Description
Mechanism of Action
Ketoconazole interferes w/ biosynthesis of triglycerides and phopholipids by blocking fungal CYP450, thus altering cell membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen peroxide.
Absorption: Variably absorbed from the GI tract, may be increased w/ decreasing gastric pH. Minimally absorbed systemically (topical). Time to peak plasma concentration: Approx 2 hr (oral).
Distribution: Widely distributed, CSF (poor penetration); enters breast milk. Plasma protein binding: >90% (mainly albumin).
Metabolism: Partially hepatic via CYP3A4 converted to inactive metabolites.
Excretion: Via faeces (57%); urine (13%). Half-life: Initial (2 hr), terminal (approx 8 hr).
MIMS Class
Antifungals / Topical Antifungals & Antiparasites / Psoriasis, Seborrhea & Ichthyosis Preparations
ATC Classification
D01AC08 – ketoconazole; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.;
G01AF11 – ketoconazole; Belongs to the class of imidazole derivative antiinfectives. Used in the treatment of gynecological infections.;
J02AB02 – ketoconazole; Belongs to the class of imidazole derivatives. Used in the systemic treatment of mycotic infections.;
