Srinivasan J, Richens A
Department of Pharmacology and Therapeutics, University of Wales College of Medicine, Heath Park, Cardiff.
Drug Saf. 1994 May;10(5):395-405. doi: 10.2165/00002018-199410050-00004.
Vigabatrin was designed to increase the levels of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in the brain. It does this by replacing GABA as a substrate for the action of the catabolic enzyme GABA-transaminase. As a result of this inhibition, neuronal GABA levels are elevated, resulting in enhanced endogenous GABA transmission. A number of clinical trials assessing the effect of vigabatrin in epilepsy have been completed. Vigabatrin is of proven benefit in partial seizures and secondarily generalised tonic clonic seizures, and it is licensed for use as adjunctive therapy in these conditions in several European countries. It has been shown to be effective in some epilepsy syndromes in children including West's syndrome, infantile spasms and cryptogenic partial seizures. Its effect on primary generalised tonic clonic seizures is variable, while there is considerable evidence that it has a deleterious effect on myoclonic and absence seizures. There have been a few reports of the benefits of vigabatrin in other neurological disorders including tardive dyskinesia, degenerative ataxias and GABA metabolism disorders. The adverse effects associated with vigabatrin are similar to those seen with other anticonvulsants, with a predominance of CNS effects including somnolence, fatigue, irritability, dizziness and headache. Psychiatric symptoms including depression and psychosis are seen in a small number of patients and cause the most problems. These often necessitate discontinuation of vigabatrin, which usually results in resolution of symptoms.
氨己烯酸旨在提高大脑中抑制性神经递质γ-氨基丁酸（GABA）的水平。它通过取代GABA作为分解代谢酶GABA转氨酶作用的底物来实现这一点。由于这种抑制作用，神经元GABA水平升高，导致内源性GABA传递增强。多项评估氨己烯酸治疗癫痫效果的临床试验已经完成。氨己烯酸在部分性癫痫发作和继发性全面强直阵挛性癫痫发作中已被证明有益，并且在几个欧洲国家被批准作为这些病症的辅助治疗药物使用。它已被证明对包括韦斯特综合征、婴儿痉挛症和隐源性部分性癫痫发作在内的儿童癫痫综合征有效。它对原发性全面强直阵挛性癫痫发作的效果不一，而有大量证据表明它对肌阵挛性癫痫发作和失神性癫痫发作有有害影响。有一些关于氨己烯酸在其他神经系统疾病（包括迟发性运动障碍、退行性共济失调和GABA代谢障碍）中的益处的报道。与氨己烯酸相关的不良反应与其他抗惊厥药物类似，主要是中枢神经系统效应，包括嗜睡、疲劳、易怒、头晕和头痛。少数患者会出现包括抑郁和精神病在内的精神症状，这些症状会引发最多问题。这些症状通常需要停用氨己烯酸，停用后症状通常会缓解。
