Generic
Linagliptin
40 brands available in the market
At a glance
Linagliptin is used in the treatment of type 2 diabetes mellitus to improve glycaemic control. It is a DPP-4 inhibitor that increases incretin hormone levels to stimulate insulin release and reduce glucagon secretion.
Description
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). Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin from pancreatic beta cells in a glucose-dependent manner and decreasing the secretion of glucagon from pancreatic alpha cells.
Indications
- Type 2 diabetes mellitus - to improve glycaemic control in adults
- Monotherapy: when diet and exercise alone are inadequate and metformin is inappropriate or contraindicated
- Combination therapy: with metformin, or with metformin and sulphonylurea
Therapeutic class
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Pharmacological class
DPP-4 Inhibitor
Pharmacology
Linagliptin inhibits the DPP-4 enzyme, increasing incretin hormone (GLP-1 and GIP) levels, which stimulates glucose-dependent insulin release and reduces glucagon secretion, lowering blood glucose levels.
Mechanism of action
Improves glycemic control by inhibiting DPP-4 enzyme and increasing incretin hormone levels.
Dosage
Adult Dose (Oral):
- 5 mg once daily
- If added to metformin, maintain metformin dose and administer concomitantly
- When used with sulfonylurea, consider lower sulfonylurea dose to reduce hypoglycemia risk
Administration
- Swallow tablet whole; do not chew, crush or break
- May be taken with or without food at any time of the day
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Hypoglycemia (low blood sugar) - especially with sulfonylurea
- Nasopharyngitis
- Cough
- Pancreatitis (rare)
Precautions & warnings
- Hypoglycemia may occur with other antidiabetic drugs, alcohol, or delayed meals
- Always carry sugary food or fruit juice for hypoglycemia symptoms (cold sweats, pale skin, tremor, anxiety)
- Be careful while driving or operating machinery
- Inform your doctor if you experience stomach pain, nausea and/or vomiting
Contraindications
- Hypersensitivity to Linagliptin or any of its excipients
Drug interactions
- Weak competitive and weak-moderate mechanism-based inhibitor of CYP3A4; low risk of clinically meaningful interactions
- No clinically relevant effect on metformin, glyburide, simvastatin, warfarin, digoxin, or oral contraceptives
Food interactions
No food interactions known.
Use in pregnancy
Use in Pregnancy: Linagliptin use in pregnancy has limited controlled studies (Category B); use only if clearly needed.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if Linagliptin passes into breast milk; caution should be exercised.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No dose adjustment needed in elderly.
Renal / hepatic impairment
Renal Impairment: No dose adjustment required, including dialysis patients.
Hepatic Impairment: No dose adjustment required.
Overdose effects
No specific overdose information available; symptomatic and supportive measures should be employed.
Storage conditions
Store in a dry place, away from light and heat; keep out of reach of children.
Chemical structure
C25H28N8O2