Yokota M, Niizato T, Inouye S, Kitasato I
Central Research Laboratories, Meiji Seika Kaisha Ltd., Yokohama, Japan.
Drugs Exp Clin Res. 1989;15(6-7):261-72.
Intramuscular administration of glucarolactam in the form of aminoglycoside salt to guinea-pigs protected the experimental ototoxicity caused by high dosing of aminoglycoside antibiotics. The protection was evidenced by the pinna reflex threshold and histochemical examinations of hair cells of cochlea as well as body weight gain. The degree of protection differed with the aminoglycosides, and high protection was observed for dibekacin, gentamicin, tobramycin, followed by kanamycin and bekanamycin. However, protection was weak or not observed when glucarolactam was administered as a mixture of glucarolactam potassium and aminoglycoside sulfate. Serum analysis of the guinea-pigs on day 14 post-administration as a measure of nephrotoxicity revealed that glucarolactam suppressed the elevation of BUN and serum creatinine caused by the aminoglycosides. The protective effect of glucarolactam on the aminoglycoside-induced nephrotoxicity in the dehydrated rats did not differ between the salt and the mixture. No difference in the in vivo antibiotic activity against bacterial infections of mice was observed between the salt and the mixture.
以氨基糖苷盐形式向豚鼠肌内注射葡醛内酯，可保护其免受高剂量氨基糖苷类抗生素所致的实验性耳毒性。通过耳廓反射阈值、耳蜗毛细胞的组织化学检查以及体重增加来证明这种保护作用。不同氨基糖苷类药物的保护程度有所不同，地贝卡星、庆大霉素、妥布霉素的保护作用较强，其次是卡那霉素和贝那霉素。然而，当葡醛内酯以葡醛内酯钾和硫酸氨基糖苷的混合物形式给药时，保护作用较弱或未观察到。给药后第14天对豚鼠进行血清分析以评估肾毒性，结果显示葡醛内酯可抑制氨基糖苷类药物引起的血尿素氮和血清肌酐升高。葡醛内酯对脱水大鼠氨基糖苷类诱导的肾毒性的保护作用在盐类和混合物之间没有差异。盐类和混合物对小鼠细菌感染的体内抗生素活性没有差异。
