Comparative Pharmacology
Head-to-head clinical analysis: AVANDAMET versus ROSIGLITAZONE MALEATE AND METFORMIN HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AVANDAMET versus ROSIGLITAZONE MALEATE AND METFORMIN HYDROCHLORIDE.
AVANDAMET vs ROSIGLITAZONE MALEATE AND METFORMIN HYDROCHLORIDE
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.
Rosiglitazone is a thiazolidinedione that activates peroxisome proliferator-activated receptor gamma (PPARγ), increasing insulin sensitivity in adipose tissue, muscle, and liver. Metformin is a biguanide that decreases hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
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.
Oral, initial: rosiglitazone 2 mg plus metformin 500 mg twice daily; maximum: rosiglitazone 8 mg plus metformin 2000 mg per day (divided twice daily).
None Documented
None Documented
Rosiglitazone: 3-4 hours (terminal); metformin: 6.2 hours (terminal). No accumulation with normal renal function.
Metformin: 4-8.7 h (elimination), prolonged in renal impairment; Rosiglitazone: 3-4 h (terminal), slightly longer in hepatic impairment.
Renal (90-95% as unchanged drug for rosiglitazone; metformin is 90% renally eliminated unchanged). Biliary/fecal: minor (<5% for both).
Metformin: 90% renal unchanged via tubular secretion; Rosiglitazone: 64% renal (metabolites), 23% fecal. Combined: minimal biliary excretion.
Category C
Category A/B
Thiazolidinedione and Biguanide Combination
Thiazolidinedione