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头孢匹胺的胆汁排泄:其与胆汁酸和磺溴酞钠胆汁排泄的关系。

Biliary cefpiramide excretion: its relation to biliary excretion of bile acids and sulfobromophthalein.

作者信息

Takikawa H, Uchida Y, Sano N, Yamanaka M

机构信息

Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan.

出版信息

Pharmacology. 1995 Jun;51(1):24-32. doi: 10.1159/000139313.

Abstract

Cefpiramide, a beta-lactam antibiotic, has been reported to be excreted from hepatocytes into the bile by a carrier-mediated system. Herein, the relationship of biliary cefpiramide excretion to the excretion of bile acids and sulfobromophthalein was studied in rats. Biliary cefpiramide excretion was markedly inhibited by sulfobromophthalein, lithocholate-3-O-glucuronide and taurolithocholate-3-sulfate, whereas it was not inhibited by ursodeoxycholate or taurocholate. However, the inhibitory effect of cefpiramide on the biliary excretion of sulfobromophthalein or lithocholate-3-sulfate was very small. These findings indicate that, although cefpiramide is excreted by a process common to organic anions and bile acid sulfate and glucuronide, two or more excretory pathways for organic anions exist and cefpiramide has affinity for only one of these carriers.

摘要

头孢匹胺是一种β-内酰胺类抗生素,据报道它通过载体介导系统从肝细胞排泄到胆汁中。在此,研究了大鼠胆汁中头孢匹胺排泄与胆汁酸和磺溴酞钠排泄之间的关系。磺溴酞钠、石胆酸-3-O-葡萄糖醛酸苷和牛磺石胆酸-3-硫酸盐可显著抑制胆汁中头孢匹胺的排泄,而熊去氧胆酸或牛磺胆酸则无此作用。然而,头孢匹胺对磺溴酞钠或石胆酸-3-硫酸盐胆汁排泄的抑制作用非常小。这些发现表明,虽然头孢匹胺通过有机阴离子、胆汁酸硫酸盐和葡萄糖醛酸苷共有的过程排泄,但有机阴离子存在两种或更多种排泄途径,且头孢匹胺仅对其中一种载体具有亲和力。

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