Linagliptin

Linagliptin Brand Name– Tradjenta

What is Linagliptin

Linagliptin belongs to the class of oral dipeptidyl peptidase-4 (DPP-4) inhibitors and is used in the treatment of type 2 diabetes mellitus (DM) in adults. DPP-4 inhibitors potentiate the effects of the incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), by inhibiting their breakdown by DPP-4.

Linagliptin is administered in a single fixed-dose once daily, with no dosage adjustments necessary for organ impairment. Use of linagliptin results in a mean hemoglobin A1C reduction of 0.7%; the drug also significantly reduces fasting plasma glucose and 2-hour postprandial glucose concentrations.

Metformin is first-line in the treatment of type 2 DM. In patients with established cardiovascular (CV) disease, heart failure (HF), or chronic kidney disease (CKD), a sodium-glucose co-transporter 2 (SGLT2) inhibitor or GLP-1 receptor agonist (GLP-1 RA) with proven CV benefit and reduction of CKD progression is recommended for add-on therapy, independent of baseline A1C or individualized A1C target.

In patients without indicators of high-risk or established CVD, HF, or CKD, DPP-4 inhibitors are a therapeutic option which are generally well tolerated, have a neutral effect on weight, and have minimal risk of hypoglycemia when used as monotherapy

Indications

  • type 2 diabetes mellitus

For the treatment of type 2 diabetes mellitus in combination with diet and exercise

Side Effects

  1. anaphylactoid reactions
  2. angioedema
  3. arthralgia
  4. bronchospasm
  5. bullous rash
  6. cough
  7. diarrhea
  8. exfoliative dermatitis
  9. heart failure
  10. hyperamylasemia
  11. hyperuricemia
  12. hypoglycemia
  13. myalgia
  14. oral ulceration
  15. pancreatitis
  16. pemphigus
  17. pharyngitis
  18. pruritus
  19. rash
  20. rhabdomyolysis
  21. stomatitis
  22. urticaria
  23. weight gain
  24. weight loss

Monitoring Parameters

  • blood glucose
  • glycosylated hemoglobin A1c (HbA1c)
  • serum creatinine/BUN

Contraindications

  • adrenal insufficiency
  • arthralgia
  • breast-feeding
  • burns
  • children
  • diabetic ketoacidosis
  • diarrhea
  • exfoliative dermatitis
  • fever
  • gastroparesis
  • geriatric
  • GI obstruction
  • heart failure
  • history of angioedema
  • hypercortisolism
  • hyperglycemia
  • hyperthyroidism
  • hypoglycemia
  • hypothyroidism
  • ileus
  • infection
  • malnutrition
  • pancreatitis
  • pituitary insufficiency
  • pregnancy
  • renal impairment
  • serious rash
  • surgery
  • trauma
  • type 1 diabetes mellitus
  • vomiting

Interactions

  • Acebutolol
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Acetaminophen; Guaifenesin; Phenylephrine
  • Acetaminophen; Pseudoephedrine
  • Acetazolamide
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