ANTIFUNGALS Flashcards
Five main classification of pathologic fungi
Yeasts
Moulds
Dermatophytes
Dimorphic fungi
Pneumocystis
Yeasts
Candida spp. (albicans, krusei, glabrata, tropicalis, prapsilosis)
Cryptococcus spp. (neoformans and gatti)
Dimorphic fungi
Histoplasma
Coccidioides
Paracoccidioides
Sporothrix
Blastomyces
Moulds
Mucor
Rhizopus
Rhizomucor
Types of antifungal agents
Polyenes
Allylamines
Echinocandins
Azoles
Griseofulvin
Flucytosine
2 main classes of azoles
Triazoles
Imidazoles
Triazoles
FIVTRIP
Fluconazole
Isavuconazole
Voriconazole
Terconazole
Ravuconazole
Itrazonazole
Posaconazole
Imidazoles
COMB SKES
Clotrimazole
Oxiconazole
Miconazole
Butoconazole
Econazole
Sertaconazole
Ketoconazole
Sulconazole
Indication of allylamines
Dermatphytosis of the skin and nails
Mechanism of action of azoles
Inhibit Cyp 450 14-α-sterol demethylase preventing the conversion of lanosterol to ergosterol
Which fungi are resistant to azoles
Candida krusei
Mucormycosis
Allylamines
Naftifine
Terbinafine
Allylamines contraindication
Acute or chronic liver disease
Hypersensitivity to allylamines
Lactation
Caution in pregnancy
Flucytosine mechanism of action
Disrupts protein synthesis by inhibiting RNA synthesis in the fungal cell
Allylamines mechanism of action
Inhibit squaline epoxidase
Preventing conversion of squalene to squalene epoxide
Naftifine vs Terbinafine
Terbinafine is more potent than naftifine
Terbinafine has oral activity against onchomycosis
Two types of polyenes
26-membered-ring such as Natamycin
38-membered-ring macrocycles such as Amphotericin B and Nystatin
Mechanism of action of echinocandins
Inhibit fungal cell wall synthesis by inhibiting β-(1,3) glucan synthesis
Mechanism of polyenes
Bind with ergosterol causing membrane disruption, cessation of membrane
enzymatic activities and loss of cellular constituents especially potassium ions
3-dimensional shape enable penetration the fungal cell membrane, acting as false membrane components
Echinocandins examples
Caspofungin
Anidulafungin
Micafungin
Griseofulvin indications
Dermatophyte infections of the skin, hair, nails and scalp where topical therapy has failed or inappropriate
Griseofulvin mechanism of action
Binds to tubulin to interfere with microtubule function thus inhibiting mitosis
Flucytosine mechanism of action
Disrupts protein synthesis by inhibiting RNA synthesis in the fungal cell