Choisy H, Millart H
Nouv Presse Med. 1980 Oct 30;9(40):2981-4.
The experimental studies carried out so far have uniformly demonstrated that probucol lowers plasma cholesterol levels in all animal species. The drug has low toxicity and has been well tolerated during long-term treatment (up to 8 years in monkeys) in most species. In some dogs, however, probucol seemed to increase myocardial sensitivity to catecholamins, but this has not been found in other species. The pharmacokinetics of probucol show a rather slow turnover and are characterized by storage of the drug in adipose tissues, which may explain why the hypocholesterolaemic effect is progressively obtained. The main channel of excretion is the bile. No other pharmacological action has been described with probucol, which in the present state of knowledge appears to be a predominantly cholesterol-lowering agent.
迄今为止所进行的实验研究一致表明,普罗布考可降低所有动物物种的血浆胆固醇水平。该药物毒性低,在大多数物种的长期治疗(猴子长达8年)中耐受性良好。然而,在一些狗中,普罗布考似乎会增加心肌对儿茶酚胺的敏感性,但在其他物种中未发现这种情况。普罗布考的药代动力学显示其周转相当缓慢,其特点是药物储存在脂肪组织中,这可能解释了为什么降胆固醇作用是逐渐显现的。排泄的主要途径是胆汁。尚未描述普罗布考的其他药理作用,就目前的知识水平而言,它似乎主要是一种降胆固醇药物。