Generic

Linagliptin

Indications

Linagliptin is used to enhance glycemic control in individuals with type 2 diabetes mellitus.

• As monotherapy: in individuals who are not sufficiently managed by diet and exercise alone, and for whom metformin is either ineffective owing to intolerance or contraindicated due to renal impairment.
• When diet and exercise, combined with metformin, do not provide adequate glycemic control; when diet and exercise, combined with metformin, do not provide adequate glycemic control; and when diet and exercise, combined with dual therapy with these medicinal products, do not provide adequate glycemic control.

Pharmacology

Linagliptin is used to enhance glycemic control in people with type 2 diabetes. Linagliptin is a DPP-4 (dipeptidyl peptidase-4) inhibitor, which is an enzyme that destroys the incretin hormones GLP-1 (glucagon like peptide-1) and GIP (glucose dependent insulinotropic polypeptide). Thus, linagliptin raises the concentrations of active incretin hormones in the blood, increasing the release of insulin from pancreatic beta () cells in a glucose-dependent manner while reducing glucagon production from pancreatic alpha () cells.

Dosage & Administration

Linagliptin 5 mg once daily. If added to metformin, the dose of metformin should be maintained and linagliptin administered concomitantly. When used in combination with a sulfonylurea, a lower dose of the sulphonylurea may be considered to reduce the risk of hypoglycaemia.

Patients with renal impairment: No dose adjustment required. Linagliptin can be taken with or without a meal at any time of the day.

Interaction

Linagliptin is a mild competitive and weak to moderate mechanism-based inhibitor of the CYP isozyme CYP3A4, however it has no effect on the other CYP isozymes. The risk of clinically important interactions with other medications is minimal, and linagliptin had no clinically relevant influence on the pharmacokinetics of metformin, glyburide, simvastatin, warfarin, digoxin, or oral contraceptives in clinical trials.

Contraindications

Hypersensitivity to the active ingredient or any of the excipients

Side Effects

In combination with metformin and sulfonylurea, there is a risk of hypoglycemia, nasopharyngitis, cough, and pancreatitis.

Pregnancy & Lactation

Pregnancy classification B. In pregnant women, there are no appropriate and well-controlled trials. As a result, Linagliptin tablets should only be taken during pregnancy if absolutely necessary. It is unknown whether Linagliptin is excreted in breast milk.

Precautions & Warnings

Hypersensitivity to the active ingredient or any of the excipients.

Therapeutic Class

Inhibitor of Dipeptidyl Peptidase-4 (DPP-4)

Storage Conditions

Keep away from light and heat in a dry area. Keep out of children’s reach.

Pharmaceutical Name

Beximco Pharma Ltd