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非诺贝特的药理学(作者译)

[Pharmacology of fenofibrate (author's transl)].

作者信息

Kritchevsky D

出版信息

Nouv Presse Med. 1980 Dec 22;9(49):3769-73.

PMID:7208345
Abstract

Fenofibrate is one of several compounds with substituted-2-phenoxy-isobutyric acids and esters. In ageing rats receiving a hyperlipidaemic diet or injections of triton, fenofibrate lowers blood lipids as much as, or more than other antilipaemic agents. It is active in man against the main types (IIa, IIb and IV) of hyperlipoproteinaemia (HLP), and this activity is sustained throughout treatment (20 months in one study). In comparative studies, the effects of fenofibrate (400 mg/day) on the lipoprotein fractions tested were superior to those of clofibrate (2 g/day) and slightly superior to those of gemfibrosil (800 mg/day) and bezafibrate (600 mg/day). The drug also enhanced the lipid-lowering effects of colestipol. In doses of 300 mg/day fenofibrate produced a significant 13-15% decrease in apoprotein B with a concomitant 19-28% increase in apoprotein A. Fenofibrate was also found to normalize platelet aggregation in patients with type IIb HLP. In animals fenofibrate is excreted in equal amounts in the urine and faeces; in man, urinary excretion predominates (85-90%). The serum half-life curve is diphasic, with a rapid (5 hours) slope and a slow (17 hours) slope. In a 10-day study conducted on 10 volunteers serum levels of fenofibric acid remained remarkably constant, indicating lack of accumulation. New data on the mode of action are needed to further differentiate fenofibrate from clofibrate.

摘要

非诺贝特是几种含取代 - 2 - 苯氧基异丁酸及其酯类的化合物之一。在接受高脂血症饮食或注射聚醚醇的老龄大鼠中,非诺贝特降低血脂的效果与其他降血脂药物相当或更佳。它对人类主要类型(IIa、IIb和IV型)的高脂蛋白血症(HLP)有效,且这种活性在整个治疗过程中持续存在(一项研究中为20个月)。在比较研究中,非诺贝特(400毫克/天)对所检测的脂蛋白组分的作用优于氯贝丁酯(2克/天),略优于吉非贝齐(800毫克/天)和苯扎贝特(600毫克/天)。该药物还增强了考来替泊的降血脂作用。非诺贝特剂量为300毫克/天时,载脂蛋白B显著降低13 - 15%,同时载脂蛋白A升高19 - 28%。还发现非诺贝特可使IIb型HLP患者的血小板聚集恢复正常。在动物中,非诺贝特经尿液和粪便等量排泄;在人类中,以尿液排泄为主(85 - 90%)。血清半衰期曲线呈双相,快速斜率为5小时,慢速斜率为17小时。在一项对10名志愿者进行的为期10天的研究中,非诺贝酸的血清水平保持显著恒定,表明无蓄积现象。需要关于作用方式的新数据来进一步区分非诺贝特和氯贝丁酯。

相似文献

2
[Pharmacokinetics of fenofibrate in man (author's transl)].
Nouv Presse Med. 1980 Dec 22;9(49):3725-7.

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