Stuyt P M, Kleinjans H A, Stalenhoef A F
Department of Internal Medicine, University Hospital Nijmegen, The Netherlands.
Neth J Med. 1998 Nov;53(5):228-33. doi: 10.1016/s0300-2977(98)00076-x.
Acipimox, a derivative of nicotinic acid, lowers serum lipid levels by reducing the production of very-low-density and low-density lipoproteins (LDL).
We studied the additional lipid-lowering effect of high doses of acipimox in 12 patients with severe familial hypercholesterolemia (FH) who were on treatment with an HMG CoA reductase inhibitor, in some cases in combination with a resin.
There was a significant reduction in total serum cholesterol (-9%), LDL-cholesterol (-9%) and serum triglycerides (-21%) when the standard doses of acipimox (750 mg/day) was added to treatment with simvastatin (and a resin). However, higher doses had no further hypolipidemic effect. In concordance with the reduction of serum cholesterol and LDL-cholesterol there was a significant decrease in apolipoprotein (apo)-B (-11%). There was no change in HDL-cholesterol, apo-A1 and lipoprotein(a). Acipimox in high doses up to 2250 mg/d was well tolerated except for initial gastric complaints and of flushing; because of these side effects one patient dropped out of the study.
Acipimox in high doses, which were well tolerated, has no additional lowering effect on LDL-levels compared to the standard dose in patients with severe FH who are already treated with simvastatin.
阿西莫司是烟酸的衍生物，通过减少极低密度脂蛋白和低密度脂蛋白（LDL）的产生来降低血脂水平。
我们研究了高剂量阿西莫司对12例重度家族性高胆固醇血症（FH）患者的额外降脂作用，这些患者正在接受HMG CoA还原酶抑制剂治疗，某些情况下还联合使用了树脂类药物。
当在辛伐他汀（和树脂类药物）治疗中添加标准剂量的阿西莫司（750毫克/天）时，血清总胆固醇（-9%）、LDL胆固醇（-9%）和血清甘油三酯（-21%）有显著降低。然而，更高剂量并没有进一步的降脂效果。与血清胆固醇和LDL胆固醇的降低相一致，载脂蛋白（apo）-B显著降低（-11%）。高密度脂蛋白胆固醇、apo-A1和脂蛋白（a）没有变化。除了最初的胃部不适和潮红外，高达2250毫克/天的高剂量阿西莫司耐受性良好；由于这些副作用，一名患者退出了研究。
对于已经接受辛伐他汀治疗的重度FH患者，高剂量且耐受性良好的阿西莫司与标准剂量相比，对LDL水平没有额外的降低作用。
