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Pharm Chapter34

Pharmacology of Fungal Infections

QuestionAnswer
MOA Flucytosine flucytosine is converted to 5FdUMP, which inhibits thymidylate synthase and thereby interferes with DNA synthesis
clinical applications flucytosine candidiasis, cryptococcosis, chromomycosis
Adverse effects flucytosine Bone marrow suppression (leukopenia, thrombocytopenia), GI disturbance, hepatic dysfunction
Contraindications flucytosine, griseofulvin pregnancy
In combination with what is flucytosine effective against Aspergillus? Amphotericin B
MOA griseofulvin binds to tubulin and a microtubule associated protein, thereby disrupting assembly of the mitotic spindle
Clinical applications griseofulvin fungal infection of the skin hair, or nail due to Tricophyton, Microsporum, or Epidermophytan
Adverse effects griseofulvin hepatotoxicity, albuminuria, leukopenia, neutropenia, monocytosis, seru sickness, angioedema, toxic epidermal necrolysis, headache, lethargy, vertigo, blurred vision (inc. with alcohol), increased fecal protoporphyrin levels
MOA terbinafine (allylamine), naftifine (allylamine), butenafine (benzylamine) Inhibit conversion of squalene to lanosterol by inhibiting squalene epoxidase
Clinical applications terbinafine, naftifine, butenafine Onychomycosis (terbinafine), tinea corporis, tinea cruris, tinea pedis, tinea capitis
Adverse effects terbinafine, naftifine, butenafine hepatotoxicity, Stevens-Johnson syndrome, neutropenia, exacerbation of psoriasis or subacute cutaneous lupus erythmatosus (oral terbinafine)
Contraindication terbinafine Renal or hepatic failure, pregnancy
Coadministration with what increases plasma levels of terbinafine? cimetidine
Coadministration with what decreases plasma levels of terbinafine? rifampin
Inhibitors of 14alpha-sterol demthylase Imidazoles- ketoconazole, butoconazole, clotrimazole, econazole, miconazole, oxconazole, sertaconazole, sulconazole; Triazoles - fluconazole, itraconazole, posaconazole, terconazole, voriconazole
Clinical applications ketoconazole Coccidioides immitis, Cryptococcus neoformans, Candida species, Histoplasma capsulatum , Blastomyces dermatitidis, variety of dermatophytes
Adverse effects ketoconazole GI disturbance, hepatic dysfunction, gynecomastia, decreased libido, menstrual irregularities
Clinical applications butoconazole, clotrimazole, econazole, miconazole, oxconazole, sertaconazole, sulconazole superficial fungal infections of the stratum corneum, squamous mucosa, and cornea
Adverse effects butoconazole, clotrimazole, econazole, miconazole, oxconazole, sertaconazole, sulconazole Pruritus and burning
Clinical applications fluconazole candidiasis, cryptococcal meningitis (inhibit P450 3A4)
Adverse effects fluconazole nausea, vomiting, abdominal pain, diarrhea
Clinical applications itraconazole aspergillosis, blstomycosis, candidiasis, histoplasmosis, onychomycosis (inhibit P450 3A4)
Adverse effects itraconazole Hepatic toxicity, Stevens-Johnson syndrome, GI disturbance
Clinical applications posaconazole aspergillosis, zygomycosis
Clinical applications terconazole vaginal candidiasis
Clinical applications voriconazole aspergillosis, candidiasis, Fusarium, Monosporium apiospermum
Adverse effects voriconazole Hepatic toxicity, photophobia and colored lights
MOA polyenes - amphotericin B, nystatin bind to ergosterol and form pores that alter fungal membrane permeability and stability
Clinical applications amphotericin B Potentially life-threatening aspergillosis, crytococcosis, North AMercan blastomycoses, systemic candidiasis, coccidioidomycosis, histoplasmosis, systemic candidiasis, zygomycosis
Adverse effects amphotericin B Renal toxicity (renal tubular acidosis, cylindruria, hypokalemia), cytokine storm (fever, chills, hypotension), anemia
Clinical applications nystatin mucocutaneous candidiasis
MOA echinocandins- - caspofungin, micafungin, anidulafungin Noncompetitively inhibit synthesis of Beta-(1,3)-D-glucans, which leads to disruption of cell wall integrity
Clinical applications caspofungin esophageal candidiasis, candidemia, salvage therapy of Aspergillus infections, empiric therapy of febrile neutropenia
Clinical applications micafungin esophageal candidiasis, antifungal prophylaxis for recipients of hematopoietic stem cell transplants
Clinical applications anidulafungin esophageal candidiasis, candidemia
Adverse effects caspofungin, micafungin, anidulafungin pruritus, rash, increased liver enzymes, headache, fever
Coadministration of what increases plasma concentration of caspofungin and elevates liver function enzymes? cyclosporine
Created by: 7958184
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