Mascolo Annamaria, Di Napoli Raffaella, Balzano Nunzia, Cappetta Donato, Urbanek Konrad, De Angelis Antonella, Scisciola Lucia, Di Meo Irene, Sullo Maria Giuseppa, Rafaniello Concetta, Sportiello Liberata
Campania Regional Centre for Pharmacovigilance and Pharmacoepidemiology, Naples, Italy.
Department of Experimental Medicine - Section of Pharmacology "L. Donatelli", University of Campania "Luigi Vanvitelli", Naples, Italy.
Front Cardiovasc Med. 2022 Sep 21;9:1010693. doi: 10.3389/fcvm.2022.1010693. eCollection 2022.
A new therapeutic class of oral agents firstly used for the treatment of type 2 diabetes mellitus is represented by gliflozines or sodium-glucose co-transporter 2 (SGLT2) inhibitors. SGLT2 inhibitors might be effective alone or in combination with any other drugs. This therapeutic class currently includes five agents: canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, and sotagliflozin. SGLT2 inhibitors prevent the renal reabsorption of filtered glucose and sodium by blocking the SGLT2 co-transporters in the proximal convoluted renal tubule, facilitating glucose excretion in the urine (glycosuria) and lowering blood glucose levels. SGLT2 inhibitors have also shown to have pleiotropic effects and determine cardiovascular and renal prevention, thus leading to an extension of their therapeutic indication to include the heart failure. Despite their clinical benefits, warnings about adverse events have been implemented by Regulatory Agencies in the product's information since their introduction to the market. In particular, SGLT2 inhibitors have shown a strong impact on a high number of risk factors. They can cause hypoglycaemia, hypotension, lower limb amputation, fractures, genito-urinary infections, and diabetic ketoacidosis with different frequencies of onset. Despite some of these events are rare, they can lead to serious and dangerous complications, highlighting the importance of a strict monitoring of patients. Overall, SLGT-2 inhibitors are effective antidiabetic drugs with favorable advantages in renal and cardiovascular protection, and with a generally well-tolerated safety profile. This review aims to summarize the safety profile of SGLT2 inhibitors available in the market.
一类新型的口服药物首次用于治疗2型糖尿病,以格列净类药物或钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂为代表。SGLT2抑制剂单独使用或与其他任何药物联合使用可能都有效。这类治疗药物目前包括五种药物:卡格列净、达格列净、恩格列净、依鲁格列净和索格列净。SGLT2抑制剂通过阻断近端曲管中的SGLT2协同转运蛋白来阻止滤过葡萄糖和钠的肾脏重吸收,促进葡萄糖经尿液排泄(糖尿)并降低血糖水平。SGLT2抑制剂还显示出具有多效性作用,并能预防心血管和肾脏疾病,因此其治疗适应症扩展到包括心力衰竭。尽管它们具有临床益处,但自上市以来,监管机构已在产品信息中对不良事件发出警告。特别是,SGLT2抑制剂对大量风险因素有强烈影响。它们可导致低血糖、低血压、下肢截肢、骨折、泌尿生殖系统感染以及糖尿病酮症酸中毒,且发病频率各不相同。尽管其中一些事件很少见,但它们可导致严重且危险的并发症,凸显了对患者进行严格监测的重要性。总体而言,SGLT-2抑制剂是有效的抗糖尿病药物,在肾脏和心血管保护方面具有有利优势,且安全性总体上耐受性良好。本综述旨在总结市场上现有SGLT2抑制剂的安全性概况。