Gazi Irene F, Daskalopoulou Stella S, Nair Devaki R, Mikhailidis Dimitri P
Department of Clinical Biochemistry (Vascular Disease Prevention Clinics), Royal Free Hospital (and University College of Medicine), London, UK.
Curr Med Res Opin. 2007 Sep;23(9):2183-92. doi: 10.1185/030079907X226267.
Recent guidelines underline the need for high-risk patients to reach strict low density lipoprotein cholesterol (LDL-C) targets (1.8-2.6 mmol/L; 70-100 mg/dL), and specifically mention the possible use of combination therapy (e.g.statin + ezetimibe) to achieve these goals.
A retrospective case-note audit was carried out to assess the response to administering ezetimibe in patients unable to tolerate statins (Group 1), or high dose of statins (Group 2) and patients who cannot achieve the LDL-C target (2.6 mmol/L; 100 mg/dL) despite taking a statin (Group 3).
Ezetimibe lowered LDL-C levels by 20-29% across the 3 patient groups after 2-3 months of treatment. High density lipoprotein cholesterol (HDL-C) levels tended to remain unchanged, although there was a consistent trend for a fall if baseline values were 'high'. However, the LDL-C/HDL-C ratio changed significantly and favourably in all groups. The fall in fasting triglyceride levels in all groups was greater (reaching 19-25%) when baseline levels were > or = 1.5 or 1.7 mmol/L (136-150 mg/dL). There were no marked abnormalities in liver function tests or creatine kinase activity. In Group 3 there was a significant trend for a fall in serum creatinine levels across the tertiles of baseline creatinine values. Limitations of the present study include the small sample size (especially in Groups 1 and 2), its short-term duration and the absence of event-based end-points. Therefore, the results are hypothesis-generating rather than conclusive.
When used alone or added to a statin, ezetimibe favourably altered the LDL-C/HDL-C ratio and lowered triglyceride levels. Ezetimibe was well tolerated in patients with statin intolerance and was associated with a 26% fall in LDL-C. An additional action may be some degree of improved renal function. Further studies are needed to confirm these findings.
近期指南强调高危患者需达到严格的低密度脂蛋白胆固醇（LDL-C）目标（1.8 - 2.6 mmol/L；70 - 100 mg/dL），并特别提及可能使用联合治疗（如他汀类药物 + 依折麦布）来实现这些目标。
进行了一项回顾性病例记录审核，以评估依折麦布用于无法耐受他汀类药物的患者（第1组）、高剂量他汀类药物的患者（第2组）以及尽管服用他汀类药物仍无法达到LDL-C目标（2.6 mmol/L；100 mg/dL）的患者（第3组）的治疗反应。
治疗2 - 3个月后，依折麦布使3组患者的LDL-C水平降低了20% - 29%。高密度脂蛋白胆固醇（HDL-C）水平往往保持不变，不过如果基线值“较高”，则有持续下降的趋势。然而，所有组的LDL-C/HDL-C比值均有显著且有利的变化。当基线水平≥1.5或1.7 mmol/L（136 - 150 mg/dL）时，所有组空腹甘油三酯水平的下降幅度更大（达到19% - 25%）。肝功能检查或肌酸激酶活性无明显异常。在第3组中，血清肌酐水平随基线肌酐值三分位数呈显著下降趋势。本研究的局限性包括样本量小（尤其是第1组和第2组）、研究持续时间短以及缺乏基于事件的终点。因此，结果只是产生假设而非结论性的。
单独使用或与他汀类药物联合使用时，依折麦布可有利地改变LDL-C/HDL-C比值并降低甘油三酯水平。依折麦布在他汀类药物不耐受的患者中耐受性良好，且与LDL-C下降26%相关。另外一个作用可能是某种程度上改善肾功能。需要进一步研究来证实这些发现。
