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Uses: Broad spectrum antifungal agent used to treat fungal infections on the skin and nails
.Class: Azole Antifungals
Mechanisom Of a*ction: Ketoconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol
This results in inhibition of ergosterol synthesis and increased fungal cellular permeability
Other mechanisms may involve the inhibition of endogenous respiration, intera*ction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis.
Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone
m*etabolism: Hepatic
Protein binding: 99% binding
Half Life: 2 Hours
Toxicity: Enzyme inhibitor lead to hepatotoxicity
Absorption: Moderate, Need Acidic medium to be completely absorped
it was noticed that a small number of male patients developed painful gynaecomastia; this led to the discovery of the inhibitory effects of the drug on gonadal and adrenal steroidogenesis. Ketoconazole has been shown to be a useful second-line treatment in patients with advanced prostate cancer, but its use has been limited by concerns over its adverse effects (notably those on the liver). Recent re-evaluation of the literature has suggested, however, that these concerns have been overstated and that the most serious potential adverse effects of ketoconazole can be avoided in the majority of patients