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吡仑帕奈与静脉注射卡马西平用于全身性癫痫发作的应用前景

Perspective on the use of perampanel and intravenous carbamazepine for generalized seizures.

作者信息

Franco Valentina, Iudice Alfonso, Grillo Elisabetta, Citraro Rita, De Sarro Giovambattista, Russo Emilio

机构信息

University of Pavia, Department of Internal Medicine and Therapeutics, Clinical Pharmacology Unit , Pavia , Italy.

出版信息

Expert Opin Pharmacother. 2014 Apr;15(5):637-44. doi: 10.1517/14656566.2014.879572. Epub 2014 Jan 17.

DOI:10.1517/14656566.2014.879572
PMID:24437529
Abstract

INTRODUCTION

Several antiepileptic drugs are available for the treatment of epileptic patients. However, the treatment of some seizure types and novel drug formulations deserve further advances in epilepsy research.

AREAS COVERED

The authors analyze the published evidence on the efficacy of perampanel against secondarily generalized seizures (SGS) and report the currently available development of intravenous (IV) formulations of carbamazepine (CBZ), commenting on their potential in the clinical setting.

EXPERT OPINION

Perampanel is the first noncompetitive AMPA receptor antagonist to be approved as adjunctive treatment in patients with partial-onset (focal) seizures (POS) with or without secondary generalization. Apart from its efficacy and safety on POS, a consistent body of evidence supports its efficacy in SGS at a minimum dose of 8 mg/day; however, such dose appears close to the best-tolerated dose. CBZ is a poorly water-soluble compound; many efforts to develop a parenteral formulation have not been successful so far. Novel IV CBZ formulations seem to exhibit favorable pharmacokinetics along with good tolerability in animal models and in patients taking oral CBZ. Further studies are needed to assess whether larger doses will be as well tolerated, allowing IV CBZ to be used as bridge therapy when the oral route is not feasible or in patients naïve to CBZ.

摘要

引言

有几种抗癫痫药物可用于治疗癫痫患者。然而,某些癫痫发作类型的治疗以及新型药物制剂仍值得在癫痫研究中取得进一步进展。

涵盖领域

作者分析了已发表的关于吡仑帕奈治疗继发全身性癫痫发作(SGS)疗效的证据,并报告了目前卡马西平(CBZ)静脉制剂的研发情况,同时对其在临床环境中的潜力进行了评论。

专家意见

吡仑帕奈是首个被批准用于治疗伴有或不伴有继发全身性发作的部分性发作(局灶性)癫痫(POS)患者的非竞争性AMPA受体拮抗剂。除了对POS的疗效和安全性外,大量证据支持其在最低剂量为8毫克/天时对SGS的疗效;然而,该剂量似乎接近耐受性最佳的剂量。CBZ是一种水溶性较差的化合物;到目前为止,许多开发肠胃外制剂的努力都没有成功。新型静脉注射CBZ制剂在动物模型和口服CBZ的患者中似乎表现出良好的药代动力学以及耐受性。需要进一步研究来评估更大剂量是否同样耐受,以便在口服途径不可行时或对CBZ初治的患者中,将静脉注射CBZ用作桥接疗法。

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引用本文的文献

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Current role of perampanel in pediatric epilepsy.吡仑帕奈在小儿癫痫中的当前作用。
Ital J Pediatr. 2017 Jun 2;43(1):51. doi: 10.1186/s13052-017-0368-6.
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Pharmacotherapy for Status Epilepticus.癫痫持续状态的药物治疗
Drugs. 2015 Sep;75(13):1499-521. doi: 10.1007/s40265-015-0454-2.
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Treating epilepsy in the setting of medical comorbidities.治疗伴有合并症的癫痫。
Curr Treat Options Neurol. 2014 Jul;16(7):298. doi: 10.1007/s11940-014-0298-1.