Lecaillon J B, Dubois J P, Coppens H, Darragon T, Theobald W, Reumond G, Beck H
Biopharmaceutical Research Center and Medical Department, Laboratoires CIBA-GEIGY, Rueil-Malmaison, France.
Eur J Drug Metab Pharmacokinet. 1990 Jul-Sep;15(3):223-30. doi: 10.1007/BF03190208.
The pharmacokinetics of oxiracetam have been studied in eighteen elderly patients and in six healthy non-geriatric adults. A 800 mg single oral dose was administered in the morning of the first day and repeatedly, every 12 h, from day 2 evening to day 10 morning, to the elderly patients. The healthy non-geriatric adults were given a 800 mg single oral dose of oxiracetam. In healthy non-geriatric subjects after a single oral administration of 800 mg, the normalized plasma levels of oxiracetam for 1 mg/kg dose were similar to those already recorded after a 2000 mg single dose of oxiracetam. Therefore, there was no tendency towards non-linear pharmacokinetics of oxiracetam between 800 and 2000 mg single doses in healthy subjects. After the single oral dose, the mean area under the plasma concentration-time curve of oxiracetam in elderly patients was increased by a factor of two as compared to that observed in non-geriatric healthy subjects whereas the maximum concentration (Cmax) was almost not modified and slightly delayed. This can be explained by a slower absorption and elimination in the elderly patients. The highest oxiracetam levels were predominantly recorded in the oldest patients. The slower elimination (mean T1/2 = 12.3 h in elderly and 7.7 h in healthy subjects) could be attributed to a physiological decrease of the renal function. The volume of distribution was not significantly modified in the elderly patients.(ABSTRACT TRUNCATED AT 250 WORDS)
已在18名老年患者和6名健康非老年成年人中研究了奥拉西坦的药代动力学。第一天上午给老年患者单次口服800毫克剂量,从第二天晚上到第十天上午,每12小时重复给药一次。给健康非老年成年人单次口服800毫克奥拉西坦。在健康非老年受试者单次口服800毫克后,每1毫克/千克剂量的奥拉西坦标准化血浆水平与单次口服2000毫克奥拉西坦后记录的水平相似。因此,在健康受试者中,800至2000毫克单次剂量之间奥拉西坦不存在非线性药代动力学趋势。单次口服给药后,老年患者奥拉西坦血浆浓度-时间曲线下的平均面积比非老年健康受试者增加了两倍,而最大浓度(Cmax)几乎未改变且略有延迟。这可以用老年患者吸收和消除较慢来解释。最高的奥拉西坦水平主要记录在年龄最大的患者中。消除较慢(老年患者平均T1/2 = 12.3小时,健康受试者为7.7小时)可能归因于肾功能的生理性下降。老年患者的分布容积没有明显改变。(摘要截短至250字)