Carlina 5

Generic

Linagliptin

 

Indications

Linagliptin is used to treat type 2 diabetes mellitus in people and enhance glycaemic control.

As monotherapy: in patients who are unable to regulate their blood sugar levels with diet and exercise alone and for whom metformin is either ineffective or contraindicated owing to renal impairment.

When diet and exercise plus metformin alone do not provide adequate glycaemic control, use in combination with a sulphonylurea and metformin. When diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control, use in combination with a sulphonylurea and metformin.

 

Pharmacology

Linagliptin is used to help people with type 2 diabetes control their blood sugar levels. DPP-4 (dipeptidyl peptidase-4) is an enzyme that degrades the incretin hormones GLP-1 (glucagon like peptide-1) and GIP (glucagon-like peptide-1). Linagliptin is an inhibitor of DPP-4 (dipeptidyl peptidase-4) (glucose dependent insulinotropic polypeptide). Linagliptin stimulates the release of insulin from pancreatic beta () cells in a glucose-dependent manner while lowering the production of glucagon from pancreatic alpha () cells in the blood, increasing the concentrations of active incretin hormones.

 

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 CYP3A4 isozyme, however it has no effect on the other CYP isozymes. The risk of clinically significant interactions with other medicines is low, and linagliptin had no clinically significant effect on the pharmacokinetics of metformin, glyburide, simvastatin, warfarin, digoxin, or oral contraceptives in clinical investigations.

 

Contraindications

Hypersensitivity to the active ingredient or any excipient.

 

Side Effects

When metformin and sulfonylurea are used together, hypoglycemia, nasopharyngitis, cough, and pancreatitis might occur.

 

Pregnancy & Lactation

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

 

Precautions & Warnings

Hypersensitivity to the active ingredient or any excipient.

 

Therapeutic Class

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

 

Storage Conditions

Keep in a dry place away from light and heat. Keep out of the reach of children.

 

Pharmaceutical Name

Radiant Pharmaceuticals Ltd.