Karolinska Trial Alliance Phase 1 Unit, M62, Karolinska University Hospital, Stockholm, Sweden.
Eur J Clin Pharmacol. 2013 Feb;69(2):143-9. doi: 10.1007/s00228-012-1320-8. Epub 2012 Jun 17.
Transdermal buprenorphine patches provide comparable pain relief to that of low-potency opioids in elderly individuals. However, specific data on their use in elderly individuals is limited. This study investigated and compared the PK of buprenorphine transdermal patches in elderly (≥ 75 years) versus younger (50-60 years) individuals.
This was a multiple-dose, open-label, parallel-group study in healthy volunteers split into two age groups (younger, 50-60 years; elderly, ≥ 75 years) with 37 individuals in each. Study participants received two consecutive 7-day buprenorphine 5 μg/h transdermal patch applications, and blood samples were collected on the week of the second patch application [day 7 (predose), days 8, 9, 10, 12, and 14] to determine PK at steady state. Pharmacokinetic parameters were determined for buprenorphine and norbuprenorphine. Safety was assessed by analyzing adverse events, hematology, clinical chemistry, urine analysis, vital signs, electrocardiogram (ECG), and physical examinations.
The area under the plasma concentration-time curve at steady state (AUC(tau)), measured over one dosing interval, was similar for elderly [mean ± standard deviation (SD) 9,940 pg/h/ml (4,827 pg/h/ml] and younger [mean ± SD 11,309 (3,670 pg/h/ml] individuals. Bioequivalence was not demonstrated between groups, which may be attributable to the relatively high level of variability in individual plasma profiles. More adverse events were reported by younger (216) than elderly (164) study participants.
No dosage alterations are necessary for PK reasons when treating elderly people with buprenorphine transdermal patches.
透皮丁丙诺啡贴片在老年人中的止痛效果与低效能阿片类药物相当。然而，关于其在老年人中使用的数据有限。本研究调查并比较了丁丙诺啡透皮贴片在老年（≥75 岁）和年轻（50-60 岁）个体中的药代动力学（PK）。
这是一项在健康志愿者中进行的、多剂量、开放标签、平行组研究，分为两个年龄组（年轻组，50-60 岁；老年组，≥75 岁），每组 37 人。研究参与者接受了两次连续的 7 天丁丙诺啡 5μg/h 透皮贴片应用，在第二次贴片应用的第 7 天（预给药）、第 8、9、10、12 和 14 天采集血样，以确定稳态时的 PK。测定了丁丙诺啡和去甲丁丙诺啡的药代动力学参数。通过分析不良事件、血液学、临床化学、尿液分析、生命体征、心电图（ECG）和体格检查来评估安全性。
稳态时（AUC(tau)），一个给药间隔的血浆浓度-时间曲线下面积，老年组（平均值±标准差[SD]，9940pg/h/ml[4827pg/h/ml]）和年轻组（平均值±SD，11309[3670pg/h/ml]）相似。两组间未显示生物等效性，这可能归因于个体血浆谱的变异性较高。年轻组（216 例）报告的不良事件多于老年组（164 例）。
对于使用丁丙诺啡透皮贴片治疗的老年人，无需出于 PK 原因调整剂量。
