II. Types: Azoles
- Background
- Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
- Block sterol 14-a-dimethylase (microsomal Cytochrome P450-dependent enzyme)
- Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
- Imidazoles (primarily used topically for candida and dermatophyte infections)
- Triazoles (primarily used orally for systemic fungal infections)
III. Types: Allylamine
- Background
- Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
- Inhibit squalene epoxidase, the enzyme that converts squalene to ergosterol
- Indicated in superficial dermatophyte infections resistant to imidazoles
- Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
- Medications
- Naftifine (Naftin, topical)
- Terbinafine (Lamisil)
- Topical for resistant dermatophyte infections
- Oral Terbinafine is the preferred agent for Onychomycosis
IV. Types: Polyene
- Background
- Polyenes bind to ergosterol within the fungal cell membrane
- Results in fungal cell Membrane Depolarization and increased permeability
- Fungal cell leaks key intracellular components, and ruptures
- Polyenes bind to ergosterol within the fungal cell membrane
-
Amphotericin B
- Preferred agent for deep fungal infections in pregnancy (long safety data record)
- Systemic, invasive, life-threatening fungal infections (including Meningitis, cystitis) and some protozoa infections
- Largely replaced by newer, less toxic fungicides
- Candidemia
- Symptomatic candida cystitis or Pyelonephritis
- Cryptococcal Meningitis (HIV Infection, administered with Flucytosine)
-
Nystatin (topical or mucosal use)
- Cutaneous Candidiasis (topical Nystatin)
- Candida Diaper Dermatitis
- Candidal Intertrigo
- Oral Candidiasis (Thrush)
- First-line agent
- Cutaneous Candidiasis (topical Nystatin)
V. Types: Echinocandin
- Background
- Echinocandins (Cyclic Lipopeptides) inhibit synthesis of beta-(1,3)-D-Glucan a key cell wall component
- Active against Candida species (including those resistant to Azole Antifungals) and some Aspergillus species
- Medications
- Caspofungin
- Micafungin
- Andulafungin
VI. Types: Miscellaneous
-
Flucytosine (categorized as an antimetabolite)
- Flucytosine is a Fluorouracil prodrug, a fluorinated cytosine analog with Antifungal activity
- Within fungal cells, Flucytosine is deaminated to the active metabolite 5-Fluorouracil
- 5-Fluorouracil substitutes for the Pyrimidine uracil during RNA synthesis
- Inhibits fungal Protein synthesis
- Indications: Systemic Fungal Infections
- Used with Amphotericin (risk of induced resistance when used alone)
- Cryptococcal Meningitis
- CNS Candidiasis (HIV Infection)
- Candida Pyelonephritis
-
Griseofulvin (categorized as a Benzofuran)
- Antifungal derived first in 1958 from the mold Penicillium griseofulvum
- Inhibits microtubule function in mitosis by binding tubulin in fungi
- Indications limited to Tinea Capitis as an alternative agent
VII. References
- (2012) Med Lett Drugs Ther 10(120): 61-8
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