Knörle Rainer, Feuerstein Thomas J, Schulze-Bonhage Andreas
Institut für biochemische Analysen und Methodenentwicklung GbR, Freiburg/Brsg., Germany.
Arzneimittelforschung. 2004;54(3):139-42. doi: 10.1055/s-0031-1296950.
Gabapentin (1-(aminomethyl)cyclohexane acetic acid, CAS 601 42-96-3, GBP, Neurontin) and its derivative gabapentin-lactam (8-aza-spiro[5,4]decan-9-one, GBP-L) were determined by HPLC in the serum of patients with focal epilepsy treated with GBP. In patients in whom serum was acquired within 3 h after oral intake, GBP-L could be detected at concentrations up to 8.2 micromol/l. As GBP-L has been previously shown to exert neuroprotective effects in a similar concentration range, this finding suggests that clinically relevant effects of GBP-L may occur in patients treated with GBP. The possible neuroprotective efficacy of GBP-L should be the subject of further preclinical and clinical investigations.
采用高效液相色谱法（HPLC）测定了接受加巴喷丁（GBP，商品名Neurontin，化学名为1-(氨甲基)环己烷乙酸，CAS 60142-96-3）治疗的局灶性癫痫患者血清中的加巴喷丁及其衍生物加巴喷丁内酰胺（8-氮杂螺[5,4]癸烷-9-酮，GBP-L）。在口服后3小时内采集血清的患者中，可检测到浓度高达8.2微摩尔/升的GBP-L。由于此前已证明GBP-L在类似浓度范围内具有神经保护作用，这一发现表明，接受GBP治疗的患者可能会出现与临床相关的GBP-L效应。GBP-L可能的神经保护功效应作为进一步临床前和临床研究的主题。
