Antifungal Drugs & Fungi B- Exam IV Flashcards
(99 cards)
Why are there fewer effective antifungal agents?
because of the similarity of human cells and fungal cells
It is easier to treat ___ fungal infections than ____ fungal infections
superficial mycoses; systemic infections
Sterol found in fungal cell membranes; human cells have cholesterol instead of tis:
ergosterol
Where is ergosterol found?
in fungal cell membranes
Antifungal treatment that binds ergosterol in fungal membranes:
polyene compounds
Give an example of a polyene compound that is used to treat systemic disease:
amphotericin B
Given an example of a polyene compound that is used to treat topical disease:
nystatin
Polyene compounds cause ___, leading to:
altered membrane permeability; leakage of cell constituents & cell death
Polyenes bind ____ in mammalian cells but this is less strongly than they bind ___
cholesterol; ergosterol
What is the basis for drug toxicity with the polyene compounds?
their ability to bind cholesterol in mammalian cells
Why is fillipin a potent but toxic anti-fungal agent?
due to the binding of cholesterol
Terbinafine (TBF) acts on the Ergosterol biosynthetic pathway at the ____ step.
squalene epoxidase
Itraconazole (ITZ) acts on the Ergosterol biosynthetic pathway at the ____ step.
C-14 demethylase
Function to block ergosterol synthesis by inhibiting squalene epoxidase activity:
Allylamines
Give an example of an Allylamine that functions to block ergosterol synthesis:
Terbinafine (TBF)
Allylamines are mainly effective on the:
dermatophytes
What form of allylamines are most effective on dermatophytes?
topical or tablet formulations
Function to block ergosterol synthesis by inhibiting cytochrome P450-dependent 14(alpha)-lanosterol demtheylation:
azoles
What was the first oral azole?
Ketoconazole
What are some downfalls to ketoconazole? (the first oral azole)
significant numbers of side effects and drug interactions
What was created to supersede/replace ketoconazole?
Itraconazole
Itraconazole is preferred over ketoconazole because:
active against many fungi and has improved safety profile
What fungal species is itraconazole effective against?
- candida species
- cryptococcus
- aspergillus
- endemic (systemic) fungi
- dermaphytes
antifungal agent that inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of fungal cells walls
Echinochandins