What is the maximum recommended dose of Vildagliptin (DPP-4 inhibitor) per day?

Maximum Recommended Dose of Vildagliptin

The maximum recommended dose of vildagliptin is 100 mg per day, typically administered as 50 mg twice daily. 1

Dosing Recommendations

Vildagliptin dosing depends on the specific clinical scenario:

• Standard dosing: 50 mg twice daily (100 mg total daily dose) when used:

  • As monotherapy
  • In combination with metformin
  • In combination with a thiazolidinedione 2

• Reduced dosing: 50 mg once daily (50 mg total daily dose) when used:

  • In combination with a sulfonylurea 2
  • In patients with moderate to severe renal impairment 3

Renal Impairment Considerations

Vildagliptin exposure increases in patients with renal impairment:

• Mild renal impairment: 40% increase in exposure
• Moderate renal impairment: 71% increase in exposure
• Severe renal impairment: 100% increase in exposure 3

Based on these pharmacokinetic findings, the appropriate dose for patients with moderate to severe renal impairment is 50 mg once daily 3.

Pharmacokinetic Properties

Vildagliptin has several favorable pharmacokinetic properties:

• Rapid absorption with 85% bioavailability
• Minimal protein binding (9.3%)
• Extensive distribution into extravascular spaces
• Renal clearance accounts for 33% of total body clearance
• Primary elimination through hydrolysis by multiple tissues/organs 1

Safety Profile

Vildagliptin is generally well-tolerated with:

• Low risk of hypoglycemia when used as monotherapy
• Weight-neutral effect
• Most common side effects include headache, nasopharyngitis, cough, constipation, and dizziness 2, 4

Clinical Efficacy

Vildagliptin effectively reduces:

• HbA1c levels
• Fasting plasma glucose
• Postprandial glucose levels

It also improves beta-cell function and has been shown to be effective in long-term treatment for up to 2 years 1.

Common Pitfalls to Avoid

1. Exceeding maximum daily dose: Never exceed 100 mg per day, as higher doses do not provide substantial additional benefits but may increase risk of adverse effects 1

2. Incorrect dosing in renal impairment: Patients with moderate to severe renal impairment should receive 50 mg once daily, not twice daily 3

3. Monitoring liver function: Liver function should be monitored in patients receiving vildagliptin, as increases in transaminase levels have been observed in some clinical trials 2

4. Drug interactions: Although vildagliptin has a low potential for drug interactions, be aware of its role as both a substrate and inhibitor of DPP-4 1