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Linagliptin 5 mg: Uses,Dosage,Side Effects

Generic Name
Linagliptin
Therapeutic Class: Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Indications:
Linagliptin is indicated in the treatment of type-2 diabetes mellitus to improve glycaemic control in adults:
As monotherapy:
  • in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to intolerance or contraindicated due to renal impairment.
As combination therapy:
  • in combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.
  • in combination with Sulphonylurea and Metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
  • in combination with Insulin with or without Metformin, when this regimen alone, with diet and exercise, does not provide adequate glycaemic control.
Presentation:
Each tablet contains Linagliptin INN 5 mg.

Description:
Linagliptin is indicated to improve glycemic control in patients with type 2 diabetes mellitus. Linagliptin is an inhibitor of DPP-4 (dipeptidyl peptidase-4), an enzyme that degrades the incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). Thus, Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin from pancreatic beta (β) cells in a glucose-dependent manner and decreasing the secretion of glucagon from pancreatic alpha (α) cells in the circulation.

Dosage & Administration:
  • The recommended dose of Linagliptin is 5 mg once daily.
  • Linagliptin can be taken with or without food at any time of the day. If a dose is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.
  • For patients with renal insufficiency, no dosage adjustment is required
  • Pharmacokinetic studies suggest that no dose adjustment is required for patients with hepatic impairment
  • When Linagliptin is added to Metformin, the dose of Metformin should be maintained, and Linagliptin administered concomitantly.
  • When Linagliptin is 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 hypoglycemia.
Interaction:
Linagliptin is a weak competitive and a weak to a moderate mechanism-based inhibitor of CYP isozyme CYP3A4 but does not inhibit other CYP isozymes. The risk for clinically meaningful interactions by other medicinal products on linagliptin is low and in clinical studies, linagliptin had no clinically relevant effect on the pharmacokinetics of metformin, glyburide, simvastatin, warfarin, digoxin, or oral contraceptives.

Contraindications:
Hypersensitivity to the active substance or to any of the excipients.

Side Effects:
There may be hypoglycemia, nasopharyngitis, cough, and pancreatitis in combination with metformin and sulfonylurea.

Pregnancy & Lactation:
  • Pregnancy:
  • The use of Linagliptin has not been studied in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of Linagliptin during pregnancy.
  • Nursing mothers:
  • Available pharmacokinetic data in animals have shown excretion of Linagliptin/metabolites in milk. A risk to the breastfed child cannot be excluded. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from Linagliptin therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
  • Pediatric Use:
  • The safety and efficacy of Linagliptin in children and adolescents have not yet been established. No data are available.
  • Geriatric Use: No dose adjustment is necessary based on age. However, clinical experience in patients > 80 years of age is limited and caution should be exercised when treating this population.
Precautions & Warnings:
  • General: Linagliptin should not be used in patients with type-1 diabetes or for the treatment of diabetic ketoacidosis.
  • Hypoglycemia:Linagliptin alone showed a comparable incidence of hypoglycemia to placebo. Caution is advised when Linagliptin is used in combination with a Sulphonylurea and/or Insulin. A dose reduction of the Sulphonylurea or Insulin may be considered.
  • Pancreatitis:In the post-marketing experience of Linagliptin, there have been spontaneously reported adverse reactions of acute pancreatitis. Patients should be informed of the characteristic symptom of acute pancreatitis: persistent, severe abdominal pain. Resolution of pancreatitis has been observed after discontinuation of Linagliptin. If pancreatitis is suspected, Linagliptin should be discontinued.
Overdose:
  • Symptoms: During controlled clinical trials in healthy subjects, single doses of up to 600 mg Linagliptin (equivalent to 120 times the recommended dose) were generally well tolerated. There is no experience with doses above 600 mg in humans.
  • Therapy: In the event of an overdose, it is reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute clinical measures if required.
Storage:
Store in a cool & dry place. Keep out of reach of children.

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