[Preclinical toxicological study of the new antibiotic eremomycin. Its acute toxicity for laboratory animals].

L E Gol'dberg, E S Stepanova, T P Vertogradova, L A Shevniuk, N G Shepelevtseva
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Abstract

Eremomycin is relatively low toxic. LD50 of eremomycin on its intravenous administration to albino mice amounted to 1760 (1460-2130) mg/kg. It is 2.6, 3.5 and 6 times less toxic than ristomycin, vancomycin and teicoplanin, respectively. The rate of intravenous administration had no significant effect on eremomycin toxicity. Sensitivity of adult and preadolescent mice to eremomycin was almost the same. Eremomycin toxicity for male mice was somewhat higher than that for female mice. The use of 5 per cent glucose solution instead of distilled water as a solvent lowered 1.3-fold the toxicity of eremomycin in albino mice when it was administered intravenously. The toxic effect of eremomycin on the renal function played a significant role in the mechanism of the animal death due to the antibiotic. In experiments with guinea pigs eremomycin showed no allergenic effect. Unlike the other representatives of glycopeptide antibiotics, eremomycin had practically no local irritating effect which provided its recommendation for clinical trials not only as an intravenous but also intramuscular antibiotic.

新型抗生素维莫霉素的临床前毒理学研究。对实验动物的急性毒性。
埃雷霉素的毒性相对较低。白化小鼠静脉给药伊雷霉素的LD50为1760 (1460 ~ 2130)mg/kg。其毒性分别比利斯托霉素、万古霉素和替可普宁低2.6倍、3.5倍和6倍。静脉给药率对伊雷霉素毒性无显著影响。成年和青春期前小鼠对伊雷霉素的敏感性几乎相同。埃雷霉素对雄性小鼠的毒性略高于雌性小鼠。使用5%的葡萄糖溶液代替蒸馏水作为溶剂,当静脉给药时,对白化小鼠的伊雷霉素毒性降低了1.3倍。伊雷霉素对肾脏功能的毒性作用在抗生素致动物死亡的机制中起着重要作用。在豚鼠实验中,维莫霉素无致敏作用。与其他代表性的糖肽类抗生素不同,伊雷霉素几乎没有局部刺激作用,这使得它不仅可以作为静脉注射抗生素,也可以作为肌肉注射抗生素进行临床试验。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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