From the Guidelines
The recommended starting dose for DPP-4 inhibitors, such as sitagliptin, in patients with impaired renal function should be adjusted based on the patient's eGFR level, with sitagliptin doses reduced to 50 mg daily for moderate renal impairment (eGFR 30-44 mL/min/1.73m²) and 25 mg daily for severe renal impairment (eGFR 15-29 mL/min/1.73m²) or end-stage renal disease requiring dialysis (eGFR <15 mL/min/1.73m²) 1.
Key Considerations for DPP-4 Inhibitors in Renal Impairment
- Dose adjustments are crucial to prevent drug accumulation and potential adverse effects in patients with impaired renal function.
- The dose of sitagliptin should be reduced to 50 mg once daily for patients with moderate renal impairment (eGFR 30-44 mL/min/1.73m²) and to 25 mg once daily for those with severe renal impairment (eGFR 15-29 mL/min/1.73m²) or end-stage renal disease requiring dialysis (eGFR <15 mL/min/1.73m²) 1.
- Other DPP-4 inhibitors, such as linagliptin, do not require dose adjustments in renal impairment, while saxagliptin and alogliptin require dose reductions based on eGFR levels 1.
Dose Adjustments for Specific DPP-4 Inhibitors
- Sitagliptin:
- Moderate renal impairment (eGFR 30-44 mL/min/1.73m²): 50 mg daily
- Severe renal impairment (eGFR 15-29 mL/min/1.73m²) or end-stage renal disease requiring dialysis (eGFR <15 mL/min/1.73m²): 25 mg daily
- Saxagliptin:
- eGFR ≤50 mL/min/1.73m²: 2.5 mg daily
- Alogliptin:
- eGFR 30-60 mL/min/1.73m²: 12.5 mg daily
- eGFR <30 mL/min/1.73m²: 6.25 mg daily
- Linagliptin: No dose adjustment required regardless of renal function 1.
From the FDA Drug Label
The recommended dosage of saxagliptin tablets is 2.5 mg or 5 mg orally once daily taken regardless of meals. The dosage of saxagliptin tablets is 2.5 mg orally once daily for patients with eGFR <45 mL/min/1.73 m2 [which includes a subset of moderate or severe renal impairment, or with end-stage renal disease (ESRD) requiring hemodialysis]
The recommended starting dose for DPP-4 inhibitors, such as saxagliptin, in patients with impaired renal function is:
- 2.5 mg orally once daily for patients with eGFR <45 mL/min/1.73 m2 (moderate or severe renal impairment, or end-stage renal disease) 2, 2, 2
- 2.5 mg or 5 mg orally once daily for patients with normal renal function or eGFR ≥45 mL/min/1.73 m2 2, 2, 2
From the Research
DPP-4 Inhibitors and Renal Function
- DPP-4 inhibitors, such as sitagliptin, are a class of oral antidiabetic drugs that improve glycaemic control without causing weight gain or increasing hypoglycaemic risk in patients with type 2 diabetes mellitus (T2DM) 3.
- The safety and efficacy of DPP-4 inhibitors as monotherapy or in combination with other oral antidiabetic agents or basal insulin are well established, including in patients with chronic renal impairment 4.
Starting Dose for Patients with Impaired Renal Function
- The recommended starting dose for sitagliptin, a DPP-4 inhibitor, is not explicitly stated in the provided studies, but it is known that sitagliptin is primarily excreted unchanged in the urine 5.
- For patients with impaired renal function, the dose of sitagliptin may need to be adjusted, but the exact starting dose is not specified in the provided studies.
- However, it is known that sitagliptin is effective and safe in patients with mild, moderate, and severe renal failure, improving glycemic control with low risk of hypoglycemia 4.
Pharmacokinetics of DPP-4 Inhibitors
- DPP-4 inhibitors, including sitagliptin, have different pharmacokinetic properties, such as oral bioavailability, elimination half-life, and metabolic pathways 6.
- Sitagliptin is 87% orally bioavailable, undergoes minimal hepatic metabolism, and is primarily excreted unchanged in the urine 5.
- The pharmacokinetic properties of DPP-4 inhibitors may influence the starting dose and dose adjustment for patients with impaired renal function, but more information is needed to determine the optimal starting dose.