Türck D, Roth W, Busch U
Department of Pharmacokinetics and Drug Metabolism, Dr Karl Thomae GmbH, Biberach/Riss, Germany
Br J Rheumatol. 1996 Apr;35 Suppl 1:13-6. doi: 10.1093/rheumatology/35.suppl_1.13.
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.
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。
