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DPP-4 Inhibitor Pregnancy: Should not be used during pregnancy — there are no adequate data in pregnant women and animal studies have shown reproductive toxicity at high doses; the potential risk for humans is unknown. Should not be used during breast-feeding (excretion in human milk unknown; excreted in animal milk).

Sitagliptin

Brand names: Januvia, Xelevia

Used in: Diabetes & DKA

Sitagliptin is a DPP-4 inhibitor (a gliptin) used in type 2 diabetes; it is weight-neutral and carries a low risk of hypoglycaemia when used alone.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 100 mg sitagliptin once daily
Route: Oral
Frequency: Once daily, with or without food
UK SPC (Sitagliptin 100 mg film coated tablets). When used in combination with metformin and/or a PPAR-gamma agonist, the dose of metformin and/or PPAR-gamma agonist should be maintained and sitagliptin administered concomitantly. When used with a sulphonylurea or with insulin, a lower dose of the sulphonylurea or insulin may be considered to reduce the risk of hypoglycaemia. Missed dose: take as soon as the patient remembers; a double dose should not be taken on the same day. Hepatic impairment: no dose adjustment for mild to moderate impairment; not studied in severe hepatic impairment — care should be exercised. Elderly: no dose adjustment based on age. Paediatric population: should not be used in children and adolescents 10 to 17 years of age because of insufficient efficacy; has not been studied in patients under 10 years of age. Should not be used in type 1 diabetes or for the treatment of diabetic ketoacidosis. Assessment of renal function is recommended prior to initiation and periodically thereafter. SOURCE GAP: section 4.5 (interactions) was truncated in the fetched bundle — clinician to check the full SPC for interaction data.

Dose adjustments

Renal

Mild impairment (GFR 60 to under 90 mL/min): no dose adjustment. Moderate impairment (GFR 45 to under 60 mL/min): no dose adjustment. Moderate impairment (GFR 30 to under 45 mL/min): 50 mg once daily. Severe impairment (GFR 15 to under 30 mL/min) or end-stage renal disease (GFR under 15 mL/min), including haemodialysis or peritoneal dialysis: 25 mg once daily — may be administered without regard to the timing of dialysis.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients

Side effects

  • Hypoglycaemia (common; reported in combination with sulphonylurea 4.7%-13.8% and insulin 9.6%)
  • Headache (common); dizziness (uncommon)
  • Constipation, pruritus (uncommon)
  • Acute pancreatitis, including fatal and non-fatal haemorrhagic and necrotising pancreatitis (frequency not known)
  • Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria and exfoliative skin conditions including Stevens-Johnson syndrome (frequency not known); bullous pemphigoid (frequency not known)
  • Thrombocytopenia (rare); impaired renal function and acute renal failure (frequency not known)

Interactions

  • Sulphonylureas — hypoglycaemia observed in combination; a lower dose of the sulphonylurea may be considered (from sections 4.2 and 4.4; section 4.5 was not captured in the fetched bundle)
  • Insulin — hypoglycaemia observed in combination; a lower dose of insulin may be considered
  • Metformin and/or PPAR-gamma agonists — dose of the co-administered agent should be maintained; rates of hypoglycaemia were similar to placebo with these combinations

Clinical monograph

How it works

It inhibits dipeptidyl peptidase-4, prolonging the action of incretin hormones to enhance glucose-dependent insulin release and suppress glucagon.

Prescribing in practice

  • Reduce the dose in renal impairment.
  • Hypoglycaemia risk is low alone but rises when combined with a sulfonylurea or insulin.
  • Stop and investigate if severe, persistent abdominal pain suggests pancreatitis.

Monitoring

Monitor HbA1c for response and renal function for dose adjustment.

Counselling the patient

  • It is generally well tolerated and does not usually cause low blood sugar on its own.
  • Report severe, persistent abdominal pain.

Evidence & guidelines

DPP-4 inhibitors are an option to intensify type 2 diabetes treatment per NICE NG28, valued for weight-neutrality and low hypoglycaemia risk.

Reference: NICE NG28; TECOS trial; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.