nabumetone的临床药物动力学。选择性cyclo-oxygenase-2抑制的黎明?
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戴维斯纳米
nabumetone的临床药物动力学。选择性cyclo-oxygenase-2抑制的黎明?
Pharmacokinet。1997年12月,33 (6):404 - 16。doi: 10.2165 / 00003088-199733060-00001。
- PubMed ID
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9435990 (在PubMed]
- 文摘
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Nabumetone是一种非甾体类抗炎药(非甾体抗炎药)2,6-disubstituted naphthyl-alkanone类。Nabumetone代谢是一个活跃的代谢物6-methoxy-2-napthylacetic酸(6-MNA)是一个相对选择性cyclo-oxygenase-2抑制剂,具有抗炎、镇痛属性。Nabumetone及其代谢物广泛结合血浆白蛋白。Nabumetone 6-MNA消除生物转化后,不接受肝肠循环和各自的glucoroconjugated代谢物排出尿液。大量6-MNA浓度达到滑液,这是他提议的行动在慢性炎性关节病。一个较小的血浆浓度时间曲线下面积(AUC)是明显的稳态与单个剂量;这可能是由于增加的体积分布和饱和的蛋白质绑定。6-MNA浓度和治疗和毒理学效应之间的关系尚未阐明非甾体抗炎药。肾功能衰竭显著减少6-MNA消除但稳态浓度的6-MNA并不增加,可能是因为非线性蛋白质绑定。老年骨性关节炎患者证明消除和减少nabumetone等离子体浓度的增加与年轻健康的志愿者。 Rheumatic disease activity also influences 6-MNA plasma concentrations, as patients with more active disease and lower serum albumin concentrations demonstrate a lower area under the plasma concentration versus time curve. A reduced bioavailability of 6-MNA in patients with severe hepatic impairment is also evident. Dosage adjustment may be required in the elderly, patients with active rheumatic disease and those with hepatic impairment, but not in patients with mild-to-moderate renal failure.
