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奈替米星:化学研发及临床研究综述

Netilmicin: chemical development and overview of clinical research.

作者信息

Herting R L, Lane A Z, Lorber R R, Wright J J

出版信息

Scand J Infect Dis Suppl. 1980;Suppl 23:20-9.

PMID:7010547
Abstract

Netilmicin is a new semisynthetic aminoglycoside which was developed by Schering Corporation, USA, for the treatment of serious gram-negative and staphylococcal infections. Nephrotoxicity and ototoxicity in animal studies have indicated that netilmicin is both quantitatively and qualitatively safer than other aminoglycosides. Also, netilmicin has a broader spectrum of activity than either gentamicin or tobramycin. 37 clinical studies were conducted by 29 investigators in 10 countries. 840 courses of treatment in 960 infection sites were analyzed for effectiveness. Of the 724 courses in which a clinical determination could be made, 91% had either complete resolution or improvement. Bacteriologic responses were available for 782 infecting organisms and showed an 82% elimination rate. The pharmacokinetic profile of netilmicin permits twice daily administration in most patients with systemic infections and in all patients with urinary tract infections. The clinical safety of netilmicin was measured in 890 evaluable treatment courses, and only 0.4% auditory reactions, 0.6% vestibular reactions, and 0.9% renal reactions were considered to be probably netilmicin related, when netilmicin was given as recommended.

摘要

奈替米星是一种新型半合成氨基糖苷类抗生素,由美国先灵公司研制,用于治疗严重的革兰氏阴性菌和葡萄球菌感染。动物研究中的肾毒性和耳毒性表明,奈替米星在数量和质量上都比其他氨基糖苷类抗生素更安全。此外,奈替米星的抗菌谱比庆大霉素或妥布霉素更广。10个国家的29名研究人员进行了37项临床研究。对960个感染部位的840个疗程进行了疗效分析。在724个可进行临床判定的疗程中,91%的患者完全治愈或病情有所改善。对782株感染菌进行了细菌学反应分析,清除率为82%。奈替米星的药代动力学特征允许大多数全身性感染患者和所有尿路感染患者每日给药两次。在890个可评估的治疗疗程中对奈替米星的临床安全性进行了测定,按照推荐剂量使用奈替米星时,仅0.4%的患者出现听觉反应,0.6%的患者出现前庭反应,0.9%的患者出现肾脏反应,这些反应可能与奈替米星有关。

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