From the Guidelines
Saxagliptin should be prescribed with caution in adults with type 2 diabetes, considering its potential increased risk of heart failure hospitalization, and the recommended dose is 2.5 mg or 5 mg once daily, with the 5 mg dose being standard for most patients, as indicated by the most recent study 1.
Key Considerations
- The Saxagliptin Assessment of Vascular Outcomes Recorded in Patients with Diabetes Mellitus – Thrombolysis in Myocardial Infarction 53 (SAVOR-TIMI 53) study showed that patients treated with saxagliptin were more likely to be hospitalized for heart failure than those given placebo 1.
- However, other cardiovascular outcomes trials did not find a significant increase in risk of heart failure hospitalization with DPP-4 inhibitor use compared with placebo 1.
- The dose of saxagliptin should be adjusted in patients with moderate to severe kidney impairment, with a maximum dose of 2.5 mg daily recommended for patients with an eGFR <15 mL/min/1.73 m2, as indicated by the consensus report 1.
Dosage and Administration
- The recommended dose of saxagliptin is 2.5 mg or 5 mg once daily, with the 5 mg dose being standard for most patients.
- The lower 2.5 mg dose is recommended for patients with moderate to severe kidney impairment or those taking strong CYP3A4/5 inhibitors like ketoconazole.
- Saxagliptin can be taken with or without food at any time of day, and no dose adjustment is needed based on meals.
Safety and Efficacy
- Saxagliptin works by inhibiting the DPP-4 enzyme, which prolongs the action of incretin hormones that stimulate insulin release and reduce glucagon secretion, ultimately lowering blood glucose levels.
- Common side effects include upper respiratory tract infections, urinary tract infections, and headache, while hypoglycemia risk is low when used alone but increases when combined with insulin or sulfonylureas.
- Saxagliptin may be used as monotherapy when metformin is contraindicated or not tolerated, but is more commonly prescribed as an add-on therapy to metformin or other antidiabetic medications when additional glycemic control is needed.
From the FDA Drug Label
Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Recommended dosage is 2.5 mg or 5 mg orally once daily taken regardless of meals. Patients with an eGFR <45 mL/min/1.73 m2 (moderate or severe renal impairment, or end-stage renal disease): Recommended dosage is 2.5 mg once daily regardless of meals. Limit the dosage of saxagliptin tablets to 2.5 mg daily for patients also taking strong cytochrome P450 3A4/5 (CYP3A4/5) inhibitors (e.g., ketoconazole).
The recommended use of Saxagliptin in adults with type 2 diabetes is as an adjunct to diet and exercise to improve glycemic control. The recommended dosage is 2.5 mg or 5 mg orally once daily, taken regardless of meals. However, for patients with:
- Moderate or severe renal impairment, or end-stage renal disease, the recommended dosage is 2.5 mg once daily.
- Concomitant use of strong CYP3A4/5 inhibitors, the dosage should be limited to 2.5 mg daily 2 2.
From the Research
Recommended Use of Saxagliptin
- Saxagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus 3, 4.
- It can be used alone or in combination with other oral antidiabetic medications, such as metformin, a sulfonylurea, or a thiazolidinedione 3, 4.
Dosage of Saxagliptin
- The recommended dosage of saxagliptin is 2.5 mg or 5 mg once daily 4.
- For patients with moderate or severe renal impairment or end-stage renal disease, or patients taking a strong inhibitor of cytochrome P-450 isoenzyme 3A4 or 3A5, the recommended dosage is 2.5 mg once daily 4.
Efficacy and Safety of Saxagliptin
- Saxagliptin has been shown to improve glycemic control, as reflected by significant decreases in glycated hemoglobin, fasting plasma glucose, and postprandial glucose levels compared with controls 3, 4, 5.
- It is generally well tolerated, with a low incidence of hypoglycemia and weight-neutral effects 3, 4, 5.
- Saxagliptin has been found to have clinically neutral effects on body weight, blood pressure, lipid levels, and other markers of cardiovascular risk compared with controls 5.