UCL Institute of Neurology, Queen Square, London, United Kingdom.
Epilepsia. 2012 Dec;53 Suppl 8:26-39. doi: 10.1111/epi.12026.
Phenobarbital (phenobarbitone) was first used as an antiepileptic drug 100 years ago, in 1912. This article tells the story of the discovery of its antiepileptic action, its early development, and the subsequent course of its clinical use over the 100-year period. The side effects, pharmacokinetics, and misuse of barbiturates are considered, along with the more recent clinical trials and the drug's current clinical utilization. The introduction of controlled drug regulations, the comparative cost of phenobarbital, and its inclusion on the World Health Organization (WHO) essential drug list are discussed. It is one of the few drugs on the formulary in 1912 that is still listed today, and remarkably its efficacy in epilepsy has not been significantly bettered. The current recommendation by the WHO is that phenobarbital should be offered as the first option for therapy for convulsive epilepsy in adults and children if availability can be ensured. This is rated as a strong recommendation because of the proven efficacy and low cost of phenobarbital, and despite its perceived side-effect profile and the practical problems of access. Whether this recommendation puts "a hierarchy on the brain," as has been suggested, is arguable. Much still needs to be learned about the drug's effects, and the issues raised by phenobarbital have lessons for all antiepileptic drug therapy.
苯巴比妥（phenobarbitone）于 100 年前的 1912 年首次被用作抗癫痫药物。本文讲述了其抗癫痫作用的发现、早期发展以及随后在 100 年期间的临床应用过程。考虑了副作用、药代动力学和巴比妥类药物的滥用，以及最近的临床试验和该药物目前的临床应用。还讨论了管制药物法规的引入、苯巴比妥的相对成本及其在世界卫生组织（WHO）基本药物清单中的列入。它是 1912 年处方中仍在今天列出的少数几种药物之一，令人惊讶的是，它在癫痫中的疗效并没有显著提高。目前，世界卫生组织建议，如果能够确保供应，苯巴比妥应作为成人和儿童惊厥性癫痫治疗的首选药物。这是一个强烈的推荐，因为苯巴比妥的疗效已得到证实，而且成本低廉，尽管它被认为存在副作用，并且在获得方面存在实际问题。这种建议是否如有人所说的那样“对大脑进行了分级”，这是有争议的。人们仍然需要了解该药物的作用，而苯巴比妥提出的问题为所有抗癫痫药物治疗提供了教训。
