Ketoconazole

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Therapeutic Indication

Systemic fungal infections
Dermatophytosis (ringworm, athlete’s foot, jock itch)
Candidiasis (oral, esophageal, systemic)
Blastomycosis, histoplasmosis, and other deep fungal infections
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Ketoconazole

Tablet

Ketoconazole is an imidazole antifungal agent used to treat systemic and superficial fungal infections. It works by inhibiting fungal cytochrome P450 enzymes, blocking ergosterol synthesis, and disrupting fungal cell membrane integrity. Ketoconazole is effective against dermatophytes, yeasts, and certain systemic fungi.

Speciality Antifungal Agent
Tags Antifungal | Dermatophytosis | Candidiasis | Systemic Fungal Infection
Strength
  • 200 mg
Packing Size
  • 10 Tablets

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Mechanism

Ketoconazole inhibits fungal cytochrome P450-dependent enzymes, blocking ergosterol synthesis. This leads to disruption of fungal cell membrane structure and function, resulting in fungal cell death.

Pharmacokinetics

  • Absorption: Oral absorption enhanced by acidic gastric environment
  • Distribution: Widely distributed in tissues, protein bound
  • Metabolism: Extensive hepatic metabolism via CYP3A4
  • Elimination: Primarily fecal excretion
  • Half-life: 6–8 hours

Side Effects

  • Nausea and vomiting
  • Abdominal pain
  • Pruritus and rash
  • Liver enzyme elevation
  • Rare adrenal suppression

Contraindication

  • Hypersensitivity to Ketoconazole
  • Severe hepatic impairment

Interaction

  • Strong CYP3A4 inhibitor — interacts with statins, anticoagulants, certain antihistamines
  • Antacids and proton pump inhibitors reduce absorption
  • Co-administration with hepatotoxic drugs increases risk of liver injury
  • Requires caution with immunosuppressants (e.g., cyclosporine, tacrolimus)

Warning and Precautions

  • Monitor liver function during therapy
  • Use cautiously in patients with adrenal insufficiency
  • Avoid alcohol during treatment (risk of hepatotoxicity)