Suppr超能文献

美洛昔康的临床药代动力学综述。

A review of the clinical pharmacokinetics of meloxicam.

作者信息

Türck D, Roth W, Busch U

机构信息

Department of Pharmacokinetics and Drug Metabolism, Dr Karl Thomae GmbH, Biberach/Riss, Germany

出版信息

Br J Rheumatol. 1996 Apr;35 Suppl 1:13-6. doi: 10.1093/rheumatology/35.suppl_1.13.

Abstract

Meloxicam is a new preferential cyclooxygenase-2 (COX-2) inhibitor currently for the treatment of osteoarthritis and rheumatoid arthritis. Its pharmacokinetic profile is characterized by a prolonged and almost complete absorption and the drug is > 99.5% bound to plasma proteins. Meloxicam is metabolized to four biologically inactive main metabolites, which are excreted in both urine and faeces. The elimination half-life (t1/2) of meloxicam is approximately 20 h. This is reflected in a total plasma clearance (CL) of 0.42-0.48 1/h. Steady-state plasma concentrations are achieved within 3-5 days. The pharmacokinetic parameters of meloxicam are linear over the dose range 7.5-30 mg and bioequivalence has been shown for a number of different formulations. No interactions were observed following the concomitant administration of food, cimetidine, antacid, aspirin, beta-acetyldigoxin, methotrexate, warfarin or furosemide. Neither hepatic insufficiency nor moderate renal dysfunction have any relevant effects on the pharmacokinetics of meloxicam and dosage adjustments in the elderly are not required.

摘要

美洛昔康是一种新型的选择性环氧化酶-2(COX-2)抑制剂,目前用于治疗骨关节炎和类风湿性关节炎。其药代动力学特征为吸收时间延长且几乎完全吸收,药物与血浆蛋白的结合率>99.5%。美洛昔康代谢为四种无生物活性的主要代谢产物,经尿液和粪便排出。美洛昔康的消除半衰期(t1/2)约为20小时,这反映在总血浆清除率(CL)为0.42 - 0.48升/小时。在3 - 5天内达到稳态血浆浓度。美洛昔康的药代动力学参数在7.5 - 30毫克的剂量范围内呈线性,并且已证明多种不同剂型具有生物等效性。同时服用食物、西咪替丁、抗酸剂、阿司匹林、β-乙酰地高辛、甲氨蝶呤、华法林或呋塞米后未观察到相互作用。肝功能不全或中度肾功能不全对美洛昔康的药代动力学均无相关影响,老年人无需调整剂量。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验