善血糖控制。一些研究描述了体重显著降低和血压改善。最常见的副作用是泌尿生殖道感染。

结论

钠-葡萄糖协同转运抑制剂似乎是一种有效的治疗方法,耐受性良好,可能成为可用于治疗2型糖尿病的又一类药物。

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