Bird H A, Francis R J, Le Gallez P, Hill J, Dixon J S, Allen J G, Wright V
Eur J Rheumatol Inflamm. 1985;8(1):60-9.
Tenoxicam is a new non-steroidal anti-inflammatory drug with a long half-life. Since such drugs may be particularly prone to accumulate in elderly patients, a group of the population in which anti-inflammatory agents are most commonly prescribed, we have studied the pharmacokinetics of tenoxicam in 18 patients (age range 62-87 years) with osteoarthrosis or rheumatoid arthritis. A pharmacokinetic profile was performed after a single 20 mg oral dose. Patients then took regular medication until they had reached steady-state for chronic dosing (20 mg/day) when a further pharmacokinetic profile was performed. Approximately five-fold accumulation was found at steady-state (mean peak plasma level 2.6 micrograms/ml for a single dose against 12.4 micrograms/ml at steady-state). Twenty percent of the dose was eliminated in the first dose interval. Mean pre-dose plasma level at steady-state was 9.6 micrograms/ml with a coefficient of variation of 11%. Serial haematological and biochemical estimations during the study showed no evidence of drug toxicity.
替诺昔康是一种新型非甾体抗炎药，半衰期较长。鉴于这类药物在老年患者（最常开具抗炎药的人群之一）中可能特别容易蓄积，我们研究了18名年龄在62至87岁之间患骨关节炎或类风湿关节炎患者体内替诺昔康的药代动力学。单次口服20毫克剂量后进行了药代动力学分析。然后患者服用常规药物，直至达到慢性给药（20毫克/天）的稳态，此时进行了进一步的药代动力学分析。稳态时发现约有五倍的蓄积（单剂量时平均血浆峰值水平为2.6微克/毫升，而稳态时为12.4微克/毫升）。20%的剂量在第一个给药间隔内消除。稳态时的平均给药前血浆水平为9.6微克/毫升，变异系数为11%。研究期间的系列血液学和生化评估未显示药物毒性迹象。
