Dipeptidylpeptidase-4 Inhibitors aka DPPIV-inhibitors
Examples
- Sitagliptin
- Saxagliptin
- Vildagliptin
Indications
- Prophylaxis of asthma in children, they are less effective than prophylaxis with corticosteroids. Rarely used in adults.
- Prophylaxis of exercise induced asthma.
- Prophylaxis against allergic rhinitis and allergic conjunctivitis. Cromones can be bought over the counter for treating these conditions
- Used in the management of food allergy when the allergy is difficult to treat by avoidance alone.
- Used as eye drop for eye hayfever symptoms.
Contraindications
Contraindication
- Pregnancy / breast feeding
- Ketoacidosis (vildagliptin and sitagliptin)
Caution
- Elderly
- Renal impairment
- History of pancreatitis
- Hepatic impairment
Mechanism
Inhibition of DPP-4 activity causes an increase in incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic polypeptide) by delaying their breakdown. This increases glucose dependent insulin secretion and reduces glucagon secretion.
Administration
Given orally.
Adverse Reactions
- Gastrointestinal upset
- Oedema
- Hepatic toxicity (vildagliptin)
- Possible increased risk of pancreatitis and pancreatic cancer
- Upper respiratory tract infection / nasopharyngitis
- Stevens-Johnson syndrome
Can cause hypoglycaemia.
Interactions
Combination therapy with other anti-diabetic drugs may increase the risk of hypoglycaemia.
Education
Patient education should include explanations about hypoglycaemia and how to recognise / manage it. Patients should also be informed of the risks of pancreatitis and the symptoms of this.
Pharmacokinetics
Nil of note.
