Kalra Sanjay, Singh Vikram, Nagrale Dinesh
Department of Endocrinology, Bharti Hospital, Karnal, India.
Medical Affairs, Janssen (Pharmaceutical Division of Johnson & Johnson), Mumbai, India.
Adv Ther. 2016 Sep;33(9):1502-18. doi: 10.1007/s12325-016-0379-5. Epub 2016 Jul 16.
Blood glucose-lowering treatment options generally target insulin action or beta-cell function. In diabetes, expression of the sodium-glucose cotransporter-2 (SGLT2) genes is up-regulated and renal threshold increased, resulting in increased glucose reabsorption from glomerular filtrate, reducing urinary glucose excretion and worsening the hyperglycemic condition. The SGLT2 inhibitors (SGLT2i) are a novel class of anti-diabetic drugs that lower blood glucose levels through the suppression of renal glucose reabsorption thereby promoting renal glucose excretion. The efficacy of SGLT2i is reduced in renal impairment because the ability of glucose-lowering is directly proportional to glomerular filtration rate. On the other hand, ongoing research suggests that SGLT2i may offer potential nephroprotection in diabetes. The SGLT2i have been shown to reduce glomerular hyperfiltration, systemic and intraglomerular pressure and the biochemical progression of chronic kidney disease. Additional mechanisms through which SGLT2i exert nephroprotection may include normalizing blood pressure and uricemia. This review explores this bidirectional relationship of the SGLT2i and the glomerulus. While SGLT2i exhibit reduced efficacy in later stages, they exhibit nephroprotective effects in early stages of renal impairment.
Janssen India (Pharmaceutical division of Johnson & Johnson).
降血糖治疗方案通常针对胰岛素作用或β细胞功能。在糖尿病中,钠-葡萄糖协同转运蛋白2(SGLT2)基因的表达上调且肾阈值升高,导致从肾小球滤液中重吸收的葡萄糖增加,减少尿糖排泄并使高血糖状况恶化。SGLT2抑制剂(SGLT2i)是一类新型抗糖尿病药物,通过抑制肾葡萄糖重吸收从而促进肾葡萄糖排泄来降低血糖水平。在肾功能损害时,SGLT2i的疗效会降低,因为其降血糖能力与肾小球滤过率直接相关。另一方面,正在进行的研究表明,SGLT2i可能对糖尿病具有潜在的肾脏保护作用。已证明SGLT2i可减少肾小球高滤过、全身和肾小球内压力以及慢性肾脏病的生化进展。SGLT2i发挥肾脏保护作用的其他机制可能包括使血压和血尿酸正常化。本综述探讨了SGLT2i与肾小球之间的这种双向关系。虽然SGLT2i在后期阶段疗效降低,但它们在肾功能损害的早期阶段具有肾脏保护作用。
杨森印度公司(强生制药部门)