Ben-Menachem E, Söderfelt B, Hamberger A, Hedner T, Persson L I
Department of Neurology, University of Göteborg, Sweden.
Epilepsy Res. 1995 Jul;21(3):231-6. doi: 10.1016/0920-1211(95)00026-7.
Gabapentin (GBP) is a non-protein-bound gamma amino acid which is not subjected to metabolic degradation in man. As part of a placebo-controlled double-blind study, patients suffering from intractable complex partial seizures with or without secondary generalization were followed with lumbar punctures at baseline and after three months of GBP treatment (900 mg/day or 1200 mg/day). Cerebrospinal fluid (CSF) was analyzed for concentrations of GBP, amino acids including GABA, homovanillic acid (HVA), and 5 hydroxyindoleacetic acid (5-HIAA). The results indicate that there were no changes in the selected amino acids, HVA, or 5-HIAA after GBP treatment. At steady state the CSF/plasma ratios of GBP ranged from 0.056 to 0.34, indicating that there may be some type of active out-transport of GBP across the blood-brain barrier. No linear relationship was observed between plasma and CSF levels in these patients.
加巴喷丁（GBP）是一种非蛋白结合的γ氨基酸，在人体内不会发生代谢降解。作为一项安慰剂对照双盲研究的一部分，对患有顽固性复杂部分性癫痫发作（伴或不伴继发性全身性发作）的患者在基线时以及接受GBP治疗三个月（900毫克/天或1200毫克/天）后进行腰椎穿刺随访。分析脑脊液（CSF）中GBP、包括γ-氨基丁酸（GABA）在内的氨基酸、高香草酸（HVA）和5-羟吲哚乙酸（5-HIAA）的浓度。结果表明，GBP治疗后所选氨基酸、HVA或5-HIAA没有变化。在稳态时，GBP的脑脊液/血浆比值在0.056至0.34之间，表明GBP可能存在某种类型的主动转运穿过血脑屏障。在这些患者中，未观察到血浆和脑脊液水平之间的线性关系。
