Sitagliptin
Regulatory sources consulted
- ema-spc-EMEA/H/C/000762
- aemps-cima-07383014
- PubMed PMID:34292203 ↗
- RxNorm rxcui 593411 ↗
Approved indications
- To improve glycaemic control in adult patients with type 2 diabetes mellitus: as monotherapy (when metformin is inappropriate); as dual oral therapy (with metformin, a sulphonylurea, or a PPARγ agonist); as triple oral therapy (with a sulphonylurea and metformin, or with a PPARγ agonist and metformin); and as add-on to insulin (with or without metformin).
Contraindications
Absolute
- Hypersensitivity to the active substance or to any of the excipients.
Clinical warnings
- Major warning · Acute pancreatitis: Cases of acute pancreatitis have been reported. Patients should be informed of the characteristic symptom (persistent, severe abdominal pain). If suspected, discontinue treatment. — EMA
- Bullous pemphigoid: Postmarketing cases of bullous pemphigoid requiring hospitalization have been reported. If suspected, discontinue sitagliptin. — EMA
Drug interactions
- ModerateDigoxinC01AA05
Mechanism: Slight increase in digoxin exposure (AUC 11%, Cmax 18%), a P-glycoprotein substrate. The mechanism may involve mild inhibition of intestinal P-gp by sitagliptin.
Recommendation: No dose adjustment of digoxin is required, but patients at risk for digoxin toxicity should be monitored appropriately when co-administered.
EMA SPC
Adverse events
Common (≥1%)
hypoglycemia (in combination) · headache · upper respiratory tract infection · nasopharyngitis
Rare but serious
acute pancreatitis · hypersensitivity reactions (anaphylaxis, angioedema) · bullous pemphigoid · acute renal failure · severe joint pain
Pregnancy and lactation
FDA category: Not Recommended
Pregnancy: There are no adequate data from the use of sitagliptin in pregnant women. Should not be used during pregnancy. Lactation: It is unknown whether sitagliptin is excreted in human milk. Not recommended during breast-feeding.
Recent literature (PubMed)
Ensayo controlado aleatorizado de viabilidad que investigó el uso de sitagliptina para síntomas depresivos en diabetes tipo 2. Aunque el estudio fue factible y la sitagliptina mejoró la HbA1c, no mostró superioridad sobre el placebo para mejorar los síntomas depresivos en esta pequeña muestra.