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Antifungals

Last updated: January 2, 2020

Summary

Antifungals are used in the treatment of mycotic infections such as candidiasis, cryptococcal disease, aspergillosis, and dermatophytosis. They are primarily divided into three major groups (polyenes, azoles, and allylamines) and are differentiated based on their chemical structure and specific spectrum of efficacy. Whereas intravenous broad-spectrum antifungals (such as fluconazole or lipid formulations of amphotericin B) cover almost all known fungi, topical agents (such as clotrimazole) often have a limited scope of activity. Hepatotoxicity, skin reactions, headaches, and gastrointestinal symptoms are common side effects.

Substances

Substance class Active substance Mechanism of action Clinical use Characteristics Important adverse effects

Polyenes

  • Very broad spectrum of efficacy
  • Available as
  • Important contraindications
    • Renal dysfunction
    • Hepatic dysfunction
  • Pregnancy and breastfeeding: not generally recommended in breastfeeding mothers
  • Nystatin (topical, oral )
Azoles Imidazole derivatives
  • Clotrimazole (topical, oral)
  • Broad spectrum of efficacy
  • Local burning, reaction, and/or pruritus
  • Miconazole (topical, oral)
  • Broad spectrum of efficacy
  • Ketoconazole (topical, oral)

Triazole derivatives

  • Fluconazole (oral, IV)
  • Voriconazole (oral, IV)
  • Itraconazole (oral)

Allylamine derivatives

  • Terbinafine (oral, topical)

Echinocandins

  • Caspofungin (IV)
  • Anidulafungin (IV)
  • Micafungin (IV)
  • Broad spectrum efficacy
  • Only minimal distribution to the CSF

Pyridone derivatives

  • Ciclopirox (topical)

Benzofurans

  • Griseofulvin (oral)
Antimetabolites
  • Flucytosine (oral)
  • Converted to 5-fluorouracil by fungal cytosine deaminase, which then inhibits DNA and RNA synthesis
  • Monotherapy: select cases of non-life-threatening infections such as genitourinary candida infections that are not covered by alternative drugs
  • Combination with amphotericin B: systemic fungal infections (especially cryptococcal meningitis)


CNS penetration of fluconazole: “FLU through the blood-brain barrier”

Voriconazole is the drug of choice for inVasive aspergillosis.

References:[1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24]

Treatment of common fungal infections

Suggested treatment
Candidiasis

Aspergillosis

Cryptococcosis

Blastomycosis

Histoplasmosis

Coccidioidomycosis

Sporotrichosis

Tinea versicolor
Dermatophytosis

References:[25][26]

References

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