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Antifungal Drugs

Kaplan

QuestionAnswer
What are the major mechanism of action of Antifungals? (4) 1. Binding to ergosterol—> create pores 2. Inhibition of 14 alpha demethylase 3. Inhibition of Squalene epoxidase 4. Inhibition of Beta-glucan (cell wall)
What are the drugs that binds to Ergosterol? (2) 1. Amphotericin B 2. Nystatin (The Polynesian) They create pores in the cell membrane and disrupt permeability
What are the drugs that inhibits 14 alpha demethylase? (4) ”-Azoles” 1. Ketoconazole 2. Fluconazole 3.Itraconazole 4. Voriconazole
What are the drugs that inhibit Squalene epoxidase? (1) 1. Terbinafine
What are the drugs that inhibits Beta-glucan? “-fungins” CASPOFUNGIN (backup drugs for mucoutaneous Candida infections and invasive Aspergillosis)
Amphotericin B is the DOC for which fungal infections? (2) 1. Cryptococus 2. Mucor
Which mode of usage is Nystatin used? Topically for Candidiasis (too toxic for systemic)
Before Amphotericin B (2) substances must be given and WHY? 1. Antihistamines 2. Steroids Because Hypotension (histamine release), fever and chills occurs with administration of Amphotericin B
What are (3) key Nephrotoxicity drugs? 1. Amphotericin B 2. AGs (Aminoglycosides) 3. Cisplatin
Which drug is DOC for esophageal and invasive candidiasis AND cryptococcal meningitis? Fluconazole
Which antifungal is used for Aspergillosis? Voriconazole
Which is the only “azole” that can penetrate the CNS? Fluconazole (that is why it is used in meningeal infection)
What is a side effect of Ketoconazole? - DECREASE steroid syhthensis (cortisol and testosterone) - Inhibition of hepatic P450s (P450 enzymes make steroids)
MOA of Flucytosine - activated by fungal cytosine deaminated to 5-FU (fluorouracil) —> after triphosphorylation added into fungal RNA - 5FU forms 5-Fd-UMP —> inhibits thymidylate synthase —> DECREASE THYMINE
Flucytosine is used in combination with what to treat severe candidates and cryptococcal infection? Amphotericin B (They enter CNS)
Griseofulvin MOA INHIBITS MICROTUBULE structure. (Binds to new keratin to protect from fungal infection) ONLY AGAINST DERMATOPHYTES
What is Terbinafine is used for? Against DERMATOPHYTES and ONYCHOMYCOSES (fungus in nails)
Created by: DVD27
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