Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It may be used as monotherapy or in combination with other hypoglycaemic agents including metformin, sulfonylurea, pioglitazone or insulin.
Recommended dose is 5 mg once daily or 2.5 mg twice daily and can be taken with or without food. No dose adjustment is required in renal or hepatic impairment. It is not recommended for use in children and adolescents under 18 years.
Each film-coated tablet contains:
Linagliptin INN ... 5 mg.
Linagliptin is described described chemically 1H-Purine-2, 6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl) -3,7-dihydro-3-methyl-1-[ (4-methyl-2-quinazolinyl) methyl]. The empirical formula is C25H28N8O2 and the molecular weight is 472.54.
Linagliptin is a competitive, reversible inhibitor of dipeptidyl peptidase-4, an enzyme that degrades the incretin hormones glucagon-like-peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), resulting in increased concentrations of active incretin hormones, stimulating the relea...
The absolute bioavailability of linagliptin is approximately 30%. High-fat meal reduced Cmax by 15% and increased AUC by 4%: this effect is not clinically relevant. Plasma protein binding of linagliptin is concentration-dependent, decreasing from about 99% at 1 nmol/L to 75%-89%at ≥30 nmol/L, reflec...
Linagliptin is contraindicated in patients with a history of hypersensitivity to linagliptin such as urticaria, angioedema or bronchial hyperreactivity; Type I diabetes, diabetes coma and ketoacidosis.
It is used with caution in patients with lactic acidosis, underlying disease, macrovascular outcomes; debilitated, malnourished or elderly patients and patients with adrenal or pituitary insufficiency or alcohol intoxication are particularly susceptible to hypoglycaemic effects. Hypoglycaemia may be...
Headache, diarrhea, nausea, abdominal discomfort, acute pancreatitis including fatal and non-fatal haemorrhage and necrotizing pancreatitis, cough, nasopharyngitis, hypoglycaemia, hyperlipidemia, hypertriglyceridemia, urinary tract infection, weight gain, back pain, myalgia, severe and disabling art...
Rifampin decreased linagliptin exposure, suggesting that the efficacy of linagliptin may be reduced when administered in combination with a strong P-glycoprotein or CYP 3A4 inducer. Therefore, use of alternative treatments (not containing linagliptin) is strongly recommended when concomitant treatme...
Insulin Secretagogues or Insulin: Co-administration of linagliptin with an insulin secretagogue (e.g., sulfonylurea) or insulin may require lower doses of the insulin secretagogue or insulin to reduce the risk of hypoglycemia.
Store below 30°C in cool, dry place. Protect from light and moisture. Keep out of reach and sight of children.
10 x 10’s Blisters.