Effects of long-term ketoconazole therapy on serum lipid levels

Summary Serum cholesterol and triglycerides were determined in 36 patients receiving an 8-month course of oral ketoconazole 200 mg/day in order to study its effect on lipid metabolism. The mean serum cholesterol concentration had decreased by 15% (p<0.001) after 1 month, but on continued medication it returned to the pretreatment state; after discontinuation of therapy it increased transiently by 13% (p<0.001). Triglycerides increased during ketoconazole administration and at the end of the trial the mean triglyceride concentration was 48% higher than the baseline value (p<0.02). Although most lipid values during therapy lay within the normal ranges, 6 patients developed transient hypertriglyceridaemia. There was no correlation between the changes in lipids and peak serum ketoconazole levels. In one subject studied in more detail the concentration of very low density lipoprotein triglycerides rose during therapy, whereas high density lipoprotein cholesterol decreased slightly. The lipoprotein lipase activity in muscle and, in particular, in adipose tissue was significantly suppressed during ketoconazole treatment. Serum lipids and, if possible, serum lipoproteins should be carefully monitored in patients receiving long-term oral ketoconazole therapy.