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Diabetes Mellitus/Anti-DM Pharmacological Management
Published in Mihai V. Putz, New Frontiers in Nanochemistry, 2020
Bogdan Bumbăcilă, Corina Duda-Seiman, Daniel Duda-Seiman, Mihai V. Putz
Glucosuria, the presence of glucose in the urine, has long been regarded as a consequence of uncontrolled diabetes. However, glucose excretion can be induced by blocking the activity of the renal sodium-glucose cotransporter 2 (SGLT-2). This mechanism corrects hyperglycemia independently of insulin, because SGLT2 is the major cotransporter involved in glucose reabsorption in the kidney. By lowering the renal threshold for glucose excretion, SGLT-2 inhibitors suppress renal glucose reabsorption (30–50% of the glucose filtered by the kidney) and thereby increase urinary glucose excretion. The advantages of this approach are reduced hyperglycemia without hypoglycemia, along with weight loss and blood pressure reduction (Chao, 2014).
Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sodium–glucose co-transporters, or sodium-glucose linked transporter (SGLTs), play an important role in the intake and elimination of glucose. SGLTs are located in the intestinal mucosa (enterocytes) of the small intestine (SGLT1), and the proximal tubule of the nephron (SGLT2 in proximal convoluted tubule, SGLT1 in proximal straight tubule). SGLT2 is the main responsible for reabsorption of glucose in kidney; thus, inhibition of SGLT2 would lead to a very low or even null glucose reabsorption and an increased glycosuria, highly desirable for patients suffering T2DM (Madaan et al., 2016; Solini, 2016).
Sodium-glucose transporter (SGLT2) inhibition: A potential target for treatment of type-2 Diabetes Mellitus with Natural and Synthetic compounds
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Shubham Batra, Prabhjeet Kaur Bamrah, Manjusha Choudhary
Canagliflozin is the first SGLT2 inhibitor approved by the FDA in 2013 for the treatment of T2DM. There are more than 80 countries that use canagliflozin for the treatment of type 2 diabetes, including Europe, The United States, Japan, and Australia. Compared to SGLT2, it is around 158 times more selective than SGLT1. By increasing urine excretion of glucose and decreasing renal reabsorption of glucose, the inhibition of SGLT2 lowers blood glucose levels without affecting insulin levels. Adults with T2DM who were older or at higher cardiovascular (CV) risk had better glycemic control because of canagliflozin, and their body weight and blood pressure also improved. It can be used as a first-line monotherapy as well given in combination with metformin and it reduces Hb1Ac, body weight, and fasting plasma glucose levels [21].