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新型抗生素埃瑞霉素的临床前毒理学研究。其对实验动物的急性毒性

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

作者信息

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

出版信息

Antibiot Med Biotekhnol. 1987 Dec;32(12):910-5.

PMID:2830839
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.

摘要

埃瑞霉素毒性相对较低。埃瑞霉素对白化小鼠静脉注射的半数致死量为1760(1460 - 2130)mg/kg。其毒性分别比瑞斯托霉素、万古霉素和替考拉宁低2.6倍、3.5倍和6倍。静脉注射速率对埃瑞霉素毒性无显著影响。成年小鼠和青春期前小鼠对埃瑞霉素的敏感性几乎相同。埃瑞霉素对雄性小鼠的毒性略高于雌性小鼠。静脉注射时,用5%葡萄糖溶液而非蒸馏水作为溶剂可使埃瑞霉素对白化小鼠的毒性降低1.3倍。埃瑞霉素对肾功能的毒性作用在该抗生素导致动物死亡的机制中起重要作用。在豚鼠实验中,埃瑞霉素无过敏作用。与糖肽类抗生素的其他代表药物不同,埃瑞霉素几乎没有局部刺激作用,这为其不仅作为静脉注射抗生素,也作为肌肉注射抗生素用于临床试验提供了依据。

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