Aminoglycosides氨基糖武类
Aminoglycosides 氨基糖甙类
1.OverviewAminoglycosides氨基糖武类·areinhibitors of proteinsynthesis,butarebactericidal杀菌·areactiveagainstgram(-）bacteria and someMycobacteria 分支杆菌·havetheir actionenhanced by inhibitors of cell wall synthesis细胞壁合成抑制剂·aretoxicfortheear耳朵andkidney肾,andhavea lowTIproteinsynthesisgram(-)inhibitorribosomeactivityenhancedbyinhibitorof cellwallsynthesisbactericide
1. Overview Aminoglycosides 氨基糖甙类 •are inhibitors of protein synthesis, but are bactericidal 杀菌 •are active against gram(-) bacteria and some Mycobacteria 分支杆菌 •have their action enhanced by inhibitors of cell wall synthesis 细胞壁 合成抑制剂 •are toxic for the ear 耳朵 and kidney 肾, and have a low TI
Position of AminoglycosidesAminoglycosidesarederivedfromStreptomyces(drugsserious,systemicending with"-mycin")-andinfections of:Micromonosporaorganisms(drugs in"-micin")lungsThey were extensively usedbloodbefore the advent of other,safer, drugs active on gram(-)abdomeninfections:3rd-generationcephalosporins头孢菌素，urinary tractfluoroquinolones氟喹诺酮类，imipenemBecauseoftheir toxicity,theyarenowreserved only for seriousandunresolved infections of the blood (septicemia), abdomen, urinarytract,andlungs,usuallyinassociationwithapenicillin盘尼西林orcephalosporin头孢菌素
Position of Aminoglycosides Aminoglycosides are derived from Streptomyces (drugs ending with “-mycin”) -and Micromonospora organisms (drugs in “-micin”) They were extensively used before the advent of other, safer, drugs active on gram(-) infections: 3rd-generation cephalosporins 头孢菌素, fluoroquinolones 氟喹诺酮类, imipenem Because of their toxicity, they are now reserved only for serious and unresolved infections of the blood (septicemia), abdomen, urinary tract, and lungs, usually in association with a penicillin 盘尼西林 or cephalosporin 头孢菌素
Aminoglycosides vs. Other Drugswater-soluble drugslipophilic drugsnarrow-wallvspectrumGram+porinsXpenicillinsouterVXmembrane盘尼西林类thick cell wallmacrolidesextended-大环内酯类wallvspectrumotherporinsvpenicillinsinfectiousouteragentsmembraneGram-fluoroquinolonestetracyclineswallX氟睦诺酮类thin cell wall四环素类porinsaminoglycosideschloramphenicolcomplexoutermembrane氨基糖类氯霉素+ someMycoplasmaSporins1
Aminoglycosides vs. Other Drugs + some Mycoplasma
Molecular StructuresCH2OHHN?HOCH2NH2H2NOHH2NHlHONH2OHONH2HOCNH2HOHNgentamicinOHtobramycinNH2Aminoglycosides contain aminosugars 氨基糖andarehighlywater-soluble水溶性
Molecular Structures Aminoglycosides contain aminosugars 氨基糖 and are highly water-soluble 水溶性