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The most prescribed antibiotic:quinolones and cephalosporins Combination use:cephalosporins along with lactamase inhibitors 7.2 Antifungal agents Master the most important antifungal drug is the triazole class,which target the fungal membrane ergosterol biosynthesis.Along this synthesis pathway,there are four drug target enzymes:the squalene oxidase,lanosterol,A14-reductase,A8,A7-isomerase.The 2nd most prescribed drug class is the polyene and the other widely used antifungal drug in the clinic is the Echinocandins;Update antifungal drug development. Structural feature of the azole drugs,specific mechanism of action,selectivity of these drugs. 7.3 Antimycobacterial agents Master the four first-line anti-TB drugs:isoniazid,ethambutol,Pyrazinamide,Rifamycin.Understand their mechanism of action, recognize the molecules when provided. Updated anti-TB drugs developed after 2000:the nitro-imidazole type,Bedaquiline The second line anti-TB drug:Streptomycin and the 4th generation quinolones 7.4 Cancer and chemotherapy Cancer chemotherapy drugtype:(1)alkylating agents;(2)Organoplatinum complexes;(3)Antimetabolites,(4)DNA Polymerase/DNA Chain Elongation Inhibitors;(5)Mitosis Inhibitor taxol;(6)Kinase inhibitors;(7)epigenetic drugs. Students are required to master the major drugs in each class,drug pharmacophore,mechanism of action,side effects. 7.5 Antiviral agents Master drugs used for the treatment of influenza (Neuramidase inhibitor),HIV,HCV; Conventional Nucleoside Analogs,specific purine and pyrimidine analogs as anti-viral drugs; 1.Nucleoside Reverse Transcriptase Inhibitor(NRTIs)as anti-HIV drugs;specific drugs:AZT,ABC,et al;(2)protease inhibitors as anti-viral drugs;(3)Integrase inhibitors as anti-viral drugs.Specific drugs include:Elvitegravir,Dolutegravir, Bictegravir. HCV drug development after 2010:Nonstructural protein 5B (NS5B):NS5B;NS3/4A Protease inhibitors;specific drugs: sofosbuvir,Telaprevir,Bocsprevir (三)课程目标与毕业要求、课程内容的对应关系 表1:课程目标与课程内容、毕业要求的对应关系表The most prescribed antibiotic: quinolones and cephalosporins. Combination use: cephalosporins along with lactamase inhibitors 7.2 Antifungal agents Master the most important antifungal drug is the triazole class, which target the fungal membrane ergosterol biosynthesis. Along this synthesis pathway, there are four drug target enzymes: the squalene oxidase, lanosterol, Δ14 -reductase, Δ8 , Δ7 -isomerase. The 2 nd most prescribed drug class is the polyene and the other widely used antifungal drug in the clinic is the Echinocandins; Update antifungal drug development. Structural feature of the azole drugs, specific mechanism of action, selectivity of these drugs. 7.3 Antimycobacterial agents Master the four first-line anti-TB drugs: isoniazid, ethambutol, Pyrazinamide, Rifamycin. Understand their mechanism of action, recognize the molecules when provided. Updated anti-TB drugs developed after 2000: the nitro-imidazole type, Bedaquiline The second line anti-TB drug: Streptomycin and the 4th generation quinolones 7.4 Cancer and chemotherapy Cancer chemotherapy drug type: (1) alkylating agents; (2) Organoplatinum complexes; (3) Antimetabolites; (4) DNA Polymerase/DNA Chain Elongation Inhibitors; (5) Mitosis Inhibitor taxol; (6) Kinase inhibitors; (7) epigenetic drugs. Students are required to master the major drugs in each class, drug pharmacophore, mechanism of action, side effects. 7.5 Antiviral agents Master drugs used for the treatment of influenza (Neuramidase inhibitor), HIV, HCV; Conventional Nucleoside Analogs, specific purine and pyrimidine analogs as anti-viral drugs; 1. Nucleoside Reverse Transcriptase Inhibitor (NRTIs) as anti-HIV drugs; specific drugs: AZT, ABC, et al; (2) protease inhibitors as anti-viral drugs; (3) Integrase inhibitors as anti-viral drugs. Specific drugs include: Elvitegravir, Dolutegravir, Bictegravir. HCV drug development after 2010: Nonstructural protein 5B (NS5B): NS5B; NS3/4A Protease inhibitors; specific drugs: sofosbuvir, Telaprevir, Bocsprevir (三)课程目标与毕业要求、课程内容的对应关系 表 1:课程目标与课程内容、毕业要求的对应关系表
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