Comparative Pharmacology
Head-to-head clinical analysis: AVANDAMET versus ROSIGLITAZONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AVANDAMET versus ROSIGLITAZONE.
AVANDAMET vs ROSIGLITAZONE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
AVANDAMET combines rosiglitazone, a thiazolidinedione that improves insulin sensitivity by activating peroxisome proliferator-activated receptor gamma (PPARγ), and metformin, a biguanide that decreases hepatic glucose production, reduces intestinal glucose absorption, and improves insulin sensitivity.
Selective agonist at peroxisome proliferator-activated receptor gamma (PPARγ), enhancing insulin sensitivity by increasing glucose uptake and storage, reducing hepatic glucose production, and improving lipid metabolism.
Oral, initial dose of rosiglitazone 4 mg/metformin 500 mg twice daily or rosiglitazone 2 mg/metformin 500 mg twice daily; maximum recommended dose rosiglitazone 8 mg/metformin 2000 mg per day.
4-8 mg orally once daily or divided twice daily; maximum 8 mg/day.
None Documented
None Documented
Clinical Note
moderateRosiglitazone + Gatifloxacin
"Rosiglitazone may increase the hypoglycemic activities of Gatifloxacin."
Clinical Note
moderateRosiglitazone + Rosoxacin
"Rosiglitazone may increase the hypoglycemic activities of Rosoxacin."
Clinical Note
moderateRosiglitazone + Levofloxacin
"Rosiglitazone may increase the hypoglycemic activities of Levofloxacin."
Clinical Note
moderateRosiglitazone + Trovafloxacin
"Rosiglitazone may increase the hypoglycemic activities of Trovafloxacin."
Rosiglitazone: 3-4 hours (terminal); metformin: 6.2 hours (terminal). No accumulation with normal renal function.
Terminal elimination half-life is 3-4 hours. Clinically, this short half-life allows twice-daily dosing; steady-state is achieved within 2 days.
Renal (90-95% as unchanged drug for rosiglitazone; metformin is 90% renally eliminated unchanged). Biliary/fecal: minor (<5% for both).
Primarily hepatic metabolism via CYP2C8; negligible renal excretion. Approximately 64% of dose excreted in urine (as metabolites) and 23% in feces over 96 hours. Less than 0.2% excreted unchanged in urine.
Category C
Category A/B
Thiazolidinedione and Biguanide Combination
Thiazolidinedione