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大环内酯类抗生素:药代动力学与药效学概述

The macrolide antibiotics: a pharmacokinetic and pharmacodynamic overview.

作者信息

Jain R, Danziger L H

机构信息

University of Illinois at Chicago, College of Pharmacy (MC 886), Dept. of Pharmacy Practice, 833 S. Wood Street, Rm 164, Chicago, IL 60612, USA.

出版信息

Curr Pharm Des. 2004;10(25):3045-53. doi: 10.2174/1381612043383322.

Abstract

The macrolide antimicrobial family is comprised of 14, 15 and 16 member-ringed compounds that are characterized by similar chemical structures, mechanisms of action and resistance, but vary in the different pharmacokinetic parameters, and spectrum of activity. The macrolides accumulate in many tissues such as the epithelial lining fluid and easily enter the host defense cells, predominantly macrophages and polymorphonuclear leukocytes (PMNs). Concentrations of the macrolides in respiratory tract tissues and extracellular fluids are in almost all cases higher than simultaneously measured serum concentrations, making them useful for respiratory tract infections. This review will focus on pharmacokinetic and pharmacodynamic aspects of the clinical relevant macrolides including azithromycin, clarithromycin, dirithromycin, erythromycin and roxithromycin.

摘要

大环内酯类抗菌药物家族由14、15和16元环化合物组成,其化学结构、作用机制和耐药性相似,但在不同的药代动力学参数和活性谱方面存在差异。大环内酯类药物在许多组织中蓄积,如上皮衬液,并易于进入宿主防御细胞,主要是巨噬细胞和多形核白细胞(PMN)。几乎在所有情况下,呼吸道组织和细胞外液中的大环内酯类药物浓度均高于同时测定的血清浓度,这使得它们对呼吸道感染有效。本综述将聚焦于临床相关大环内酯类药物(包括阿奇霉素、克拉霉素、地红霉素、红霉素和罗红霉素)的药代动力学和药效学方面。

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