Chapter41AntiviralandAntifungalAgents.pptVIP

Anti-HIV Agents Anti-HIV agents Nucleoside reverse transcriptase inhibitors(NRTIs, 核苷类逆转录酶抑制剂） Non-nucleoside reverse transcriptase inhibitors (NNRTIs, 非核苷类逆转录酶抑制剂） Protease inhibitor(PI, 蛋白酶抑制剂） Cocktail therapy Nucleoside reverse transcriptase inhibitors (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） The first reverse transcriptase inhibitor for treatment of AIDS Treatment of AIDS and HIV-associated dementia(痴呆) and thrombocytopenia(血小板减少症) Mechanism: Toxicity: myelosuppression(骨髓抑制) Non-nucleoside reverse transcriptase inhibitors Delavirdine(地拉韦定） Nevirapine（奈韦拉平） Efavirenz （依法韦恩茨） Mechanism: different with NRTIs Used in combination with NRTIs and PI Toxicity: rash Protease inhibitor Drugs :saquinavir（沙奎那韦）, ritonavir(利托那韦）,indinavir（英地那韦）, nelfinavir（奈非地韦） Mechanism: inhibit precursor molecules convert to mature virions(病毒颗粒) during HIV replication Protease inhibitor Clinical uses: in combination with other agents to treat AIDS Toxicity abnormality in metabolism include altered body fat distribution, insulin resistance and hyperlipidemia(高脂血症) Cocktail therapy 将2-3种药物联合应用，以减少耐药性的产生。 优点：（1）疗效 （2）延缓耐药性 缺点：（1）毒性 （2）服药次数多 （3）价格 Other Antiviral agents Antiviral agents Acyclovir (ACV) Active against HSV-1 , HSV-2 Convert to ACV triphosphate and inhibit viral DNA polymerase Treatment of a variety of herpes infections include primary and recurrent genital herpes(生殖器疱疹) (one of the most effective) Valacyclovir (伐昔洛韦） Higher blood concentration Ganciclovir(更昔洛韦) CMV Antiviral agents Vidarabine （阿糖腺苷,Ara-A） Convert to Ara-A triphosphate and inhibit DNA polymerase Active against HSV, VZV(水痘带状疱疹病毒), CMV, HBV etc Toxicity : neurotoxicity Idoxuridine（碘苷,疱疹净,IDU） Inhibit DNA synthesis by blocking thymidylic acid(脱氧胸苷酸) synthetase Topical use for treatment of HSV infections of the eyelid, cornea(角膜) and