Abstract

Nineteen hypercholesterolaemic patients were randomly treated with either 16 or 8 g cholestyramine with a changeover after 6 weeks for a second 6-week period. During a third consecutive 6-week period all patients received 4 g cholestyramine daily. The low density lipoprotein (LDL) cholesterol and triglyceride concentrations decreased significantly (−11%, −21% and −26% for LDL cholesterol on 4, 8 and 16 g, respectively) with a dose-response effect. However, the increase from 8 g to 16 g only caused a modest additional reduction of the lipid levels. The serum concentration of apolipoprotein (apo) B was correlated to the LDL cholesterol and decreased similarly in a dose-response fashion. However, the average reduction of apo B was less pronounced (−4%, − 13% and −17% on 4, 8 and 16 g of cholestyramine, respectively) resulting in a significant change of the apo, B/LDL cholesterol ratio during treatment. There was a significant increase of the high density lipoprotein (HDL) cholesterol concentration, which was similar at all dose levels. Also, the apo A-1 concentration in serum increased significantly but the relative decrease was less pronounced than that of HDL cholesterol, causing a significant decrease of the apo A-I/HDL cholesterol ratio. The apo A-11 concentration in serum was unchanged or slightly decreased and the apo A-1/apo A-II ratio increased significantly. The lipoprotein (a) [Lp(a)] distribution was markedly skewed before treatment, without any significant correlations between the serum concentrations of Lp(a) and other lipid or apolipoprotein concentrations. The serum concentration of Lp(a) was not affected by treatment with cholestyramine and there was no significant correlation between the change of Lp(a) and the change in LDL cholesterol or apo B. The absence of effect on Lp(a) concentrations in serum by cholestyramine treatment may indicate that the major route of Lp(a) metabolism is not identical with that of LDL.

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