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首页> 外文期刊>Drugs of today: Medicamentos de actualidad >Enhanced hypercholesterolemia therapy: The ezetimibe/simvastatin tablet.
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Enhanced hypercholesterolemia therapy: The ezetimibe/simvastatin tablet.

机译：增强的高胆固醇血症治疗：依泽替米贝/辛伐他汀片。

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While therapy with HMG-CoA reductase inhibitors, or statins, has provided the principal pharmacological innovation in the treatment of hypercholesterolemia in recent years, extensive use of these agents has shown that not all patients respond to them and that still greater reductions in low-density lipoprotein (LDL) cholesterol can further protect patients from cardiovascular events. The strategy of increasing the doses of statins is effective but associated with an increase in adverse effects. The combination of statins with other agents has also, in some cases, increased efficacy, but has likewise been limited by toxicity. The administration of a new agent with a novel mechanism of action, ezetimibe, with a well-characterized and effective statin, simvastatin, in a single tablet now appears to provide enhanced treatment without compromising safety. Monotherapy with either ezetimibe or simvastatin has demonstrated the ability to significantly lower LDL cholesterol. Simultaneous administration of the two agents benefits from their two distinct mechanisms of action: inhibition of biliary and dietary cholesterol absorption by ezetimibe and inhibition of hepatic cholesterol synthesis by simvastatin. The two mechanisms have exhibited complementary activity in preclinical evaluation and have demonstrated an absence of pharmacokinetic interaction in humans. Large clinical trials have consistently shown that the addition of ezetimibe to simvastatin produces significantly greater reductions in LDL cholesterol than simvastatin alone, with tolerability similar to statin monotherapy. Ezetimibe/simvastatin has also been associated with other beneficial effects on lipids, and it achieves greater efficacy than monotherapy with the use of lower, safer doses of the statin. These findings indicate that use of the ezetimibe/simvastatin single tablet will allow more patients to meet increasingly stringent LDL cholesterol goals, thereby avoiding negative cardiovascular outcomes. (c) 2005 Prous Science. All rights reserved.
机译：尽管近年来使用HMG-CoA还原酶抑制剂或他汀类药物的治疗在治疗高胆固醇血症方面提供了主要的药理学创新，但这些药物的广泛使用表明并非所有患者都能对它们产生反应，而且低密度药物的使用率仍有较大降低脂蛋白（LDL）胆固醇可以进一步保护患者免受心血管事件的影响。增加他汀类药物剂量的策略是有效的，但与副作用增加有关。他汀类药物与其他药物的组合在某些情况下还提高了疗效，但同样受到毒性的限制。现在，在单一片剂中施用具有新颖作用机制的新药依泽替米贝，以及特征明确且有效的他汀类药物辛伐他汀，似乎可以提供增强的治疗效果而不会损害安全性。依泽替米贝或辛伐他汀的单药治疗已证明能够显着降低LDL胆固醇。两种药物的同时给药受益于它们两种不同的作用机理：依泽替米贝抑制胆汁和饮食中胆固醇的吸收，辛伐他汀抑制肝胆固醇的合成。这两种机制在临床前评估中表现出互补的活性，并证明在人体中没有药代动力学相互作用。大型临床试验一致表明，在辛伐他汀中添加依折麦布比单独使用辛伐他汀能显着提高LDL胆固醇的降低，其耐受性与他汀单药相似。依泽替米贝/辛伐他汀还与对脂质的其他有益作用有关，并且与单一疗法相比，使用较低，更安全的他汀类药物可获得更高的疗效。这些发现表明，依泽替米贝/辛伐他汀单片的使用将使更多的患者达到日益严格的LDL胆固醇目标，从而避免了不良的心血管结果。 （c）2005 Prous科学。版权所有。

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