LINAGLIPTIN

Background and Date of Approval

Linagliptin received approval from the United States Food and Drug Administration (FDA) on May 2, 2011. A 2013 randomised, double-blind, placebo-controlled study evaluated the long-term safety and efficacy of linagliptin in patients with type 2 diabetes and severe renal impairment. The study demonstrated that linagliptin produced significant improvement in glycemic control, with a low incidence of severe hypoglycaemia and stable body weight.

Uses

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.

How is it administered?

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.

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

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.

Word of Advice

Inform your doctor if you have a history of heart failure. Monitor blood glucose levels regularly to prevent hypoglycaemia while taking linagliptin. Report any symptoms of low blood sugar to your doctor. Disclose all other medications you are currently taking to your doctor to avoid potential interactions. Use linagliptin during pregnancy only when necessary. Watch for signs of allergic reactions and report any adverse effects to your doctor immediately.

References

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 https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201280lbl.pdf https://www.ema.europa.eu/en/documents/product-information/trajenta-epar-product-information_en.pdf https://medlineplus.gov/druginfo/meds/a611036.html

Frequently Asked Questions

Is linagliptin the same as metformin?

No, linagliptin and metformin are not the same. Linagliptin is a DPP-4 inhibitor that helps increase insulin secretion, while metformin is a biguanide that primarily reduces glucose production in the liver. Both medications are used to manage type 2 diabetes but work through different mechanisms.

Who should not take linagliptin?

Avoid linagliptin if you have a history of severe allergic reactions to it or any DPP-4 inhibitors. It is also not recommended for patients with severe renal impairment. Always consult your doctor before starting.

Is linagliptin safe for kidneys?

Linagliptin is usually safe for mild to moderate kidney impairment and doesn’t require dose adjustments. However, use caution in patients with severe kidney issues. Always consult your healthcare provider for personalised advice.

When to stop taking linagliptin?

Stop taking linagliptin if you experience severe allergic reactions, symptoms of pancreatitis, or persistent low blood sugar. Consult your doctor immediately if any of these occur.

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Written By: Muskan Patel, M.Pharm

Reviewed By: Dr. Vishwa Patel, MBBS