Products
Ketoconazole has been approved in many countries since 1981 and is now only commercially available as a shampoo and as a cream for external treatment (Nizoral, generics). Nizoral tablets were taken off the market in 2012 due to declining demand. This article refers to external use.
Structure and properties
Ketoconazole (C26H28Cl2N4O4, Mr = 531.4 g/mol) exists as a racemate and white powder that is practically insoluble in water. It is an imidazole, dioxolane, and piperazine derivative and belongs to the azole antifungals.
Effects
Ketoconazole (ATC D01AC08) has antifungal properties against dermatophytes and yeasts such as and as well as some Gram-positive bacteria. The properties are based on inhibition of the synthesis of ergosterol, which is essential for the fungal cell membrane.
Indications
The shampoo is used for the treatment and relapse prevention of diseases in which the yeast fungus is involved. These include pityriasis versicolor and seborrheic dermatitis. The cream is applied against fungal skin infections.
Dosage
According to the package insert.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
There are no known drug-drug interactions when used topically. Ketoconazole is a potent CYP inhibitor (including CYP3A4) and may cause numerous interactions when used systemically.
Adverse effects
Possible adverse effects include local reactions such as rashes and skin irritation, hypersensitivity reactions, taste disturbances, and eye irritation.
