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使用依折麦布/辛伐他汀药物组合双重抑制胆固醇?

[Dual inhibition of cholesterol using the drug combination ezetimibe/simvastatin?].

作者信息

Vaverková H

机构信息

III. interní klinika Lékarské fakulty UP a FN Olomouc.

出版信息

Vnitr Lek. 2007 Apr;53(4):421-7.

Abstract

The latest clinical intervention studies of statins have shown that more aggressive reductions in LDL-cholesterol to values lower than existing target values for persons with a high risk of cardiovascular disease produce greater success in terms of halted progression and even regression of the atherosclerotic process and fewer cardiovascular events. This has lead to a series of international and national recommendations for a further reduction in target values for LDL-cholesterol, which is often difficult to achieve with the usual dosage of statins. The combination of a statin with ezetimibe, acting as a dual inhibition mechanism against the synthesis and absorption of cholesterol, reduces LDL-cholesterol significantly more than treatment with a statin in monotherapy. This allows many more patients to achieve the target value for LDL-cholesterol. At present a drug combination comprising ezetimibe 10 mg and simvastatin in all doses (10, 20, 40 and 80 mg) is being introduced into our market under the company name Inegy. In addition to reducing LDL-cholesterol by up to 61% this combination has a positive effect on a range of other parameters for lipid metabolism and inflamation. A typical initial dose of ezetimibe 10 mg/simvastatin 20 mg reduces LDL-cholesterol by around 50%, which is necessary for the stabilisation of atherosclerotic plaque. For patients requiring more aggressive reduction of LDL-cholesterol it is best to start with a dose of ezetimibe 10 mg/simvastatin 40 mg. The highest dose of 10 mg/80 mg is intended for patients with the highest level of risk and reduces LDL-cholesterol by around 60%. In all the studies that have been carried out so far, the combination of ezetimibe and statin was very well tolerated and the safety profile of this combination was the same a treatment with the statin alone. At present a wide range of large clinical studies are underway to test whether LDL-cholesterol reduction using the ezetimibe + statin combination will also lead to a lower risk of cardiovascular events.

摘要

他汀类药物的最新临床干预研究表明,对于心血管疾病高危人群,更积极地将低密度脂蛋白胆固醇(LDL -胆固醇)降至低于现有目标值的水平,在阻止动脉粥样硬化进程甚至使其逆转以及减少心血管事件方面取得了更大的成功。这导致了一系列国际和国内关于进一步降低LDL -胆固醇目标值的建议,而使用常规剂量的他汀类药物往往难以实现这一目标。他汀类药物与依泽替米贝联合使用,通过对胆固醇合成和吸收的双重抑制机制,比单独使用他汀类药物治疗能更显著地降低LDL -胆固醇。这使得更多患者能够达到LDL -胆固醇的目标值。目前,一种由10毫克依泽替米贝和所有剂量(10、20、40和80毫克)辛伐他汀组成的药物组合正在以Inegy的公司名称进入我们的市场。除了将LDL -胆固醇降低多达61%外,这种组合对一系列其他脂质代谢和炎症参数也有积极作用。典型的初始剂量10毫克依泽替米贝/20毫克辛伐他汀可使LDL -胆固醇降低约50%,这对于稳定动脉粥样硬化斑块是必要的。对于需要更积极降低LDL -胆固醇的患者,最好从10毫克依泽替米贝/40毫克辛伐他汀的剂量开始。最高剂量10毫克/80毫克适用于风险最高的患者,可使LDL -胆固醇降低约60%。在迄今为止进行的所有研究中,依泽替米贝和他汀类药物的组合耐受性良好,这种组合的安全性与单独使用他汀类药物治疗相同。目前正在进行广泛的大型临床研究,以测试使用依泽替米贝 + 他汀类药物组合降低LDL -胆固醇是否也会降低心血管事件的风险。

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