Each tablet contains 10 mg of empagliflozin.
Empagliflozin is a reversible, highly potent (IC₅₀ = 1.3 nmol/L) and selective competitive inhibitor of sodium-glucose cotransporter 2 (SGLT2). Empagliflozin does not inhibit other glucose transporters that are important for glucose transport into peripheral tissues and is more than 5,000-fold more selective for SGLT2 than for SGLT1, the major transporter responsible for glucose absorption in the intestine.
SGLT2 is highly expressed in the kidneys, whereas its expression in other tissues is absent or very low. As the primary transporter, it is responsible for the reabsorption of glucose from the glomerular filtrate back into the bloodstream. In patients with type 2 diabetes mellitus and hyperglycaemia, larger amounts of glucose are filtered and reabsorbed.
Empagliflozin improves glycaemic control in patients with type 2 diabetes mellitus by reducing renal glucose reabsorption. Through this glucosuric mechanism, the amount of glucose excreted by the kidneys depends on the blood glucose concentration and the glomerular filtration rate (GFR).
The mechanism of action of empagliflozin is independent of beta-cell function and the insulin pathway, which contributes to a low risk of hypoglycaemia. Improvements have been observed in surrogate markers of beta-cell function, including the Homeostatic Model Assessment of β-cell function (HOMA-β).
In addition, urinary glucose excretion results in caloric loss, thereby contributing to reductions in body fat and body weight.
The glucosuria observed with empagliflozin is accompanied by diuresis, which may contribute to a sustained and moderate reduction in blood pressure.
The glucosuria, natriuresis and osmotic diuresis observed with empagliflozin may contribute to improved cardiovascular outcomes.
Indications
Empagliflozin is indicated for the treatment of adults with inadequately controlled type 2 diabetes mellitus as an adjunct to diet and exercise:
- As monotherapy when metformin is considered inappropriate due to intolerance.
- In addition to other medicinal products used for the treatment of diabetes mellitus.
Empagliflozin is also indicated for the treatment of symptomatic chronic heart failure in adults.