T2D Medicine SGLT2 inhibitors

Submitted by Thiruvelan on Sat, 07/27/2013
T2D Medicine SGLT2 inhibitors

SGLT2 inhibitors are a class of diabetes medication prevents the body to reabsorb glucose, increasing glucose excretions in urine to lower blood-glucose level.

SGLT2 inhibitors

SGLT2 inhibitors are sodium-glucose co-transporter 2 (SGLT2) inhibitors; it blocks the reabsorption of glucose into the body by the kidney and increasing glucose excretions in the urine. It is not recommendable for type 1 diabetes or diabetic ketoacidosis.

SGLT2 inhibitors mechanism of action

SGLT2 is a protein in humans that facilitates glucose reabsorption in the kidney. SGLT2 is responsible for almost 90% of the glucose reabsorption in the kidney. Inhibiting this transporter leads to a decrease in blood glucose due to the increase in renal glucose excretion.

The mechanism of action of this new class of drugs is by increasing insulin sensitivity, and uptake of glucose in the muscle cells decreased gluconeogenesis and improved first phase insulin release from the beta cells.

Drugs in the SGLT2 inhibitors class

  • Generic name: Canagliflozin (Brand name: Invokana),
  • Generic name: Dapagliflozin (Brand name: Farxiga (in the US), Forxiga (in EU)),
  • Generic name: Ipragliflozin (Brand name: Suglat)

SGLT2 inhibitors dosage

  • Canagliflozin – start with a minimum dose of 100 mg once daily for eGFR 45 to < 60 mL/min/1.73 m2, maximum dose of up to 300 mg once daily is allowable for patients with eGFR ≥60 mL/min/1.73 m2.
  • Dapagliflozin - start with a minimum dose of 5 mg orally once a day; take in the morning with or without food. You may increase to 10 mg once a day in patients is tolerating 5 mg/day who have an eGFR ≥60 mL/min/1.73 m² and require additional glycemic control.
  • Ipragliflozin - The recommended dose is 50 mg once daily, in the morning. If the effects are insufficient, the dosage may increase to up to 100 mg once a day, while carefully monitoring disease progress.

SGLT2 can increase the risk of hypoglycemia combined with insulin or an insulin secretagogue.

What can you expect from SGLT2 inhibitors?

SGLT2 inhibitors as monotherapy can reduce HbA1c levels. You can use SGLT2 inhibitors as a monotherapy or in combination with most other oral diabetes drugs and insulin.

Possible side effects of SGLT2 inhibitors

SGLT2 inhibitors can

increase LDL cholesterol,

urinary tract infections,

genital mycotic infections,

associated with increased urination and

episodes of hypotension and hypoglycemia).

The same report did show that the drug decreased weight by a 1.9 to 3% as well as reduced systolic and diastolic blood pressures and raised HDL cholesterol. Some common side effects are rapid weight loss, tiredness, and dehydration.

Who should avoid using SGLT2 inhibitors?

Avoid SGLT2 inhibitors, if you are

  • Type 1 diabetes
  • People with low kidney function
  • People taking strong diuretic medication