Overview
Vildagliptin is an oral antidiabetic medication used in the management of type 2 diabetes mellitus. It belongs to the dipeptidyl peptidase-4 (DPP-4) inhibitor class, which works by increasing the levels of incretin hormones (GLP-1 and GIP) to enhance glucose-dependent insulin secretion and reduce glucagon secretion. It is typically prescribed as an adjunct to diet and exercise, either as monotherapy or in combination with other antidiabetic agents like metformin, sulfonylureas, or thiazolidinediones.
Mechanism of Action
Vildagliptin is a selective, reversible inhibitor of dipeptidyl peptidase-4 (DPP-4). DPP-4 is an enzyme that rapidly degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, vildagliptin increases the concentration of active incretin hormones, which in turn stimulates glucose-dependent insulin secretion from pancreatic beta cells and suppresses glucagon secretion from pancreatic alpha cells. This results in improved glycemic control without causing hypoglycemia when used alone.
Indications
- Type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control.
- May be used as monotherapy or in combination with other oral antidiabetic agents (e.g., metformin, sulfonylureas, thiazolidinediones) when single therapy is insufficient.
Dosage
The recommended dose is 50 mg twice daily, taken orally with or without food. When used in combination with a sulfonylurea, a lower dose of the sulfonylurea may be considered to reduce the risk of hypoglycemia. Dosage adjustments may be required in patients with renal impairment (e.g., moderate to severe renal impairment may require dose reduction to 50 mg once daily).
Contraindications
- Hypersensitivity to vildagliptin or any component of the formulation.
- Type 1 diabetes mellitus or diabetic ketoacidosis.
- Severe renal impairment (eGFR <30 mL/min/1.73 m²) unless closely monitored.
- History of pancreatitis.
Side Effects
- Common: Headache, dizziness, nasopharyngitis, upper respiratory tract infection, arthralgia.
- Less common: Hypoglycemia (when combined with other agents), nausea, diarrhea, peripheral edema.
- Rare: Pancreatitis, hepatic dysfunction, severe skin reactions (e.g., Stevens-Johnson syndrome), angioedema.
Interactions
- Sulfonylureas or insulin: Increased risk of hypoglycemia; may require dose reduction of these agents.
- Strong CYP450 inducers (e.g., rifampin): May decrease vildagliptin plasma concentrations; monitor glycemic control.
- No clinically significant interactions with metformin, digoxin, warfarin, or simvastatin have been observed in studies.