Version June 2024
| DPP-4 inhibitor | Dosing (adult) | |||
| Single agent oral formulations | Combined oral formulations* | |||
| Normal kidney function | Impaired kidney function | Normal kidney function | Impaired kidney function | |
| Alogliptin | 25 mg once daily | CrCl 30 to 60 mL/min: 12.5 mg once daily CrCl <30 mL/min or dialysis: 6.25 mg once daily | Alogliptin-metformin (taken twice daily): 12.5 mg/500 mg, Alogliptin-pioglitazone (taken once daily): 12.5 mg/30 mg, | Alogliptin-metformin: eGFR 30 to 60 mL/min/1.73 m2: Use is not recommended. eGFR <30 mL/min/1.73 m2: Use is contraindicated. Alogliptin-pioglitazone: CrCl 30 to <60 mL/min: Do not exceed 12.5 mg alogliptin component daily. CrCl <30 mL/min or dialysis: Use is not recommended. Appropriately adjusted dose of individual components may be considered. |
| Linagliptin¶ | 5 mg once daily | No dose adjustment needed | Linagliptin-metformin (taken twice daily with meals): 2.5 mg/500 mg, Linagliptin-metformin ER (taken once daily): 2.5 mg/1000 mg, Empagliflozin-linagliptin (taken once daily): 10 mg/5 mg, Empagliflozin-linagliptin-metformin ER (taken once daily): 5 mg/2.5 mg/1000 mg, | Linagliptin-metformin: eGFR 30 to 45 mL/min/1.73 m2: Initiation of therapy is not recommended. If existing therapy is continued, a 50% reduction of the metformin dose (maximum 1 g/day) with close monitoring is recommended. eGFR <30 mL/min/1.73 m2: Use is contraindicated. Empagliflozin-linagliptin: eGFR <30 mL/min/1.73 m2: Use is not recommended. Dialysis: Use is contraindicated. Empagliflozin-linagliptin-metformin: eGFR 30 to <45 mL/min/1.73 m2: Use is not recommended. Appropriately adjusted dose of individual components may be considered. eGFR <30 mL/min/1.73 m2 or dialysis: Use is contraindicated. |
| SaxagliptinΔ | 2.5 or 5 mg once daily | eGFR <45 mL/min/1.73 m2 or dialysis: 2.5 mg once daily | Saxagliptin-metformin (Canada only; taken twice daily with meals): 2.5 mg/500 mg, Saxagliptin-metformin ER (United States only; taken once daily): 2.5 mg/1000 mg, Dapagliflozin-saxagliptin: 5 mg/5 mg, | Saxagliptin-metformin: eGFR 30 to 45 mL/min/1.73 m2: Initiation of therapy is not recommended. If existing therapy is continued, do not exceed 2.5 mg saxagliptin component daily. A 50% reduction of the metformin dose (maximum 1 g/day) with close monitoring is recommended. eGFR <30 mL/min/1.73 m2 or dialysis: Use is contraindicated. Dapagliflozin-saxagliptin: eGFR <45 mL/min/1.73 m2 or dialysis: Use is contraindicated. |
| Sitagliptin | 100 mg once daily | eGFR 30 to <45 mL/min/1.73 m2: 50 mg once daily eGFR <30 mL/min/1.73 m2 or dialysis: 25 mg once daily | Sitagliptin-metformin (taken twice daily with meals): 50 mg/500 mg, Sitagliptin-metformin ER (taken once daily): 50 mg/500 mg, Ertugliflozin-sitagliptin (United States only; taken once daily): 5 mg/100 mg, | Sitagliptin-metformin: eGFR 30 to 45 mL/min/1.73 m2: Initiation of therapy is not recommended. If existing therapy is continued, do not exceed 50 mg sitagliptin component daily. A 50% reduction of the metformin dose (maximum 1 g/day) with close monitoring is recommended. eGFR <30 mL/min/1.73 m2: Use is contraindicated. Ertugliflozin-sitagliptin: eGFR 30 to <45 mL/min/1.73 m2: Use is not recommended. eGFR <30 mL/min 1.73 m2 or dialysis: Use is contraindicated. |
| Vildagliptin◊ | Monotherapy or in combination with metformin or a thiazolidinedione: 50 mg twice daily Dual therapy with a sulfonylurea (eg, without metformin): 50 mg once daily | CrCl <50 mL/min: 50 mg once daily | Vildagliptin-metformin (Canada only; taken twice daily): 50 mg/850 mg, | Vildagliptin-metformin: eGFR <50 mL/min/1.73 m2: Do not use combined formulation. Appropriately adjusted dose of individual components may be considered. |
CrCl: creatinine clearance; eGFR: estimated glomerular filtration rate; ER: extended release; SGLT2: sodium-glucose cotransporter 2.
* In general, the initial dose of a combined formulation is selected based on current daily dose for individual components in patients currently maintained on both agents separately. For patients who currently use one of the components and require additional glucose lowering, a starting dose of the second agent should be used. Combined formulations available in the United States and Canada are shown.
¶ Linagliptin should not be used in patients taking strong inducers of cytochrome P450 3A4 or P-glycoprotein. Lists of CYP3A4 and P-glycoprotein inducers are provided in separate tables within UpToDate.
Δ For patients taking strong cytochrome P450 3A4/5 inhibitors, the 2.5 mg dose of saxagliptin is recommended. A list of strong CYP3A4/5 inhibitors is provided in a separate table within UpToDate.
◊ Vildagliptin is available in many countries and regions including Japan, Europe, India, and Latin America, but not in the United States.آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
