制造商：
葛兰素史克制药
活性成分（S）：
加巴喷丁enacarbil 600毫克;缓释片。
指示（S）：
治疗中度至重度原发性不宁腿综合征（RLS）的在成年人。
药理学：
加巴喷丁enacarbil加巴喷丁是一种前体药物，因此，在RLS的治疗效果归属于加巴喷丁。加巴喷丁是有效在RLS的确切机制不明。加巴喷丁在结构上相关的神经递质γ-氨基丁酸（GABA），但没有对GABA结合，吸收，或退化的影响。在体外研究表明，加巴喷丁与亲和力高电压激活的钙通道α2δ亚基结合;然而，这种绑定关系的影响，加巴喷丁的RLS enacarbil，是未知的。
临床试验：
Horizant在治疗中度至重度原发性RLS的成效体现在为期12周的临床研究与使用国际不宁腿综合征研究小组的诊断标准的RLS诊断成人。与RLS的继发其他条件的患者（例如，怀孕，缺铁性贫血，肾功能衰竭）被排除在外。在研究中，患者随机接受Horizant 1200mg或安慰剂，下午约五时，每日一次与食品。在研究2中，患者随机接受Horizant 600毫克，Horizant 1200mg，或采取每日一次在下午5时与食物有关的安慰剂。
疗效评价使用IRLS评定量表和临床总体印象改进（CGI - I）的分数。 IRLS量表包含10个项目，旨在评估感觉和运动症状的严重程度，睡眠障碍，白天嗜睡/镇静，并影响日常生活和心情与RLS相关的活动。分数范围是0到40，与0的RLS症状的情况下，40个最严重的症状。 IRLS量表在第12周的基线的变化和应答者的CGI - I定义为“大为改善”或“大大改善”在第12周的评级量表的比例在这些研究中的合作主要成果。
观察12周时接受600毫克的治疗组和Horizant 1200mg和安慰剂组之间差异有统计学意义，从基线的平均变化IRLS量表总得分（研究1：Horizant 1200mg：-13.2，安慰剂：-8.8研究2：600毫克Horizant：-13.8，Horizant 1200mg：-13，安慰剂：-9.8）和应答者的比例（“大为改善”或“大大改善”）的CGI我秤（研究1：Horizant 1200mg ：76％，安慰剂组：39％;研究2：Horizant 600毫克：73％Horizant 1200mg：77％，安慰剂组：45％）。
法律分类：
接收
成人：
燕子整体。随身携带食物。 600毫克，每日一次，约于下午五时（1200mg剂量看到没有额外的好处）。如果剂量不建议的时间，下一个剂量应采取以下的一天。肾损害：肌酐清除率30-59mL/min：第1天，3天，此后每天600毫克。肌酐清除率<30mL/min或血液透析：不建议。
儿童：
不推荐。
警告/注意事项：
加巴喷丁与其他产品互换。谁是白天睡觉，并保持彻夜难眠的患者不推荐。可能造成重大的驾驶减值;不开车，直到减值评估。癫痫。监测恶化的抑郁症，自杀的念头/行为，不寻常的变化和情绪/行为。怀孕（部件C）。哺乳母亲：不推荐。
不良反应（S）：
嗜睡/镇静，头晕，平衡障碍，视力模糊，神志不清，醉酒，嗜睡，眩晕的感觉。
如何提供：
标签30
最后更新：
2011年7月21日
HORIZANT
Manufacturer:
GlaxoSmithKline Pharmaceuticals
Active Ingredient(s):
Gabapentin enacarbil 600mg; extended-release tablets.
Indication(s):
Treatment of moderate-to-severe primary restless legs syndrome (RLS) in adults.
Pharmacology:
Gabapentin enacarbil is a prodrug of gabapentin and, accordingly, its therapeutic effects in RLS are attributable to gabapentin. The precise mechanism by which gabapentin is efficacious in RLS is unknown. Gabapentin is structurally related to the neurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation. In vitro studies have shown that gabapentin binds with high affinity to the α2δ subunit of voltage-activated calcium channels; however, the relationship of this binding to the effects of gabapentin enacarbil in RLS is unknown.
Clinical Trials:
The effectiveness of Horizant in the treatment of moderate-to-severe primary RLS was demonstrated in two 12-week clinical studies in adults diagnosed with RLS using the International Restless Legs Syndrome Study Group diagnostic criteria. Patients with RLS secondary to other conditions (eg, pregnancy, renal failure, iron deficiency anemia) were excluded. In Study 1, patients were randomized to receive Horizant 1200mg or placebo taken once daily at about 5pm with food. In Study 2, patients were randomized to receive Horizant 600mg, Horizant 1200mg, or placebo taken once daily at about 5pm with food.
Efficacy was evaluated using the IRLS Rating Scale and Clinical Global Impression of Improvement (CGI-I) scores. The IRLS Rating Scale contains 10 items designed to assess the severity of sensory and motor symptoms, sleep disturbance, daytime somnolence/sedation, and impact on activities of daily living and mood associated with RLS. The range of scores is 0 to 40, with 0 being absence of RLS symptoms and 40 the most severe symptoms. The change from baseline in the IRLS Rating Scale at Week 12 and the proportion of responders on the CGI-I Scale defined as a rating of “much improved” or “very much improved” at Week 12 were co-primary outcomes in these studies.
Statistically significant differences between the treatment groups receiving 600mg and 1200mg of Horizant and the group receiving placebo were observed at Week 12 for both the mean change from baseline in the IRLS Scale total score (Study 1: Horizant 1200mg: –13.2, placebo: –8.8; Study 2: Horizant 600mg: –13.8, Horizant 1200mg: –13, placebo: –9.8) and the proportion of responders (“much improved” or “very much improved”) on the CGI-I Scale (Study 1: Horizant 1200mg: 76%, placebo: 39%; Study 2: Horizant 600mg: 73%, Horizant 1200mg: 77%, placebo: 45%).
Legal Classification:
Rx
Adults:
Swallow whole. Take with food. 600mg once daily at about 5pm (no additional benefit seen with 1200mg dose). If dose is not taken at recommended time, next dose should be taken the following day. Renal impairment: CrCl 30–59mL/min: 600mg on Day 1, Day 3, and every day thereafter. CrCl<30mL/min or on hemodialysis: not recommended.
Children:
Not recommended.
Warnings/Precautions:
Not interchangeable with other gabapentin products. Not recommended for patients who are required to sleep during the day and remain awake at night. May cause significant driving impairment; do not drive until impairment is assessed. Epilepsy. Monitor for worsening of depression, suicidal thoughts/behavior, and unusual changes in mood/behavior. Pregnancy (Cat. C). Nursing mothers: not recommended.
Adverse Reaction(s):
Somnolence/sedation, dizziness, balance disorder, blurred vision, disorientation, feeling drunk, lethargy, vertigo.
How Supplied:
Tabs—30