Pechère J C
Department of Genetics and Microbiology, University of Geneva Medical School, Switzerland.
Eur J Clin Microbiol Infect Dis. 1991 Oct;10(10):821-7. doi: 10.1007/BF01975834.
High and prolonged tissue levels accompanied by low serum concentrations are a feature of azithromycin, an azalide antibiotic. It has a broad spectrum of activity against gram-positive and gram-negative microorganisms and several intracellular pathogens. A number of animal models of localised infection have been developed which demonstrate that the efficacy of azithromycin correlates with its extravascular pharmacokinetics and not with blood levels. In many instances, because of high tissue bioavailability, azithromycin has better in vivo efficacy than comparative agents, despite a similar or higher minimum inhibitory concentration. Additionally, the extravascular kinetics of azithromycin are associated with bactericidal activity against pathogens such as Staphylococcus aureus, Streptococcus pneumoniae and Escherichia coli. Intracellular pathogens are susceptible to azithromycin and it is believed that the agent penetrates and remains within host cells infected by organisms including Mycobacterium avium, Legionella pneumophila and Borrelia burgdorferi. This paper reviews the in vivo efficacy of azithromycin and standard agents in animal models of infection, especially those involving intracellular pathogens.
阿奇霉素是一种氮杂内酯类抗生素，其特点是组织浓度高且持续时间长，而血清浓度低。它对革兰氏阳性和革兰氏阴性微生物以及几种细胞内病原体具有广泛的活性。已经建立了许多局部感染的动物模型，这些模型表明阿奇霉素的疗效与其血管外药代动力学相关，而与血液水平无关。在许多情况下，由于组织生物利用度高，尽管阿奇霉素的最低抑菌浓度相似或更高，但它在体内的疗效优于对照药物。此外，阿奇霉素的血管外动力学与对金黄色葡萄球菌、肺炎链球菌和大肠杆菌等病原体的杀菌活性有关。细胞内病原体对阿奇霉素敏感，据信该药物可穿透并留在被鸟分枝杆菌、嗜肺军团菌和伯氏疏螺旋体等生物体感染的宿主细胞内。本文综述了阿奇霉素和标准药物在感染动物模型中的体内疗效，尤其是那些涉及细胞内病原体的模型。
