Gevers Leuven J A, vd Voort H, Kempen H J, de Wit E, Havekes L
Drugs. 1987;33 Suppl 2:131-5. doi: 10.2165/00003495-198700332-00024.
Heterozygous familial hypercholesterolaemia (HtFH) is associated with an increased risk of coronary artery disease. Prevention is possible by increasing the number of functioning receptors of low density lipoproteins (LDLs) in the liver. This is partly achieved by treatment with bile acid sequestrants, such as cholestyramine, but the effect is limited because of a concomitant increase in cholesterol synthesis. It was the purpose of this study to determine whether the increase in cholesterol synthesis could be influenced by treatment with cyclandelate, since it is known that cyclandelate inhibits cholesterol synthesis in rats. Ten patients received cyclandelate (3.2 g daily in 2 doses) or placebo in a double-blind cross-over study, with each treatment period of 3 months' duration. During these periods, treatment with cholestyramine (16 g daily) was continued. No evidence was found of inhibition of cholesterol synthesis by cyclandelate, as indicated by the serum concentration of the cholesterol precursor, lanosterol, which remained unchanged. Neither the serum concentration of LDL, nor those of high density lipoprotein (HDL) cholesterol, apolipoprotein B, A-I or A-II, were affected. Thus, it can be concluded that treatment with cyclandelate was not effective in lowering serum cholesterol concentrations in patients with familial hypercholesterolaemia who received concomitant cholestyramine therapy.
杂合子家族性高胆固醇血症（HtFH）与冠状动脉疾病风险增加相关。通过增加肝脏中低密度脂蛋白（LDL）功能性受体的数量可实现预防。这部分可通过使用胆汁酸螯合剂（如消胆胺）治疗来达成，但由于胆固醇合成同时增加，效果有限。本研究的目的是确定环扁桃酯治疗是否能影响胆固醇合成的增加，因为已知环扁桃酯可抑制大鼠体内的胆固醇合成。在一项双盲交叉研究中，10名患者接受环扁桃酯（每日3.2 g，分2次服用）或安慰剂治疗，每个治疗期持续3个月。在此期间，继续使用消胆胺（每日16 g）治疗。胆固醇前体羊毛甾醇的血清浓度未发生变化，这表明未发现环扁桃酯对胆固醇合成有抑制作用。LDL的血清浓度、高密度脂蛋白（HDL）胆固醇、载脂蛋白B、A-I或A-II的血清浓度均未受影响。因此，可以得出结论，对于接受消胆胺联合治疗的家族性高胆固醇血症患者，环扁桃酯治疗在降低血清胆固醇浓度方面无效。
