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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。

相似文献

1
[Preclinical toxicological study of the new antibiotic eremomycin. Its acute toxicity for laboratory animals].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
Antibiot Med Biotekhnol. 1987 Dec;32(12):910-5.
2
[Glycopeptide antibiotics: eremomycin, vancomycin, and teicoplanin. Comparison of several parameters of pharmacokinetics and antimicrobial activity].[糖肽类抗生素:埃瑞霉素、万古霉素和替考拉宁。药代动力学和抗菌活性若干参数的比较]
Antibiot Khimioter. 1989 Jul;34(7):523-6.
3
[Preclinical toxicological study of the new antibiotic eremomycin. Chronic toxicity and effect on intrauterine development of rats].
Antibiot Khimioter. 1988 Apr;33(4):280-6.
4
[Comparative study of the therapeutic effect of the glycopeptide antibiotics eremomycin, vancomycin and ristomycin in a model of antibiotic-associated colitis in golden hamsters].
Antibiot Khimioter. 1992 Nov;37(11):32-5.
5
[Eremomycin--a new antibiotic of the polycyclic glycopeptide group].埃瑞霉素——一种新型多环糖肽类抗生素
Antibiot Khimioter. 1989 May;34(5):348-52.
6
[Pharmacokinetic study of eremomycin in an experiment].[埃瑞莫霉素在实验中的药代动力学研究]
Antibiot Med Biotekhnol. 1987 Jul;32(7):511-6.
7
[Experimental study on chemotherapeutic efficacy, acute toxic action and nephrotoxicity of combinations of eremomycin with tobramycin].[埃瑞霉素与妥布霉素联合应用的化疗疗效、急性毒性作用及肾毒性的实验研究]
Antibiot Khimioter. 1990 Nov;35(11):21-4.
8
[Eremomycin--a new antibiotic from the cyclic glycopeptide group].埃瑞莫霉素——一种来自环糖肽类的新型抗生素
Antibiot Med Biotekhnol. 1987 Aug;32(8):571-6.
9
[Experimental study of the antibacterial activity and chemotherapeutic efficacy of the novel glycopeptide eremomycin].新型糖肽类抗生素埃瑞霉素抗菌活性及化疗效果的实验研究
Antibiot Khimioter. 1989 Jan;34(1):52-6.
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[In vitro activity of a new glycopeptide antibiotic eremomycin in relation to obligate anaerobic Gram-positive bacteria].[新型糖肽类抗生素埃瑞霉素对专性厌氧革兰氏阳性菌的体外活性]
Antibiot Khimioter. 1991 Apr;36(4):17-20.

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Eremomycin pyrrolidide: a novel semisynthetic glycopeptide with improved chemotherapeutic properties.埃瑞莫霉素吡咯烷化物:一种具有改善化疗特性的新型半合成糖肽。
Drug Des Devel Ther. 2018 Sep 10;12:2875-2885. doi: 10.2147/DDDT.S173923. eCollection 2018.