What it does
Ketoconazole is an antifungal medicine that helps treat infections caused by fungi.
Commonly used for: fungal infections of the skin (like athlete's foot), fungal infections of the nails, fungal infections in the mouth or throat (oral thrush)
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Source: Pharmacy and Medicines Regulatory Authority · fetched 2026-04-21 17:37:45 · updated 2026-09-19 04:30:23
About this medicine
Ketoconazole is an antifungal medicine that helps treat infections caused by fungi.
What it treats
- fungal infections of the skin (like athlete's foot)
- fungal infections of the nails
- fungal infections in the mouth or throat (oral thrush)
How it works
It works by stopping the growth of fungi, helping to clear up the infection.
Who it's for
Ketoconazole is for adults and children with certain fungal infections.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: ketaconazole
Ketoconazole is an antifungal agent belonging to the imidazole class. It is primarily used to treat various fungal infections by inhibiting the synthesis of ergosterol, an essential component of fungal cell membranes. Ketoconazole has a broad spectrum of activity against dermatophytes, yeasts, and certain systemic fungi. Additionally, it has anti-androgenic effects, which can be beneficial in specific conditions such as Cushing's syndrome.
Indications
- Candidiasis
- Dermatophyte infections
- Tinea corporis
- Tinea pedis
- Seborrheic dermatitis
- Cushing's syndrome
Dosage
Children: Refer to specific guidelines and recommendations for appropriate dosing.
Adults: Refer to specific guidelines and recommendations for appropriate dosing.
Mechanism of action
Ketoconazole works by inhibiting the enzyme lanosterol 14α-demethylase, which is crucial for the conversion of lanosterol to ergosterol. This inhibition disrupts the fungal cell membrane integrity, leading to cell death. Ketoconazole also affects the synthesis of steroid hormones in humans by inhibiting steroidogenic enzymes, which is the basis for its use in conditions like Cushing's syndrome.
Pharmacodynamics
Ketoconazole exhibits fungistatic activity against a wide range of fungi. The drug's effectiveness is influenced by factors such as pH and concentration. At higher concentrations, ketoconazole can exert fungicidal effects. Its anti-androgenic properties arise from its ability to inhibit steroidogenesis, which can lead to decreased levels of testosterone and cortisol in the body.
Pharmacokinetics
Ketoconazole is well absorbed from the gastrointestinal tract, with absorption significantly enhanced in acidic environments. It is extensively metabolized in the liver, with a half-life of approximately 2 to 8 hours. The drug is primarily excreted in bile as metabolites, with minimal unchanged drug excreted in urine. Ketoconazole has a high volume of distribution, indicating extensive tissue binding.
Contra-indications
- Hypersensitivity to ketoconazole or any excipients
- Concomitant use with terfenadine, astemizole, or cisapride
- Liver disease
- Adrenal insufficiency
Adverse effects
- Nausea
- Vomiting
- Abdominal pain
- Headache
- Rash
- Itching
- Hepatotoxicity
- Gynecomastia
- Decreased libido
- QT interval prolongation
Interactions
- Increased plasma concentrations of drugs metabolized by CYP3A4
- Potentially increased effects of warfarin and other anticoagulants
- Concomitant use with drugs that prolong the QT interval may increase the risk of arrhythmias
Precautions
- Use with caution in patients with liver disease or history of liver dysfunction
- Monitor liver function tests during treatment
- Assess risk of adrenal insufficiency in patients on long-term therapy
- Patients should be advised to report any signs of liver dysfunction, such as jaundice or unusual fatigue
Pregnancy
Ketoconazole is classified as Category C. Use only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
Ketoconazole is excreted in breast milk. Caution should be exercised when administering to nursing mothers.
Storage
Store in a cool, dry place, away from light. Do not store above 25°C.
Formulations
- Oral tablets
- Topical cream
- Topical shampoo
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.