20xx年醫(yī)學專題—人工合成抗菌藥ppt-文庫吧資料
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【正文】 要指標———光毒性方面，它的毒性明顯低于現(xiàn)有主要產(chǎn)品洛美沙星、司帕沙星、氟羅沙星、環(huán)丙沙星。,鹽酸(y225。,Pipemidic acid (吡哌酸) Norfloxacin (諾氟沙星) Ciprofloxacin (環(huán)丙殺星) Ofloxacin（氧氟沙星） Levofloxacin（左氧氟沙星） Lomefloxacin（洛美沙星） Fleroxacin（氟羅沙星） Sparfloxacin（司帕沙星）,Quinolones agents,Quinolones,第二十八頁，共五十四頁。,(1)Gastrointestinal effects. The most common reactions (2)CNS side effects. Penetrate BBB→ GABA↓ (3)Allergic reaction. Skin rashses, itchs, angioneuroedema , etc. Photosensitivity (4)other effects. Cardiac toxicity： QT interval↑ Liver and renal injury,Adverse reactions,Quinolones,第二十六頁，共五十四頁。 xu232。,(2) GI and abdominal infections. Excellent in vitro activity against many enteric pathogens, including Escherichia coli大腸桿菌, Aeromonas氣單胞菌屬, Shigella志賀(氏)桿菌(gǎnjūn), Salmonella沙門氏菌, Campylobacter彎曲桿菌屬, Vibrio弧菌屬, and Yersinia species耶爾森菌 Furthermore, quinolone drug concentrations in feces are exceedingly high.,Clinical Uses,Quinolones,第二十四頁，共五十四頁。,Urinary tract infections. The main indication for quinolones In the treatment of uncomplicated and complicated UTIs, cure rates can exceed 90% and 80%, respectively. Potent agents to use against Haemophilus ducreyi (軟性(ruǎn x236。,(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.,Resistance Mechanism,Quinolones,第二十一頁，共五十四頁。,Inhibition of topoisomerase IV → interferes with separation of replicated chromosomal DNA into the respective daughter cells during cell division.,Inhibition of DNA gyrase →prevents the relaxation of positively supercoiled DNA that is required for normal transcription and replication.,Mechanism of action,Quinolones,第十九頁，共五十四頁。,Quinolones,Quinolones,第十七頁，共五十四頁。 spectrum (4) They also are effective against Chlamydia spp.（衣原體）, Legionella pneumophila(軍團菌) ,anaerobic bacteria, mycobacteria(分枝桿菌). (5) Some agents have limited activity against multipleresistance strains. （6）Bactericidal concentration≥ bacteriostatic concentration,Quinolones,Quinolones,第十五頁，共五十四頁。 spectrum (1) Bactericidal and have significant PAE. (2)Excellent activity against aerobic gramnegative bacteria, some agents have activity against Pesudomonas. (3) Several newer agents with improved activity against aerobic grampositive bacteria.,Quinolones,Quinolones,第十四頁，共五十四頁。,Fourthgeneration agents (1997 ) Grepafloxacin 格帕沙星，Clinafloxacin 克林沙星，Gatifloxacin 加替沙星，Moxifloxacin 莫西沙
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