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外観
白色〜わずかにうすい褐色, 結晶性粉末〜粉末
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溶解性
アセトンに溶け、水にほとんど溶けない。
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用途
チアゾリジン系のPPARγ 作
用剤で、インスリン抵抗性を改善し、血糖低
下作用を示します。
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用途
チアゾリジン系のPPARγ作 用剤で、インスリン抵抗性を改善し、血糖低 下作用を示します。
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効能
糖尿病治療薬, ペルオキシソーム増殖因子活性化受容体(PPAR)γ作動薬
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使用上の注意
不活性ガス封入
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使用
Rosiglitazone is an insulin sensitizer; binds to peroxisome proliferator activated receptor gamma (PPAR- γ).
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適応症
Rosiglitazone is approved for use as monotherapy
and in conjunction with metformin, though it is sometimes
combined with a sulfonylurea or insulin. It is usually
taken once or twice a day with or without food.
Rosiglitazone may cause a modest increase in lowdensity
lipoprotein and triglyceride concentrations, but
it is unclear whether this effect has any clinical significance
or persists in the long term.
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一般的な説明
Rosiglitazone is 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, and is availableas the maleate salt in tablets containing the drug alone(Avandia) or in combination products with metformin(Avandamet) or with glimepiride (Avandaryl). The2-aminopyridine moiety allows for salt formation; the marketedformulations contain the 1:1 salt with maleic acid, inwhich the pyridine nitrogen accepts a proton, forming the2-aminopyridinium species.
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臨床応用
Although rosiglitazone is extensively biotransformed—playing the major role in both transformations, and some involvementof CYP2C9.21,47 The sulfate conjugate M10 is thepredominant circulating metabolite by 4-hour postdose. Theextraordinarily high plasma protein binding of this metabolite(and the N-demethylated sulfate conjugate M4) in humans accountsfor the lengthy residence time of the radioactivity in thebody, despite the relatively short pharmacokinetic half-life(4–4.5 hours) of rosiglitazone itself.
