Term
| Polyene Antibiotics (MOA) |
|
Definition
| Binds to ergosterol, and thereby disrupts fungal cell membrane |
|
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Term
|
Definition
| Disrupts synthesis of RNA and DNA |
|
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Term
|
Definition
| Inhibit synthesis of ergosterol, and therby disrupt the fungal cell membrane |
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Term
|
Definition
| inhibit synthesis of beta-1,3-glucan, and thereby disrupt the cell wall |
|
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Term
|
Definition
| Targets squalene-epoxidase to inhibit ergosterol synthesis |
|
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Term
|
Definition
| inhibits microtubule polymerization |
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Term
| Which antifungals do not target the fungal cell membrane or cell wall? |
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Definition
| flucytosine (a pyrimidine analog) and griseofulvin (mitotic inhibitor) |
|
|
Term
| Amphotericin B (clinical use) |
|
Definition
| IV broad spectrum against many fungi including candidiasis, aspergillosis, cryptococcosis, mucormycosis |
|
|
Term
|
Definition
|
|
Term
| Anti-fungals approved for pregnancy use? |
|
Definition
|
|
Term
|
Definition
| ketoconazole, itraconazole, fluconazole, voriconazole, posaconazole, griseofulvin, echinocandins |
|
|
Term
| Amphotericin B (adverse effects) |
|
Definition
| holes in mammalian membrane; renal toxicity; infusion-related rxns (phlebitis, febrile rxn); toxicities reduced with lipid forumulations |
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Term
|
Definition
|
|
Term
|
Definition
| Topical formulation usually for intestinal/oral mucosa, esophageal CANDIDA, and dermatophyte |
|
|
Term
| Nystatin (adverse effects) |
|
Definition
|
|
Term
|
Definition
| Antimetabolite (pyrimidine analog) |
|
|
Term
| Flucytosine (pharmokinetics) |
|
Definition
|
|
Term
| Flucytosine (clinical uses) |
|
Definition
| -used againt Candidia and Cryptococcus |
|
|
Term
|
Definition
-Cryptococcal meningitis (w/ amphotericin B)
-Chromoblastomycosis (w/ itraconazole) |
|
|
Term
| Flucytosine (adverse effects) |
|
Definition
| bone marrow suppression; affects rapidly dividing cells |
|
|
Term
|
Definition
| inhibits cytochrome activitiy!!!***, QT prolongation, teratogenic |
|
|
Term
| Ketoconazole (clinical use) |
|
Definition
|
|
Term
| Itraconazole (clinical uses) |
|
Definition
Broad spectrum, mostly against:
-histoplasmosis
-sporotrichosis
-blastomycosis
-candidiasis
-aspergillosis
-sporotrichosis
-NOT mucormycosis
alternative to ampho B |
|
|
Term
| Itraconazole (pharmacokinetics |
|
Definition
no CNS penetration
absorption reduced by drugs reducing stomach acid |
|
|
Term
| Itraconazole (adverse effects) |
|
Definition
-cardiosuppression -> drug contraindicated with ventricular dysfunction (QT prolongation)
-teratogenic
-strong inhibitor of CYP3A4 (and it is a substrate) -> increases concentrations of cyclosporine and some statins |
|
|
Term
| Itraconazole (drug-drug interactions) |
|
Definition
| Strong inhibitor of CYP3A4 |
|
|
Term
|
Definition
|
|
Term
| Fluconazole (clinical use) |
|
Definition
Narrow spectrum
-Blastomycocis
-Histoplasmosis
-Cryptococcal meningitis in AIDS (good CSF levels)
-candidiasis (often for this!!)
-excreted renally unchanged -> UTI
NOT active: aspergillosis or mucormycosis |
|
|
Term
| Fluconazole (drug-drug interactions) |
|
Definition
| Lower than other azoles, but strong inhibitor of CYP2C9 |
|
|
Term
| Fluconazole (adverse effects) |
|
Definition
Well tolerated in general
-Headache
-Rash
-GI
-Teratogenic
-QT Prolongation |
|
|
Term
|
Definition
|
|
Term
| Voriconazole (clinical use) |
|
Definition
| Better activity against invasive aspergillosis and candidiasis than itraconazole |
|
|
Term
| Voriconazole (adverse effects) |
|
Definition
-photosensitivity
-visual disturbances
-QT prolongation risk |
|
|
Term
|
Definition
|
|
Term
| Posaconazole (clinical use) |
|
Definition
-Itraconazole like (Candidiasis, Aspergillosis) but better for Mucormycosis
-Often used empirically |
|
|
Term
| Posaconazole (adverse effects) |
|
Definition
-QT prolongation
-teratogenic |
|
|
Term
| Echinocandins (clinical use) |
|
Definition
-Narrow spectrum (most Candidia, Aspergillus)
-Used for strains resistant to Amphotericin B and Voriconazole
-Empiric fungal infections |
|
|
Term
|
Definition
-caspofungin
-anidulafungin
-micafungin |
|
|
Term
| Echinocandins (adverse effects) |
|
Definition
-flushing (pretreat w/ antihistamine)
-embryotoxic in animals
-D-D interactions w/ cyclosporine, sirolimus, tacrolimus -> raises levels |
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|
Term
|
Definition
|
|
Term
| Terbinafine (clinical use) |
|
Definition
-oral for dermatophytes (onychomycosis or nails)
-topical drug for ringworm infxns |
|
|
Term
|
Definition
terbinafine
naftifine
amorolfine
butenafine |
|
|
Term
|
Definition
|
|
Term
| Griseofulvin (clinical use) |
|
Definition
| Treats dermatophytes infections (ringworm infections) |
|
|
Term
| Griseofulvin (adverse effects) |
|
Definition
| Hepatotoxicity, Photosensitivity, GI irritaiton, headache, hypersensitivity |
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