Ketoconazole

Author: Prof. Dr. med. Peter Altmeyer

Our authors

Last updated on: 29.10.2020

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Synonym(s)

Ketoconazole

Definition
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Imidazole antifungal.

Half-life
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2 h or 6-10 h (metabolites).

Pharmacodynamics (Effect)
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Inhibition of the ergosterol synthesis of the fungal cell membrane of dermatophytes, yeasts and moulds.

Indication
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Mycoses of the skin, hair and mucous membrane, caused by dermatophytes, candida and other pathogens. Organ and system mycoses, fungal prophylaxis, chronic recurrent vaginal mycoses.

Limited indication
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Diabetes mellitus, nursing.

Dosage and method of use
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  • Topical:
    • Mycoses and candidoses of the skin: Apply cream thinly to the affected areas 1-2 times/day for 2-3 weeks or apply solution once/day for max. 5 days.
    • Seborrheic eczema: Cream: Apply 2 times/day for 4 weeks on the affected areas. Solution: 2 times/week for 2-4 weeks, apply half a cap to damp hair, massage in, leave on for 3-5 minutes, then rinse with warm water. To prevent recurrence, apply at 1-2 weekly intervals for 4 months.
  • Systemic:
    • 1 time a day 200 mg p.o. for 1-2 months.
    • Vaginal mycoses: 1 time per day 400 mg p.o. for 5-10 days.
    • Children from 2 years up to 20 kg KG: once/day 50 mg p.o.
    • Children up to 30 kg KG: once/day 100 mg p.o.

Remember! Exclude pregnancy by pregnancy test before the therapy. Women of childbearing age must use effective contraception during the therapy!

Standard concentration
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2% as cream or solution.

Undesirable effects
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Interactions
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s. Table 1.

Contraindication
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  • Topical: Use on the eye, imidazole hypersensitivity.
  • Systemic: Imidazole hypersensitivity, chron. alcohol abuse, acute or chronic liver disease, pregnancy, prostate cancer.

Preparations
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Nizoral, Terzolin

Tables
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Main interactions of ketoconazole

Alcohol

Disulfiram-like reactions

Antacids

Ketoconazole level ↓ (to be taken at 2-hour intervals)

Anticoagulants, oral

Bleeding tendency ↑

Barbiturates

Avoid combination, increased hang-over

Ciclosporin A

Ciclosporin levels ↑

Didanosine

Didanosine effect ↓ (take ketoconazole 2 hours before didanosine)

Isoniazid

Ketoconazole levels ↓

Phenytoin

Phenytoin level ↑, Ketoconazole level ↓

Prednisolone

Prednisolone mirror ↑

Rifampicin

reciprocal effect ↓ (take in 12 hours interval)

Theophyllins

Theophylline toxicity ↑

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Last updated on: 29.10.2020