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与合成及吸收联合抑制相关的胆固醇代谢变化

[Change in the cholesterol metabolism associated with the combined inhibition of synthesis and absorption].

作者信息

Márk László, Paragh György

机构信息

Békés Megyei Képviselo-testület Pándy Kálmán Kórháza II. Belgyógyászat-Kardiológia Gyula.

出版信息

Orv Hetil. 2007 Apr 8;148(14):627-32. doi: 10.1556/OH.2007.28065.

DOI:10.1556/OH.2007.28065
PMID:17403635
Abstract

Lowering lipid levels in the cardiovascular prevention we confine ourselves to measure the cholesterol level and care less for the background effects. Namely blood cholesterol level beyond the amount consumed with the diet highly depends on balance of intestinal absorption/secretion and synthesis. Studying the rate of absorption and synthesis has come only recently into the foreground of interest. Many observations proved that using even the strongest cholesterol lowering drug - beyond reducing the synthesis in the liver - may be associated with an up to 50 percent increase of the intestinal cholesterol absorption. When studying the effectiveness of statins in everyday practice we measure only the decrease of serum cholesterol level as the final result, and do not examine the changes in the synthesis and absorption. The amount of cholesterol synthesized or absorbed can be determined in an indirect way by measuring that of the non-cholesterol sterols (phytosterols). The absorption markers are campesterol, sitosterol, avenasterol as well as cholestanol. The biosynthesis of cholesterol correlates with the level of lathosterol, cholestanol, desmostenol. In practice the concentration of lathosterol or lathosterol/cholesterol can be considered the marker of synthesis and the campesterol or campesterol/cholesterol ratio the marker of absorption. So recent study results show that while inhibiting the cholesterol synthesis with statin the cholesterol absorption increases and the absorption inhibitor ezetimibe is associated with boost of synthesis. The increase in absorption caused by statins can be reduced or prevented by combining with ezetimibe. These data confirm that combination of statin and ezetimibe, inhibiting simultaneously both the synthesis and absorption provides the most effective cholesterol-level lowering with the least side-effects.

摘要

在心血管疾病预防中降低血脂水平时,我们往往只关注测量胆固醇水平,而较少关注其背后的影响因素。也就是说,血液中超出饮食摄入量的胆固醇水平很大程度上取决于肠道吸收/分泌与合成之间的平衡。对吸收和合成速率的研究直到最近才受到关注。许多观察结果证明,即使使用最强效的降胆固醇药物,除了降低肝脏中的合成外,还可能导致肠道胆固醇吸收增加多达50%。在日常实践中研究他汀类药物的疗效时,我们仅将血清胆固醇水平的降低作为最终结果来衡量,而不研究合成和吸收的变化。胆固醇的合成或吸收量可以通过测量非胆固醇固醇(植物固醇)的量来间接确定。吸收标志物有菜油甾醇、谷甾醇、燕麦甾醇以及胆甾烷醇。胆固醇的生物合成与羊毛甾醇、胆甾烷醇、去氢胆甾醇的水平相关。在实际应用中,羊毛甾醇的浓度或羊毛甾醇/胆固醇的比值可被视为合成的标志物,而菜油甾醇或菜油甾醇/胆固醇的比值则为吸收的标志物。因此,最近的研究结果表明,在使用他汀类药物抑制胆固醇合成时,胆固醇吸收会增加,而吸收抑制剂依泽替米贝则与合成增加有关。他汀类药物引起的吸收增加可通过与依泽替米贝联合使用来减少或预防。这些数据证实,他汀类药物和依泽替米贝联合使用,同时抑制合成和吸收,能以最少的副作用提供最有效的降胆固醇效果。

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Effects of ezetimibe on markers of synthesis and absorption of cholesterol in high-risk patients with elevated C-reactive protein.依泽替米贝对高敏 C 反应蛋白升高的高危患者胆固醇合成和吸收标志物的影响。
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Where does the interplay between cholesterol absorption and synthesis in the context of statin and/or ezetimibe treatment stand today?在他汀类药物和/或依折麦布治疗的情况下,胆固醇吸收和合成之间的相互作用处于什么地位?
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[Ezetimibe--intestinal cholesterol absorbtion inhibitor].[依折麦布——肠道胆固醇吸收抑制剂]
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