Nilsen O G, Walstad R A, Eckert M, Heizmann P, Bückert A, Am T, Løge I, Unnvik J, Thue E
Department of Pharmacology and Toxicology, Faculty of Medicine, University of Trondheim, Norway.
Eur J Clin Pharmacol. 1988;35(5):563-6. doi: 10.1007/BF00558254.
Fourteen elderly subjects (10 women, 4 men) with a mean age of 81 (SD 6.7) years and in need of anti-inflammatory drug treatment were given a single dose of 20 mg tenoxicam. After a drug-free interval of 5 weeks, multiple dose treatment with 20 mg tenoxicam once daily for 56 days was initiated. The single and multiple dose kinetics of tenoxicam were investigated after HPLC determination of tenoxicam in the plasma. The elimination half-life of tenoxicam ranged from 44 to 132 h (mean 71.9 h) with no significant difference between the single and multiple dosage regimens. Tenoxicam reached maximum plasma concentrations after 1.4 and 1.1 h, with values of 3.6 and 15.5 micrograms.ml-1, for the single and multiple dosage regimen respectively. The corresponding trough values (24-h values) were 1.8 and 11.7 micrograms.ml-1. A mean accumulation ratio of 5.1 was calculated. The mean increase in the area under the plasma concentration time curves at steady-state was 21% more than predicted from the initial single dose. This deviation from linearity was considered to be of minor clinical significance. The kinetics of tenoxicam in elderly were similar to that published for young healthy volunteers.
14名平均年龄为81岁（标准差6.7）且需要抗炎药物治疗的老年受试者（10名女性，4名男性）接受了20毫克替诺昔康的单次给药。在5周的无药间隔期后，开始进行为期56天、每日一次20毫克替诺昔康的多剂量治疗。在通过高效液相色谱法测定血浆中的替诺昔康后，对替诺昔康的单剂量和多剂量动力学进行了研究。替诺昔康的消除半衰期为44至132小时（平均71.9小时），单剂量和多剂量给药方案之间无显著差异。替诺昔康在1.4小时和1.1小时后达到最大血浆浓度，单剂量和多剂量给药方案的相应值分别为3.6和15.5微克·毫升-1。相应的谷值（24小时值）分别为1.8和11.7微克·毫升-1。计算出平均蓄积比为5.1。稳态时血浆浓度时间曲线下面积的平均增加比初始单剂量预测值高21%。这种与线性的偏差被认为具有较小的临床意义。替诺昔康在老年人中的动力学与年轻健康志愿者发表的情况相似。
