Pharm -11- Antifungals
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| What type of antifungal is Fluconazole (Diflucan) | Azole antifungal that targets cell membrane synthesis of ergosterol
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| What type of drug is Itraconazole (Sporanox) | Azole antifungal that targets cell membrane synthesis of ergosterol
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| What type of drug is Ketoconazole (Nizoral) | Azole antifungal that targets cell membrane synthesis of ergosterol
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| What type of drug is Voriconazole (Vfend) | Azole antifungal that targets cell membrane synthesis of ergosterol
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| What type of drug is Posaconazole (Noxafil) | Azole antifungal that targets cell membrane synthesis of ergosterol
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| What type of drug is Terbinafine (Lamisil) | Allylamine antifungal that targets cell membrane synthesis of ergosterol
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| What are the therapeutic uses for ketoconazole | used in shampoos rarely PO used for mucosal infections only.
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| What are the s/e of ketoconazole | N/V, hepatotoxicity, gynecomastia, oligospermatism, decreased libido (inhibits CYP 450 responsible for testosterone synthesis)
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| How can you increase absorption of ketoconazole | give it with cola or fruit juice since its absorption is dependent on pH
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| What caution do you have to use when prescribing ketoconazole | it has severe drug interactions with drugs such as cyclosporine, warfarin, corticosteroid and theophylline
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| What are the most common Candida spp. That infect humans | C. Albicans, Tropicalis, Parapsilosis, Glabrata, Krusei
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| What drug has historically been first line tx for Candida infections (but due to increasing resistance has been loosing that status) | Fluconazole also covers Cryptococcus neoformans and coccidiomycosis
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| What are the major s/e of using Fluconazole | N/V and rash and a lot of drug interactions but not as severe as some of the other azoles
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| How are fungi becoming resistant to fluconazole | genetic mutation, altered target site and up regulation of efflux pumps
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| Which azole has greater coverage itraconazole or fluconazole | itraconazole
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| What is one of the biggest limitations in using itraconazole (where doesn't it get) | doesn’t cross the BBB
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| What are the major s/e of using Itraconazole | taste disturbances, N/V, osmotic diarrhea, rash, hepatic toxicity, avoid using in pts with ventricular dysfunction
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| What is itraconazoles place in therapy | preferred azole to tx many varied infections 2nd line for Blastomyces, histoplasmosis, and 3rd line for Aspergillus
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| What place in therapy does Voriconazole have | used to tx invasive aspergillosis (1st line) and resistant Candida infections esp. Glabrata and Krusei.
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| What is the best antifungal to tx Mucor and Rhizopus fungus | Posaconazole
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| What are the major s/e of using Voriconazole | Visual disturbances (30%)
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| What type of drug is amphotericin B | Polyene antifungal that targets ergosterol
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| What type of drug is Nystatin | Polyene antifungal that targets ergosterol and is only used topically
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| Why is Amphotericin B considered the big gun of antifungal tx | is targets major fungi such as aspergillosis, blasto, Candida, coccidio, crypto, histo and Mucor just not Fusarium, lusitaniae and other rare fungi
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| What are the major s/e of using Amphotericin B in antifungal tx | delayed toxicity, wasting of potassium and magnesium, (Na+ loading can combat this side effect), fevers, chills, hypotension (pretreat with Benadryl, APAP or hydrocortisone)
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| What drug interactions does amphotericin B have | enhances nephrotoxicity (cyclosporins, aminoglycosides, foscarnet, pentamidine) Antineoplastic drugs (cisplatin and nitrogen mustard toxicities are enhanced)
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| What type of drug is Caspofungin | Echinocandin (Glucan synthesis inhibitor)
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| What type of drug is micafungin | Echinocandin (Glucan synthesis inhibitor)
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| What type of drug is Anidulafungin | Echinocandin (Glucan synthesis inhibitor)
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| What are the advantages of Echinocandins in tx of fungal infections and what are the limitations | tx most common fungal infections (Candida and Apergillus) limited adverse effects, no drug interactions, but IV only and limited activity against fungi outside Candida and Aspergillus
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| What are the major s/e of using Echinocandins for tx fungi | infusion related affects (IV site irritation, fever, HA, flushing, erythema and rash), histamine release
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| What type of drug is flucytosine | DNA/RNA synthesis inhibitor
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| What are the major s/e of using flucytosine | Bone marrow toxicity, monitor blood levels when using with ampho B
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| If you need an extremely effective antifungal what is your gold standard choice | Amphotericin B
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