【正文】
Chapter 38 Macrolides, Linycins and Polymycins 大環(huán)內(nèi)酯類(lèi)藥物 ? 14元大環(huán)內(nèi)酯類(lèi) :紅霉素、 羅紅霉素、克拉霉素 、地紅霉素 ? 15元大環(huán)內(nèi)酯類(lèi) : 阿奇霉素 ? 16元大環(huán)內(nèi)酯類(lèi) :螺旋霉素、乙酰螺旋霉素、麥迪霉素、麥白霉素、羅他霉素、柱晶白霉素、交沙霉素、米歐卡霉素 Macrolides ? First generation : 1950’ s— erythromycin ? Second generation: 1970’ s— claithromycin azithromycin ? Third generation: Common properties of Macrolides Antibacterial activity ? First generation ? Most G+ anisms: pneumococci, streptococci, staphylococci , diphtheriae etc ? Part G anisms:legionella(軍團(tuán)菌) ,bacillus pertussis(百日咳 ), brucella(布氏 ) etc ? Others: mycoplasma(支原體 ), chlamydia trachomatis(沙眼衣原體 ), rickettsia(立克次體 ), spirochete ,anaerobes etc. ? Second generation ? More active on G anisms Mechanism of action ? Target 50s ribosomal RNA ? Mechanism inhibition of translocation of mRNA Mechanism of resistance ? Production of inactivating enzymes ? Modification of the ribosomal binding site ? Active efflux system