Ketoconazole is first orally available azole antifungal for the treatment of superficial and systemic fungal infections.
Ketoconazole impairs the synthesis of ergosterol, which is a vital component of fungal cell membranes.
It has activity against a no.of candida spp.,dermatophytes, malassezia furfur and some dimorphic fungi such as Blastomycesdermatitidis and coccidioides.
Technical Specification
Ketoconazole is a synthetic broad spectrum Anti-Fungal which is white to slightly beige, odorless powder, soluble in acids, with molecular wt.of 531.44
Mean peak plasma levels of approx.3.5mcg./ml are reached in 1-2 hours of oral administration.
In Vitro Plasma Protein Binding is 99%.
About 13% of dose is excreted in urine, the major route of excretion is through the bile into intestinal tract.