Cutler Andrew J, Kalali Amir H, Weiden Peter J, Hamilton Jennifer, Wolfgang Curt D
University of Florida, Gainesville, FL, USA.
J Clin Psychopharmacol. 2008 Apr;28(2 Suppl 1):S20-8. doi: 10.1097/JCP.0b013e318169d4ce.
Iloperidone is a mixed D2/5-HT2 antagonist in development for treatment of schizophrenia. This trial aimed to evaluate the efficacy and safety of a fixed dose of iloperidone in patients with acute exacerbations of schizophrenia. This randomized, placebo-controlled, multicenter study comprised a 1-week titration period and a 3-week double-blind maintenance period. Eligible patients (n = 593) were randomized to iloperidone 24 mg/d, ziprasidone 160 mg/d as an active control, or placebo. Primary efficacy variable was change from baseline in the Positive and Negative Syndrome Scale Total (PANSS-T) score, using a mixed-effects model repeated measures analysis. Iloperidone demonstrated significant reduction versus placebo on the PANSS-T score (P< 0.01). Significant improvement versus placebo was also demonstrated with ziprasidone (P < 0.05). Compared with ziprasidone, iloperidone was associated with lower rates of many adverse events (AEs) that are particularly troublesome with antipsychotics, including sedation, somnolence, extrapyramidal symptoms, akathisia, agitation, and restlessness; iloperidone was associated with higher rates of weight gain, tachycardia, orthostatic hypotension, dizziness, and nasal congestion as reported as an AE. Most AEs were mild to moderate. A similar amount of QT prolongation was observed with both active treatments, although no patient had a treatment-emergent postbaseline corrected QT interval of 500 msec or greater. The incidence of clinically relevant changes in laboratory parameters was comparable between iloperidone and ziprasidone. Iloperidone was associated with a low incidence of extrapyramidal symptoms. Overall, there was improvement in akathisia with iloperidone treatment. Iloperidone treatment was effective, safe, and well tolerated in patients with acute exacerbation of schizophrenia.
伊潘立酮是一种正在研发用于治疗精神分裂症的D2/5 - HT2混合拮抗剂。该试验旨在评估固定剂量伊潘立酮治疗精神分裂症急性加重患者的疗效和安全性。这项随机、安慰剂对照、多中心研究包括1周的滴定期和3周的双盲维持期。符合条件的患者(n = 593)被随机分为接受24毫克/天伊潘立酮、160毫克/天齐拉西酮作为活性对照或安慰剂治疗。主要疗效变量是采用混合效应模型重复测量分析的阳性和阴性症状量表总分(PANSS - T)较基线的变化。与安慰剂相比,伊潘立酮在PANSS - T评分上有显著降低(P < 0.01)。齐拉西酮与安慰剂相比也有显著改善(P < 0.05)。与齐拉西酮相比,伊潘立酮与许多抗精神病药物特别棘手的不良事件(AE)发生率较低相关,包括镇静、嗜睡、锥体外系症状、静坐不能、激越和烦躁不安;伊潘立酮作为AE报告的体重增加、心动过速、体位性低血压、头晕和鼻充血发生率较高。大多数AE为轻度至中度。两种活性治疗观察到的QT延长量相似,尽管没有患者在基线后出现治疗引发的校正QT间期≥500毫秒。伊潘立酮和齐拉西酮之间实验室参数临床相关变化的发生率相当。伊潘立酮锥体外系症状发生率较低。总体而言,伊潘立酮治疗使静坐不能有所改善。伊潘立酮治疗对精神分裂症急性加重患者有效、安全且耐受性良好。