Anti-Fungals Flashcards
What cellular structure do Echinocandins target?
Cell wall: glucan synthesis
What cellular structure do Polyenes and Azoles target?
Cell membrane: ergosterol synthesis
What cellular structure do Flucytosines target?
DNA/RNA synthesis: pyrimidine analogues
What is the mechanism of action of polyenes?
Bind directly to ergosterol
What are the polyenes?
Amp-B
Nystatin
How would you treat cryptococcal meningitis?
- Amp-B w/ Flucytosine
2. Fluconazole
Which azole crosses the BBB?
Fluconazole
What is the mechanism of action of Allylamines?
Inhibit fungal squalene epoxidase –> cannot convert squalene to lanosterol
Interfere with ergosterol synthesis
What is ergosterol?
Sterol that is part of the fungal bilayered cell membrane
What are fungal cell walls comprised of?
90% chitin, GLUCAN, mannan
10% proteins, glycoproteins
What do anti-fungals target?
Proteins
Nucleus
Cell wall, especially glucan
Cell membrane, especially ergosterol
Effective anti-fungals typically have a _____, which leads to ______.
High therapeutic index / many adverse side effects
What was the first anti-fungal and when was it approved?
Nystatin – 1954
What class of anti-fungals is Terbinafine?
Allylamine (targets squalene epoxidase)
What is the mechanism of action of Azoles?
Bind to and inhibit cytochrome p450 and 14-alpha demethylase –> cannot convert lanosterol to ergosterol