Parnetti L, Mecocci P, Gaiti A, Cadini D, Lombardi F, Visconti M, Senin U
Chair of Gerontology and Geriatrics, Perugia University, Italy.
Eur J Drug Metab Pharmacokinet. 1990 Jan-Mar;15(1):75-8. doi: 10.1007/BF03190131.
The purpose of the study was to determine whether oxiracetam crosses the human blood-brain barrier and to evaluate its comparative kinetics in serum and in cerebro-spinal fluid (CSF). Six DAT patients, undergoing CSF collection for diagnostic purposes, received 2 g oxiracetam daily, by a 60 min i.v. infusion, for 7 days. On the last day, in four patients blood samples were collected at time 0, 30, 60 and 120 min, and lumbar drainage was performed at the end of infusion: at this time mean CSF concentration was 3.5 micrograms/ml, i.e. 4.0% of the serum one, demonstrating that oxiracetam crosses the blood-brain barrier. In two patients, blood samples were collected at time 0, 60, 120 and 240 min, and lumbar drainage was performed 60 min after the end of infusion: at this time mean CSF concentration was 2.8 micrograms/ml, i.e. 5.3% of the serum one, indicating a persistence of oxiracetam within this deep compartment. These results provide the first evidence in humans that oxiracetam penetrates the central nervous system and contribute to the understanding of its long-lasting pharmacodynamic effect in man.
本研究的目的是确定奥拉西坦是否能穿过血脑屏障，并评估其在血清和脑脊液（CSF）中的相对动力学。6例因诊断目的接受脑脊液采集的痴呆患者，每天静脉输注2 g奥拉西坦，输注时间为60分钟，共7天。在最后一天，4例患者在0、30、60和120分钟时采集血样，并在输注结束时进行腰椎引流：此时脑脊液平均浓度为3.5微克/毫升，即血清浓度的4.0%，表明奥拉西坦能穿过血脑屏障。另外2例患者在0、60、120和240分钟时采集血样，并在输注结束60分钟后进行腰椎引流：此时脑脊液平均浓度为2.8微克/毫升，即血清浓度的5.3%，表明奥拉西坦在这个深部腔室中持续存在。这些结果首次在人体中证明奥拉西坦能穿透中枢神经系统，并有助于理解其在人体中的持久药效学作用。
