Adkins J C, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1997 Oct;54(4):615-33. doi: 10.2165/00003495-199754040-00007.
Micronised fenofibrate is a new formulation of the fibric acid derivative fenofibrate. It is indicated for the treatment of patients with type IIa, IIb, III or IV dyslipidaemia who have failed to respond to dietary control or other nonpharmacological interventions. Micronised fenofibrate has improved absorption characteristics compared with the standard preparation, allowing a lower daily dosage and once-daily administration. The lipid-modifying profile of micronised fenofibrate is characterised by a decrease in low density lipoprotein (LDL) and total cholesterol levels, a marked reduction in elevated plasma triglyceride levels and an increase in high density lipoprotein (HDL) cholesterol levels. Consistent with the standard formulation, which is administered as 300mg daily in divided doses, the micronised preparation has demonstrated efficacy in the treatment of type IIa, IIb and IV primary dyslipidaemias but at a lower daily dosage of 200mg once daily. Because of its significant triglyceride-lowering effect, micronised fenofibrate appears to be of greatest benefit in patients with hypertriglyceridaemia (with or without hypercholesterolaemia), including patients with type 2 (non-insulin-dependent) diabetes mellitus and dyslipidaemia. In the comparisons available, micronised fenofibrate 200mg once daily was of similar efficacy to or less effective than the HMG-CoA reductase inhibitors simvastatin 20mg daily and pravastatin 20mg daily at reducing LDL and total cholesterol levels. However micronised fenofibrate produced greater improvements in triglyceride and, generally, HDL cholesterol levels than both simvastatin and pravastatin. Data on the long term tolerability of micronised fenofibrate are limited. However, data from a large short term (3-month) study have indicated that gastrointestinal disorders are the most frequent adverse events associated with therapy. Elevations in serum transaminase and creatine phosphokinase levels have been reported rarely with micronised fenofibrate. In conclusion, available data suggest that the more convenient lower once-daily dosage of micronisedfeno fibrate retains the beneficial lipid-modifying effects of the standard formulation. Further studies are required to determine whether the lipid changes achieved with micronised fenofibrate result in a reduction in cardiovascular morbidity and mortality.
微粒化非诺贝特是纤维酸衍生物非诺贝特的一种新剂型。它适用于治疗IIa型、IIb型、III型或IV型血脂异常且对饮食控制或其他非药物干预无反应的患者。与标准制剂相比，微粒化非诺贝特具有更好的吸收特性，每日剂量更低且只需每日服用一次。微粒化非诺贝特的调脂作用表现为低密度脂蛋白（LDL）和总胆固醇水平降低，血浆甘油三酯水平显著降低，高密度脂蛋白（HDL）胆固醇水平升高。与标准制剂（每日300mg分剂量服用）一致，微粒化制剂在治疗IIa型、IIb型和IV型原发性血脂异常方面已显示出疗效，但每日剂量更低，为200mg每日一次。由于其显著的降低甘油三酯作用，微粒化非诺贝特似乎对高甘油三酯血症（无论有无高胆固醇血症）患者，包括2型（非胰岛素依赖型）糖尿病和血脂异常患者，益处最大。在现有比较中，每日一次服用200mg微粒化非诺贝特在降低LDL和总胆固醇水平方面与每日服用20mg辛伐他汀和20mg普伐他汀这两种HMG - CoA还原酶抑制剂疗效相当或稍差。然而，微粒化非诺贝特在降低甘油三酯以及总体上提高HDL胆固醇水平方面比辛伐他汀和普伐他汀都有更大改善。关于微粒化非诺贝特长期耐受性的数据有限。然而，一项大型短期（3个月）研究的数据表明，胃肠道疾病是与治疗相关的最常见不良事件。微粒化非诺贝特很少有血清转氨酶和肌酸磷酸激酶水平升高的报道。总之，现有数据表明，微粒化非诺贝特更方便的较低每日一次剂量保留了标准制剂有益的调脂作用。需要进一步研究以确定微粒化非诺贝特实现的血脂变化是否能降低心血管发病率和死亡率。
