Walters Arthur S, Ondo William G, Kushida Clete A, Becker Philip M, Ellenbogen Aaron L, Canafax Daniel M, Barrett Ronald W
Department of Neurology, Vanderbilt University Medical Center, 1161 21st Ave., Nashville, TN 37232-2551, USA.
Clin Neuropharmacol. 2009 Nov-Dec;32(6):311-20. doi: 10.1097/WNF.0b013e3181b3ab16.
Assess the efficacy and tolerability of gabapentin enacarbil (GEn), a transported prodrug of gabapentin with improved gabapentin exposure, in adults with moderate-to-severe primary restless legs syndrome.
This 14-day, double-blind, randomized, controlled trial of GEn at 1200 or 600 mg or placebo taken once daily, evaluated the mean change from baseline International Restless Legs Scale (IRLS) total score at end of treatment (day 14:primary comparison, GEn at 1200 mg vs placebo). Secondary end points included Clinical Global Impression-Improvement scale outcomes at day 14.
Ninety-five subjects were randomized (GEn: 1200 mg, n = 33 and 600 mg, n = 29; placebo, n = 33); 2 subjects (GEn at 1200 mg) withdrew because of adverse events. At day 14,the mean (SD) change from baseline IRLS total score was significantly greater with GEn at 1200 mg (-16.1 [7.93]) compared with placebo (-8.9 [7.72]; adjusted mean treatment difference, -7.2; P < 0.0001). Investigator-rated Clinical Global Impression-Improvement scale responses also significantly favored GEn at 1200 mg compared with placebo (P G 0.0001).The mean (SD) change from baseline IRLS total score with GEn at 600 mg at day 14 was -9.1 (5.95), similar to placebo. The most commonly reported treatment-emergent adverse events were somnolence (GEn: 1200 mg, 36% and 600 mg, 14%; placebo,15%) and dizziness (GEn: 1200 mg, 18% and 600 mg, 14%; placebo, 3%), most of which were rated mild or moderate in intensity.
Gabapentin enacarbil at 1200 mg significantly improved restless legs syndrome symptoms compared with placebo. Efficacy outcomes for GEn at 600 mg were similar to placebo. Both GEn doses were generally well tolerated.
评估加巴喷丁乙酯（GEn），一种加巴喷丁的转运前体药物，其加巴喷丁暴露量有所改善，在中重度原发性不宁腿综合征成人患者中的疗效和耐受性。
这项为期14天的双盲、随机、对照试验，将GEn以1200或600毫克或安慰剂的剂量每日服用一次，评估治疗结束时（第14天：主要比较，1200毫克GEn与安慰剂）国际不宁腿量表（IRLS）总分相对于基线的平均变化。次要终点包括第14天的临床总体印象改善量表结果。
95名受试者被随机分组（GEn：1200毫克组，n = 33；600毫克组，n = 29；安慰剂组，n = 33）；2名受试者（1200毫克GEn组）因不良事件退出。在第14天，1200毫克GEn组相对于基线的IRLS总分平均（标准差）变化（-16.1 [7.93]）显著大于安慰剂组（-8.9 [7.72]；调整后的平均治疗差异，-7.2；P < 0.0001）。研究者评定的临床总体印象改善量表反应也显示，1200毫克GEn组相对于安慰剂组有显著优势（P ≤ 0.0001）。第14天，600毫克GEn组相对于基线的IRLS总分平均（标准差）变化为-9.1（5.95），与安慰剂组相似。最常报告的治疗中出现的不良事件为嗜睡（GEn：1200毫克组，36%；600毫克组，14%；安慰剂组，15%）和头晕（GEn：1200毫克组，18%；600毫克组，14%；安慰剂组，3%），其中大多数强度评定为轻度或中度。
与安慰剂相比，1200毫克的加巴喷丁乙酯显著改善了不宁腿综合征症状。600毫克GEn的疗效结果与安慰剂相似。两种GEn剂量总体耐受性良好。
