PRESENTATION: Dapagliflozin 5 mg /10 mg, Metformin 500mg

DRUG CLASS: SGLT2 Inhibitor and Bigaunides

MECHANISM OF ACTION: By inhibiting sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubules, dapagliflozin reduces reabsorption of filtered glucose from the tubular lumen and lowers the renal threshold for glucose (RT ).

SGLT2 is the main site of filtered glucose reabsorption; reduction of filtered glucose reabsorption and lowering of RT result in increased urinary excretion of glucose, thereby reducing plasma glucose concentrations.

Dapagliflozin also reduces sodium reabsorption and increases sodium delivery to the distal tubule, which may decrease cardiac preload/afterload, downregulate sympathetic activity, and decrease intraglomerular pressure.

Hyperglycemia: Oral: Initial: 5 mg once daily; may increase to 10 mg once daily after 4 to 12 weeks if needed to achieve glycemic goals (ref1) or in combination with Metformin 500mg

Heart failure: In patients with type 2 diabetes mellitus and established ASCVD, multiple risk factors for ASCVD, or heart failure with reduced ejection fraction, dapagliflozin has been shown to reduce the risk of heart failure hospitalization (Ref2). In patients with type 2 diabetes mellitus and heart failure with reduced ejection fraction, dapagliflozin has also been shown to reduce the risk of cardiovascular death (Ref 3).

Oral: 10 mg once daily (Ref2).

Altered kidney function:

eGFR ≥45 mL/minute/1.73 m²: No dosage adjustment necessary.

eGFR 25 to <45 mL/minute/1.73 m²:

Chronic kidney disease: No dosage adjustment necessary.