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大环内酯类抗生素的新方向:药代动力学与临床疗效

New directions for macrolide antibiotics: pharmacokinetics and clinical efficacy.

作者信息

Kirst H A, Sides G D

机构信息

Lilly Research Laboratories, Eli Lilly & Co., Indianapolis, Indiana 46285.

出版信息

Antimicrob Agents Chemother. 1989 Sep;33(9):1419-22. doi: 10.1128/AAC.33.9.1419.

Abstract

Erythromycin and related macrolide antibiotics have recently enjoyed a resurgence of clinical interest. This is a result of activity against organisms which are becoming more prevalent, particularly in immunocompromised hosts and, in addition, better understanding of the unique tissue penetration properties and potential immunomodulating properties of macrolides. Other features of clinical interest possessed by certain of the newer macrolides include the potential for once-daily dosing, resistance to acid degradation in the stomach without enteric coating, and possibly reduced gastrointestinal side effects. The new macrolides are expected to retain the clinical indications of erythromycin, which include upper and lower respiratory tract infections, skin and skin structure infections, and genital tract infections caused by erythromycin-susceptible organisms. In addition, enhanced activity has been demonstrated in animal models and in vitro against toxoplasma, Legionella, Haemophilus, and Campylobacter spp. New macrolide derivatives also show promise to expand the antimicrobial spectrum of erythromycin to include Mycobacterium and Borrelia spp.

摘要

红霉素及相关大环内酯类抗生素最近在临床上重新受到关注。这是由于它们对越来越普遍的病原体具有活性,特别是在免疫功能低下的宿主中,此外,对大环内酯类独特的组织穿透特性和潜在的免疫调节特性有了更好的理解。某些新型大环内酯类药物具有的其他临床相关特性包括每日一次给药的可能性、无需肠溶包衣即可抵抗胃酸降解,以及可能减少胃肠道副作用。新型大环内酯类药物预计将保留红霉素的临床适应症,包括由红霉素敏感病原体引起的上、下呼吸道感染、皮肤及皮肤结构感染和生殖道感染。此外,在动物模型和体外实验中已证明其对弓形虫、军团菌、嗜血杆菌和弯曲杆菌属的活性增强。新型大环内酯类衍生物也有望扩大红霉素的抗菌谱,使其包括分枝杆菌属和疏螺旋体属。

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