• Clinical science

Antifungals (Antimycotics)


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.


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


  • Very broad spectrum of efficacy
  • Available as
  • Important contraindications
    • Renal dysfunction
    • Hepatic dysfunction
  • Pregnancy and breastfeeding: not generally recommended in breastfeeding mothers
Azoles Imidazole derivatives
  • Broad spectrum of efficacy
  • Local burning, reaction, and/or pruritus
  • Broad spectrum of efficacy
  • Broad spectrum of efficacy
  • Pregnancy and breastfeeding
  • Important contraindications
    • Cardiac arrhythmias (e.g., prolonged QT)
    • Severe cardiac insufficiency
    • Avoid cross-reactions with drugs metabolized by cytochrome P-450
  • Use with caution in patients with:
    • Renal dysfunction
    • Hepatic dysfunction
  • If given orally, discontinue PPIs, as they require a low pH to be absorbed

Triazole derivatives

Allylamine derivatives

  • Inhibit fungal squalene epoxidase, which decreases ergosterol synthesis


  • Inhibit synthesis of β-glucan (a component of the fungal cell wall)
  • Broad spectrum efficacy
  • Only minimal distribution to the CSF
  • Flushing
  • Hypotension
  • Hepatotoxicity
  • Gastrointestinal upset
  • Phlebitis/pain at injection site
  • Fever, shivering

Pyridone derivatives

  • Broad spectrum efficacy
  • Important contraindications: do not apply to eye or mucous membranes


  • Narrow range of efficacy
  • Important contraindications: porphyria, hepatic failure
  • Avoid during pregnancy and breastfeeding
  • Hepatotoxicity
  • Rashes and severe skin reactions (e.g., Stevens-Johnson syndrome)
  • Urticaria
  • Carcinogenic
  • Teratogenic
  • Induces cytochrome P-450↓ concentration of many drugs metabolized by P-450 (e.g., warfarin)
  • 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)
  • Use with extreme caution in patients with renal impairment
  • Avoid during pregnancy and breastfeeding
  • Hepatic injury
  • Renal failure
  • Gastrointestinal (e.g. nausea)
  • Bone marrow suppression with pancytopenia

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

Voriconazole is the drug of choice for inVasive aspergillosis.


Treatment of common fungal infections

Suggested treatment







Tinea versicolor