交互的呋喃苯胺酸血清thyroxine-binding网站:体内和体外研究和比较与其他抑制剂。
文章的细节
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引用
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Stockigt JR Lim CF,巴洛JW,魏恩KN,莫尔VS, Topliss DJ,汉布林PS,英国J
交互的呋喃苯胺酸血清thyroxine-binding网站:体内和体外研究和比较与其他抑制剂。
中国性金属底座,1985可能;60(5):1025 - 31所示。doi: 10.1210 /研究报告- 60 - 5 - 1025。
- PubMed ID
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2579968 (在PubMed]
- 文摘
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T4的利尿剂呋喃苯胺酸抑制血清蛋白结合平衡透析,dextran-charcoal,和竞争配体结合分离系统和取代[125 i] T4从孤立的准备T4-binding球蛋白(油管)、前白蛋白,白蛋白。平衡透析未稀释的正常血清的研究表明,大约10微克/毫升呋喃苯胺酸增加了自由T4和自由T3分数。beplayapp位移发生在低药物浓度与弱智者血清白蛋白和TBG水平。绑定的[14 c]呋喃苯胺酸TBG被标记T4抑制,表明呋喃苯胺酸和T4共享一个共同的结合位点。单剂量口服500毫克呋喃苯胺酸给五个病人保持腹膜透析增加的百分比木炭吸收[125 i] T4(使用血清稀释1:10)从4.1 + / - 1.0 (+ / - SE) 10.8 + / - 4.3 (P小于0.01)2 h后,同时减少总T3从75 + / - 5 - 56 + / - 13毫微克/分升(P小于0.01)和总T4从6.7 + / - 0.9到4.8 + / - 0.8微克/分升5 h后(P小于0.01)。各种配体抑制[125 i] T4结合血清蛋白在以下相对摩尔关系:T4, 1;呋喃苯胺酸,1.5 X 10 (3);芬氯酸,2 X 10 (4);甲灭酸。2.5 X 10 (4);diphenylhydantoin, 4 X 10 (4); ethacrynic acid, 10(5); heparin 5 X 10(5); 2-hydroxybenzoylglycine, 10(6); and sodium salicylate, 1.5 X 10(6). These studies demonstrate that furosemide competes for T4-binding sites on TBG, prealbumin, and albumin, so that a single high dose can acutely lower total T4 and T3 levels. The drug is much more potent on a molar basis than other drug inhibitors of T4 binding, but at normal therapeutic concentrations, furosemide is unlikely to decrease serum T4 or T3. However, high doses, diminished renal clearance, hypoalbuminemia, and low TBG accentuate its T4- and T3-lowering effect. Hence, furosemide should be considered a possible cause of low thyroid hormone levels in patients with critical illness. The significance of this drug in reports of impaired hormone and drug binding in renal failure requires further assessment.
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药物 航空公司 类 生物 药理作用 行动 呋喃苯胺酸 Thyroxine-binding球蛋白 蛋白质 人类 没有粘结剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">