Ben-Menachem E, Persson L I, Hedner T
Department of Neurology, University of Göteborg, Sweden.
Epilepsy Res. 1992 Mar;11(1):45-9. doi: 10.1016/0920-1211(92)90020-t.
Gabapentin (GBP) is a neutral amino acid and a GABA analog which in animal experimental models has shown a broad anticonvulsant spectrum. To evaluate the penetration of GBP into the CSF in humans as well as its possible effects on free and total GABA, homovanillic acid (HVA), and 5-hydroxyindoleacetic acid (5-HIAA), a special investigation was performed as part of a placebo controlled add-on study of GBP in partial epilepsy. At the end of the 3-month double-blind period, 5 patients on placebo were given a single oral dose of GBP. Four patients received 600 mg and 1 patient 1200 mg GBP. CSF was collected immediately before and at 6, 24 and 72 h after the single dose. 5 ml of plasma was collected at 1, 2, 3, 6, 12, 24, 48 and 72 h. Plasma concentrations and plasma elimination half-life (4-6 h) of GBP were in agreement with the results of previous studies. The CSF/plasma concentration ratio of GBP 6 h after drug was 0.1. After 24 h, GBP could only be recovered in the CSF of the patient given 1200 mg. The CSF/plasma ratio at that time was 0.3. Free and total GABA concentrations did not change, but CSF 5-HIAA and HVA increased at 24 and 72 h post dose. The CSF/plasma ratio of gabapentin is similar to that of other amino acids.
加巴喷丁（GBP）是一种中性氨基酸，也是一种γ-氨基丁酸（GABA）类似物，在动物实验模型中显示出广泛的抗惊厥谱。为了评估GBP在人体脑脊液中的渗透情况以及它对游离和总GABA、高香草酸（HVA）和5-羟吲哚乙酸（5-HIAA）可能产生的影响，作为GBP用于部分性癫痫的安慰剂对照附加研究的一部分，进行了一项专项调查。在为期3个月的双盲期结束时，给5名服用安慰剂的患者单次口服GBP。4名患者服用600mg，1名患者服用1200mg GBP。在单次给药前以及给药后6、24和72小时立即采集脑脊液。在1、2、3、6、12、24、48和72小时采集5ml血浆。GBP的血浆浓度和血浆消除半衰期（4 - 6小时）与先前研究结果一致。给药6小时后GBP的脑脊液/血浆浓度比为0.1。24小时后，仅在服用1200mg的患者脑脊液中检测到GBP。此时的脑脊液/血浆比为0.3。游离和总GABA浓度未发生变化，但给药后24和72小时脑脊液中5-HIAA和HVA升高。加巴喷丁的脑脊液/血浆比与其他氨基酸相似。
