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加巴喷丁恩卡比(XP13512/GSK1838262)作为一种替代多巴胺能药物治疗不宁腿综合征的方法。

Gabapentin enacarbil (XP13512/GSK1838262) as an alternative treatment to dopaminergic agents for restless legs syndrome.

机构信息

Stanford Hospital and Clinics, 401 Quarry Road, Rm 2142, Palo Alto, CA 94304-1419, USA.

出版信息

Expert Opin Pharmacother. 2010 Aug;11(11):1925-32. doi: 10.1517/14656566.2010.494598.

Abstract

IMPORTANCE TO THE FIELD

Gabapentin enacarbil (XP13512/GSK1838262) is being explored as an alternative treatment for restless legs syndrome (RLS), which currently relies heavily on dopaminergic agents; however, these latter medications have the reported complications of augmentation. Gabapentin enacarbil shows promising data that it may be equally to more efficacious and have an improved side effect profile than treatment with dopaminergic agents.

AREAS COVERED IN THIS REVIEW

Gabapentin enacarbil, examined in studies from 2004 to 2009, is a precursor to gabapentin and overcomes gabapentin's unfavorable pharmacokinetic profile and dose-dependent bioavailability. Randomized, controlled studies published in 2009 showed that gabapentin enacarbil outperformed placebo in improving quality and duration of sleep based on subjective report, investigator observation and objective measures in clinical trials. These trials show gabapentin enacarbil is well tolerated and safe, with a side-effect profile similar to gabapentin.

WHAT THE READER WILL GAIN

The reader will gain a thorough understanding of the current treatments available for RLS and how gabapentin enacarbil offers a potential breakthrough in expanding on these treatment options for both improved efficacy and tolerability.

TAKE HOME MESSAGE

Based on these findings, gabapentin enacarbil offers a promising alternative treatment for individuals requiring pharmacological intervention for their RLS symptoms.

摘要

重要性

加巴喷丁恩卡比(XP13512/GSK1838262)正在被探索作为治疗不宁腿综合征(RLS)的替代疗法,目前该疾病严重依赖于多巴胺能药物;然而,这些药物有报道的并发症,如药物增效。加巴喷丁恩卡比显示出有希望的数据,它可能与多巴胺能药物一样有效,且具有改善的副作用特征。

本篇综述涵盖的内容

加巴喷丁恩卡比是加巴喷丁的前体药物,克服了加巴喷丁不利的药代动力学特征和剂量依赖性生物利用度。2004 年至 2009 年期间进行的研究表明,加巴喷丁恩卡比在改善睡眠质量和持续时间方面优于安慰剂,这些研究结果基于主观报告、研究者观察和临床试验中的客观测量。这些试验表明,加巴喷丁恩卡比耐受性良好且安全,副作用特征与加巴喷丁相似。

读者将获得的收益

读者将全面了解目前可用的 RLS 治疗方法,以及加巴喷丁恩卡比如何在提高疗效和耐受性方面为这些治疗选择提供潜在突破。

结论

基于这些发现,加巴喷丁恩卡比为需要药物干预治疗 RLS 症状的患者提供了一种有前途的替代治疗方法。

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