Sabers A, Gram L
University Clinic of Neurology, Hvidovre Hospital, Denmark.
Pharmacol Toxicol. 1992 Apr;70(4):237-43. doi: 10.1111/j.1600-0773.1992.tb00465.x.
Vigabatrin (gamma-vinyl GABA) is a relatively new antiepileptic drug. Vigabatrin increases the concentration of gamma-aminobutyric acid (GABA) in the brain by inhibiting the major GABA metabolizing enzyme, GABA transaminase. Controlled clinical trials have demonstrated an excellent antiepileptic effect of vigabatrin, especially in the treatment of partial epilepsies. Long-term evaluations have shown no signs of tolerance development. Vigabatrin decreases the plasma concentration of phenytoin during concomitant therapy, the only drug with which an interaction seems to occur. In general, vigabatrin is well tolerated. Psychotic reactions occur in 3-6% of patients. Other frequent side effects are sedation and weight increase. Chronic vigabatrin intoxication in animals caused development of intramyelinic oedema, appearing as microvacuoles in brain white matter. No microvacuolation has been observed in humans, even after long-term treatment. Vigabatrin seems a very valuable new antiepileptic drug.
氨己烯酸（γ-乙烯基-GABA）是一种相对较新的抗癫痫药物。氨己烯酸通过抑制主要的γ-氨基丁酸（GABA）代谢酶——GABA转氨酶，来提高大脑中GABA的浓度。对照临床试验已证明氨己烯酸具有出色的抗癫痫效果，尤其是在治疗部分性癫痫方面。长期评估表明没有出现耐受性发展的迹象。在联合治疗期间，氨己烯酸会降低苯妥英的血浆浓度，它似乎是唯一与之发生相互作用的药物。总体而言，氨己烯酸耐受性良好。3%至6%的患者会出现精神反应。其他常见副作用为镇静和体重增加。动物慢性氨己烯酸中毒会导致髓鞘内水肿的发展，表现为脑白质中的微泡。即使经过长期治疗，在人类中也未观察到微泡形成。氨己烯酸似乎是一种非常有价值的新型抗癫痫药物。
