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15 Cards in this Set
- Front
- Back
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what antifungals are cell membrane inhibitors?
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amphotericin B
nystatin fluconazole (azoles) allylamine drugs (terbinafine) ciclopirox |
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what antifungals inhibit RNA?
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flucytosine
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what antifungals inhibit mitosis?
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griseofulvin
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polyene antibiotic -
Amphotericin B |
Amphotericin B
Class: polyene antibiotic MOA: bind to ergosterol and form a pore (increase cell membrane permeability) Use: severe systemic, subQ mycoses.. cryptococcal meningitis, histo, blasto, coccidio AE: renal toxicity 90% {decreased GFR -> azotemia, hypokal, hypomg... chills, fever, headache (shake and bake)... liver, heart, hematopoietic toxicity (suppress EPO, anemia)... anaphylaxis, convulsions.. decrease dosage when electrolytes get bad Contra: pregnancy, crosses placenta Interaction: nephrotoxicity exacerbated by aminoglycoside, cyclosporine, pentamidine... hypokal careful in digitalis pt... increase anemia in zidovudine pt Admin: IV - lipid formulations sequestered and slowly released from reticuloendothelial system - has decreased renal drug [] / toxicity |
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Azole Derivatives-
Clotrimazole |
Clotrimazole
Class: azole derivative MOA: inhibit 14-alpha-demethylase (cyto P450 enzyme) that converts lanosterol to ergosterol Use: superficial mycoses - cadidiasis, tinea MALASSEZIA FURFUR - HYPO/HYPERPIGMENTED LESIONS AE: contact dermatitis, vulvar irritation, edema... typical azole effect: well tolerated, rash, liver, hematologic, GI Contra: Interaction: inhibit P450 enzymes - increase levels of warfarin, lovastatin, benzodiazepines, carbamazepine LIKE ERYTHRO & CLARITHRO MACROLIDES... rifampin decreases azole duration of axn Admin: topical |
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Azole Derivatives
Fluconazole |
Fluconazole
Class: azole MOA: inhibit 14 alpha demethylase, enzyme that converts lanosterol to ergosterol Use: fungal (cryptococcal) meningitis prophy and rx - penetrates CNS... candidasis (single oral dose for vaginal infection) DOC crypto, candida, coccidio AE: N/V/rashes/hepatitis Contra: preg Interaction: inhibit P450 enzymes Admin: oral, IV (penetrates CNS).. good absorption, bad metabolism |
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Azole Derivative
Itraconazole |
Itraconazole
Class: azole MOA: inhibit 14 alpha demethylase, P450 enzyme that converts lanosterol to ergosterol Use: blasto, histo (+AIDS histo), coccidio onychomycosis, sporotrichosis (give K Iodide for cutaneous lesions) AE: N/V/rash, hypokal, HTN, edema, headache Contra: preg Interaction: oral anticoag, statin, quinidine... inducers of P450 increase intraconazole metab Admin: oral - need gastric acid for dissolution.. active metabolite |
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Azole Derivative
Ketoconazole |
Ketoconazole
Class: azole MOA: inhibit 14 alpha demethylase, a P450 enzyme that converts lanosterol to ergosterol Use: NOT aspergillosus, shampoo for seborrheic dermatitis... AE: inhibit human gonadal (testosterone) synth... inhibit adrenal steroid (cortisol synth)... N/V/anorexia, allergies, transient elevated serum transaminases Contra: preg Interaction: require gastric acid for breakdown and absorbed in gastric mucosa.. PPI, H2 inhibitor, sucralfate, antacids impair absorption... acidifying agents improve absorption in pt with achlorhydria Admin: oral |
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Azole Derivative
Voriconazole |
Voriconazole
Class: azole MOA: inhibit 14 alpha demethylase, P450 enzyme that converts lanosterol to ergosterol Use: invasive aspergillosis, DRUG RESISTANT CANDIDA, DRUGS RESISTANT TO FLUCONAZOLE, additive effects with caspofungin AE: normal azole (N/V/rash, hematologic) + transient visual disturbance after dose Contra: preg Interaction: inhibit P450 Admin: oral, penetrates tissues/CNS well |
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Echinocandin
Caspofungin |
Caspofungin
Class: echinocandin MOA: inhibit cell wall glucan synthesis Use: aspergillus, resistant candida, alternative use for allergic amphotericin B/ itraconazole AE: fever, rash, nausea, phlebitis, flushing Contra: it pt taking cyclosporine Interaction: slowly metab by hydrolysis/ acetylation Admin: |
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Allylamine drugs -
Terbinafine |
Terbinafine
Class: allylamine MOA: inhibit squaline epoxidase, enzyme for ergosterol synthesis Use: superficial infections, onychomycosis, dermatophytoses, candida AE: GI, headache, rash, taste/visual disturbance Contra: nursing mom Interaction: rifampin decreases serum terbinafine level... Cimetidine increases serum terbinafine level Admin: topical, oral |
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Flucytosine
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Flucytosine
Class: MOA: inhibits thymidilate synthase (RNA synth) Use: crypto meningitis, systemic candidiasis (used with amphotericin B)... systemic/ subQ mycoses AE: reversible neutropenia, thrombocytopenia, bone marrow depression, reversible hepatic dysfxn, N/V/D, enterocolitis Contra: Interaction: dose must be adjusted in renal compromise pt Admin: oral, penetrates CSF |
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Griseofulvin
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Griseofulvin
Class: MOA: inhibits microtubule fxn, mitosis - concentrates in keratin precursor cells of dermis (works from inside out) Use: superficial mycoses AE: Contra: alcohol - potentiates alcohol effects Interaction: induces P450 Admin: oral - bioavailability increased by micronized drug particle + fatty meals |
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what are drugs used for systemic and subQ mycoses
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amphotericin B
itraconazole, fluconazole voriconazole, caspofungin (drug resistant and invasive candidiasis and aspergillosus) flucytosine |
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what drugs are used for superficial mycoses
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clotrimazole
terbinafine friseofulvin nystatin - (binds ergocholesterol), for oral candida "swish and swallow" ciclopirox (membrane structure), nail lacquer formation for onychomycosis tolnaftate |
