Isojärvi J I, Tokola R A
Department of Neurology, University of Oulu, Finland.
J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92.
All the benzodiazepines (BZDs) in clinical use have the capacity to promote the binding of the major inhibitory neurotransmitter, gamma-amino-butyric acid (GABA), to sub-types of GABA receptors which exist as multi-subunit ligand-gated chloride channels. Thus, the BZDs facilitate the actions of GABA in the brain. The BZDs in use as antiepileptic drugs are diazepam, clonazepam, clobazam, nitrazepam, and lately, also lorazepam and midazolam as emergency therapy. The BZDs have a wide-spectrum of proven clinical efficacy in the prevention of different kind of seizures. Clonazepam and clobazam, as well as nitrazepam in some cases, can be useful as an adjunct treatment in refractory epilepsies. However, the clinical use of BZDs for the prophylactic treatment of epilepsy is associated with two major problems which have limited the long-term use of these drugs: the potential for side-effects, especially sedative effects, and the high risk of development of tolerance. Despite the limitations of BZDs in the prophylactic treatment of epilepsies, these drugs play a prominent role in clinical practice in the emergency management of acute seizures and status epilepticus. Diazepam, clonazepam and lorazepam are all considered first-line agents in the emergency management of acute seizures and status epilepticus. Furthermore, the value of midazolam as an emergency therapy in epilepsy has been increasingly recognized in recent years.
所有临床使用的苯二氮䓬类药物（BZDs）都有促进主要抑制性神经递质γ-氨基丁酸（GABA）与GABA受体亚型结合的能力，这些受体以多亚基配体门控氯离子通道的形式存在。因此，BZDs可促进GABA在大脑中的作用。用作抗癫痫药物的BZDs有地西泮、氯硝西泮、氯巴占、硝西泮，最近，劳拉西泮和咪达唑仑也作为急救疗法使用。BZDs在预防不同类型癫痫发作方面有广泛且已证实的临床疗效。氯硝西泮和氯巴占，以及在某些情况下的硝西泮，可作为难治性癫痫的辅助治疗药物。然而，BZDs用于癫痫预防性治疗的临床应用存在两个主要问题，这限制了这些药物的长期使用：副作用的可能性，尤其是镇静作用，以及产生耐受性的高风险。尽管BZDs在癫痫预防性治疗方面存在局限性，但这些药物在急性癫痫发作和癫痫持续状态的急救管理临床实践中发挥着重要作用。地西泮、氯硝西泮和劳拉西泮均被视为急性癫痫发作和癫痫持续状态急救管理的一线药物。此外，近年来，咪达唑仑作为癫痫急救疗法的价值越来越受到认可。
