Ketoconazole
Uses: Broad spectrum antifungal agent used to treat fungal infections on the skin and nails
Mechanisom Of action: 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, interaction 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
Metabolism: 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