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Cholestyramine

考來烯胺
Mechanism of action:
Cholestyramine 是一種陰離子交換樹脂(anion-exchange resin),屬於膽汁酸結合樹脂(bile acid sequestrant)。Cholestyramine 具有帶正電的胺基團,可與腸內帶負電的膽汁酸(bile salts)形成不可溶複合物。這些膽汁酸複合物無法被重新吸收,隨糞便排出。為補充膽汁酸流失,肝臟會增加膽固醇轉換成膽汁酸的速率,藉由上調膽固醇7α-羥化酶(cholesterol 7α-hydroxylase)的表達量。之後肝臟內膽固醇濃度下降,肝細胞上調低密度脂蛋白受體(low-density lipoprotein (LDL) receptor)表達,增加對血漿中低密度脂蛋白的吸收,降低血液中低密度脂蛋白-膽固醇的含量。
Reference(s):
1. Nichifor M et al. (1998). Aminated polysaccharides as bile acid sorbents: in vitro study. J Biomater Sci Polym Ed.
2. Benson GM et al. (1997). SK&F 97426-A: a novel bile acid sequestrant with higher affinities and slower dissociation rates for bile acids in vitro than cholestyramine. J Pharm Sci.
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