Comparative Pharmacology
Head-to-head clinical analysis: DAPAGLIFLOZIN versus INVOKAMET XR.
Head-to-head clinical analysis: DAPAGLIFLOZIN versus INVOKAMET XR.
DAPAGLIFLOZIN vs INVOKAMET XR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective inhibitor of sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubule, reducing renal glucose reabsorption and lowering blood glucose.
Combination of canagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, which reduces renal glucose reabsorption and lowers blood glucose, and metformin, an activator of AMP-activated protein kinase (AMPK) that decreases hepatic glucose production and improves insulin sensitivity.
10 mg orally once daily.
Maximum daily dose: canagliflozin 300 mg/metformin ER 2000 mg orally once daily with the morning meal. Initial dose: canagliflozin 50 mg/metformin ER 500 mg orally twice daily or canagliflozin 150 mg/metformin ER 1000 mg orally once daily; for patients not currently on metformin, start with canagliflozin 50 mg/metformin ER 500 mg orally twice daily; for patients on metformin, switch to INVOKAMET XR based on current metformin dose.
None Documented
None Documented
Clinical Note
moderateDapagliflozin + Gatifloxacin
"Dapagliflozin may increase the hypoglycemic activities of Gatifloxacin."
Clinical Note
moderateDapagliflozin + Rosoxacin
"Dapagliflozin may increase the hypoglycemic activities of Rosoxacin."
Clinical Note
moderateDapagliflozin + Levofloxacin
"Dapagliflozin may increase the hypoglycemic activities of Levofloxacin."
Clinical Note
moderateDapagliflozin + Trovafloxacin
"Dapagliflozin may increase the hypoglycemic activities of Trovafloxacin."
Terminal elimination half-life is approximately 12.9 hours (range 10-16 hours) for dapagliflozin, supporting once-daily dosing. At steady state, effective half-life is ~23 hours due to metabolite.
Canagliflozin: mean terminal elimination half-life is 13.1 hours (range 11-16 hours) for the 300 mg dose, consistent with once-daily dosing. Metformin: terminal elimination half-life is approximately 6.2 hours (range 4-9 hours) in patients with normal renal function; prolonged in renal impairment.
Primarily renal and fecal: ~75% of dose excreted in urine (as unchanged dapagliflozin and glucuronide conjugates), ~21% in feces. Biliary elimination is negligible.
Canagliflozin is primarily excreted as unchanged drug in urine (approximately 33%) and feces (approximately 41%), with about 7% as metabolites in urine and 34% as metabolites in feces. Metformin is excreted unchanged in urine (90-100% of absorbed dose) via tubular secretion and glomerular filtration.
Category C
Category C
SGLT2 Inhibitor
SGLT2 Inhibitor / Biguanide Combination