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考来替泊:对其在高胆固醇血症患者中的药理特性及治疗效果的综述

Colestipol: a review of its pharmacological properties and therapeutic efficacy in patients with hypercholesterolaemia.

作者信息

Heel R C, Brogden R N, Pakes G E, Speight T M, Avery G S

出版信息

Drugs. 1980 Mar;19(3):161-80. doi: 10.2165/00003495-198019030-00001.

DOI:10.2165/00003495-198019030-00001
PMID:6988203
Abstract

Colestipol is an anion exchange resin with bile acid sequestering properties resembling those of cholestyramine, another lipid-lowering binding resin. In daily doses of 15 to 30g colestipol reduces total plasma cholesterol concentrations (primarily low density lipoprotein cholesterol) by about 15 to 30%, but plasma triglyceride concentrations may be unchanged or in some patients increased. Thus, like cholestyramine, colestipol is of benefit in patients with primary hypercholesterolaemia without associated hypertriglyceridaemia (type IIa hyperlipoproteinaemia). Colestipol is odourless and tasteless, and is said by some to be more readily tolerated by patients than cholestyramine, leading to improved compliance, but such data has not been documented in most studies. Side effects of colestipol treatment are primarily gastrointestinal in nature since the drug is essentially unabsorbed. As with cholestyramine, colestipol may bind with other concomitantly administered drugs reducing their absorption or enterohepatic recirculation; dosage intervals of other concurrent medications should be adjusted to minimise the potential for such an interaction.

摘要

考来替泊是一种阴离子交换树脂,具有与另一种降脂结合树脂考来烯胺相似的胆汁酸螯合特性。每日服用15至30克考来替泊可使血浆总胆固醇浓度(主要是低密度脂蛋白胆固醇)降低约15%至30%,但血浆甘油三酯浓度可能保持不变,或在某些患者中升高。因此,与考来烯胺一样,考来替泊对无相关高甘油三酯血症的原发性高胆固醇血症患者(IIa型高脂蛋白血症)有益。考来替泊无味无臭,有人认为患者对其耐受性比考来烯胺更好,从而提高了依从性,但大多数研究中尚未记录此类数据。考来替泊治疗的副作用主要是胃肠道方面的,因为该药物基本不被吸收。与考来烯胺一样,考来替泊可能与其他同时服用的药物结合,减少它们的吸收或肠肝循环;应调整其他同时服用药物的给药间隔,以尽量减少这种相互作用的可能性。

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The effect of cholestyramine and colestipol on the absorption of hydrochlorothiazide.消胆胺和考来替泊对氢氯噻嗪吸收的影响。
Int J Clin Pharmacol Ther Toxicol. 1982 Apr;20(4):151-4.
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Effect of cholestyramine and colestipol on the absorption of phenytoin.消胆胺和考来替泊对苯妥英吸收的影响。
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Effects of colestipol (U-26,597A), a new bile acid sequestrant, on serum lipids in experimental animals and man.新型胆汁酸螯合剂考来替泊(U-26,597A)对实验动物和人类血清脂质的影响。
血脂异常:药物治疗的叙述性综述
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Development of Novel siRNA Therapeutics: A Review with a Focus on Inclisiran for the Treatment of Hypercholesterolemia.新型 siRNA 治疗药物的开发:以治疗高胆固醇血症的inclisiran 为例的综述
Int J Mol Sci. 2023 Feb 16;24(4):4019. doi: 10.3390/ijms24044019.
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A Recent Ten-Year Perspective: Bile Acid Metabolism and Signaling.近年来的研究进展:胆汁酸代谢与信号转导。
Molecules. 2022 Mar 18;27(6):1983. doi: 10.3390/molecules27061983.
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Metabolic effects of intestinal absorption and enterohepatic cycling of bile acids.胆汁酸肠道吸收和肠肝循环的代谢效应。
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