抗生素簡介_1

IntroductionforAntibioticsR3孔祥琪Lastrevised July6 2003SectionofInfectiousDiseasesDepartmentofInternalMedicineNationalTaiwanUniversityHospital Taipei 臨床上常見的致病微生物 BacteriaVirusesFungiMycobacteriumMycoplasmaProtozoa 臨床上常見的致病菌 AerobicGram positivebacteriaGram negativebacteriaAnaerobicGram positivebacteriaGram negativebacteria AerobicGram positivebacteria CocciStaphylococcusspp Streptococcusspp Enterococcusspp BacilliListeriaspp Bacillusspp Staphylococci Coagulase positiveStaphylococcusaureusCoagulase negativeStaphylococcusepidermidisStaphylococcussaprophyticusStaphylococcushaemolyticus Methicillin resistantMRSAMRCNSMethicillin sensitiveMSSAMSCNS Streptococci 1 ClassificationLancefield basedontheantigeniccharacteristicsoftheoutermembraneBrown typeofhemolysisClinical combinesLancefield Brown diseaseproducingcharacterstics Streptococci 2 alphahemolysisincompletehemolysisS viridansandS pneumoniaebetahemolysiscompletehemolysisGroupAStrep S pyogenesGammahemolysisnonhemolyticSomeGroupDStrep S pyogenes GroupA hemolytic PharyngitisImpetigoViridansgroup alphahemolytic EndocarditisS pneumoniae Pneumococcus BacteremiaPneumoniaMeningitis Gram positivebacilli BacilluscereusDiptheroidsCorynebacteriumdiptheriaeJKgroupCorynebacteriumListeriamonocytogenes AerobicGram negativebacteria BacilliEnterobacteriaceaeNFGNB GlucoseNon fermentativeGram negativebacilliHaemophilusspecies H influenzae H parainfluenzae LegionellapneumophiliaCocciNeisseriagonorrhoeae gonococcus Neisseriameningitidis meningococcus Moraxellacatarrhalis Gram negativebacteria EnterobacteriaceaeE coliKlebsiellaspp Proteusspp Salmonellaspp Shigellaspp Enterobacterspp Citrobacterspp Serratiaspp Edwardsiellaspp Yersiniaspp NFGNBPseudomonasaeruginosaAcinetobacterbaumanniiStenotrophomonasmaltophilia Pseudomonasmaltophilia Burkholderiacepacia Pseudomonascepacia Anaerobicbacteria Gram positiveCocciStreptococcus GemellaPeptococcus PeptostreptocuccusBacilliClostridium C perfringes C tenani C difficile C botulinum PropionibacteriumBifidobacteriumLactobacillus Gram negativeBacilliFusobacteriumBacteroidesPrevotellaCampylobacterCocci 臨床上常見的致病菌 Gram positivebacteriaStaphylococcusaureusStreptococcusEnterococcusGram negativebacteriaE coli Klebsiella Proteus EKP Enterobacter SerratiaNon fermentativeGram negativebacilli NFGNB HaemophilusinfluenzaeMeningococcusAnaerobicbacteriaBacteroidesfragilisOthers Lactamantibiotics PenicillinCephemCephalosporinCephamycinMonobactamCarbapenem lactam lactamaseinhibitor Penicillins NaturalpenicillinsPenicillinG IV PenicillinV oral Penicillinase resistantpenicillinsOxacillin IV MethicillinDicloxacillin oral Broad spectrumpenicillinsAmpicillin IV oral Amoxicillin oral Extended spectrumpenicillinsCarbenicillin IV oral Ticarcillin IV Piperacillin IV NaturalPcPcnase RBroadPcExtendedPcGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides lactam lactamaseinhibitors ClinicallyusedClavulanicacidSulbactamTazobactamSpecialnotesNoantibacterialactivityNeverusedalone lactam lactamaseinhibitorAmpicillin Sulbactam UnasynAmoxicillin Clavulanicacid AugmentinTicarcillin Clavulanicacid TimentinPiperacillin Tazobactam Tazocin AmpicillinUnasynAmoxicillinAugmentinGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides TicarcillinTimentinPiperacillinTazocinGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides Cephems First generationcephemCefazolin IV Cephalexin oral Second generationcephemAbovediaphragm Cefuroxime IV oral Cefotiam IV Belowdiaphragm Cefoxitin cefmetazole IVcephamycin Third generationcephemWithoutantipseudomonalactivityWithantipseudomonalactivityFourth generationcephemCefepime Cefpirome First generationcephems CefazolinActivity MSSA StreptococcusE coli K pneumoniae P mirabilisIneffective Enterococcus anaerobesOtherGNbacteria Second generationcephems Truecephems Cefotiam cefuroxime cefaclorEnhancetheanti GNBeffectof1stcephemsLesseffectiveforGPCCephamycins Cefmetazole cefoxitinWiththeeffectforanaerobesIneffective MRSA Enterococcus otherGNB Third generationcephems 1 Truecephem cefotaxime ceftriaxone ceftazidimeCephamycin flomoxefActivity Around50 forMSSAEnhancedactivityforstreptococcusStrongeffectforEnterobactereaceaCeftazidimeandcefoperazonearealsoeffectiveforP aeruginosa Third generationcephems 2 Flumarin flomoxef EffectiveforanaerobesandmostMSSAIneffective MRSA EnterococcusMoreresistantEnterobactereacea suchasEnterobacter Citrobacter Serratia Morganella 若為有效 應combineaminoglycosides Fourth generationcephems Cefepime cefpiromeActivity MostMSSA StreptococcusMostenterobactereacea includingEnterobacter Citrobacter Serratia MorganellaPseudomonasaeruginosaIneffective Enterococcus MRSAAnaerobes 1 2 2 3 3 cephemcephalosporincephamycincephemcephemGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides Monobactam Onlyonedrug aztreonamActivity MostGNB includingP aeruginosaIneffective GPbacteria anaerobesSpecialconsideration lactamallergy impairingrenalfunction Carbapenems Imipenem meropenemActivity AlmostallbacteriaaresusceptibleIneffective MRSA Enterococcusfaceium Burkholderiacepaciae StenotrophomonasmaltophiliaSpecialconsideration MeropenemispreferredinCNSinfection MonobactamCarbapenemGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides Exception MRSAEnterococcusfaeciumStenotrophomonasmaltophiliaBurkholderiacepacia Monobactam Aztreonam Carbapenem Imipenem Cilastatinsodium Meropenem ClassificationofQuinolones FirstgenerationNalidixicacidOxolinicacidCinoxacinSecondgenerationNorfloxacinCiprofloxacinEnoxacinLomefloxacinOfloxacin ThirdgenerationLevofloxacinSparfloxacinGatifloxacinGrepafloxacinFourthgenerationTrovafloxacinMoxifloxacin Fluoroquinolones Activity MSSA someenterococcus mostGNB salmonella shigella mycobacterium clamydia mycoplasma legionella dipheria pertusis3rd generationhavetheeffectforstreptococcus anaerobesIneffective MRSA Fluoroquinolones Specialconsideration OnestepmutationresultsinresistanceCrossresistanceisacommonphenomenonCiprofloxacinisnoteffectiveforstreptococcusinvivoSignificanthepatotoxicity trovafloxacin grepafloxacinSignificantphotosensitivity sparfloxacin clinafloxacinSignificantcardiacadverseeffect grepafloxacin QTc SignificantCNSexcitatoryeffect clinafloxacin Fluoroquinolone PathogenGNBNFGNBGPCAtypicalAnaerobic1stgenerationPipemidicacid Dolcol 2ndgenerationCiprofloaxin Cirpoxin Norfloxacin Baccidal 3rdgenerationLevofloxacin Cravit Moxifloxacin Avelox Gatifloxacin4thgenerationTrovafloxacin Sparfloxacin Aminoglycosides StreptomycinKanamycinGentamicinTobramycinNetilmicinAmikacin Anti Gram negativebacteriaCouldbeusedalone butseldomusedaloneIncombinationwithotherantibiotics lactam aminoglycoside Aminoglycosides Drugs Gentamicin tobramycin amikacinActivity MostbacteriaIneffective H influenzae anaerobesSpecialconsideration NotactiveinanaerobicandacidicareaOncedailyregimenSynergismwith lactams Aminoglycosides Anti Gram positivebacteriaHasanti Gram positiveactivity butneverusedaloneforGram positiveinfectionIncombinationwithotherantibioticsInfectiveendocarditisPenicillinG gentamicinEnterococcusinfectionAmpicillin gentamicinStaphylococcusinfectionOxacillin gentamicinVancomycin gentamicin Aminoglycosides TheonlybactericidalagentamongproteinsynthesisinhibitorsAlwaysusedincombinationtherapy With lactamandglycopeptides thebestsynergisticeffectsWithclindamycinandmetronidazoleformixedinfectionsWithquinolones additive antagonism synergism NotpenetratingBBBImportantindications SevereaerobicGm bacillibacteremiaFortreatmentofPseudomonas Enterobacter Serratia Enterococcus StreptococcalendocarditisEmergenceofresistanceduringtherapyisrare Anti Gram PositiveAntibiotics Glycopeptides Vancomycin Teicoplanin Mainlyanti Gram positiveactivityStreptogramins Quinupristin dalfopristin Synercid Antibiotic resistantGPC esp VRE MRSA VISA andantibiotics resistantstrainsofS pneumoniaeOxazolidinones Linezolid Zyvox AerobicandanaerobicGPbacteria includingVRE MRSA antibiotics resistantstrainsofS pneumoniae Glycopeptides Vancomycin teicoplaninActivity MostGPbacteria includinganaerobesInvitro effectiveforChryseobacteriummeningosepticumIneffective AlmostallGNbacteriaGPbacteriaonly LeukonostocandPediococcus Glycopeptides Vancomycincomparedwithteicoplanin Generally recognizedasthesameeffectBenefits SerumlevelastheguideofdosageCouldcombinedwithrifampinShortage Shouldbeinfusedat500mg hourwithlargeamountoffluid redmansyndromeRenaltoxicityandototoxicityIneffectiveforVanBphenotypeVRE Newanti GPAntibiotics Newanti GPantibiotics FusidicacidQuinupristin dalfopristin Synercid Oxazolidinones eperezolid linezolid Zyvox Activity AlmostallGPbacteria includingMRSASynercidandZyvoxarealsoeffectiveforVREFusidicacidisalsoeffectiveforH influenzaeandM catarrhalis Marcolides ErythromycinRoxithromycinClarithromycinAzithromycin Newmarcolides Newmarcolidesv s Erythromycin SimilarantibacterialactivityBetterpharmacokineticsLongerhalflife qdorbid HigherintracellularconcentrationLesssideeffect especiallyGIsideeffect Macrolides Old macrolides erythromycin New macrolides Clarithromycin roxithromycin azithromycinActivity GPC MSSA S pneumoniae notinTaiwan B pertusis C diphtheria L pneumophila M pneumoniae syphilis Chlamydia U urealyticum Campylobacter Helicobacter NTM Marcolides Anti Gram positiveactivityStaphylococcusStreptococcusMSSAMRSAPneumoGroupAR 30 50 80 90 30 Anti atypical pathogensMycoplasmaLegionellaChlamydia FluoroquinoloneVancomycinMarcolideGram StaphMSSA MRSA Streptococcus Enterococcus Gram E coli Kleb Enterobacter Pseudomonas Haemophilus AnaerobicBacteroides Sulfadrugs Sulfamethoxazole Trimethoprim Co trimoxazole Baktar Septrim ClinicalapplicationsSimpleUTIPneumocystiscariniiinfectionTravelerdiarrheaSalmonellosisSuppressiontherapyofMRSAinfectionsPneumocystiscariniiinfectionsToxoplasmosisInflammatoryboweldiseases Tetracyclines Tetracycline Minocycline Doxycyc