Drug Guide
Sitagliptin Phosphate
Classification
Therapeutic: Antidiabetic agent
Pharmacological: Dipeptidyl peptidase-4 (DPP-4) inhibitor
FDA Approved Indications
- Improved glycemic control in adults with type 2 diabetes mellitus as monotherapy or in combination with other hypoglycemic agents
Mechanism of Action
Sitagliptin inhibits DPP-4 enzyme, prolonging the activity of incretin hormones (GLP-1 and GIP), which increase insulin production and decrease glucagon levels in response to meals.
Dosage and Administration
Adult: 100 mg once daily, with or without food
Pediatric: Not approved for use in pediatric patients
Geriatric: No dosage adjustment necessary, but renal function should be monitored
Renal Impairment: Dose adjustment recommended for moderate to severe renal impairment (eGFR<60 mL/min/1.73m²)
Hepatic Impairment: No dose adjustment necessary
Pharmacokinetics
Absorption: Rapidly absorbed with peak plasma levels in 1-4 hours
Distribution: Approximately 38% bound to plasma proteins
Metabolism: Minimal hepatic metabolism; mostly excreted unchanged
Excretion: Primarily via the kidneys (~79% as unchanged drug), small amount in feces
Half Life: 12.4 hours
Contraindications
- History of serious hypersensitivity to sitagliptin or any component
Precautions
- Renal impairment, pancreatitis, hypersensitivity reactions, potential for immune-mediated disorders
Adverse Reactions - Common
- Respiratory tract infection (Frequent)
- Headache (Frequent)
Adverse Reactions - Serious
- Pancreatitis (Uncommon)
- Hypersensitivity reactions, including anaphylaxis (Rare)
Drug-Drug Interactions
- Metformin (risk of lactic acidosis), insulins (risk of hypoglycemia)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood glucose, renal function, and for signs of pancreatitis
Diagnoses:
- Risk for unstable blood glucose levels
Implementation: Administer as prescribed; monitor for adverse effects and blood glucose response.
Evaluation: Assess blood glucose levels and patient adherence; monitor for adverse reactions.
Patient/Family Teaching
- Take medication as prescribed, with or without food
- Report symptoms of pancreatitis (severe abdominal pain, nausea, vomiting)
- Maintain regular blood glucose monitoring
- Avoid sudden discontinuation without medical advice
Special Considerations
Black Box Warnings:
- None specifically for sitagliptin
Genetic Factors: Genetic variations in DPP-4 or incretin pathways may affect response
Lab Test Interference: May affect hematology and renal function tests
Overdose Management
Signs/Symptoms: Hypoglycemia, gastrointestinal symptoms
Treatment: Supportive care; monitor blood glucose levels; administer carbohydrate if needed; no specific antidote.
Storage and Handling
Storage: Store at room temperature, 20-25°C (68-77°F)
Stability: Stable up to the expiration date on the package