Chapman M J
Lipoprotein Research Group, National Institute for Health and Medical Research, Hôpital de la Pitie, Paris, France.
Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9.
This discussion outlines the major aspects of the human pharmacology of fenofibrate, a hypolipidemic agent. In view of its short half-life, efficient absorption, and elimination, fenofibrate would not appear to accumulate in either plasma or tissues. It is extensively absorbed only in the presence of food and is transported through the bloodstream by albumin. Fenofibrate is taken up by both the liver and kidney. Except for a small percentage (about 5 percent) reduced at the ketone moiety before conjugation, most drug is excreted as a conjugate in the urine. Less than 20 percent is excreted through the bile. In normal persons, at steady state with usual doses of 100 mg three times daily, the plasma half-life approximates 30 hours. Because fenofibrate is not dialyzable, it has a markedly prolonged half life in patients with renal failure and should not be used.
本讨论概述了降血脂药物非诺贝特的人体药理学主要方面。鉴于其半衰期短、吸收和消除效率高,非诺贝特似乎不会在血浆或组织中蓄积。它仅在有食物存在时被广泛吸收,并通过白蛋白在血液中运输。非诺贝特可被肝脏和肾脏摄取。除了一小部分(约5%)在结合前酮部分被还原外,大多数药物以结合物形式经尿液排泄。经胆汁排泄的不到20%。在正常人中,每日三次常规剂量100mg达到稳态时,血浆半衰期约为30小时。由于非诺贝特不可透析,在肾衰竭患者中其半衰期会显著延长,因此不应使用。