Carbon C
Internal Medicine Unit, Institut National de la Santé et Recherche Medical, Hôpital Bichat-Claude Bernard, Paris, France.
Clin Infect Dis. 1998 Jul;27(1):28-32. doi: 10.1086/514619.
The efficacy of macrolides against extracellular pathogens depends on extracellular levels of free drug and the organisms' patterns of susceptibility to the macrolides. The effect of macrolides against most bacteria is considered time-dependent. The size of inoculum affects erythromycin's activity against streptococci and, moreover, against staphylococci. The optimal effect is observed at a pH of 8. A significant postantibiotic effect (PAE), lasting approximately 9 hours, has been shown with erythromycin and roxithromycin against gram-positive cocci. Azalides share the same properties. For the streptogramin synercid, a dose-dependent bactericidal activity within a range of low concentrations has been demonstrated. The serum area under the curve appeared to be the best predictor of in vivo effect on the mouse thigh model. Synercid also exhibited a prolonged PAE (approximately 10 hours) against the main pathogens of its spectrum. A better knowledge of the pharmacodynamic properties of macrolides and streptogramins is essential for definition of proper dosing regimens.
大环内酯类药物对细胞外病原体的疗效取决于游离药物的细胞外水平以及病原体对大环内酯类药物的敏感模式。大环内酯类药物对大多数细菌的作用被认为是时间依赖性的。接种量的大小会影响红霉素对链球菌的活性，此外，也会影响其对葡萄球菌的活性。在pH值为8时可观察到最佳效果。红霉素和罗红霉素对革兰氏阳性球菌显示出显著的抗生素后效应（PAE），持续约9小时。氮杂内酯类药物具有相同的特性。对于链阳菌素类药物协同杀菌素，已证实在低浓度范围内具有剂量依赖性杀菌活性。在小鼠大腿模型中，血清曲线下面积似乎是体内效应的最佳预测指标。协同杀菌素对其作用谱中的主要病原体也表现出延长的PAE（约10小时）。更好地了解大环内酯类药物和链阳菌素类药物的药效学特性对于确定合适的给药方案至关重要。
