Linagliptin (Rx)

Linagliptin Brand name: Tradjenta

Dea Class: Rx (Prescription drug)

Drug Class: Antidiabetics, Dipeptyl Peptidase-IV Inhibitors

Dosage form: Tablet 5mg

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What is Linagliptin and how does it work?

Linagliptin is oral DPP-4 inhibitor given once daily; reduces breakdown of GLP-1 which increases insulin secretion

Used in adults with type 2 diabetes mellitus; mean A1C reduction 0.7%

Used as monotherapy or in combination with other medications, with the exception of GLP-1 agonists


What are Linagliptin uses?

Linagliptin is used for adults with type 2 diabetes mellitus along with diet and exercise to lower blood sugar; may be used as monotherapy or in combination with other common antidiabetic medications including metformin, sulfonylurea, pioglitazone, or insulin


How should I take Linagliptin?

Linagliptin comes as a tablet to take by mouth. It is usually taken once a day with or without food. Take it at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take linagliptin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Linagliptin helps to control high blood sugar but does not cure diabetes. Continue to take linagliptin even if you feel well. Do not stop taking it without talking to your doctor.

Your doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with Tradjenta and each time you refill your prescription.


Linagliptin Side Effects

Nasopharyngitis (4.3%)

Hyperlipidemia (2.8%; with pioglitazone)

Cough (2.4%; with metformin and sulfonylurea)

Hypertriglyceridemia (2.4%; with sulfonylurea)

Weight gain (2.3%; with pioglitazone)

Hypoglycemia

  • 7.6% overall incidence
  • 22.9% incidence compared with placebo plus metformin and a sulfonylurea
  • Incidence similar to placebo with monotherapy or combined with metformin or pioglitazone

Acute pancreatitis, including fatal pancreatitis

Hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions

Severe and disabling arthralgia

Bullous pemphigoid

Rash

Mouth ulceration, stomatitis

Rhabdomyolysis

Heart failure

Hypoglycemia with concomitant use of insulin and insulin secretagogues


What Are Warnings and Precautions for Linagliptin?

Warnings

Use in combination with an insulin secretagogue (eg, sulfonylurea) was associated with a higher rate of hypoglycemia compared with placebo in a clinical trial; a lower dose of insulin secretagogue or insulin may be required to reduce risk of hypoglycemia when used in combination with this drug

Rifampin decreased Tradjenta 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 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 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

Before taking Linagliptin, Cautions

Hypersensitivity (eg, anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity)

Type 1 diabetes mellitus

Diabetic ketoacidosis

Pregnancy and Lactation

Pregnancy

  • 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

Lactation

  • There is no information regarding presence of drug in human milk, the effects on breastfed infant, or effects on milk production

What Are Dosages of Linagliptin?

Dosage Forms & Strengths

Tablet 5mg

Adults

5 mg/day PO.

Geriatric

5 mg/day PO.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Infants

Not indicated.


Linagliptin brand name

Brand name: Tradjenta Tablet 5mg


Brand names of Linagliptin combination products

  • Trijardy® (as a combination product containing Empagliflozin, Linagliptin, Metformin)
  • Glyxambi® (containing Linagliptin, Empagliflozin)
  • Jentadueto® (containing Linagliptin, Metformin)
  • (containing Empagliflozin, Linagliptin, Metformin)

 

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