Antifungal drug ketoconazole causes severe drug-drug interactions by influencing gene expression and catalytic activity of major drug-metabolizing enzyme cytochrome P450 CYP3A4. Ketoconazole is administered in the form of racemic mixture of two cis-enantiomers, i.e. (+)-ketoconazole and (-)-ketoconazole. Many enantiopure drugs were introduced to human pharmacotherapy in last two decades. In the...

Ketoconazole (Ketoconazole HRA™), an imidazole derivative, is a useful treatment option in the management of endogenous Cushing’s syndrome adults and adolescents > 12 years age, based on evidence from more than three decades use drug clinical practice. Originally developed as antifungal agent, ketoconazole potent steroidogenesis inhibitor. Approximately 60% (range, 45–88% across key studies) pa...

Ketoconazole is an imidazole oral antifungal agent with a broad spectrum of activity. Ketoconazole has been reported to cause liver damage, but the mechanism is unknown. However, ketoconazole and a related rug, miconazole, have been shown to have inhibitory effects on oxidative phosphorylation in fungi. Fluconazole, another orally administered antifungal azole, has also been reported to cause l...

We previously demonstrated that ketoconazole is a potent inhibitor of triazolam biotransformation in vitro and in vivo. Despite significant elevations in triazolam plasma levels with coadministration of ketoconazole, the pharmacodynamic enhancement was lower than predicted based on plasma levels of triazolam. The present study examines the effects of ketoconazole on benzodiazepine receptor bind...

Background: Seborrheic dermatitis is one of the most common skin diseases. Objective: The purpose of this study was to compare the topical and oral ketoconazole in treatment of intractable cases of seborrheic dermatitis referring to Faghihi Hospital in Shiraz. Patients and Methods: This study was performed on 80 cases of intractable seborrheic dermatitis in 1376-1378. The patients were randomiz...