Dapagliflozin is a potent, selective, and reversible inhibitor of sodium-glucose co-transporter 2 (SGLT2). It is an oral anti-diabetic agent (gliflozin class) used primarily for the management of type 2 diabetes mellitus (T2DM). By inhibiting SGLT2 in the proximal renal tubules, it reduces renal glucose reabsorption, leading to increased urinary glucose excretion (glucosuria) and a consequent reduction in plasma glucose levels. It is also indicated for heart failure and chronic kidney disease, irrespective of diabetes status.
Adult: Recommended starting dose is 10mg once daily, taken orally in the morning, with or without food. For T2DM, can be initiated at 5mg and increased to 10mg based on efficacy and tolerability. For HF and CKD, the recommended dose is 10mg once daily.
Note: Tablet should be swallowed whole with a glass of water. Can be taken with or without food, but taking it in the morning is preferred to minimize the risk of nocturia. Patients should maintain adequate fluid intake to prevent volume depletion.
Dapagliflozin selectively and competitively inhibits SGLT2, the primary transporter responsible for reabsorbing approximately 90% of filtered glucose from the proximal renal tubule back into the circulation. Inhibition of SGLT2 reduces the renal threshold for glucose (RTG), leading to increased excretion of glucose in the urine (glucosuria). This results in a reduction of plasma glucose concentrations and HbA1c. The caloric loss (approximately 200-300 kcal/day) and osmotic diuresis contribute to weight loss and modest reductions in systolic blood pressure.
Pregnancy: Not recommended during the second and third trimesters. Animal studies have shown renal pelvic and tubule dilatation in offspring. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Insulin is the preferred drug for glycemic control in pregnancy.
Driving: Dapagliflozin may cause dizziness and postural hypotension, especially during initiation. Patients should be cautioned about operating machinery or driving until they are sure they are not affected.
| Insulin or Insulin Secretagogues (Sulfonylureas, Meglitinides) | Increased risk of hypoglycemia. Dose reduction of insulin/secretagogue may be required. | Major |
| Loop Diuretics (e.g., Furosemide) | Potentiation of diuresis and increased risk of volume depletion and hypotension. | Moderate |
| Other SGLT2 Inhibitors | Concomitant use not recommended due to additive effects and increased risk of adverse reactions. | Major |
| Rifampicin | Decreases systemic exposure of dapagliflozin. May require monitoring of glycemic control. | Moderate |
| Lithium | SGLT2 inhibitors may decrease lithium concentrations. Monitor lithium levels closely. | Moderate |
Same composition (Dapagliflozin (10mg)), different brands: