Reviewed on 1/14/2022

What Is Linagliptin and How Does It Work?

Linagliptin is a prescription medication used to treat Type 2 Diabetes Mellitus.

  • Linagliptin is available under the following different brand names: Tradjenta.

What Are Dosages of Linagliptin?

Adult dosage


  • 5mg 

Type 2 Diabetes Mellitus

  • 5 mg orally once daily

Dosage Considerations – Should be Given as Follows: 

  • See “Dosages”.

What Are Side Effects Associated with Using Linagliptin?

Common side effects of Linagliptin include:

Serious side effects of Linagliptin include:

  • hives, 
  • rash, 
  • itching, 
  • peeling skin, 
  • difficulty breathing, 
  • swelling in the face or throat, 
  • fever, 
  • sore throat, 
  • burning eyes,  
  • red or purple skin rash with blistering and peeling, 
  • severe pain in the upper stomach spreading to the back, with or without vomiting (pancreatitis), 
  • severe or ongoing pain in the joints, 
  • blisters,
  • breakdown of the outer layer of skin, 
  • shortness of breath, 
  • swelling in legs or feet, and 
  • rapid weight gain

Rare side effects of Linagliptin include:

  • none 
This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

What Other Drugs Interact with Linagliptin?

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

  • Linagliptin has severe interactions with no other drugs.
  • Linagliptin has serious interactions with at least 16 other drugs.
  • Linagliptin has moderate interactions with at least 92 other drugs.
  • Linagliptin has minor interactions with the following drugs:
    • ribociclib

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

What Are Warnings and Precautions for Linagliptin?


Effects of drug abuse

  • None

Short-Term Effects

  • See “What Are Side Effects Associated with Using Linagliptin?”

Long-Term Effects

  • See “What Are Side Effects Associated with Using Linagliptin?”


  • Use in combination with an insulin secretagogue (eg, sulfonylurea) was associated with a higher rate of hypoglycemia compared with placebo in a clinical trial
  • Rifampin decreased linagliptin exposure suggesting that the levels may be reduced when administered in combination with a strong P-gp or CYP 3A4 inducer; alternative treatment is strongly recommended when linagliptin is to be administered with P-gp or CYP 3A4 inducers
  • Serious hypersensitivity reactions were reported including anaphylaxis, angioedema, and exfoliative skin conditions
  • Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate
  • Heart failure has been observed with two other members of the DPP-4 inhibitor class; consider risks and benefits of empagliflozin in patients with risk factors for heart failure; monitor for signs and symptoms; if heart failure develops, manage accordingly to the standard of care and consider interrupting treatment
  • Bullous pemphigoid reported with DPP-4 inhibitor use, which required hospitalization; in reported cases, patients recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor; patients should report development blisters/erosions; discontinue DPP-4 therapy and consult a dermatologist if bullous pemphigoid suspected
  • There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with therapy


  • Post-marketing reports of acute pancreatitis, including fatal pancreatitis; monitor for signs and symptoms of pancreatitis, and discontinue if suspected
  • Unknown if patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using linagliptin

Drug interaction overview

  • Strong CYP3A4 or P-gp inducers may decrease linagliptin systemic exposure
  • Avoid coadministration with strong CYP3A4 or P-gp inducers; alternant drug strongly recommended to maintain linagliptin efficacy

Pregnancy and Lactation

  • The limited data in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy
  • In animal reproduction studies, no adverse developmental effects were observed when linagliptin was administered to pregnant rats during the period of organogenesis at doses similar to the maximum recommended clinical dose, based on exposure
  • Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, and delivery complications; poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth, and macrosomia related morbidity
  • There is no information regarding the presence of linagliptin in human milk, the effects on the breastfed infant, or effects on milk production; however, linagliptin is present in rat milk; developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or underlying maternal condition
Medscape. Linagliptin.

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