Pharmacology · DPP-4 inhibitors (gliptins)
Vildagliptin !
A DPP-4 inhibitor used in Europe and other regions, not in the US. It binds the enzyme covalently and is cleared mainly by the kidney.
Updated 2026-11-01
The figure shows vildagliptin in the active site of human DPP-4.
Mechanism of action
Vildagliptin, like saxagliptin a cyanopyrrolidine, forms a reversible covalent bond with the catalytic serine of DPP-4. Active GLP-1 and GIP last longer after meals, raising glucose-dependent insulin release and lowering glucagon.
- Blocks the DPP-4 enzyme in plasma and on cells
- Active GLP-1 and GIP last longer after meals
- More insulin and less glucagon when glucose is high
- Glucose falls without weight change
Pharmacokinetics
- Absorption
- Oral, well absorbed from the small intestine.
- Elimination
- Mainly through the urine, so lower doses are used when kidney function is reduced.
Indications
- Type 2 diabetes, alone or combined with metformin and other drugs Type 2 diabetes mellitus →
Adverse effects
Common
- Hypoglycemia when combined with insulin or a sulfonylurea
Contraindications
- Hypersensitivity to vildagliptin
- Not for type 1 diabetes or ketoacidosis
Key interactions
- Insulin or sulfonylureas
- Higher risk of hypoglycemia.
- GLP-1 receptor agonists
- Not combined: same pathway.
What is monitored
- Kidney function
- HbA1c
Administration and safety
- Oral tablet.
- Not given together with a GLP-1 receptor agonist.
Nursing care
- Before: kidney function, history of pancreatitis and heart failure.
- During: abdominal pain, skin blisters, joint pain, swelling or breathlessness.
- Capillary glucose when combined with insulin or a sulfonylurea.
Pregnancy and breastfeeding
Data in pregnancy are limited; insulin is the usual choice.
Test yourself
Think of the answer, then tap the question to see it.
Which two gliptins bind DPP-4 covalently?
Vildagliptin and saxagliptin.
Why is the vildagliptin dose lowered when kidney function falls?
It is cleared mainly in the urine, so it accumulates when filtration falls.
Is vildagliptin expected to cause hypoglycemia alone?
Rarely. Like other gliptins, its effect is glucose-dependent; the risk rises with insulin or sulfonylureas.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: The structure of DPP4 in complex with Vildagliptin (RCSB Protein Data Bank, 2017); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 51 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.