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辛伐他汀和苯扎贝特:对家族性高胆固醇血症患者血清脂蛋白及卵磷脂胆固醇酰基转移酶活性的影响

Simvastatin and bezafibrate: effects on serum lipoproteins and lecithin: cholesterol acyltransferase activity in familial hypercholesterolaemia.

作者信息

Weisweiler P

机构信息

MRM-Metabolic Research Munich, Federal Republic of Germany.

出版信息

Eur J Clin Pharmacol. 1988;35(6):579-83. doi: 10.1007/BF00637592.

DOI:10.1007/BF00637592
PMID:3234467
Abstract

Sixteen subjects with familial hypercholesterolaemia were randomly assigned to treatment with simvastatin 20-40 mg/day (an inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase) or with bezafibrate 600 mg/day (a clofibrate analogue) for 12 weeks. Both drugs produced significant reductions in serum and LDL cholesterol; mean percentage fall -30.5% and -38.1% (simvastatin) and -17.8% and -20.6% (bezafibrate), respectively. Both drugs also caused a decrease in VLDL cholesterol, while only bezafibrate decreased the serum and VLDL triglyceride levels and increased HDL cholesterol and serum apolipoprotein A-I and A-II levels. Serum apolipoprotein B fell by 33.3% (simvastatin) and 15.7% (bezafibrate). Simvastatin and bezafibrate produced significant increases in the mean fractional esterification rate of LCAT, by +124.1% and +20.6%, respectively. Thus simvastatin was clearly more effective than bezafibrate in lowering LDL by enhancing its turnover, but bezafibrate had specific effects on VLDL and HDL that might be favourable in combined treatment regimens.

摘要

16名家族性高胆固醇血症患者被随机分配接受辛伐他汀20 - 40毫克/天(一种3 - 羟基 - 3 - 甲基戊二酰辅酶A还原酶抑制剂)或苯扎贝特600毫克/天(一种氯贝丁酯类似物)治疗12周。两种药物均使血清和低密度脂蛋白胆固醇显著降低;平均降低百分比分别为-30.5%和-38.1%(辛伐他汀)以及-17.8%和-20.6%(苯扎贝特)。两种药物还使极低密度脂蛋白胆固醇降低,而只有苯扎贝特降低了血清和极低密度脂蛋白甘油三酯水平,并提高了高密度脂蛋白胆固醇以及血清载脂蛋白A - I和A - II水平。血清载脂蛋白B分别降低了33.3%(辛伐他汀)和15.7%(苯扎贝特)。辛伐他汀和苯扎贝特分别使卵磷脂胆固醇酰基转移酶的平均酯化率显著提高,提高幅度分别为+124.1%和+20.6%。因此,辛伐他汀通过增强低密度脂蛋白的代谢在降低低密度脂蛋白方面明显比苯扎贝特更有效,但苯扎贝特对极低密度脂蛋白和高密度脂蛋白有特定作用,这在联合治疗方案中可能是有利的。

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Turnover of apoproteins A-I and A-II of high density lipoprotein and the relationship to other lipoproteins in normal and hyperlipidemic individuals.正常人和高脂血症患者中高密度脂蛋白载脂蛋白A-I和A-II的周转率及其与其他脂蛋白的关系。
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Mevinolin and colestipol stimulate receptor-mediated clearance of low density lipoprotein from plasma in familial hypercholesterolemia heterozygotes.美维诺林和考来替泊可刺激家族性高胆固醇血症杂合子患者血浆中低密度脂蛋白通过受体介导的清除。
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