Overview
Vildagliptin/Metformin is a fixed-dose combination oral antidiabetic medication containing a dipeptidyl peptidase-4 (DPP-4) inhibitor (vildagliptin) and a biguanide (metformin). It is used for the management of type 2 diabetes mellitus when treatment with both components is appropriate. Vildagliptin enhances incretin activity by inhibiting DPP-4, increasing insulin secretion and decreasing glucagon secretion in a glucose-dependent manner. Metformin decreases hepatic glucose production and intestinal absorption of glucose, while improving insulin sensitivity.
Mechanism of Action
Vildagliptin: Inhibits dipeptidyl peptidase-4 (DPP-4), increasing levels of active incretin hormones (GLP-1 and GIP). This stimulates glucose-dependent insulin release from pancreatic beta cells and reduces glucagon secretion from pancreatic alpha cells. Metformin: Decreases hepatic glucose production (gluconeogenesis), reduces intestinal glucose absorption, and improves peripheral glucose uptake and utilization by increasing insulin sensitivity.
Indications
- Type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control in adults when treatment with both vildagliptin and metformin is appropriate
- Not indicated for type 1 diabetes or diabetic ketoacidosis
Dosage
Individualized based on efficacy and tolerability. Typically initiated with vildagliptin 50 mg/metformin 500 mg or 850 mg twice daily with meals. Maximum recommended daily dose: vildagliptin 100 mg/metformin 2000 mg. Dose adjustments may be needed based on renal function and metformin tolerance.
Contraindications
- Severe renal impairment (eGFR <30 mL/min/1.73 m²)
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis
- Hypersensitivity to vildagliptin, metformin, or any component
- Acute conditions that may alter renal function (dehydration, severe infection, shock)
Side Effects
- Common: Nausea, vomiting, diarrhea, abdominal pain, headache
- Less common: Hypoglycemia (when combined with other agents), nasopharyngitis, dizziness
- Rare: Pancreatitis, hepatic enzyme elevations, allergic reactions, lactic acidosis
- Metformin-associated: Gastrointestinal disturbances, metallic taste
Interactions
- Cationic drugs (e.g., cimetidine, ranitidine) may increase metformin levels
- Alcohol increases risk of lactic acidosis
- Iodinated contrast media may increase renal impairment risk
- Insulin and sulfonylureas increase hypoglycemia risk
- Carbonic anhydrase inhibitors may increase acidosis risk