Ketoconazole For prostate cancer


UsesBroad spectrum antifungal agent used to treat fungal infections on the skin and nails

.Class: Azole Antifungals

 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

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