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18 Cards in this Set
- Front
- Back
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Antifungal Agents are generally divided into
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Cutanous/subcutaneous vs. systemic mycoses
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Generally in fungal infections, what occurs?
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Host defense mechanism disabled or other conditions optimal for fungal growth.
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Polyenes: Amphotericin B/Nystatin
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Bind to ergosterols in fungal membrane, resulting in pore formation and loss of K+/intracellular function.
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Flucytosine:
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Enters through a permease and is selectively converted by cytosine deaminase to 5-FU, which inhibits thymidylate synthase necessary for DNA synthesis.
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Azoles:
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Ketoconazole, fluconazole, itraconazole, voriconazole;
inhibit fungal P-450-mediated synthesis of ergosterol and inhibition of fungal ATPase. Also inhibit P450 of other agents, which may lead to side-effects |
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Griseofulvin:
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binds to fungal microtubules and inhibits mitosis through preventing polymerization of tubulin
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Griseofulvin
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Binds to fungal microtubules and inhibits mitosis through preventing polymerization of tubulin
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Allylamines: Terbinafine
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inhibits squalene oxidase necessary for production of ergosterol.
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Echinocandins: Caspofungin (CANCIDAS)
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Blocks β-1,3-D-glucan integration into fungal cell wall.
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Drugs for Systemic fungal infections:
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amphotericin B (parenteral, renal elimination), Flucytosine (oral, parenteral and topical), caspofungin (parenteral, metabolic elimination)
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Drugs for Oral candidiasis:
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fluconazole (renal elimination), voriconazole (oral suspension, tablets, parenteral; hepatic metabolism) as well as nystatin (oral) and caspofungin, clotrimazole (lozenges, cream).
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Drugs for Dermatophytes:
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griseofulvin (oral), terbinafine (oral), tolnaftate (topical)
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Clotrimazole attacks:
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cell membrane
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Tolnaftate attacks:
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cell membrane
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Amphotericin B side effects:
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nephrotoxicity, anemia, flu-syndrome, hypokalemia, GI disturbances.
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Caspofungin side effects:
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Fever, thrombophlebitis (injectable)
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Azoles side effects:
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GI disturbances, Hepatotoxicity, drug interactions through Cyt. P-450
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Flucytosine side effects:
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Bone marrow suppression, hepatotoxicity, GI disturbances.
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