Membrane transport mechanisms of quinidine and procainamide in renal LLC-PK and intestinal LS180 cells

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  • Masago Miki
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Takaai Mari
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Sakata Jumpei
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Horie Asuka
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Ito Toshikazu
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Ishida Kazuya
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Taguchi Masato
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
  • Hashimoto Yukiya
    Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama

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タイトル別名
  • Membrane Transport Mechanisms of Quinidine and Procainamide in Renal LLC-PK1 and Intestinal LS180 Cells

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The aim of the present study was to compare the membrane transport mechanisms of procainamide with those of quinidine using renal epithelial LLC-PK1 and intestinal epithelial LS180 cells. In LLC-PK1 cells, the transcellular transport of 10 μM quinidine in the basolateral-to-apical direction was similar to that in the opposite direction, and 1 mM tetraethylammonium (TEA) did not affect the transcellular transport of the drug. On the other hand, the transcellular transport of 10 μM TEA and procainamide in LLC-PK1 cells was directional from the basolateral side to the apical side. In addition, this directional transcellular transport of procainamide was diminished in the presence of 1 mM TEA. In LS180 cells, the temperature-dependent cellular uptake of 100 μM quinidine and procainamide was markedly increased by alkalization of the apical medium, and was inhibited significantly by 1 mM several hydrophobic cationic drugs, but not by TEA. The rank order of the inhibitory effects of hydrophobic cationic drugs on the uptake of procainamide in LS180 cells was imipramine>quinidine>diphenhydramine≈pyrilamine>procainamide, which was consistent with that on the uptake of quinidine. These findings suggested that procainamide (but not quinidine) was transported by cation transport systems in renal epithelial cells, but that both procainamide and quinidine were taken up by another cation transport system in intestinal epithelial cells.

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