Linagliptin
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 a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
Pharmacology
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
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.
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 weak competitive and a weak to 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 hypoglycaemia, nasopharyngitis, cough and pancreatitis in combination with metformin and sulfonylurea.
Pregnancy & Lactation
Pregnancy category B. There are no adequate and well controlled studies in pregnant women. So, Linagliptin tablets should be used during pregnancy only if clearly needed. It is not known whether Linagliptin passes into breast milk or not.
Precautions & Warnings
Hypersensitivity to the active substance or to any of the excipients.
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.
Chemical Structure
| Molecular Formula : | C25H28N8O2 |
| Chemical Structure : |  |
Common Questions about Linagliptin
What is Linagliptin?
Linagliptin is an inhibitor of DPP-4 enzyme.
What is Linagliptin used for?
Linagliptin is used for the treatment of type 2 diabetes mellitus to improve glycaemic control in adults.
How long do I need to use Linagliptin before I see improvement in my condition?
Linagliptin is to be taken till the time you see an improvement in your health conditions.
At what frequency do I need to use Linagliptin?
Linagliptin should be taken in the dosage as prescribed by the doctor.
Should I use Linagliptin empty stomach, before food or after food?
Linagliptin should be taken after food in a prescribed dosage.
What are the instructions for the storage and disposal of Linagliptin?
Linagliptin should be kept in a cool dry place and in its original packaging. Make sure this medication remains unreachable to children and pets.
Quick Tips
- Linagliptin should be taken at the same time every day since this helps you remember to take it.
- Linagliptin may cause hypoglycemia (low blood sugar level) when used with other antidiabetic medicines, alcohol or if you delay or miss a meal.
- Always carry some sugary food or fruit juice with you in case you experience hypoglycemia symptoms such as cold sweats, cool pale skin, tremor and anxiety.
- Be careful while driving or operating machinery until you know how Linagliptin affects you.
- Inform your doctor if you notice joint pains or develop symptoms such as stomach pain, nausea and/or vomiting.
