Biochemical and clinical effects of γ‐vinyl GABA in patients with epilepsy

Biochemical and clinical effects of γ‐vinyl GABA in patients with epilepsy
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γ-乙烯基 GABA 对癫痫患者的生化和临床效果

DOI:
10.1212/wnl.34.2.182
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发表时间:
1984
期刊:
影响因子:
9.9
通讯作者:
A. Sjoerdsma
A. Sjoerdsma
中科院分区:
医学1区
文献类型:
--
作者:
P. Schechter;N. Hanke;J. Grove;N. Huebert;A. Sjoerdsma

文献摘要

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本文采用单盲试验性研究方法,对10例常规抗惊厥药物治疗无效的癫痫患者,口服一种酶激活的不可逆转氨酶抑制剂--γ-乙烯基氨基丁酸。每日剂量分别为1g和2g,各2周,作为补充治疗,随后是2周的安慰剂治疗。枕下和腰椎针刺脑脊液中游离和总GABA及同型肌氨酸的浓度随治疗剂量的增加而升高,但5-羟基吲哚乙酸或高香草酸的浓度无明显变化,表明中枢神经系统GABA-T的抑制是有效的和选择性的。这些生化变化与7例患者癫痫发作频率降低、1例癫痫发作严重程度降低、1例无变化、1例可能恶化有关。γ-乙烯基氨基丁酸可用于癫痫的治疗。
Article abstract-In a pilot single-blind study, γ-vinyl GABA, an enzyme-activated irreversible inhibitor of GABA-transaminase (GABA-T), was administered orally to 10 epileptic patients who were refractory to conventional anticonvulsant therapy. Daily doses of 1 g and 2 g for 2 weeks each as add-on therapy were followed by 2 weeks of placebo treatment. CSF obtained from suboccipital and lumbar punctures demonstrated dose-related increases in concentrations of free and total GABA and homocarnosine with treatment, but no changes in 5-hydroxyindoleacetic acid or homovanillic acid levels, indicating effective and selective CNS GABA-T inhibition. These biochemical changes were associated with decreased seizure frequency in seven patients, decreased seizure severity in one, no change in one, and possible worsening in one. γ-Vinyl GABA may be useful in the therapy of epilepsy.