Antifungal drugs

59 Pages·2013·2.59 MB·English

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12th ESCMID Summer School i
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6 – 13 July 2013, Vravrona, Greece
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Antifungal dr ugs: an update.
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George Petrikkos, MD,
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Professor of Internal Medicine
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[email protected]
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National and Kapodistrian University of Athens
ATTIKON Hospital
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Transparency Declaration
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• I have received research graunts from Gilead,
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Pfizer, Astellas, and Astrea-Zeneca

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• Acted as paid consultant to MSD and Astellas
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The history of antifungals
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1950s
1960s t
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Nystatin 1980s
Miconazole e

Amphotericin B L Flucytrosine Ketoconazole
Clotrimazole o

Griseofulvin e h
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2000s
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1990s
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Caspofungin 2010s
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FluconazoIle
M Isavuconazol
Itraconazole caps
C Ravuconazol
Voriconazole
ItraSconazole soln Albaconazol
Posaconazole susp
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Terbinafine Aminocandin

Lipid Ampho Posaconazol tabl,IV
Anidulafungin
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Micafungin
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How do they work? r
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Cell membrane
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• Polyene antibiotics
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• Azole antifungals
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Cell wall
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-Caspofungin acetate (Cancidas)
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The ideal antifungal agent
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• Broad spectrum of activity (yeasts and filamentous fungi)
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• Rapidly and highly fungicidal, stable to resistance
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• Potent in vivo activity (even in neutropenia)
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• Both oral and parnenteral foramulations
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• Low toxicity , minimal dbrug-drug interactions
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• Good Mpharmacokinetics (AUC)
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• SGood penetration into all tissue compartments
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• Cost effective
HEM/00223M
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FUNGI
AMB FCZ ΙTZ VZ PCZ RCZ CF MF AF

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Candida albicans
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Candida tropicalis
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Candida parapsilosis e

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Candida krusei
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Candida glabrata
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Cryptococcus neoformans n a
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Histoplasma capsulatum
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Blastomyces dermatitidis
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Coccidiodes imMmitis
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Paracocci brasiliensis
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PneE umocystis carinii
Aspergillus fumigatus
Mucor spp
Rhizopus spp
Fusarium spp
Adapted from JP Donnelly
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• A pcolyene
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• Isolateod from Streptomyces

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nodosus
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© • Solubilized by sodium
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deoxycholate
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E • Available for IV use as
amphotericin B deoxycholate
(Fungizone®)
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AMB-d
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Imidazoles Fluconazole Lipid-AMB Echinocandins/
Itraconazole New Triazoles
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 AmBisome®:
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 amphotericin B
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Hiemenz JW, et al. Clin Infect Dis. 1996;22(suppl 2):S133-S144.