Ketoconazole, a widely used fungicide in patients, has been associated with Q-T prolongation and torsade de pointes when co-administered with terfenadine (Seldane). Both compounds use the same cytochrome-P450 metabolic pathway, resulting in an increase in plasma concentration of terfenadine. We previously showed that terfenadine blocked HERG (Human Ether-a-Gogo Related Gene), an important compo...

AIMS Two clinical studies were conducted to determine possible drug-drug interactions between apremilast and a strong CYP3A4 inhibitor, ketoconazole, or a potent CYP3A4 inducer, rifampicin. The main objectives of these two studies were to evaluate the impact of multiple doses of ketoconazole on the pharmacokinetics of apremilast and its metabolites, and the effect of multiple oral doses of rifa...

BACKGROUND Many medicines, including several cholesterol-lowering agents (eg, lovastatin, simvastatin), antihypertensives (eg, diltiazem, nifedipine, verapamil), and antifungals (eg, ketoconazole) are metabolized by and/or inhibit the cytochrome P450 (CYP) 3A4 metabolic pathway. These types of medicines are commonly coprescribed to treat comorbidities in patients with type 2 diabetes mellitus (...

Human peripheral blood lymphocytes stimulated with Histoplasma capsulatum yeasts were exposed in culture to graded concentrations of ketoconazole or amphotericin B and subsequently assessed for membrane integrity, thymidine uptake, and blastogenesis. Lymphocyte reactivity varied with concentration and duration of exposure to ketoconazole. Overt membrane toxicity resulted from exposure to 40 mic...

This paper describes a sensitive spectrophotometric method developed for determination of Ketoconazole (KC) in tablets based on amplification reactions. Ketoconazole was oxidized with periodate, resulting in formation of KC2+ and iodate ions. After masking the excess periodate with molybdate, the iodate was treated with iodide to release iodine. The liberated iodine was transformed to [Formula:...

The three imidazole antimycotics clotrimazole, miconazole, and ketoconazole all inhibit the demethylation of lanosterol to ergosterol, resulting in inhibition of growth of Saccharomyces cerevisiae; this is a fungistatic action. At higher concentrations clotrimazole and miconazole are fungicidal, whereas ketoconazole is not. The fungicidal action reflects direct membrane damage by the imidazoles...

The oxidation of ketoconazole on a bare carbon paste electrode was studied voltammetrically. The results indicated that the process is irreversible and controlled by an adsorption-extraction process which allows the accumulation of the drug at the electrode surface. After the optimization of solution pH, accumulation variables and instrumental parameters, sensitive differential pulse and linear...

Background: Tinea versicolor is a superficial fungal infection caused by normal skin flora and treatable by topical and oral anti-fungal medications. Objective: To evaluate the clinical and paraclinical response and to compare possible side-effects of a single oral dose of fluconazole and ketoconazole in treatment of tinea versicolor. Patients and Methods: In this clinical trial, sixty-si...

K etoconazole, an imidazole derivative, is a broad-spectrum antifungal agent. The development of gynecomastia in some men receiving ketoconazole fostered research into the drug's inhibitory effects on the production of testosteronel 2 and, subsequently, other steroid hormones.3-5 Ketoconazole has been used in the treatment of adrenocorticotropic hormone (ACTH)-dependent Cushing's syndrome (Cush...