Micronised fenofibrate - Review of its pharmacodynamic properties and clinical efficacy in the management of dyslipidaemia
Micronised fenofibrate - Review of its pharmacodynamic properties and clinical efficacy in the management of dyslipidaemia
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DOI：
10.2165/00003495-199754040-00007
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发表时间：
1997-10-01
期刊：
影响因子：
11.5
通讯作者：
Faulds, D
中科院分区：
文献类型：
--
作者：
Adkins, JC;Faulds, D
非诺贝特是纤维酸衍生物非诺贝特的一种新剂型。适用于治疗饮食控制或其他非药物干预无效的IIa、IIb、III或IV型血脂异常患者。微粉化非诺贝特与标准制剂相比具有改善的吸收特性，允许较低的日剂量和每日一次给药。微粉化非诺贝特的脂质修饰特征在于低密度脂蛋白（LDL）和总胆固醇水平的降低，血浆甘油三酯水平升高显著降低，高密度脂蛋白（HDL）升高与每天以300mg分次剂量给药的标准制剂一致，微粉化制剂已证明在治疗IIa、IIb和IV型原发性血脂异常中有效，但每日剂量较低，为200mg，每日一次。由于其显著的降血脂作用，微粒化非诺贝特似乎对高血脂症患者最有益（伴或不伴高胆固醇血症），包括2型糖尿病患者（非胰岛素依赖型）糖尿病和血脂异常。在现有的比较中，微粉化非诺贝特200 mg每日一次的疗效与HMG相似或不如HMG有效。辅酶A还原酶抑制剂辛伐他汀20毫克，每天和普伐他汀20毫克，每天在降低低密度脂蛋白和总胆固醇水平。然而，微粉化非诺贝特产生更大的改善甘油三酯，一般来说，HDL胆固醇水平比辛伐他汀和普伐他汀。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。血清转氨酶和肌酸磷酸激酶水平的升高已很少与微粉化fenofibrate.In结论，现有的数据表明，更方便的较低的每日一次剂量的微粉化fenofibrate仍然是有益的脂质修饰作用的标准配方。需要进一步的研究来确定微粒化非诺贝特实现的脂质变化是否会导致心血管发病率和死亡率的降低。
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 micronised fenofibrate remains 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.