Yamaoka-Tojo Minako, Tojo Taiki, Kosugi Rie, Hatakeyama Yuko, Yoshida Yuki, Machida Yoji, Aoyama Naoyoshi, Masuda Takashi, Izumi Tohru
Department of Rehabilitation, Kitasato University School of Allied Health Sciences, 1-15-1 Kitasato, Sagamihara, Kanagawa 228-8555, Japan.
Lipids Health Dis. 2009 Oct 12;8:41. doi: 10.1186/1476-511X-8-41.
Ezetimibe (Zetia) is a potent inhibitor of cholesterol absorption that has been approved for the treatment of hypercholesterolemia. Statin, an inhibitor of cholesterol synthesis, is the first-choice drug to reduce low-density lipoprotein-cholesterol (LDL-C) for patients with hypercholesterolemia, due to its strong effect to lower the circulating LDL-C levels. Because a high dose of statins cause concern about rhabdomyolysis, it is sometimes difficult to achieve the guideline-recommended levels of LDL-C in high-risk patients with hypercholesterolemia treated with statin monotherapy. Ezetimibe has been reported to reduce LDL-C safely with both monotherapy and combination therapy with statins.
To investigate the effect of ezetimibe as "add-on" therapy to statin on hypercholesterolemia, we examined biomarkers and vascular endothelial function in 14 patients with hypercholesterolemia before and after the 22-week ezetimibe add-on therapy. Ezetimibe add-on therapy reduced LDL-C by 24% compared with baseline (p < 0.005), with 13 patients (93%) reaching their LDL cholesterol goals. Of the Ezetimibe add-on therapy significantly improved not only LDL-C, high-density lipoprotein-cholesterol (HDL-C), and apolipoprotein (apo)B levels, but also reduced levels of triglyceride (TG), the ratio of LDL/HDL-C, the ratio of apoB/apoA-I, and a biomarker for oxidative stress (d-ROMs). Furthermore, ezetimibe add-on therapy improved vascular endothelial function in high-risk patients with hypercholesterolemia.
In conclusion, ezetimibe as add-on therapy to statin might be a therapeutic good option for high-risk patients with atherosclerosis.
依折麦布(益适纯)是一种有效的胆固醇吸收抑制剂,已被批准用于治疗高胆固醇血症。他汀类药物作为胆固醇合成抑制剂,因其能显著降低循环低密度脂蛋白胆固醇(LDL-C)水平,是高胆固醇血症患者降低LDL-C的首选药物。由于高剂量他汀类药物会引发横纹肌溶解的担忧,对于接受他汀类单药治疗的高风险高胆固醇血症患者,有时难以达到指南推荐的LDL-C水平。据报道,依折麦布单药治疗及与他汀类药物联合治疗均能安全降低LDL-C。
为研究依折麦布作为他汀类药物的“附加”疗法对高胆固醇血症的影响,我们在14例高胆固醇血症患者接受为期22周的依折麦布附加治疗前后,检测了生物标志物和血管内皮功能。与基线相比,依折麦布附加治疗使LDL-C降低了24%(p < 0.005),13例患者(93%)达到了LDL胆固醇目标。依折麦布附加治疗不仅显著改善了LDL-C、高密度脂蛋白胆固醇(HDL-C)和载脂蛋白(apo)B水平,还降低了甘油三酯(TG)水平、LDL/HDL-C比值、apoB/apoA-I比值以及氧化应激生物标志物(d-ROMs)。此外,依折麦布附加治疗改善了高风险高胆固醇血症患者的血管内皮功能。
总之,依折麦布作为他汀类药物的附加疗法可能是动脉粥样硬化高风险患者的一种良好治疗选择。