PHARMA Anti Fungals Flashcards
2 antifungals that are amphoteric polyene macrolides
Ampho b
Nystatin
Systemic antifungal drugs for systemic infections
Ampho b
Flucytosine
Azoles
Echinocandins
Ampho b only available in this form
Parenteral only, bc it is water insoluble and poorly absorbed in the git
DOC for systemic fungal infections except in CNS
Ampho b
Ampho b moa
Alters permeability by forming ampho b associated pores in the cell membrane, causing contents to leak out
Dosage of ampho b
0.5-1 mg per kg per day as slow IV infusion up to 1-2 g end point
2 adverse effects of ampho b
Infusion related toxicity (fever chills etc) and cumulative toxicity (renal damage)
Water soluble pyrimidine analog, good CSF penetration, related to fluoroura il
Flucytosine
Enzyme that allows flucytosine to enter fungal cells
Cytosine permease
Flucytosine MOA
Converted to 5dUMP (inhibit dna synthesis) and to FUTP (inhibit rna synthesis)
Tx for chromoblastomycosis
Flucytosine plus ampho b plus ITRACONAZOLE
First DOC for cryptococcys neoformans
Ampho b and flucytosine
Give 3 imidazoles (2 nitrogens)
Ketoconazole
Miconazole
Clotrimazole
Give 4 triazoles (3 nitrogens)
Itraconazole
Fluconazole
Voriconazole
Posaconazole
Azoles moa
Reduction of ergosterol synth by inhibiting cytP450 AND demethylation of lanosterol
Only imidazole in oral form
Ketoconazole
Topical imidazoles
Miconazole
Clotrimazole
Azole with greatest propensity to inhibit liver enzymes
Ketoconazole
2nd DOC for px and tx of cryptococcal meningitis
Fluconazole
Comes in newer formulations with better solubility and bioavailability due to CYCLODEXTRAN
Itraconazole
Azole of choice fir dimorphic fungi
Itraconazole
Tx for invasive aspergillosis, and 2 salvage therapies
DOC - itraconazole
Salvage therapy - Posaconazole and echinocandins
Azole with visual disturbances
Voriconazole
Only azole with significant activity against MUCORMYCOSIS
Posaconazole
Echinocandins moa
Inhibit beta glucan synthase
Echinocandins examples
Caspofungin
Micafungin
Anidulafungin
Systemic antifungal drugs for MUCOCUTANEOUS infections
Griseofulvin
Terbinafine
Griseofulvin vs terbinafine
Griseofulvin - fungistatic
Terbinafine - fungicidal
Terbinafine moa
Inhibits squalene epoxidase
Topical anti fungal therapy
Nystatin
Topical azoles - miconazole and clotrimazole
Topical allylamines - terbinafine and naftifine
Nystatin use
Active against most candida - thrush, vaginal candidiasis, interrtrigo