Linagliptin

Antidiabetic Drug

Drug class: Dipeptidyl peptidase-4 (DPP-4) inhibitor

Linagliptin (TRAJENTA)（中文：利格列汀）

Common Strengths of Linagliptin Tablet

Linagliptin tablets are available in the following strengths:

• 5 mg tablets

Drug Trade Names of Linagliptin Tablet

Trajenta is the trade name for Linagliptin.

It is also sold under various brand names when combined with other antidiabetic medications, such as:

• GLYXAMBI TABLET 10MG/5MG: Empagliflozin 10mg + Linagliptin 5mg
• GLYXAMBI TABLET 25MG/5MG: Empagliflozin 25mg + Linagliptin 5mg
• TRAJENTA DUO TABLET 2.5/1000MG: Linagliptin 2.5mg + Metformin 1000mg
• TRAJENTA DUO TABLET 2.5/850MG: Linagliptin 2.5mg + Metformin 850mg
• TRAJENTA DUO TABLET 2.5/500MG: Linagliptin 2.5mg + Metformin 500mg

Drug Usage

Treatment of type 2 diabetes mellitus in adults, as an adjunct to diet and exercise.

Mechanism of Action

Inhibits DPP-4 enzyme, increasing levels of incretin hormones (GLP-1 and GIP) which stimulate insulin release and decrease glucagon secretion, thereby lowering blood glucose.

Route of Administration

Oral

Dosages

• 5 mg once daily
• No dose adjustment needed for hypertension, heart failure or diabetic kidney disease

Side Effects

Frequency	Adverse reactions
Common	Upper respiratory tract infection
	Nasopharyngitis
	Headache
Uncommon	Hypoglycemia
	Cough
	Rash
	Pancreatitis
	Angioedema
	Stevens-Johnson syndrome

Pharmacokinetics

• Absorption
  • Rapidly absorbed, 30% bioavailable. Maximum inhibition of DPP-4 activity is seen 30 minutes after a linagliptin dose
• Distribution
  • 75 - 99% protein bound
• Metabolism
  • Minimal metabolism
• Elimination
  • Primarily excreted unchanged in feces (80%) and urine (5%), half-life ~12 hours

Linagliptin begins to work within 30 - 60 minutes of administration, with peak effects occurring around 1.5 - 2 hours after taking the dose. Linagliptin provides >80% inhibition of DPP-4 up to 24 hours.

Drug Precautions

Pregnancy

Not recommended, limited data available

Breastfeeding

Not recommended

Children and Elderly

• Children: Safety and efficacy not established in <18 years
• Elderly: No dose adjustment required based on age

Renal Impairment

No dose adjustment required

Monitoring Requirements

• Blood glucose
• HbA1c
• Signs of pancreatitis

The main symptoms of pancreatitis include:

• Severe abdominal pain, typically in the upper abdomen, that may:
  • Feel worse after eating
  • Be sudden and intense in acute cases
• Nausea and vomiting
• Fever
• Rapid pulse/heart rate

Drug interactions

May increase risk of hypoglycemia when used with insulin or sulfonylureas

FAQ

How Should I Take the Tablet?

Take 5 mg once daily with or without food

What Should I Avoid While Taking?

Alcohol (may increase risk of hypoglycemia)

What Happens if I Miss a Dose?

Take as soon as remembered unless close to next dose, do not double dose