Kolovou Genovefa D, Kostakou Peggy M, Anagnostopoulou Katherine K, Cokkinos Dennis V
1st Cardiology Department, Onassis Cardiac Surgery Center, Athens, Greece.
Am J Cardiovasc Drugs. 2008;8(4):243-55. doi: 10.2165/00129784-200808040-00004.
Hypertriglyceridemia is observed in many metabolic diseases such as the metabolic syndrome, diabetes mellitus, or mixed dyslipidemia frequently leading to premature coronary heart disease (CHD). Additionally, several studies have shown that postprandial hypertriglyceridemia is pronounced in patients with CHD, metabolic syndrome, hypertension, and other pathologic conditions. The triglyceride-rich lipoprotein remnants accumulating in the postprandial state seem to be involved in atherogenesis and in events leading to thrombosis. Since abnormal postprandial lipemia is associated with pathologic conditions, its treatment is of clinical importance.Fibrates are of significant help in managing hypertriglyceridemia. This review summarizes the effect of fibric acid derivatives on postprandial lipemia. Fibrates decrease the production of and enhance the catabolism of triglyceride-rich lipoproteins through the activation of peroxisome proliferator-activated receptor-alpha. Results of clinical studies with fibrates have confirmed their action in decreasing postprandial triglyceride levels by increasing lipoprotein lipase activity, decreasing apolipoprotein CIII production, and by increasing fatty acid oxidation in the liver.It is concluded that fibrates are effective agents in lowering the postprandial increase in remnant lipoprotein particles and retinyl palmitate. Furthermore, fibrates can also affect the postprandial lipid profile by increasing hepatic lipase levels and in some cases, by reducing cholesterol ester transfer protein activity. The main target of fibrate therapy is to improve fasting hypertriglyceridemia, which is an essential component associated with improving postprandial lipemia. Fibrates are well tolerated by patients and adverse effects have been reported rarely after their administration.
高甘油三酯血症在许多代谢性疾病中都有观察到,如代谢综合征、糖尿病或混合性血脂异常,这些疾病常常导致早发性冠心病(CHD)。此外,多项研究表明,冠心病、代谢综合征、高血压和其他病理状况患者的餐后高甘油三酯血症较为明显。餐后状态下积累的富含甘油三酯的脂蛋白残粒似乎参与了动脉粥样硬化的发生以及导致血栓形成的过程。由于异常的餐后血脂异常与病理状况相关,因此其治疗具有临床重要性。贝特类药物在治疗高甘油三酯血症方面有显著帮助。本综述总结了纤维酸衍生物对餐后血脂异常的影响。贝特类药物通过激活过氧化物酶体增殖物激活受体α来减少富含甘油三酯的脂蛋白的产生并增强其分解代谢。使用贝特类药物的临床研究结果证实了它们通过增加脂蛋白脂肪酶活性、减少载脂蛋白CIII的产生以及增加肝脏中的脂肪酸氧化来降低餐后甘油三酯水平的作用。得出的结论是,贝特类药物是降低餐后残留脂蛋白颗粒和视黄醇棕榈酸酯增加的有效药物。此外,贝特类药物还可以通过增加肝脂肪酶水平,在某些情况下通过降低胆固醇酯转移蛋白活性来影响餐后血脂谱。贝特类药物治疗的主要目标是改善空腹高甘油三酯血症,这是改善餐后血脂异常的一个重要组成部分。患者对贝特类药物耐受性良好,用药后很少有不良反应报告。