Pechère J C
Department of Genetics and Microbiology, University of Geneva Medical School, Switzerland.
Drugs. 1996;51 Suppl 1:13-9. doi: 10.2165/00003495-199600511-00005.
Streptogramin antibiotics represent a unique class of antibacterials in that each member of the class consists of at least 2 structurally unrelated molecules: group A streptogramins (macrolactones) and group B streptogramins (cyclic hexadepsipeptides). Both group A and group B streptogramins inhibit protein synthesis at the ribosomal level, and they act synergistically against many isolates, their combination generating bactericidal activities and reducing the possibility of emergence of resistant strains. The mechanisms of acquired resistance to group B streptogramins are similar to those induced by erythromycin, but group A streptogramins remain unaffected by target modifications and active efflux. The pharmacokinetic parameters of group A and group B streptogramins in blood are quite similar. In addition, both the A and B groups penetrate and accumulate in macrophages and in the bacterial vegetations of experimental endocarditis. There are important structural and biological differences between the streptogramins and the macrolides. The main differentiating features are the rapid anti-bacterial killing of streptogramins and the rarity of cross-resistance between the 2 groups of antibiotics.
链阳菌素类抗生素是一类独特的抗菌药物，该类药物的每个成员至少由2个结构不相关的分子组成：A组链阳菌素（大环内酯类）和B组链阳菌素（环六缩肽）。A组和B组链阳菌素均在核糖体水平抑制蛋白质合成，它们对许多分离株具有协同作用，两者联合产生杀菌活性并降低耐药菌株出现的可能性。获得性对B组链阳菌素耐药的机制与红霉素诱导的机制相似，但A组链阳菌素不受靶点修饰和主动外排的影响。A组和B组链阳菌素在血液中的药代动力学参数非常相似。此外，A组和B组链阳菌素均可渗透并积聚在巨噬细胞以及实验性心内膜炎的细菌赘生物中。链阳菌素类和大环内酯类之间存在重要的结构和生物学差异。主要区别特征是链阳菌素类具有快速杀菌作用以及两组抗生素之间很少出现交叉耐药。
