糖尿病 (DPP4I) Type 2 diabetes mellitus.

Antidiabetic Agent, Dipeptidyl Peptidase 4 (DPP-4) Inhibitor
Saxagliptin inhibits DPP-4 enzyme resulting in prolonged active incretin levels. Incretin hormones (eg, GLP1, glucose-dependent insulinotropic polypeptide) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decreased glucagon secretion results in decreased hepatic glucose production.

Metabolism:
1. Hepatic: primarily via CYP450 3A4/5 enzyme subsystems
2. Elimination Half Life: 2.5 hr
Excretion:
Renal: 60% (24% unchanged)

Hypersensitivity reaction to saxagliptin (eg, anaphylaxis, angioedema, or exfoliative skin conditions)

B (FDA)

Infant risk cannot be ruled out

1. Common: Peripheral edema, Hypoglycemia, Headache, Urinary tract infectious disease, Upper respiratory infection
2. Serious: Heart failure, Hypersensitivity reaction, Tuberculosis, Arthralgia, Fracture of bone

2.5 mg or 5 mg orally once daily with or without food

Safety and effectiveness have not been established in pediatric patients.

1. eGFR ≥45 mL/minute/1.73 m2: No dosage adjustment necessary
2. eGFR <45 mL/minute/1.73 m2: 2.5 mg once daily
3. ESRD requiring hemodialysis: 2.5 mg once daily; administer postdialysis
4. Peritoneal dialysis: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Mild to severe impairment: No dosage adjustment necessary.