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IOS 11 Exam 1

Antifungal Pharmacology/Drug Interactions

QuestionAnswer
What are targets for antifungal medications (7) membrane dysruption, ergosterol synthesis inhibitors, nucleic acid inhibitor, anti-mitotic, Glucan synthesis inhibitors, Chitan synthesis inhibitors, Protein synthesis inhibitors
Nystatin MOA Bings ergosterol in fungal cell membrane & alters membrane permibility releasing intracellular K, sugars, and metabolites
Nystatin- SE nausea, vomiting, diarrhea, and Gi discomfort
Nystatin spectrum of activity Fungicidal- Oral candidiasis, mucocutaneous infections, gut decontamination
Amphotericin B- MOA Binding to ergosterol leading to intercalation of cell membrane causin leakage of K, sugars, and metabolites
Amphotericin B- ADME Insoluble in water, not absorbed, 95% protein bound, biphasic elimentation via bile and feces t=1-2 days and t2=several
Amphotericin B PD Concentration dependant
Amphotericin B DI Other nephrotoxins and agents that effect electrolytes
Spectrum of activity of Amphotericin B Candida spp. Aspergillus, Cryptococcus neoformans, Mucor, Blastomyces dermatitidis, Histoplasma capsulatum, Paracoccidioides
Griseofulvin MOA Inhibits the spindle and cytoplasmic microtubule function--Old drug we do not use
Azoles MOA Bind C-14 alpha demethylase blocking the conversion of lantosterol to form ergesterol
Fluconazole ADME Good absorption, Complete distribution, Renal elimination
Posasonasole ADME 400mg of Absorption max, highly protein bound, and hepatic clearance
Azoles PD Time dependant
Voriconazole DI's many- Rifampin, phenytoin, carbamezepine, phenobarbital, warfarin, loratidine, protease inhibitors, chemotheraputics
Fluconazole spectrum of activity Candida, cryptoccus neoformans, histoplasma, balstomycosis, coccidimycosis
Voriconazole specturm of activity Candida, cryptoccus neoformans, histoplasma, balstomycosis, coccidimycosis, Fusarium, Scedosporium
Posaconazole spectrum of resistance Candida, cryptoccus neoformans, histoplasma, balstomycosis, coccidimycosis, Fusarium, Scedosporium, Zygomycetes
Flucytosine MOA Inhibition of cytosine deaminase which is intrinsic only in fungi. Leads to decrease in 5FU and decrease in DNA synthesis.
Flucytosine ADME Oral form- good distribution,low protein binding, great distribution, renal elimination, Monitor serum levels
Fungistatics are Azoles, Flucytosine
Fungicidals are Nystatin, Amphotericin B, Caspofungin, nikkomycin
Crytpotoccal meningitis Combination therapy Flcytosine + Amphotericin B
Trichosporon Combination therapy Fluconazole +Amphotericin B
Azole + AmB In theory not an ideal combination. Azole depletes ergosterol and AMb needs ergosterol.
Created by: liza001
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