Vildagliptin Dosing for Adults with Type 2 Diabetes
The recommended dose of vildagliptin for adults with type 2 diabetes is 50 mg twice daily (total 100 mg/day) when used as monotherapy or in combination with metformin or a thiazolidinedione, and 50 mg once daily when combined with a sulfonylurea. 1, 2
Standard Dosing Regimen
- Primary dosing: 50 mg twice daily is the standard regimen for monotherapy or when combined with metformin, providing optimal glycemic control with complete DPP-4 inhibition 1, 2
- Combination with sulfonylureas: Reduce to 50 mg once daily to minimize hypoglycemia risk when adding vildagliptin to sulfonylurea therapy 2
- Food considerations: Vildagliptin can be taken without regard to meals, as food does not have clinically relevant impact on its pharmacokinetics 1
Renal Impairment Dose Adjustments
For patients with moderate to severe chronic kidney disease, the dose must be reduced by half to 50 mg once daily. 3, 4
Specific eGFR-Based Dosing:
- eGFR >50 mL/min/1.73 m²: No dose adjustment required; use standard 50 mg twice daily 4
- eGFR 30-50 mL/min/1.73 m² (moderate CKD): Reduce to 50 mg once daily 3, 4
- eGFR <30 mL/min/1.73 m² (severe CKD): Reduce to 50 mg once daily 3, 4, 5
The dose reduction is necessary because vildagliptin exposure increases approximately 2-fold in patients with renal impairment, though this increase does not directly correlate with severity of renal dysfunction due to the kidneys' dual role in both excretion and hydrolysis metabolism of the drug 1.
Special Populations
- Elderly patients: No dose adjustment required despite approximately 30% increase in exposure, which is primarily attributable to age-related decline in renal function and is not clinically significant 1, 2
- Hepatic impairment: No dose adjustment needed 1
- Gender, BMI, ethnicity: These factors do not influence vildagliptin pharmacokinetics and require no dose modifications 1
Clinical Efficacy by Dose
The 50 mg twice daily regimen demonstrates superior efficacy compared to lower doses:
- HbA1c reduction: Vildagliptin 50 mg twice daily reduces HbA1c by approximately 0.9% from baseline in patients with severe renal impairment on insulin therapy 3
- Dose-response relationship: Doses greater than 50 mg twice daily provide no substantial additional glycemic benefit 1
- Renal impairment efficacy: Even at the reduced dose of 50 mg once daily, vildagliptin maintains efficacy in severe renal impairment comparable to standard dosing in patients with normal renal function 3, 5
Safety Considerations
Vildagliptin has a favorable safety profile with low hypoglycemia risk and weight neutrality. 1, 2
Key Safety Points:
- Hypoglycemia: Lower incidence compared to sulfonylureas, particularly when used as monotherapy or with metformin 1, 2
- Weight: Weight-neutral; does not cause weight gain 3, 2
- Liver function: Monitor liver enzymes, particularly with 100 mg once daily dosing (off-label), though meta-analyses show 50 mg once or twice daily is not associated with increased hepatic adverse events 2
- Pancreatitis: Reported in clinical trials but causality not established 2
Comparative Dosing with Other DPP-4 Inhibitors
In severe renal impairment (eGFR <30 mL/min/1.73 m²), vildagliptin 50 mg once daily demonstrates similar efficacy and safety to sitagliptin 25 mg once daily, with both drugs well-tolerated in this challenging population 5. Unlike linagliptin, vildagliptin requires dose reduction in moderate to severe CKD 4.