Fungi
6 flashcards · Other · by Jared Blackwell
Amphotericin B
Bind to ergosterol causing pores that leak K+ causing cell death. Kinetics are non-linear; t ½ is 15 days. Can find drug up to 6 weeks later; Little drug metabolism. Start with daily injection then go to 3 times a week. Side Effect: fever & chills, cardiac arrhythmias, 1. Renal toxicity causing K+, Mg++ wasting 2. Renal tubular acidosis 3. Suppresses EPO à Anemia. Give dose of Meperidine to mitigate Fever and Chills. b. Nystatin – only used topically because very toxic. Oral candidiasis, vagina…
Flucytosine
Only used for cryptococcus meningitis with addition of amphotericin B
Triazoles
Bind to CYP51 blocking demethylation of Lanosterol, an ergosterol precursor. Can NOT make ergosterol causing disruption of cell membrane integrity. a. Yeasts; Cryptococcus & Candida = Fluconazole b. Dimorphic; Histoplasma, Blastomyces, Coccidiodes = Itraconazole c. Molds; aspergillus & mucorales = Voriconazole, Posaconazole, itraconazole, isavuconazole.
Echinocandins
Inhibits cell wall synthesis of 1,3 B glucan by blocking interaction of UDP-glucose and glucan synthase subunit Rho Only for Candida & Aspergillus.
Terbinafine
Inhibits squalene epoxidase blocking conversion of squalene to ergosterol Onychomycosis, Tinea capitis, Sporotrichosis.
Nikkomycin
Chitin inhibitor used for dimorphic fungi i.e. Blastomyces, Coccidiodes.