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Drug Description
DESCRIPTION
AVANDAMET (rosiglitazone maleate and metformin HCl) tablets contain 2 oral antihyperglycemic drugs used in the management of type 2 diabetes: Rosiglitazone maleate and metformin hydrochloride. Text Continues Below
The combination of rosiglitazone maleate and metformin hydrochloride has been previously approved based on clinical trials in people with type 2 diabetes mellitus inadequately controlled on metformin alone. Additional efficacy and safety information about rosiglitazone and metformin monotherapies may be found in the prescribing information for each individual drug. Rosiglitazone maleate is an oral antidiabetic agent, which acts primarily by increasing insulin sensitivity. Rosiglitazone improves glycemic control while reducing circulating insulin levels. Pharmacologic studies in animal models indicate that rosiglitazone improves sensitivity to insulin in muscle and adipose tissue and inhibits hepatic gluconeogenesis. Rosiglitazone maleate is not chemically or functionally related to the sulfonylureas, the biguanides, or the -glucosidase inhibitors. Chemically, rosiglitazone maleate is (±)-5-[[ 4-[ 2-( methyl-2-pyridinylamino) ethoxy] phenyl] methyl]-2,4-thiazolidinedione, (Z)-2-butenedioate (1: 1) with a molecular weight of 473.52 (357.44 free base). The molecule has a single chiral center and is present as a racemate.
Due to rapid interconversion, the enantiomers are functionally indistinguishable. The molecular formula is C 18 H 19 N 3 O 3 S C 4 H 4 O 4 . Rosiglitazone maleate is a white to off-white solid with a
melting point range of 122° to 123° C. The pKa values of rosiglitazone maleate are 6.8 and 6.1. It is readily soluble in ethanol and a buffered aqueous solution with pH of 2.3; solubility decreases with increasing pH in the physiological range. Metformin hydrochloride (N, N-dimethylimidodicarbonimidic diamide hydrochloride) is not chemically or pharmacologically related to any other classes of oral antihyperglycemic agents. Page: 1 | 2 | Next >>
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