Sitagliptin is a potent, selective, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor used for the management of type 2 diabetes mellitus. It enhances the body's own ability to control blood sugar levels by increasing the concentration of active incretin hormones (GLP-1 and GIP), which stimulate insulin release in a glucose-dependent manner and reduce glucagon secretion. It is not indicated for type 1 diabetes or diabetic ketoacidosis.
Adult: The recommended dose is 100 mg once daily.
Note: Can be taken with or without food. Tablet should be swallowed whole with a glass of water. It is typically taken at the same time each day to maintain consistent blood levels.
Sitagliptin is a competitive, reversible inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 rapidly inactivates the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, sitagliptin increases the plasma concentrations of active incretins. This leads to increased insulin synthesis and release from pancreatic beta cells in a glucose-dependent manner and suppresses glucagon secretion from pancreatic alpha cells. The net effect is a reduction in fasting and postprandial glucose levels without causing hypoglycemia.
Pregnancy: Category B. Animal studies have shown no risk, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. Insulin is the preferred drug for glycemic control in pregnancy.
Driving: Unlikely to affect driving ability. However, patients should be warned about the risk of hypoglycemia, especially when used in combination with other anti-diabetic drugs, which can cause dizziness and impair concentration.
| Digoxin | Sitagliptin may slightly increase digoxin AUC by ~11%. Monitor digoxin levels. | Moderate |
| Sulfonylureas (e.g., Glimepiride, Glipizide) | Increased risk of hypoglycemia. May require reduction in sulfonylurea dose. | Moderate |
| Insulin | Increased risk of hypoglycemia. May require reduction in insulin dose. | Moderate |
| Strong CYP3A4/CYP2C8 Inducers (e.g., Rifampicin) | May decrease sitagliptin plasma concentration. Efficacy should be monitored. | Moderate |
| Loop Diuretics (e.g., Furosemide) | May potentiate risk of dehydration and acute kidney injury. Monitor renal function. | Moderate |
Same composition (Sitagliptin (100mg)), different brands: