Ketoconazole
Synonym(s)
Ketoconazole
Definition
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Imidazole antifungal.
Half-life
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2 h or 6-10 h (metabolites).
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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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- Top. Anw.: Allergic reactions.
- Syst. Anw: Pruritus, alopecia, allergic to anaphylactic reactions, hepatocellular necrosis 1:1000, abdominal pain, nausea, constipation, gynecomastia.
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 ↑ |