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28 Cards in this Set
- Front
- Back
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Name some Polyenes |
Amphotericin, Nystatin, Natamycin |
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Indications for Amphotericin? |
First choice for systemic fungal infections, like severe fungal pneumonia or meningititis. |
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Indications for Nystatin and Natamycin? |
Oral and vaginal candidiasis topically. |
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Mechanism of action of Polyenes? |
They bind to ergosterol in the fungal cell membrane, increasing the membrane permeability and kills the fungal cell. |
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How can Amphotericin be given so it is less toxic? |
It can be given as a liposomal formulation, where Amphotericin B is enveloped in liposomes and endocytosed by the fungal cell. This is more expensive. |
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Why is Amphotericin toxic? |
It binds to human cholesterol as well. |
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What are the adverse effects of Amphotericin? |
- Nephrotoxicity - QT prolongation - Phlebitis at site of infusion - Nausea and vomiting - Cytokine storm with fever, shivering and headaches due to release of TNF-a and IL-1 |
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What are the two classes of Azoles? |
Imidazoles and Triazoles |
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Name the Imidazoles? |
Ketoconazole and clotrimazole |
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Name the Triazoles |
Fluconazole, itraconazole, voriconazole |
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Indications of clotrimazole and ketoconazole? |
Used to treat topical fungal infections like vaginal yeast infection, tinia |
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Indications for fluconazole, itraconazole and voriconazole? |
They are only used systemically against cryptococcal meningitis and invasive aspergillosis. |
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Mechanism of action of Azoles? |
They inhibit the fungal CYP450 system, which leads to no synthesis of ergosterol. The precursor of ergosterol accumulates, and it is toxic to the fungus. |
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Where do Fluconazole and itraconazole accumulate? |
In keratin |
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What are the interactions of Azoles? |
They inhibit human CYP450 in addition to fungal, especially CYP3A4, which leads to interactions with many other drugs. |
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Adverse effects of ketoconazole? |
It can lead to adrenal cortex failure due to inhibition of steroid hormone synthesis. Therefore, it is only used topically. |
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Adverse effects of Azoles? |
Hepatotoxicity |
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Mechanism of Terbinafine? |
Inhibit ergosterol synthesis so the toxic precursor of ergosterol accumulates in the fungus. |
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Name Echinocandins |
Caspofungin, Micafungin, Anidulafungin. |
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When are echinocandins indicated? |
In invasive aspergillosis or candidiasis in HIV-patients |
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Mechanism of action of echinocandins? |
They inhibit the synthesis of beta-glycan which is a component of the fungus cell wall. |
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Which drug is Flucytosine usually combined with? |
Amphotericin |
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Mechanism of action of flucytosine? |
It gets converted into 5-flourouracil inside the fungus which inhibits DNA and RNA synthesis |
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Name benzofurans |
Griseofulvin |
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What can we treat with Griseofulvin? |
Tinea infections like tinea pedis |
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Name topical antifungals |
Nystatin, clotrimazole, naftifine, tolnaftate |
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Name antifungals that can be used both systemically and topically? |
Ketoconazole, miconazole, terninafine |
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Name antifungals that are given systemically |
Amphotericin, flucytosine, griseofulvin, fluconazole, itraconazole, variconazole, caspofungin, micafungin, anidulafungin |
