抗结核药——胡薇薇.pdf

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1、AntituberculousAntituberculousDrugsDrugsHuHuWeiweiWeiwei20092009--1212--2424Estimatednumbersoftuberculosiscasesbycountryin2000Corbett,E.L.etal.ArchInternMed2003;163:1009-1021.AntituberculousAntituberculousDrugsDrugsòFirstFirst--lineagentslineagents：：Isoniazid(INHIsoniazid(INH,,异烟肼异烟肼))

2、RifampinRifampin((利福平利福平))PyrazinamidePyrazinamide((吡嗪酰胺吡嗪酰胺))EthambutolEthambutol((乙胺丁醇乙胺丁醇))Streptomycin(Streptomycin(链霉素链霉素))AntituberculousAntituberculousDrugsDrugsòSecondSecond--lineagentslineagents：：ParaPara--aminosalicylicaminosalicylic((对氨水杨酸对氨水杨酸))EthionamideEthionamide((乙硫异烟胺

3、乙硫异烟胺))AmikacinAmikacin((阿米卡星阿米卡星))CapreomycinCapreomycin((卷曲霉素卷曲霉素))FluoroquinolonesFluoroquinolones((氟喹诺酮类氟喹诺酮类))IsoniazidIsoniazid((异烟肼异烟肼))1．AntituberculousactivityòBacteriostaticforrestingtuberclebacilli,bactericidalforactivelygrowingtuberclebacilliòRemarkablyselectiveformycobacte

4、ria(0.025~0.05μg/ml,othermicroorganisms500μg/ml).òResistancemutantsoccurseasilywhengivenasthesoledrug.IsoniazidIsoniazid((异烟肼异烟肼))1．AntituberculousactivityòPenetratingintophagocytes,andisactiveagainstbothextracelluarandintracellulartuberclebacilli.òDiffusingreadilyintoallbodyfluidandti

5、ssues,includingcaseousmaterial(干酪化结核病灶).IsoniazidIsoniazid((异烟肼异烟肼))2．MechanismofactionòInhibitingsynthesisofmycolicacids,whichareessentialcomponentsofmycobacterialcellwalls.IsoniazidIsoniazid((异烟肼异烟肼))3．ADMEòReadilyabsorbedfromthegastrointestinaltract.òWidelydistributedinallbodyfluids

6、andtissues.IsoniazidIsoniazid((异烟肼异烟肼))3．ADMEòMetabolismofisoniazid,especiallyacetylationbyliverN-acetyltransferase,isgeneticallydetermined.Thereareslowacetylatorsandrapidacetylators,.òExcretedmainlyintheurine.IsoniazidIsoniazid((异烟肼异烟肼))4．ClinicalUsesòFirstchoiceforallkindstuberculosi

7、sòCombinationwithrifampinorotherfirst-lineagents,isoniazidisusedforsevereinfectionswithM.tuberculosis.òAsasingleagent,isoniazidisindicatedforpreventtuberculosis.IsoniazidIsoniazid((异烟肼异烟肼))5．AdversereactionsòAllergicreactionsòHepatotoxicityòPeripheralneuritisòCNStoxiceffectsòGIeffect