II. Types: Azoles

  1. Background
    1. Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
      1. Block sterol 14-a-dimethylase (microsomal Cytochrome P450-dependent enzyme)
  2. Imidazoles (primarily used topically for candida and dermatophyte infections)
    1. Clotrimazole
    2. Miconazole
    3. Ketoconazole
  3. Triazoles (primarily used orally for systemic fungal infections)
    1. Fluconazole
    2. Isavuconazole
    3. Itraconazole
    4. Voriconazole
    5. Posaconazole

III. Types: Allylamine

  1. Background
    1. Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
      1. Inhibit squalene epoxidase, the enzyme that converts squalene to ergosterol
    2. Indicated in superficial dermatophyte infections resistant to imidazoles
  2. Medications
    1. Naftifine (Naftin, topical)
    2. Terbinafine (Lamisil)
      1. Topical for resistant dermatophyte infections
      2. Oral Terbinafine is the preferred agent for Onychomycosis

IV. Types: Polyene

  1. Background
    1. Polyenes bind to ergosterol within the fungal cell membrane
      1. Results in fungal cell Membrane Depolarization and increased permeability
      2. Fungal cell leaks key intracellular components, and ruptures
  2. Amphotericin B
    1. Preferred agent for deep fungal infections in pregnancy (long safety data record)
    2. Systemic, invasive, life-threatening fungal infections (including Meningitis, cystitis) and some protozoa infections
      1. Largely replaced by newer, less toxic fungicides
      2. Candidemia
      3. Symptomatic candida cystitis or Pyelonephritis
      4. Cryptococcal Meningitis (HIV Infection, administered with Flucytosine)
  3. Nystatin (topical or mucosal use)
    1. Cutaneous Candidiasis (topical Nystatin)
      1. Candida Diaper Dermatitis
      2. Candidal Intertrigo
    2. Oral Candidiasis (Thrush)
      1. First-line agent

V. Types: Echinocandin

  1. Background
    1. Echinocandins (Cyclic Lipopeptides) inhibit synthesis of beta-(1,3)-D-Glucan a key cell wall component
    2. Active against Candida species (including those resistant to Azole Antifungals) and some Aspergillus species
  2. Medications
    1. Caspofungin
    2. Micafungin
    3. Andulafungin

VI. Types: Miscellaneous

  1. Flucytosine (categorized as an antimetabolite)
    1. Flucytosine is a Fluorouracil prodrug, a fluorinated cytosine analog with Antifungal activity
    2. Within fungal cells, Flucytosine is deaminated to the active metabolite 5-Fluorouracil
      1. 5-Fluorouracil substitutes for the Pyrimidine uracil during RNA synthesis
      2. Inhibits fungal Protein synthesis
    3. Indications: Systemic Fungal Infections
      1. Used with Amphotericin (risk of induced resistance when used alone)
      2. Cryptococcal Meningitis
      3. CNS Candidiasis (HIV Infection)
      4. Candida Pyelonephritis
  2. Griseofulvin (categorized as a Benzofuran)
    1. Antifungal derived first in 1958 from the mold Penicillium griseofulvum
    2. Inhibits microtubule function in mitosis by binding tubulin in fungi
    3. Indications limited to Tinea Capitis as an alternative agent

VII. References

  1. (2012) Med Lett Drugs Ther 10(120): 61-8

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Cost: Medications

antifungal (on 8/23/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
ANTIFUNGAL 1% CREAM Generic OTC $0.10 per gram
ANTIFUNGAL 1% TOPICAL CREAM Generic OTC $0.16 per gram
ANTIFUNGAL 2% POWDER Generic OTC $0.05 per gram