Bergogne-Bérézin E
Service de Microbiologie, CHU Bichat-Claude Bernard, Paris.
Presse Med. 1996 Dec 14;25(39):1982-8.
Macrolides, one of the oldest antibiotic classes, are widely used in out-patient, clinics and hospitals. The major improvement in developing newer derivatives concerns pharmacokinetic properties. Increased half-lives, persisting concentrations in tissues, interstitial fluids and macrophages confer upon newer macrolides significant advantages as compared to the parent compound erythromycin. Roxithromycin, a newer macrolide has a high peak serum concentration, providing very high levels both in the interstitial fluid and intracellularly. Pharmacodynamic approaches are still limited with macrolides, however the very high inhibitory quotient established for tissue concentrations and interstitial fluid suggests the potential clinical efficacy of these drugs.
大环内酯类抗生素是最古老的抗生素类别之一，广泛应用于门诊、诊所和医院。开发新型衍生物的主要改进在于药代动力学特性。与母体化合物红霉素相比，新型大环内酯类抗生素的半衰期延长，在组织、间质液和巨噬细胞中的浓度持续存在，具有显著优势。新型大环内酯类抗生素罗红霉素具有较高的血清峰值浓度，在间质液和细胞内均能达到很高水平。然而，大环内酯类抗生素的药效学方法仍然有限，不过针对组织浓度和间质液建立的非常高的抑制商表明了这些药物潜在的临床疗效。
