Vildagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus, as monotherapy or in dual combination with metformin, a sulphonylurea, a thiazolidinedione, or insulin when diet, exercise, and a single antidiabetic agent do not provide adequate glycemic control.

Vildagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that acts in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released from the intestine throughout the day, and their levels increase after meals. These hormones are rapidly inactivated by the enzyme DPP-4. Incretins are part of the endogenous system involved in the physiological regulation of glucose homeostasis. When blood glucose levels are normal or elevated, GLP-1 and GIP increase insulin synthesis and secretion from pancreatic beta cells via intracellular signaling pathways involving cyclic AMP. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, thereby decreasing hepatic glucose production. By increasing and prolonging active incretin levels, Vildagliptin enhances insulin release and reduces glucagon levels in a glucose-dependent manner.

The recommended dose of Vildagliptin is

• 50 mg or 100 mg daily for monotherapy.
• 50 mg twice daily (morning and evening) when used in dual combination with Metformin or a Thiazolidinedione;
• 50 mg once daily in the morning when used in dual combination with a Sulphonylurea.

Vildagliptin may be taken with or without a meal. No dosage adjustment is required in the elderly, or in patients with mild renal impairment.

Pediatric use: Vildagliptin is not recommended in patients 18 years of age.

In pharmacokinetic studies, no clinically relevant interactions were observed with pioglitazone, metformin, glibenclamide, digoxin, warfarin, amlodipine, ramipril, valsartan, or simvastatin. As with other oral antidiabetic medicines, the glucose-lowering effect of Vildagliptin may be reduced by certain substances, including thiazides, corticosteroids, thyroid products, and sympathomimetics.

Vildagliptin is contraindicated in patients with:

• Hypersensitivity to the active substance or any excipients
• Moderate to severe renal impairment
• Hepatic impairment (ALT or AST >3 times upper limit of normal)
• Type 1 diabetes mellitus

Most adverse reactions were mild and transient and did not require discontinuation of therapy. Rare cases of hepatic dysfunction have been reported. Clinical trials up to and beyond 2 years did not show additional safety concerns or unexpected risks.

Vildagliptin should not be used during pregnancy or lactation.

Caution is required in patients aged 75 years and older due to limited clinical experience. Liver function tests (LFTs) should be performed before starting treatment, every 3 months during the first year, and periodically thereafter. If transaminase levels increase, repeat testing is required to confirm the result and monitor frequently until normalization. If AST or ALT remains above 3 times the upper limit of normal, treatment should be discontinued. Patients developing jaundice or signs of liver dysfunction should stop Vildagliptin immediately. After normalization of liver function, treatment should not be restarted. Use with caution in patients with congestive heart failure (NYHA class I–II) and avoid use in NYHA class III–IV.

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Store below 30°C, away from light and moisture. Keep out of reach of children.