Bergogne-Bérézin E
Service de Microbiologie, CHU Bichat-Claude Bernard, Paris.
Presse Med. 1997 Mar;26 Suppl 2:4-10.
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 with 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,新型大环内酯类药物的半衰期延长、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。罗红霉素作为一种新型大环内酯类药物,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,大环内酯类药物的药效学研究方法仍然有限,不过针对组织浓度和间质液建立的极高抑制指数表明了这些药物潜在的临床疗效。