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Linagliptin (Trajenta® Tablets)

Linagliptin, marketed as Trajenta®, is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used to manage type 2 diabetes mellitus (T2DM). It is available only as a tablet; there is no injectable form of linagliptin. This article clarifies this distinction while detailing the pharmacology, clinical applications, and safety profile of linagliptin tablets, referencing the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Linagliptin inhibits the enzyme DPP-4, which degrades incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By preventing their breakdown, linagliptin:

  • Enhances Insulin Secretion: Increases glucose-dependent insulin release from pancreatic β-cells.
  • Suppresses Glucagon: Reduces inappropriate glucagon secretion from α-cells, lowering hepatic glucose production.
  • Slows Gastric Emptying: Mildly delays gastric emptying via GLP-1 activity, moderating postprandial glucose spikes (Lippincott).

Unlike other DPP-4 inhibitors, linagliptin has a non-renal route of excretion, making it unique in its pharmacokinetics (Lange).

  1. Type 2 Diabetes Mellitus:
    • Monotherapy or combined with other agents (e.g., metformin, sulfonylureas, insulin) when diet/exercise alone are insufficient.
    • Preferred in patients with renal impairment due to no dose adjustment requirements (BNF).
  2. Cardiovascular Safety:
    • Neutral effect on cardiovascular outcomes but safe in patients with heart disease (Lippincott).
  • Standard Dose: 5 mg once daily, taken orally with or without food.
  • Special Populations:
    • Renal Impairment: No dose adjustment required (unlike other DPP-4 inhibitors). Safe in all stages, including end-stage renal disease (BNF).
    • Hepatic Impairment: No adjustment needed.

Elderly: Safe without dose changes

  • Nasopharyngitis, headache, upper respiratory infections.
  • Hypoglycemia (when combined with sulfonylureas or insulin).

Serious (Rare):

  • Pancreatitis: Monitor for severe abdominal pain.
  • Hypersensitivity Reactions: Angioedema, rash, or anaphylaxis.
  • Arthralgia: Severe joint pain reported in post-marketing data (BNF).

• Contraindications:
o Hypersensitivity to linagliptin or DPP-4 inhibitors.
o History of pancreatitis (relative contraindication).

    • Renal function (baseline and periodically).
    • HbA1c, blood glucose, and signs of pancreatitis.
    • Pregnancy: Category B; use only if benefits outweigh risks.
    • Lactation: Avoid—limited data on excretion in breast milk (Lange).
  • Strong CYP3A4 Inducers (e.g., rifampicin): May reduce linagliptin efficacy.
  • Insulin/Sulfonylureas: Increased hypoglycemia risk; consider dose reduction.
  • ACE Inhibitors: Theoretical risk of angioedema (rare) (BNF).
  • Generic: Linagliptin.
  • Brand Name: Trajenta® (Boehringer Ingelheim).

Trajenta® is exclusively an oral tablet. There is no injectable form of linagliptin. Injectable diabetes medications include:

  • GLP-1 Receptor Agonists: Semaglutide (Ozempic®), Dulaglutide (Trulicity®).
  • Insulins: Insulin glargine (Lantus®), insulin aspart (NovoRapid®).

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