资源描述：
《大环内酯类药物.pptx》由会员上传分享，免费在线阅读，更多相关内容在应用文档-天天文库。
1、Chapter38Macrolides,LincomycinsandPolymycins大环内酯类药物14元大环内酯类：红霉素、罗红霉素、克拉霉素、地红霉素15元大环内酯类：阿奇霉素16元大环内酯类：螺旋霉素、乙酰螺旋霉素、麦迪霉素、麦白霉素、罗他霉素、柱晶白霉素、交沙霉素、米欧卡霉素MacrolidesFirstgeneration：1950’s—erythromycinSecondgeneration：1970’s—claithromycinazithromycinThirdgeneration：CommonpropertiesofMacrolidesAntibacterialacti
2、vityFirstgenerationMostG+organisms:pneumococci,streptococci,staphylococci,diphtheriaeetcPartG-organisms:legionella（军团菌）,bacilluspertussis(百日咳),brucella(布氏)etcOthers:mycoplasma(支原体),chlamydiatrachomatis(沙眼衣原体),rickettsia(立克次体),spirochete,anaerobesetc.SecondgenerationMoreactiveonG-organismsMechanism
3、ofactionTarget50sribosomalRNAMechanisminhibitionoftranslocationofmRNAMechanismofresistanceProductionofinactivatingenzymesModificationoftheribosomalbindingsiteActiveeffluxsystemMLSRPharmokineticsAbsorptionErythromycin:notstableatacidpHNewmacrolides:stablepoDistributionMetabolism:Erythromycin&clarit
4、hromycin:inliverExcretionErythromycin&azithromycin:bileClarithromycin:kidneyCommomlyusedmacrolidesErythromycinAntimicrobialactivityGram-positiveorganisms:pneumococci,streptococci,staphylococci,diphtheriaeetcGram-negativeorganisms:legionella（军团菌）,bacilluspertussis(百日咳),brucella(布氏),meningococci,dip
5、lococcusgonorrhoeaeetcOthers:mycoplasma(支原体),chlamydiatrachomatis(沙眼衣原体),rickettsia(立克次体),spirochete,anaerobesetc.ErythromycinClinicalusesAspenicillinsubstituteinpenicillin-allergicorresistantpatientswithinfectionscausedbystaphylococci,streptococciandpneumococciPertussis，diphtheriaeLegionellaandmy
6、coplasmapneumoniaH.pinfectionErythromycinAdversereactionsGastrointestinaleffectsLivertoxicityCardiotoxicityErythromycinErythromycinlactobionate(乳糖酸红霉素）erythromycinestolate（无味红霉素)erythromycinstearate(硬脂酸红霉素）erythromycinethylsuccinate（琥乙红霉素，利君沙）NewmacrolidesantibioticsAdvantage:Broaderspectrum,highe
7、ractivityOrallyeffectiveHighbloodconcentrationLongert1/2LesstoxicityMainlyusedinrespiratorytractinfectionClarithromycin（甲红霉素,克拉霉素）HasthestrongestactivityonGram-positivebacteria,legionellapneumophila,chlamydiapneu
