Drug Guide
Saxagliptin Hydrochloride
Classification
Therapeutic: Antidiabetic agents, DPP-4 inhibitors
Pharmacological: Inhibitor of dipeptidyl peptidase-4 (DPP-4) enzyme
FDA Approved Indications
- Improvement of glycemic control in adults with type 2 diabetes mellitus
Mechanism of Action
Saxagliptin inhibits the DPP-4 enzyme, prolonging the activity of incretin hormones, which increase insulin synthesis and release from pancreatic beta cells and decrease glucagon levels, thereby lowering blood glucose levels.
Dosage and Administration
Adult: 5 mg once daily, with or without food
Pediatric: Not approved for pediatric use
Geriatric: Start at 5 mg daily; no specific adjustment required but monitor elderly patients closely
Renal Impairment: Adjust dose to 2.5 mg daily in moderate impairment (eGFR 30-59 mL/min); use not recommended in severe impairment or dialysis
Hepatic Impairment: No dosage adjustment needed
Pharmacokinetics
Absorption: Quick absorption with peak plasma concentrations at approximately 1-2 hours
Distribution: Moderate protein binding (~40-50%)
Metabolism: Primarily metabolized by CYP3A4/5 to an inactive metabolite
Excretion: Excreted mainly via the kidneys; minor fecal excretion
Half Life: 2.5 hours (approximate)
Contraindications
- Hypersensitivity to saxagliptin or any component
Precautions
- Use with caution in patients with history of pancreatitis; assess kidney function before initiation and periodically thereafter
Adverse Reactions - Common
- Infections (such as nasopharyngitis) (Common)
- Headache (Common)
Adverse Reactions - Serious
- Pancreatitis (Uncommon)
- Hypersensitivity reactions including anaphylaxis and angioedema (Rare)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole) may increase saxagliptin levels, adjust dose accordingly
Drug-Food Interactions
- No significant food interactions
Drug-Herb Interactions
- Limited data, caution advised with herbal supplements
Nursing Implications
Assessment: Monitor blood glucose levels regularly; assess for signs of pancreatitis including persistent severe abdominal pain
Diagnoses:
- Risk for unstable blood glucose levels
- Risk for pancreatitis
Implementation: Administer once daily at the same time each day; educate patient on recognizing symptoms of hypoglycemia and pancreatitis
Evaluation: Evaluate glycemic control and adherence; monitor for adverse effects
Patient/Family Teaching
- Take medication exactly as prescribed, once daily
- Report symptoms of pancreatitis such as severe abdominal pain, nausea, vomiting
- Maintain a balanced diet and monitor blood glucose levels regularly
- Inform healthcare provider of all medications and herbal supplements being taken
Special Considerations
Black Box Warnings:
- None specified for saxagliptin
Genetic Factors: No known genetic factors affecting efficacy or safety
Lab Test Interference: No significant interference reported
Overdose Management
Signs/Symptoms: Potential hypoglycemia or adverse effects from overdose
Treatment: Symptomatic and supportive care; hemodialysis may be considered as saxagliptin is renally excreted
Storage and Handling
Storage: Store at room temperature between 20°C and 25°C (68°F to 77°F); protect from moisture
Stability: Stable when stored properly; discard expired medication