[Effects of probucol on skin cholesterol concentrations in patients with type II hyperlipoproteineamia (author's...

Twenty patients (14 male and 6 female) with hyperlipoproteineamia (type IIa in 10 and type IIb in 10) were given probucol 500 mg b.d. during 6 months. Eleven patients had xanthoma tendinosum and 4 had xanthelasma. The mean plasma cholesterol and plasma triglyceride levels were 435 +/- 100 mg/dl and 210 +/- 138 mg/dl respectively. Normal diet was continued throughout. Skin biopsies were performed on the forearm before and after treatment. The skin fragments were freeze-dried, and free (FCh) and esterified (ECh) cholesterol concentrations were measured by gas chromatography after preliminary thin layer chromatography on silica gel. FCh and ECh were found to be significantly increased before treatment when compared with skin concentrations in 10 control subjects; FCh ranged from 2.25 to 1.58 microgram/mg (p < 0.001) and ECh from 0.44 to 0.16 microgram/mg of dry tissue (p < 0.001). After 6 months' treatment with probucol, there was no significant change in FCh (2.25 to 2.16 microgram/mg), but a significant rise was observed in ECh (0.44 to 0.66 microgram/mg; p < 0.01). This effect suggests that probucol interferes with cholesterol synthesis and transport in human tissues, which might help to comprehend the action of this and other drugs on xanthelasma, xanthoma tendinosum and atherosclerosis. In one of the patients, a xanthelasma was considerably reduced in size following probucol treatment.