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1、37氨基甙类抗生素及多粘菌素90096（37aminoglycosideantibioticsandpolymyxin90096）37aminoglycosideantibioticsandpolymyxin.Txtrunwithjoy,listenattentively,developwiththinking,strugglewitheffort,measurewithgoal,andlivewithlove.Moremoney,lessmoney,oftengood!Goodhealthisbetterforoldpeoplethanforoldpeopl
2、e!Hishomeisrich,harmonious.Thefortiethchapter,aminoglycosideantibioticsandpolymyxinAminoglycosideantibioticsGeneralityof1.aminoglycosideantibiotics1).ChemicalstructureTheyareallcomposedofaminosugarmoleculesandaglyconeofnonsugarparts.Theyarestrongorganicacids,solubleinwater,stableinn
3、ature,andoftenmadeintosulfateforclinicalapplication.2)antimicrobialspectrumForaerobicG-bacteria(E.coli,Klebsiella,Enterobacter),.Pneumonia,deformation,Salmonellaspp.anddrug-resistantstaphylococcusaureushavestrongeffectonG-coccus,suchasNeisseriagonorrhoeaeandNeisseriameningitidis.Ami
4、kacin,gentamicin,tobramycin,effectiveagainstPseudomonasaeruginosa,withstrongesttobramycin.Itisabactericideinreproductiveperiodandstationaryphase.3)mechanismofactionInhibitionofbacterialproteinsynthesisprocess,inhibitingtheformationof70sinitiationcomplexesintheinitialstage;inthestage
5、ofpeptidechainelongationselectivelywith30SsubunitofP10proteinbindingtomRNAtemplategeneticcodemistranslation,synthesisofnonfunctionalproteins;terminationphaseterminationfactorandhinderribosomebinding,thesyntheticpeptidehasnotreleased70snuclearproteinbodydissociation,ribosomecelldeple
6、tion.Inaddition,aminoglycosidewasattachedtothecellsurfacebyionadsorption,resultingincellmembranedefects,andleakageofnutrientsinthecellanddeath.4)drugresistanceBacteriacanproduceresistancetoaminoglycoside,whichisarrangedfromeasytodifficultsequence,streptomycin>kanamycin>gentamicin>am
7、ikacin.Whichpartofcrossresistancebetweenthedrugs,suchasstreptomycinresistantstrains,werestillsensitivetogentamicin,amikacin,kanamycinorviceversa,amikacinresistanttostreptomycinorgentamicinresistancealso.Themaindrugresistancemechanismofbacterialproductionofinactiveenzyme,drugacetylat
8、ion,phosphorylation
