Generic Name

Sitagliptin

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Classification

FDA Approved Indications

• Type 2 diabetes mellitus as an adjunct to diet and exercise

Mechanism of Action

Inhibits dipeptidyl peptidase-4 enzyme, prolonging the action of incretin hormones, which increases insulin secretion and decreases glucagon levels in a glucose-dependent manner.

Dosage and Administration

Adult: 100 mg once daily, with or without food

Pediatric: Not approved for pediatric use

Geriatric: Start at usual dose, consider renal function in dose adjustments

Renal Impairment: Dose adjustment is recommended based on renal function; eGFR < 45 mL/min/1.73 m²: 50 mg daily; eGFR < 30 mL/min/1.73 m²: 25 mg daily

Hepatic Impairment: No dose adjustment necessary

Pharmacokinetics

Absorption: Rapidly absorbed, bioavailability approximately 87%

Distribution: Vd approximately 0.1 L/kg, primarily free drug in plasma

Metabolism: Minimal hepatic metabolism, primarily excreted unchanged

Excretion: Renal excretion (about 80%) and some fecal elimination

Half Life: ≈12.4 hours

Contraindications

• History of hypersensitivity to sitagliptin or any component of the formulation

Precautions

• Renal impairment, risk of pancreatitis, hypersensitivity reactions, severe gastrointestinal disease, monitor for signs of hypersensitivity or pancreatitis

Adverse Reactions - Common

• Nasopharyngitis (Common)
• Headache (Common)
• Gastrointestinal discomfort (Common)

Adverse Reactions - Serious

• Pancreatitis (Serious)
• Hypersensitivity reactions (including anaphylaxis, angioedema) (Serious)
• Severe cutaneous adverse reactions (e.g., Stevens-Johnson syndrome) (Rare)

Drug-Drug Interactions

• Insulin and sulfonylureas: increased risk of hypoglycemia when used concomitantly

Drug-Food Interactions

• None specifically noted

Drug-Herb Interactions

• None well-characterized, caution with herbal supplements

Nursing Implications

Patient/Family Teaching

• Take medication as prescribed, monitor blood glucose levels, recognize symptoms of hypoglycemia and pancreatitis, report any allergic or severe skin reactions

Special Considerations

Black Box Warnings:

• Risk of severe joint pain, pancreatitis

Genetic Factors: None significant for this drug

Lab Test Interference: None known

Overdose Management

Signs/Symptoms: Hypoglycemia, nausea, vomiting, pancreatitis symptoms

Treatment: Supportive care, monitor blood glucose, no specific antidote; for hypoglycemia, administer glucose as needed

Storage and Handling

Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F)

Stability: Stable as per manufacturer instructions, typically 24 months