Hirsch Edouard, Genton Pierre
Department of Functional Explorations of Epilepsies, Civil Hospital, Strasbourg, France.
CNS Drugs. 2003;17(9):633-40. doi: 10.2165/00023210-200317090-00003.
Thirty-five years since its introduction into clinical use, valproate (valproic acid) has established itself as one of the most widely used antiepileptic drugs (AEDs). In recent years, there has been a growing awareness of the potential aggravation of seizure disorders by AEDs. Such aggravation may be due to a variety of factors that include a paradoxical pharmacodynamic effect. In order to address this important safety aspect of AED treatment, we reviewed all available published evidence in search of factors related to seizure aggravation during valproate therapy. We analysed the 20 available publications, which outline about 99 case reports (in some papers, the exact number was not specified) of aggravation of seizures associated with valproate. Almost all of these cases occurred in a specific clinical context known to be linked to seizure aggravation, such as overdose, encephalopathy, hepatopathy or metabolic disorders. However, we found no consistent evidence of pure pharmacodynamic aggravation in the absence of any of the above quoted factors. In view of the large number of patients treated worldwide with valproate, the number of reported cases of seizure aggravation in patients taking the drug in the literature is low. Conditions in which worsening of seizures as a result of valproate use may occur are well known and often avoidable. Thus, unlike most AEDs, including the newer ones, valproate appears to have a very low potential for pharmacodynamic paradoxical seizure aggravation. This knowledge is in accordance with long-standing clinical experience and practice.
丙戊酸盐(丙戊酸)自引入临床使用35年来,已成为使用最广泛的抗癫痫药物(AEDs)之一。近年来,人们越来越意识到AEDs可能会加重癫痫疾病。这种加重可能是由于多种因素引起的,包括矛盾的药效学效应。为了解决AED治疗这一重要的安全问题,我们回顾了所有已发表的证据,以寻找与丙戊酸盐治疗期间癫痫发作加重相关的因素。我们分析了20篇可用的出版物,这些出版物概述了约99例与丙戊酸盐相关的癫痫发作加重的病例报告(在一些论文中,确切数字未明确说明)。几乎所有这些病例都发生在已知与癫痫发作加重相关的特定临床背景下,如过量用药、脑病、肝病或代谢紊乱。然而,我们没有发现任何一致的证据表明在没有上述任何因素的情况下存在单纯的药效学加重。鉴于全球范围内使用丙戊酸盐治疗的患者数量众多,文献中报道的服用该药物患者癫痫发作加重的病例数量较少。因使用丙戊酸盐而导致癫痫发作恶化的情况是众所周知的,并且通常是可以避免的。因此,与大多数AEDs(包括新型药物)不同,丙戊酸盐似乎具有非常低的药效学矛盾性癫痫发作加重的可能性。这一认识与长期的临床经验和实践一致。