(人工合成抗菌药)Synthetic antimicrobial agents 英文版.ppt

 Synthetic antimicrobial agents(人工合成抗菌药) Huifang Tang tanghuifang@zju.edu.cn Classification of Synthetic antimicrobial agents General features Broad antimicrobial activity and are effective after oral administration for the treatment of a wide variety of infectious disease. Relatively few side effects. Microbial resistance to their action does not develop rapidly. Classification Generation Examples 1 st (1962-1969) Nalidixic acid, 萘啶酸 2 nd (1969-1979) Pipemidic acid 吡哌酸 Cinoxacin 西诺沙星 3 rd (1980-1996) Norfloxacin 诺氟沙星 Levofloxacin 左氧氟沙星 Ciprofloxacin 环丙沙星 Ofloxacin 氧氟沙星 sparfloxacin 司帕沙星 4 th (1997-) Grepafloxacin 格帕沙星 Clinafloxacin 克林沙星 Gatifloxacin 加替沙星 Moxifloxacin 莫西沙星 Summary of antimicrobial spectrum of quinolones. Typical therapeutic applications of uoroquinolones. Antimicrobial activity spectrum (1) Bactericidal and have significant PAE. (2)Excellent activity against aerobic gram-negative bacteria, some agents have activity against Pesudomonas. (3) Several newer agents with improved activity against aerobic gram-positive bacteria. Antimicrobial activity spectrum (4) They also are effective against Chlamydia spp.（衣原体）, Legionella pneumophila(军团菌) ,anaerobic bacteria, mycobacteria(分枝杆菌). (5) Some agents have limited activity against multiple-resistance strains. （6）Bactericidal concentration≥ bacteriostatic concentration (1) Mutation of the gyrA gene that encoded the A subunit polypeptide can confer resistance to these drugs. (2) Mutation of the gene cfxB and nfxB that encoded the porin decreased permeability of cell membrance. (3) The high expression of norA gene (encoded active pump protein) increased drugs efflex by a active transport protein pump. (4) Plasmid mediated resistance. (1) Well absorbed after oral administration. (2) Distributed widely i