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Linagliptin

Dipeptidyl peptidase 4 (DPP-4) inhibitor – gliptin

ATC code: A10BH05

Brand names: Tradjenta, Jentadueto, Glyxambi

Updated · Methodology

Indications

A

Type 2 diabetes mellitus

Second line

Linagliptin is second-line DPP-4 inhibitor for type 2 diabetes. redGDPS 2024 recommends linagliptin as an option in patients with chronic kidney disease (eGFR below 45 mL/min) when metformin is contraindicated and a drug without dose adjustment is needed. No significant cardiovascular risk reduction (neutral profile per CARMELINA 2018).

Sources

  1. EMA: Trajenta (linagliptin) SmPC (2024)
  2. redGDPS: Algoritmo de tratamiento de la diabetes tipo 2 - redGDPS 2024 (2024)

ICD-10: E11 · ICD-11: 5A11

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Selective reversible DPP-4 inhibitor – the enzyme that degrades incretins GLP-1 and GIP. Raises active incretin levels 2–3 fold, enhancing glucose-dependent insulin release and suppressing glucagon. Hypoglycaemia is rare because effect is glucose-dependent. Unique among gliptins – minimal renal clearance (5%), excreted mostly via bile, so no dose adjustment for renal impairment.

Safety

Contraindications

  • Known linagliptin hypersensitivity
  • Type 1 diabetes
  • Diabetic ketoacidosis

Serious adverse effects

  • Acute pancreatitis
  • Severe joint pain
  • Bullous skin reactions (bullous pemphigoid)

Common adverse effects

  • Nasopharyngitis
  • Hypersensitivity with rash
  • Hypoglycaemia (rare, more often combined with insulin or sulfonylurea)

Pregnancy: can you take Linagliptin?

Pregnancy data limited. Switch to insulin when planning pregnancy.

Breastfeeding: can you take Linagliptin?

Limited milk data. Breastfeeding not recommended.

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Label mentions4 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • Majorinsulinclass named in the label
    «Insulin Secretagogues or Insulin: Insulin and insulin secretagogues are known to cause hypoglycemia. The risk of hypoglycemia is increased when linagliptin is used in combination with an insulin…»

    FDA, section 7 · Open on DailyMed

  • Majorsulfonylureasclass named in the label
    «Insulin Secretagogues or Insulin: Insulin and insulin secretagogues are known to cause hypoglycemia. The risk of hypoglycemia is increased when linagliptin is used in combination with an insulin…»

    FDA, section 7 · Open on DailyMed

  • CYP3A4 inducersclass named in the label
    «DRUG INTERACTIONS: Strong P-glycoprotein/CYP3A4 inducer: The efficacy of TRADJENTA may be reduced when administered in combination (e.g., with rifampin). Use of alternative treatments is strongly…»

    FDA, section 7 · Open on DailyMed

From other drugs’ labels

  • Empagliflozin
    «Los estudios de interacciones sugieren que la farmacocinética de empagliflozina no se vio influida por la administración conjunta de metformina, glimepirida, pioglitazona, sitagliptina, linagliptina…»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Linagliptin used for?

Linagliptin is evaluated for the following indications with varying evidence strength: Type 2 diabetes mellitus (evidence tier A). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Linagliptin?

Common side effects of Linagliptin (≥ 1 in 100): Nasopharyngitis, Hypersensitivity with rash, Hypoglycaemia (rare, more often combined with insulin or sulfonylurea). See the Safety section for uncommon and serious reactions.

Is Linagliptin safe during pregnancy?

Pregnancy data limited. Switch to insulin when planning pregnancy.

Is Linagliptin compatible with breastfeeding?

Limited milk data. Breastfeeding not recommended.

Who should not take Linagliptin?

Linagliptin is contraindicated in: Known linagliptin hypersensitivity; Type 1 diabetes; Diabetic ketoacidosis. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Liraglutide, Metformin, Pioglitazone, Repaglinide, Vildagliptin, Gliclazide, Insulin detemir, Semaglutide