Hypocholesteremic Effect of Phenoxybenzamine (Dibenzyline), An Adrenergic Blocking Agent

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Abstract
The effect of an orally effective adrenergic blocking agent, Dibenzyline, on serum cholesterol levels was studied in human subjects and in monkeys on high-fat diets. In addition, the effect of the phenoxyethyl analogue of Dibenzyline, G-D 131, was also investigated in monkeys. The studies showed that the increase in serum cholesterol level brought about by a high-fat diet in monkeys could be considerably reduced by supplementation with Dibenzyline. This hypocholesteremic action was also observed with the analogue of Dibenzyline, G-D 131, which does not possess the adrenergic blocking property. It appears, therefore, that the hypocholesteremic action of Dibenzyline is independent of its adrenergic blocking activity. When a high-fat diet which also contained a high amount of cholesterol was used, Dibenzyline retarded the increase in serum cholesterol of monkeys for a considerable length of time. Administration of Dibenzyline, 10 mg. daily for 11 days, brought about a fall in serum cholesterol in two of the three human subjects and arrested the further increase in serum cholesterol in the third subject on a high-butterfat diet. All the subjects showed increased fecal elimination of cholic and dihydroxycholanic acids during the Dibenzyline-supplemented period, suggesting that the hypocholesteremic effect of the drug is at least partly mediated through increased elimination of cholesterol as bile acids.