Julkunen H, Michelsson J E, Mattila M J
Ann Clin Res. 1983 Jun;15(3):99-103.
Nine male and fourteen female hospital in-patients aged 45-82 years and suffering from advanced osteoarthritis participated in an open pharmacodynamic and pharmacokinetic study. After the clinical examination the patients were given piroxicam 30 mg daily for one to seven days before the elective hip joint operation. Drug effects were assessed by measuring the duration of morning stiffness and scoring pains at night and on motion. Concentrations of piroxicam were measured from serum and tissue (joint capsule, cartilage, cancellous bone) samples taken during the operation. Piroxicam concentrations in tissues were negligible on the first two days; measurable concentrations appeared from the third day on. They correlated to serum piroxicam levels but were much lower. Generally, the appearance of piroxicam in joint tissues coincided with the appearance of the analgesic effect of piroxicam. Skin samples from four patients showed piroxicam concentrations which were negligible or at least definitely lower than respective concentrations in serum. It is concluded that in patients with osteoarthritis the piroxicam concentrations in joint tissues are fairly low, and their correlation to the analgesic effect of piroxicam is not convincing.
9名年龄在45 - 82岁之间、患有晚期骨关节炎的男性住院患者和14名女性住院患者参与了一项开放的药效学和药代动力学研究。临床检查后,患者在择期髋关节手术前每天服用30毫克吡罗昔康,持续1至7天。通过测量晨僵持续时间以及对夜间和活动时的疼痛进行评分来评估药物效果。在手术期间采集血清和组织(关节囊、软骨、松质骨)样本,测量吡罗昔康的浓度。前两天组织中的吡罗昔康浓度可忽略不计;从第三天开始出现可测量的浓度。它们与血清吡罗昔康水平相关,但要低得多。一般来说,吡罗昔康在关节组织中的出现与吡罗昔康镇痛效果的出现相吻合。4名患者的皮肤样本显示吡罗昔康浓度可忽略不计,或至少明显低于血清中的相应浓度。得出的结论是,在骨关节炎患者中,关节组织中的吡罗昔康浓度相当低,并且它们与吡罗昔康镇痛效果的相关性并不令人信服。