Long‐Term Oral Administration of Probucol [4, 4‘‐(Isopropylidenedithio) bis (2, 6‐di‐t‐Butylphenol)] (DH‐581) in the Management of Hypercholesterolemia*

Abstract

ABSTRACT: Fifty patients who received a new hypocholesterolemic agent, probucol, in a dosage of 0.5 gm twice daily, were studied for one year. Mean pretreatment serum cholesterol and triglyceride values were 329 mg/100 ml and 360 mg/100 ml respectively. Baseline lipoprotein electrophoreses showed 17 Fredrickson phenotypic patterns of type 2, 6 of type 3, 10 of type 4, 3 of type 5, and 14 non‐definitive patterns. After twelve months of treatment with probucol, the mean serum cholesterol level was 263 mg/100 ml (a minus 20 per cent change) and the mean triglyceride level was 293 mg/100 ml (a minus 19 per cent change) for all patients. The median baseline cholesterol level was 311 mg/100 ml and the median cholesterol value during twelve months of therapy was 252 mg/100 ml, a reduction of 19 per cent. The median baseline triglyceride level was 174 mg/100 ml and the median triglyceride value during twelve months of therapy was 147 mg/100 ml, a reduction of 16 per cent. Significant changes were noted in the serum lipoprotein patterns; the majority of type 2 and type 3 changed to the non‐definitive pattern, but the majority of type 4 and type 5 remained unchanged. Seven patients had xanthelasmas, but all these lesions decreased in size and 3 lesions disappeared during probucol therapy. Side effects were minimal. About a third of the patients had mild transient flatulence or slight transient eosinophilia. There was no effect on prothrombin time. Probucol appears to be a safe and effective hypolipidemic agent. It can also induce changes in serum lipoprotein patterns and markedly reduce the size of xanthelasmas.