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拉莫三嗪——最新进展

Lamotrigine--an update.

作者信息

Brodie M J

机构信息

University Department of Medicine and Therapeutics, Western Infirmary, Glasgow, Scotland.

出版信息

Can J Neurol Sci. 1996 Nov;23(4 Suppl 2):S6-9. doi: 10.1017/s0317167100020904.

Abstract

Lamotrigine (LTG) inhibits repetitive high frequency firing in depolarised neurones by selectively prolonging slow inactivation of the sodium channel, thereby suppressing the release of excitatory amino acids. It has been shown to be effective in 11 pivotal double-blind add-on trials in patients with refractory partial seizures with or without secondary generalisation. Subsequent anecdotal data support its efficacy for typical and atypical absences, myoclonic jerks, tonic or clonic seizures, Lennox-Gastaut syndrome and infantile spasms. Most recently LTG has been compared with carbamazepine and phenytoin in double-blind trials in patients with newly diagnosed partial and primary and secondary generalised tonic-clonic seizures. At the doses used, its efficacy was similar to the older agents for all seizure types, but LTG was better tolerated than both of the older agents. The commonest side-effects with LTG include headache, nausea, diplopia, dizziness, ataxia and tremor. Rash occurs in fewer than 5% patients. Its incidence can be reduced by starting treatment with a low dose, particularly in patients receiving concomitant sodium valproate which inhibits LTG metabolism. Enzyme inducers, such as carbamazepine, phenytoin and phenobarbital, accelerate its elimination, but LTG itself has no effect on hepatic metabolic processes. A pharmacodynamic interaction with carbamazepine necessitates a dosage reduction in some patients when LTG is introduced. LTG is a new antiepileptic agent with a long elimination half-life, a broad spectrum of activity, and a wide therapeutic ratio.

摘要

拉莫三嗪(LTG)通过选择性延长钠通道的缓慢失活来抑制去极化神经元的重复性高频放电,从而抑制兴奋性氨基酸的释放。在11项针对难治性部分性癫痫发作(伴或不伴继发性全面发作)患者的关键双盲附加试验中,已证明其有效。后续的轶事性数据支持其对典型和非典型失神发作、肌阵挛抽搐、强直或阵挛性发作、Lennox-Gastaut综合征及婴儿痉挛症有效。最近,在针对新诊断的部分性、原发性和继发性全面性强直-阵挛性发作患者的双盲试验中,将LTG与卡马西平和苯妥英进行了比较。在所使用的剂量下,对于所有发作类型,其疗效与这两种老药相似,但LTG的耐受性优于这两种老药。LTG最常见的副作用包括头痛、恶心、复视、头晕、共济失调和震颤。皮疹发生率低于5%的患者。通过低剂量开始治疗可降低其发生率,尤其是在同时接受抑制LTG代谢的丙戊酸钠的患者中。酶诱导剂,如卡马西平、苯妥英和苯巴比妥,会加速其消除,但LTG本身对肝脏代谢过程无影响。当引入LTG时,与卡马西平的药效学相互作用使一些患者需要减少剂量。LTG是一种新型抗癫痫药,消除半衰期长,活性谱广,治疗窗宽。

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