Ketaconazole toxicity

In addition to allergies, dose-dependent gastrointestinal disturbances, including nausea, anorexia, and vomiting, are the most common adverse effects of ketoconazole treatment. Endocrine effects, such as gynecomastia, decreased libido, impotence, and menstrual irregularities, result from the blocking of androgen and adrenal steroid synthesis by ketoconazole. Transient increases in serum transaminases occur in 2 to 10 percent of patients receiving ketoconazole.Frank hepatitis occurs rarely, but requires immediate cessation of ketoconazole treatment.[Note: Ketoconazole may accumulate in patients with hepatic dysfunction.Plasma concentrations of the drug should be monitored in these individuals.]immediate cessation of ketoconazole treatment. [Note: Ketoconazole may accumulate in patients with hepatic dysfunction. Plasma concentrations of the drug should be monitored in these individuals.]By inhibiting CYP450, ketoconazole can potentiate the toxicities of drugs such as cyclosporine, phenytoin, triazolam, and warfarin, among others Rifampin, an inducer of the CYP450 system, can shorten the duration of action of ketoconazole and the other azoles. Drugs that decrease gastric acidity, such as H2-receptor blockers, antacids, proton-pump inhibitors, and sucralfate, can decrease absorption of ketoconazole. Ketoconazole and amphotericin B should not be used together, because the decrease in ergosterol in the fungal membrane reduces the fungicidal action of amphotericin B ketoconazole is teratogenic