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[哈贝卡星:一种新型氨基糖苷类抗生素。与庆大霉素、奈替米星和阿米卡星相比对大鼠肾毒性的研究]

[Habekacin: a new aminoglycoside. Study of nephrotoxicity in rats in comparison with gentamicin, netilmicin and amikacin].

作者信息

Olier B, Morin J P, Thomas N, Fillastre J P

机构信息

Centre Hospitalier Régional et Universitaire de Rouen, Service de Néphrologie, Hôpital de Bois-Guillaume, France.

出版信息

Pathol Biol (Paris). 1988 Jun;36(6):795-800.

PMID:3047639
Abstract

Habekacin is a new aminoglycoside antibiotic. In this study we want to know the effect of increasing dose of habekacin on renal function and on renal morphology. We decide to compare the renal alterations induced by habekacin to these provoked by gentamicin, netilmicin and amikacin. Female Wistar rats received intraperitonally a single injection daily of 10, 30, 50, 150 mg/kg of habekacin for seven days. Wistar rats received also 50 mg/kg gentamicin, 50 mg/kg netilmicin and 150 mg/kg amikacin. No mortality was observed in groups treated with 10, 30, 50 mg/kg habekacin but 50 per cent of rats died with 150 mg/kg habekacin. Habekacin--30 mg/kg seven days--induced a decrease of cortical enzymatic activities, an increase of the number of lysosomes, a great accumulation of myeloid bodies, an alteration of lysosomal membranes Habekacin--50 mg/kg seven days and 150 mg/kg--induced a decrease of creatinine clearance and ultrastructural alterations of renal tubular cells. Comparative studies with other aminoglycosides showed that amikacin--150 mg/kg was the lesser nephrotoxic drug. With a same dose of 50 mg/kg, gentamicin appeared lesser nephrotoxic than habekacin and habekacin seemed to induce a same degree of renal modifications than netilmicin. With the dose of 150 mg/kg habekacin this drug was higher nephrotoxic than 50 mg/kg gentamicin. In conclusion, if it could be necessary to use habekacin and to prefer this aminoglycoside to gentamicin from an antibacterial activity point of view it is necessary to keep in mind that this drug is potentially nephrotoxic and that the dosage had to be strictly respected.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

阿贝卡星是一种新型氨基糖苷类抗生素。在本研究中,我们想了解增加阿贝卡星剂量对肾功能和肾脏形态的影响。我们决定将阿贝卡星引起的肾脏改变与庆大霉素、奈替米星和阿米卡星所引发的改变进行比较。雌性Wistar大鼠腹腔内每日单次注射10、30、50、150mg/kg阿贝卡星,持续7天。Wistar大鼠还接受了50mg/kg庆大霉素、50mg/kg奈替米星和150mg/kg阿米卡星。接受10、30、50mg/kg阿贝卡星治疗的组未观察到死亡,但接受150mg/kg阿贝卡星治疗的大鼠有50%死亡。阿贝卡星——30mg/kg,7天——导致皮质酶活性降低、溶酶体数量增加、髓样小体大量积聚、溶酶体膜改变。阿贝卡星——50mg/kg,7天和150mg/kg——导致肌酐清除率降低和肾小管细胞超微结构改变。与其他氨基糖苷类药物的比较研究表明,150mg/kg阿米卡星是肾毒性较小的药物。在相同剂量50mg/kg时,庆大霉素的肾毒性似乎比阿贝卡星小,且阿贝卡星似乎比奈替米星引起相同程度的肾脏改变。在150mg/kg阿贝卡星剂量下,该药物的肾毒性高于50mg/kg庆大霉素。总之,如果有必要使用阿贝卡星,并且从抗菌活性角度更倾向于这种氨基糖苷类药物而非庆大霉素,那么必须牢记该药物具有潜在肾毒性,必须严格遵守剂量。(摘要截断于250字)

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