Airaksinen E M, Koivisto K, Keränen T, Pitkänen A, Riekkinen P J, Oja S S, Marnela K M, Partanen J V, Tokola O, Gothóni G
Department of Pediatrics, University of Kuopio, Finland.
Epilepsy Res. 1987 Sep;1(5):308-11. doi: 10.1016/0920-1211(87)90008-8.
Taltrimide (2-phthalimidoethanesulphon-N-isopropylamide), a lipophilic derivative of taurine and a potent anticonvulsant in animal studies, was administered in daily doses of 1 and 2 g for 2 weeks with an interval of 2.5 months in 2 phase I clinical trials to 9 drug-resistant epileptic patients. Seizures and EEG were recorded, and routine laboratory studies conducted. Concentrations of antiepileptic drugs in plasma, of amino acids in urine and plasma, and contents of amino acids, homovanillic acid (HVA), 5-hydroxyindoleacetic acid (5-HIAA) and cyclic nucleotides in the cerebrospinal fluid were determined. Although no clinical or neurophysiological effects were observed, an increase in the cerebrospinal fluid contents of HVA and cyclic nucleotides and changes in the concentrations of antiepileptic drugs and amino acids were found. The concentrations of HVA correlated with those of 5-HIAA and also with those of the main active metabolite of taltrimide. Biochemical changes due to taltrimide treatment resembled only partly those found after taurine treatment.
酞谷酰亚胺（2-邻苯二甲酰亚胺基乙磺酰-N-异丙基酰胺）是牛磺酸的亲脂性衍生物，在动物研究中是一种有效的抗惊厥剂。在两项I期临床试验中，对9名耐药癫痫患者每日给予1克和2克的剂量，持续2周，间隔2.5个月。记录癫痫发作和脑电图，并进行常规实验室研究。测定血浆中抗癫痫药物的浓度、尿液和血浆中氨基酸的浓度，以及脑脊液中氨基酸、高香草酸（HVA）、5-羟吲哚乙酸（5-HIAA）和环核苷酸的含量。虽然未观察到临床或神经生理学效应，但发现脑脊液中HVA和环核苷酸含量增加，以及抗癫痫药物和氨基酸浓度发生变化。HVA的浓度与5-HIAA的浓度相关，也与酞谷酰亚胺的主要活性代谢物的浓度相关。酞谷酰亚胺治疗引起的生化变化仅部分类似于牛磺酸治疗后发现的变化。
