（表皮癣菌）课件

Chapter43AntifungalandAntiviralDrugs Antifungaldrugs FungalinfectionSuperficialinfectionSystemicinfectionAntifungaldrugsAntifungalantibioticsAzole imidazoleandtriazoleOthers terbinafineandflucytosine Antifungalantibiotics GriseofuvinAmphotericinBNystatin Griseofulvin Antifungalactivityinihibitthegrowthofdermatophytesincludeepidermophyton 表皮癣菌 microsporum 小孢子菌 andtrichophyton 发癣菌属 noeffectonbacteriaandsystemicinfectionsoffungiMechanismofactioninterferewithfungalnucleicacidsynthesis Griseofulvin Clinicaluseitisonlyusedinthesystemictreatmentofdermatophotosisincludeskin hairandnailsAdverseeffectsNausea vomiting headacheAllergicreaction fever skinrashandleukopeniaTeratogenesis AmphotericinB AntifungalactivityHasthebroadestspectrumofantifungalactionActiveagainstcandidaalbicans cryptococcusneoformans histoplasmacapsulatumetc AmphotericinB MechanismofactionBindtoergosterolonfungalcellmembraneandalterthepermeabilityofthecellbyformingamphotericinB associatedporesinthecellmembrane allowtheleakageofintra cellularions K andmoleculesleadingtocelldeath AmphotericinB ClinicalusesDrugofchoicefornearlyalllife threateningmycoticinfectionsincludeseverefungalpneumonia crypotoccalmeningitisorsepsissyndrome AmphotericinB AdversereactionsInfusion relatedtoxicity fever chills musclespasm headache hypotensionRenaldamage azotemia K Mg2 wastingOthers Liverdamage arrthymia anemia Newpreparation LiposomalamphotericinB 两性霉素B脂质体 AmphotericinBlipidcomplex 两性霉素B脂质复合体 AmphotericinBcolloidaldispersion 两性霉素B胶质复合体 Lowerrenaltoxicity Nystatin HasthesamemechanismwithamphotericinBOnlyusedtopicallyforsuppressionoflocalcandidalinfection Azole ImidazoleClotrimazole miconazole ketoconazoleTriazoleFluconazole itraconazole Azole MechanismofactionreductionofergosterolsynthesisbyinhibitionoffungalcytochromeP450 dependent14 demethylaseClinicalusesBroad spectrum candidaspecies cryptococcusneoformans anddermatophytes Topicalazoles clotrimazoleandmiconazole BroadspectrumPoorlyabsorbedTootoxicforsystemicusesTopicuseintreatmentofdermatophytosis Ketoconazole Thefirstbroad spectrumoralazoleintroducedintoclinicaluseTreatmentofmucocutaneouscandidisisanddermatophytosisMajortoxicity Endocrinedisturbance infertility gynecomastiaandmenstrualirregularityHepatoxicity hepatitisDruginteraction Itraconazole AbsorbedwellF55 ClinicalusesSystemicfungalinfectionChoiceinthetreatmentofdermatophytosisandonychomycosisLowertoxicitythanketoconazoleCannotpenetrateBBB Fluconazole Canbeadminsteredorallyandintravenously highbioavalibility95 LeasteffectonhepaticmicrosomalenzymeDrugofchoiceinthetreatmentofcyrptococcalmenigitis 隐球菌性脑膜炎 ofAIDSandothersystemicfungalinfectionsHighconcentrationinCSF Otherantifungalagents Terbinafine 丁克 InhibitfungalsqualeneepoxidaseandinterferewithergosterolbiosynthesisHigheffectandlowtoxicityTreatmentofdermatophytosesespeciallyonychomycosis 甲癣 FlucytosineEffectiveagainstcryptococcusandcandidaspeciesConvertto5 FU inhibitDNAsynthesisSynergismwithAmphotericinB Antiviraldrugs Antiviraldrugs Acyclovir ACV ActiveagainstHSV 1 HSV 2ConverttoACVtriphosphateandinhibitviralDNApolymeraseTreatmentofavarietyofherpesinfectionsincludeprimaryandrecurrentgenitalherpes oneofthemosteffective Antiviraldrugs Idoxuridine IDU ActiveagainstHSVandVZV 牛痘病毒 InhibitDNAsynthesisbyblockingthymidylicacidsynthetaseTopicalusefortreatmentofHSVinfectionsoftheeyelid corneaandskinHightoxicity Antiviraldrugs Ribavirin virazole InhibitreplicationofbothDNAandRNAvirusesTreatmentofinfluenzaAandBinfectionsTeratogenesisVidarabine Ara A ConverttoAra AtriphosphateandinhibitDNApolymeraseActiveagainstHSVandvaccinavirusTreatmentofHSVencephalitisandherpetickeratitis Antiviraldrugs AmantadineInhibitpenetrationofvirustocellsandtheuncoatingofcertainvirusPreventdiseasescausedbyinfluenzaATreatmentofParkinson sdisease Anti HIVdrugs Anti HIVdrugs Nucleosidereversetranscriptaseinhibitors NRTIs 核苷类逆转录酶抑制剂 Non nucleosidereversetranscriptaseinhibitors NNRTIs 核苷类逆转录酶抑制剂 Proteaseinhibitor PI 蛋白酶抑制剂 Cocktailtherapy Nucleosidereversetranscriptaseinhibitors NRTIs Zidovudine 齐多夫定 AZT ZDV Lamivudine 拉米夫定 3TC Stavudine 司他夫定 d4T Zalcitabine 扎西他宾 ddC Didanosine 去羟肌苷 ddI Abacavir 阿巴卡韦 ABC Zidovudine 齐多夫定 AZT ZDV ThefirstreversetranscriptaseinhibitorfortreatmentofAIDSTreatmentofAIDSandHIV associateddementiaandthrombocytopeniaMechanism Toxicity myelosuppression Non nucleosidereversetranscriptaseinhibitors Delavirdine 地拉韦定 Nevirapine 奈韦拉平 Efavirenz 依法韦恩茨 Mechanism differentwithNRTIsUsedincombinationwithNRTIsandPIToxicity rash Proteaseinhibitor Drugs saquinavir 沙奎那韦 ritonavir 利托那韦 indinavir 英地那韦 nelfinavir 奈非地韦 Mechanism i