We investigated the cytotoxicity of erythromycin stearate, roxithromycin, clarithromycin and minocycline using lactate dehydrogenase (LDH) in cultured human intestinal epithelial cells Caco- 2, in vitro, and rat intestinal enzymes LDH and alkaline phosphatase (ALP) as end points of toxicity, in viro. The cytotoxicity after the addition of roxithromycin and clarithromycin to the Caco- 2 cells tended to be larger than that after the addition of erythromycin and minocycline. The intestinal toxicity induced by repeated 5 -day orally administered macrolide antibiotics was examined. The reduction in intestinal ALP after the administration of erythromycin and clarithromycin to rats tended to be larger than that after the addition of roxithromycin and minocycline. However, there were no significant changes in the intestinal LDH when macrolide antibiotics were orally administered. In addition, there were no significant changes or differences in either the body weight gain or the histological findings of the rat intestine. These results do not suggest any substantial risk for intestinal disorders related to the use of erythromycin, clarithromycin and roxithromycin.
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