Sitagliptin

Antidiabetic Drug

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

Sitagliptin (JANUVIA)（中文：西格列汀）

Pronunciation

Sitagliptin 100mg (JANUVIA 100mg)

Common Strengths of Sitagliptin Tablet

Sitagliptin tablets are available in the following strengths:

• 25 mg, 50 mg, 100 mg tablets

Drug Trade Names of Sitagliptin Tablet

Januvia is the trade name for Sitagliptin

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

• JANUMET TABLET 50MG/1000MG: Sitagliptin 50mg + Metformin 1000mg
• JANUMET TABLET 50MG/500MG: Sitagliptin 50mg + Metformin 500mg
• JANUMET XR TABLET 100MG/1000MG : Sitagliptin 100mg + Metformin 1000mg
• JANUMET XR TABLET 50MG/1000MG: Sitagliptin 50mg + Metformin 1000mg
• JANUMET XR TABLET 50MG/500MG: Sitagliptin 50mg + Metformin 500mg
• STEGLUJAN TABLET 5MG/100MG: Ertugliflozin 5mg + Sitagliptin 100mg

Drug Usage

Treatment of type 2 diabetes mellitus.

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

• 100 mg once daily
• Hypertension/Heart failure: No specific dosage adjustments
• Diabetic kidney disease:
  • eGFR 45 - 90 mL/min/1.73 m²: No adjustment
  • eGFR 30 - 45 mL/min/1.73 m²: 50 mg once daily
  • eGFR <30 mL/min/1.73 m²: 25 mg once daily

Side Effects

Frequency	Adverse reactions
Common	Upper respiratory tract infection, headache
Uncommon	Dizziness, nausea, vomiting
	Pancreatitis
	Bullous pemphigoid
	Severe cutaneous adverse reactions

Pharmacokinetics

• Absorption
  • Rapid, 87% bioavailability. The drug reaches maximum plasma concentration in 1 to 4 hours after taking a dose.
• Metabolism
  • Limited metabolism, primarily by CYP3A4 and CYP2C8
• Elimination
  • 79% excreted unchanged in urine, half-life approximately 12 hours

Drug Precautions

Pregnancy

Limited data, use only if clearly needed

Breastfeeding

Not recommended

Children and Elderly

Not approved for children, use with caution in elderly

Renal Impairment

Dose adjustment required (see dosages)

Monitoring Requirements

• Renal function
• 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 enhance hypoglycemic effects of insulin or sulfonylureas

FAQ

How Should I Take the Tablet?

Once daily, with or without food

What Should I Avoid While Taking?

Alcohol, skipping meals

What Happens if I Miss a Dose?

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