摘要
2型糖尿病是一种以胰岛素分泌缺陷、胰岛素抵抗或者两者并存所致的高血糖为特征的慢性代谢性疾病。早期血糖控制不佳可以促进微血管并发症的进展,以及大血管风险的发生。虽然有众多的降糖药物在临床使用,但只有约50%的患者能实现血糖控制,传统药物仍存在某些不足,因此,需要开发具有新机制的治疗药物。钠-葡萄糖共转运蛋白2(SGLT2)是近年来发现的具有全新作用机制的一个糖尿病治疗靶点。SGLT2抑制剂通过抑制肾脏近端小管对葡萄糖的重吸收来增加尿中葡萄糖的排泄而达到控制血糖的目的,其独立于葡萄糖依赖的胰岛素途径,能使低血糖发生风险降低。临床试验数据表明,SGLT2抑制剂单药治疗和与传统降糖药物联合治疗均可以有效地控制血糖,并改善胰岛素抵抗,同时也有降血压和减少体质量作用。尽管后续的研究显示了SGLT2抑制剂具有良好的耐受性,该类药物在临床上报道的意想不到的风险仍需要大量和长期的临床数据证实。
Type 2 diabetes is a chronic metabolic disease characterized by impaired insulin secretion and/or reduced response of target tissues to insulin. Good glycemic control delays the development and slows the progression of micro- and macrovascular complications. Although there are numerous glucose-lowering agents in clinical use, only approximately 50% of type 2 diabetic patients achieve glycemic control, and undesirable side effects often exist in the traditional treatment. There is a need for novel treatment options that can help overcome these difficulties. Sodium glucose cotransporter 2 （SGLT2） inhibitors have recently been developed as a novel potential therapeutic option for the treatment of type 2 diabetes. These drugs could lower the plasma glucose concentration through inhibition of the glucose reuptake in kidney, independent of insulin secretion and insulin action, with a consequent lower risk of hypoglycemia. The data of clinical trials with monotherapy as well as combination therapy show that SGLT2 inhibitors have a blood glucose-lowering effect and also reduce body weight. A follow-up study shows long-term efficacy and durability of these effects. SGLT2 inhibitors have the potential to reverse glucose toxicity and to improve the insulin resistance, blood pressure, and lipid profile. The available data suggest a good tolerability profile. However, clinicians should carefully prescribe these drugs in light of already reported and/or unexpected side-effects. Further studies in larger numbers and longer-term clinical use data are required to apply these agents in standard treatment of type 2 diabetes.
出处
《药物评价研究》
CAS
2014年第5期463-471,共9页
Drug Evaluation Research
关键词
2型糖尿病
SGLT2抑制剂
糖化血红蛋白
重吸收
type 2 diabetes
reabsorption
sodium glucose transporter 2 inhibitors
glycosylated hemoglobin
reabsorption
