Amphotericin
- Polyene macrolide
- Broad-spectrum
- 1st line treatment for systemic fungal infections due to Candida, Cryptococcus & Aspergillus
- Adverse: Fever, Chills & Nausea
- Long-term therapy: renal damage
- Liposomal formulations (less toxic)
- Selectively toxic to ergosterol
- MOA:
1) Binds to ergosterol of fungal cell membrane
2) Pores form in membrane
3) Membrane becomes unstable
4) Fungal cell constituents escape

Nystatin
- Polyene macrolide
- Treat skin & mucous membrane infection due to C. albicans
- MOA:
1) Binds to ergosterol of fungal cell membrane
2) Pores form in membrane
3) Membrane becomes unstable
4) Fungal cell constituents escape

Flucytosine
-Synthetic pyrimidine antimetabolite
- Less toxic than amphotericin
- Active against yeast
- Treat systemic candidiasis or cryptococcal infections
- MOA:
1) Converted in fungal cells to fluorouracil
2) Fluorouracil competes with uracil 3) RNA & protein synthesis is interfered
4) Synthesis of nucleic acid in fungi is inhibited as a result.
- Use is limited:
i) Narrow-spectrum
ii) Resistance to drug can rapidly develop
iii) Synergistic antifungal activity when taken with Amphotericin

Imidazole
- Broad-spectrum
- Often for topical use
- Treat infections due to dermatophytes OR C. albicans
- Not effective against Aspergillus
- MOA:
i) Inhibit lanosterol 14 alpha-demethylase
ii) Ergosterol synthesis is inhibited as a result

Triazole
- Similar structure to imidazole
- Wider antifungal activity than imidazole
- Less adverse events than imidazole due to specificity
- MOA:
1) Inhibit lanosterol 14 alpha-demethylase
2) Ergosterol synthesis is inhibited as a result

Griseofulvin
- Treat some dermatophyte
infections (Eg. Scalp ringworm)
-MOA: Inhibits fungal mitosis

Terbinafine
- Allylamine
- Treat dermatophyte infections of skin & nails
- MOA:
1) Inhibit squalene epoxide
2) Ergosterol synthesis is inhibited as a result
3) Squalene accumulates, which is toxic

Echinocandins
-MOA:
1) Inhibit Beta-(1,3)-D-glucans
2) Fungal wall synthesis is inhibited as a result
3) Osmotic stress builds
4) Fungal cell lyses

	Created by wade.barrett777 over 9 years ago

Bachelors Anti-infectives (Anti-fungals) Note on Anti-fungals, created by wade.barrett777 on 12/03/2015.