SGLT2 is a transporter responsible the reabsorption of glucose that is localized in the kidney. SGLT2 is responsible for 90 % of glucose reabsorption in the proximal tubule. Canagliflozin, Dapagliflozin, and Empagliflozin inhibits the reabsorption of glucose by the kidney and excretes glucose in the urine. This improves glycemic control.
Pharmacodynamics
Each of the three drugs has similar effects in improving glycemic control when used in conjunction with another first line therapy such as metformin or sulfonylurea. These drugs are also effective as monotherapy. Results from phase three clinical trials showed a drop in the mean Hb A1C levels by 1.03% for Canagliflozin. The data also showed weight loss in patients along with a decrease in fasting plasma glucose and blood pressure. Dapagliflozin and Empagliflozin also showed similar results in their efficacy testing. Renal protection was seen in patients that initiated early therapy with SGLT2 inhibitors. …show more content…
The plasma peak time of these drugs ranges between 1-2 hours with Empagliflozin peak level at 1.5 hours. Studies have shown a slight reduction in circulation of Empagliflozin after the consumption of a high-fat meal. Dapagliflozin has the highest bioavailability in this class of drugs at 78 percent and the bioavailability of Canagliflozin is 65 percent. The excretion of the drug is through the urine and feces by way of the O-glucuronidation pathway. The half-life for Canagliflozin is dose dependent and ranges between 10-13 hours. The half-life of Dapagliflozin is 12.9 hours and the half-life of Empagliflozin is between 10-19 hours. In patients with mild to moderate hepatic disease, no dose adjustment is necessary for this class of drugs. However, in severe disease, Empagliflozin has shown a retention of the drug in the