This page contains brief details about the drug , it's indication, dosage & administaration, mechanism of action, related brands with strength, warnings and common side effects.

Background and Date of Approval

Linagliptin was initially approved by the United States Food and Drug Administration (FDA) on May 2, 2011. 

A 2013 randomised, double-blind, placebo-controlled study assessed the long-term safety and effectiveness of linagliptin in patients with type 2 diabetes and severe renal impairment. The study found that linagliptin significantly improved glycemic control, with a low risk of severe hypoglycemia and stable body weight.

Mechanism of Action of undefined

Linagliptin acts as an inhibitor of the DPP-4 enzyme, which degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, linagliptin increases the concentrations of active incretin hormones, thereby stimulating insulin release in a glucose-dependent manner and reducing glucagon levels in circulation. 

Both GLP-1 and GIP are integral to the physiological regulation of glucose homeostasis. They are secreted at low basal levels throughout the day, with their concentrations rising immediately following meal intake. These incretin hormones enhance insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 decreases glucagon secretion from pancreatic alpha cells, resulting in reduced hepatic glucose output.

Uses of undefined

Linagliptin helps manage type 2 diabetes mellitus by increasing the levels of incretin hormones. This action stimulates insulin secretion in response to meals and reduces glucagon secretion, effectively regulating blood sugar levels. Doctors prescribe it alongside diet and exercise, either alone or in combination with other diabetes medications.

undefined Drug administaration and Dosage available

The recommended dose of linagliptin is 5 mg, taken once daily. Patients can take the tablets with or without food. When used in combination with an insulin secretagogue, such as a sulfonylurea, a lower dose of the insulin secretagogue may be necessary to reduce the risk of hypoglycemia.

Warnings, Precautions and Side Effects of undefined

Warnings

Insulin secretagogues can cause hypoglycemia. Clinical trials show that combining linagliptin with an insulin secretagogue, such as a sulfonylurea, leads to a higher rate of hypoglycemia compared to a placebo. Therefore, healthcare providers may need to lower the dose of the insulin secretagogue to reduce the risk of hypoglycemia when prescribing linagliptin.

Precautions

  • Hypoglycaemia risk: Monitor patients for signs of low blood sugar, particularly when linagliptin is used alongside insulin secretagogues (e.g., sulfonylureas) or insulin. Adjust dosages accordingly to lower this risk.
  • Pancreatitis: Assess for symptoms of pancreatitis, as linagliptin may increase the risk. Discontinue treatment if pancreatitis is suspected.
  • Heart failure: Exercise caution in patients with a history of heart failure, as there may be an elevated risk of hospitalisation due to heart failure.
  • Renal impairment: Although linagliptin does not require dose adjustment for mild to moderate renal impairment, exercise caution in patients with severe renal impairment.
  • Allergic reactions: Monitor for signs of hypersensitivity, such as rash or angioedema, and discontinue use if these reactions occur.
  • Monitoring: Regularly monitor blood glucose levels to ensure effective control.
  • Pregnancy and nursing: Advise patients to discuss their situation with a healthcare provider if they are pregnant, planning to become pregnant, or breastfeeding, as the effects on fetal development or nursing infants are not fully established.

Side Effects

Common side effects of linagliptin include:

  • Stuffy or runny nose
  • Sore throat

Serious side effects of linagliptin may include:

Low blood sugar (hypoglycemia) may occur, particularly when used with sulfonylureas or insulin, which may require a dosage adjustment of those medications.

Signs and symptoms of low blood sugar include:

  • Headache
  • Drowsiness
  • Weakness
  • Dizziness
  • Confusion
  • Irritability
  • Hunger
  • Fast heartbeat
  • Sweating
  • Feeling nervous

Word Of Advice

Tell your doctor if you have a history of heart failure and regularly monitor your blood glucose levels to avoid hypoglycaemia while using linagliptin. Report any symptoms of low blood sugar, and make sure to inform your doctor about all other medications you are taking to prevent interactions. Use linagliptin during pregnancy only if necessary, and watch for allergic reactions—report any issues immediately.

Frequently Asked Question

References

  1. Janet B. McGill, Lance Sloan, Jennifer Newman, Sanjay Patel, Christophe Sauce, Maximilian von Eynatten, Hans-Juergen Woerle; Long-Term Efficacy and Safety of Linagliptin in Patients With Type 2 Diabetes and Severe Renal Impairment: A 1-year, randomised, double-blind, placebo-controlled study. Diabetes Care 1 February 2013; 36 (2): 237–244. https://doi.org/10.2337/dc12-0706
  2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201280lbl.pdf
  3. https://www.ema.europa.eu/en/documents/product-information/trajenta-epar-product-information_en.pdf
  4. https://medlineplus.gov/druginfo/meds/a611036.html

Disclaimer

The drug information on this page is not a substitute for medical advice, it is meant for educational purposes only. For further details consult your doctor about your medical condition to know if you are eligible to receive this treatment.