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The use of gabapentin enacarbil in the treatment of restless legs syndrome.
Therapeutic Advances in Neurological Disorders ( IF 4.7 ) Pub Date : 2010-09-01 , DOI: 10.1177/1756285610378059
Toby C Yaltho 1 , William G Ondo
Affiliation  

Restless legs syndrome (RLS) is a common sleep-related neurological disorder that is characterized by the urge to move, worsening at rest, improvement with activity, and worsening in the evening and night. Dopamine agonists are usually the first-line therapy. Other agents including benzodiazepines, narcotics, and anticonvulsants have been used to treat RLS. Gabapentin has been shown to improve RLS in a small number of clinical studies, but is limited by its short half-life and variable bioavailability. Gabapentin enacarbil is a novel prodrug of gabapentin designed to overcome these pharmacokinetic limitations. In vitro and in vivo studies have demonstrated that gabapentin enacarbil has improved absorption, bioavailability and pharmacokinetics compared with gabapentin. Phase II and III studies have demonstrated that gabapentin enacarbil is generally well tolerated and is useful in the treatment of RLS.

中文翻译:

加巴喷丁依那卡比在治疗不宁腿综合征中的应用。

不宁腿综合征 (RLS) 是一种常见的睡眠相关神经系统疾病,其特征是运动冲动、休息时恶化、活动时好转以及夜间恶化。多巴胺激动剂通常是一线治疗。其他药物包括苯二氮卓类药物、麻醉剂和抗惊厥药已用于治疗 RLS。在少数临床研究中,加巴喷丁已被证明可以改善 RLS,但受到其短半衰期和可变生物利用度的限制。Gabapentin enacarbil 是一种新型加巴喷丁前药,旨在克服这些药代动力学限制。体外和体内研究表明,与加巴喷丁相比,加巴喷丁依那卡比具有更好的吸收、生物利用度和药代动力学。
更新日期:2019-11-01
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