(精选)Challenges in Antibiotic Design教学课件.pptVIP

Current Antifungal Agents Structure Mechanism of Action Primary Use Ampho B ergosterol inhibition moulds/dimorphic fungi Terbinafine cutaneous infxn Azoles ergosterol inhibition dimorphic fungi, Fluc Candida, Itra Aspergillus Vori Posa Echinocandins inhibit glucan synthesis Candida/ Micafungin Aspergillus Caspofungin Anidulafungin Azole Antifungal Agents Two major types Imidazoles– ketoconazole, miconazole Triazoles- Fluconazole, Itraconazole, Posaconazole, Voraconizole Major limiting adverse effect- hepatotoxicity Lots of potential drug interactions Spectrum C. alb Non-C. alb Crypto Dimorphic Aspergillus mycoses Flu + + + + - Vori + + + + + Posa + + + + + AmB + + + + + Echino + + - +/- + Busse et al. J Okla State Med Assoc, 2007 Posaconazole General Structural analogue of itraconazole, oral preparation Developed in the era of increased prevalence of invasive fungal infection Indications Prophylaxis against Candida and Aspergillus infections in severely immunocompromised patients Oropharyngeal candidiasis Action Induces loss of cell membrane integrity Active against Yeasts- Candida, Blasto, Crypto, Histo, Coccidio, Sporo (less active against C. tropicalis) Moulds- Aspergillus, Zygomycetes, Chromoblastomycoses Schiller et al, Clin Therapeutics, 2007 Antibiotic Update2009 Michael S. Bronze, MD Professor and Chair Department of Medicine, OUHSC Objectives To briefly review some of the current issues with antibiotics To discuss several newer agents To discuss several clinical situations in which newer agents may have an expanding role I have no conflicts of interest to report! Challenges in Antibiotic Design Drug No. Rx Worldwide World-wide Sales (Rx; 000s) (USD; 000s) Amox/clav 136,000 1,971,927 Cipro 80,217 877,718 Clarithro 74,689 1,495,006 Azithro 66,061 2,002,082 Lev