Dosage |
100 mg once daily |
5 mg once daily |
50 mg twice daily |
5 mg once daily |
25 mg once daily |
Approximate half-life (h) |
12 |
2 |
3 |
>120 |
21 |
Elimination |
Metabolism is a minor pathway; primarily eliminated unchanged in urine (75%) |
Elimination by metabolism (cytochrome P450 3A4/5) and renal clearance (24%) |
Elimination by metabolism (not CYP450 enzymes) and renal clearance (23%) |
Enterohepatic; eliminated unchanged in feces via biliary excretion (85%) |
Metabolism is a minor pathway; primarily eliminated unchanged in urine (63%) |
Effect on weight |
Weight neutral |
Weight neutral |
Weight neutral |
Weight neutral |
Weight neutral |
HbA1c reduction (monotherapy) |
Clinically important; up to −0.8% |
Clinically important; up to −0.8% |
Clinically important; up to −0.8% |
Clinically important; up to −0.8% |
Clinically important; up to −0.8% |
Use in CKD |
Reduce dose to 50 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); reduce dose to 25 mg/day for severe CKD (CrCl <30 mL/min); assess renal function before use and on a regular basis |
Reduce dose to 2.5 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); give reduced dose after dialysis in chronic renal failure |
Reduce dose to 50 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min) and severe CKD (CrCl <30 mL/min) |
No dosage reduction required |
Reduce dose to 12.5 mg/day for moderate CKD (CrCl ≥30 to ≤50 mL/min); reduce dose to 6.25 mg/day for severe CKD (CrCl <30 mL/min) |
Adverse events |
Low |
Low |
Low |
Low |
Low |