Metabolic studies with probucol in hypercholesterolaemia

Probucol (1 g/day) was administered for 6 months to 16 hypercholesterolaemic patients previously stabilized on diet alone. Total plasma cholesterol fell by 16%, LDL cholesterol by 14% and HDL cholesterol by 41%. The ratio of total cholesterol to HDL cholesterol increased by 40%. Total plasma triglycerides showed a slight upward trend. The extent of the fall in HDL cholesterol was directly proportional to the pre-treatment HDL cholesterol concentration. In 2 patients studied, treatment with Probucol produced a sustained increase in the excretion of endogenous faecal steroids, due to increased faecal bile acids. In 3 patients studied, Probucol increased the degree of cholesterol saturation in gall bladder bile. The Lithogenic Index approximated to pathological levels in 1 patient whose bile was previously relatively saturated with cholesterol. Probucol also appeared to cause a modest reduction in the degree of platelet activation in vivo, with reduced platelet prostaglandin synthesis and reduced release of platelet peptides.