DPP-4 Inhibitor (Gliptin) Pregnancy: Use has not been studied in pregnant women; as a precautionary measure it is preferable to avoid use during pregnancy. A risk to the breast-fed child cannot be excluded - decide whether to discontinue breast-feeding or linagliptin.

Linagliptin

Brand names: Trajenta

Linagliptin is an oral DPP-4 inhibitor ('gliptin') for type 2 diabetes — weight-neutral with a low risk of hypoglycaemia on its own.

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: 5 mg once daily

Route: Oral - tablets can be taken with or without a meal at any time of the day

Frequency: Once daily

SPC source: Linagliptin 5 mg film-coated tablets (previously known as Trajenta). When linagliptin is added to metformin, the dose of metformin should be maintained and linagliptin administered concomitantly. When used in combination with a sulphonylurea or with insulin, a lower dose of the sulphonylurea or insulin may be considered to reduce the risk of hypoglycaemia. If a dose is missed, it should be taken as soon as the patient remembers, but a double dose should not be taken on the same day. Should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Hepatic impairment: pharmacokinetic studies suggest no dose adjustment is required, but clinical experience in such patients is lacking. Elderly: no dose adjustment necessary based on age. PAEDIATRIC: 'A clinical trial did not establish efficacy in paediatric patients 10 to 17 years of age. Therefore, treatment of children and adolescents with linagliptin is not recommended. Linagliptin has not been studied in paediatric patients under 10 years of age.' No paediatric dose is stated. Discontinue if pancreatitis is suspected (do not restart if acute pancreatitis is confirmed) or if bullous pemphigoid is suspected.

Dose adjustments

Renal

For patients with renal impairment, no dose adjustment for linagliptin is required.

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 (very common) - driven by background therapy; 14.8% under the triple combination linagliptin plus metformin plus sulphonylurea versus 7.6% on placebo
Lipase increased (common, based on elevations greater than 3 x ULN)
Nasopharyngitis, cough, rash, constipation, amylase increased, hypersensitivity e.g. bronchial hyperreactivity (uncommon)
Pancreatitis (rare) - discontinue if suspected; do not restart if acute pancreatitis is confirmed
Bullous pemphigoid (rare); angioedema and urticaria (rare, post-marketing)

Interactions

Rifampicin (potent inducer of P-glycoprotein and CYP3A4) - decreased linagliptin steady-state AUC by 39.6% and Cmax by 43.8%, with about 30% decreased DPP-4 inhibition at trough; full efficacy of linagliptin may not be achieved
Linagliptin is a P-glycoprotein substrate and inhibits P-gp-mediated transport of digoxin with low potency; it is considered unlikely to cause interactions with other P-gp substrates
Linagliptin is a weak competitive and weak to moderate mechanism-based inhibitor of CYP3A4 but does not inhibit other CYP isozymes and is not an inducer
Sulphonylureas and insulin - known to cause hypoglycaemia; caution is advised and a dose reduction of the sulphonylurea or insulin may be considered
NOTE: SPC §4.5 was truncated in the fetched source - the remainder of the interactions section still needs review

Clinical monograph

How it works

It inhibits dipeptidyl peptidase-4, raising endogenous incretin (GLP-1/GIP) levels and so increasing glucose-dependent insulin secretion and reducing glucagon.

Prescribing in practice

It is eliminated mainly via the bile, so — unlike other gliptins — it needs no dose adjustment in renal impairment.
Pancreatitis is a rare risk; rare bullous pemphigoid (a blistering skin condition) is reported.
Its low intrinsic hypoglycaemia risk rises when combined with a sulfonylurea or insulin.

Monitoring

Monitor glycaemic response; review for pancreatitis or blistering skin reactions.

Counselling the patient

It is generally well tolerated and weight-neutral.
Report severe abdominal pain or a blistering rash.

Evidence & guidelines

A weight-neutral oral option in type 2 diabetes (NICE NG28), convenient in renal impairment.

Reference: NICE NG28 (Type 2 DM); CARMELINA Trial (JAMA 2018); 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).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways