New York University School of Medicine, New York City, NY, USA.
Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1.
Iloperidone is a newly commercialized second-generation (atypical) antipsychotic approved for the acute treatment of schizophrenia in adults.
the purpose of this review is to describe the pharmacokinetic profile of iloperidone and its clinical implications in the treatment of schizophrenia. Background information is also provided regarding chemistry, pharmacodynamics, clinical efficacy and safety data, and regulatory affairs.
the reader will have an understanding of the pharmacokinetics and overall metabolism of iloperidone within the context of efficacy and safety.
time to peak plasma concentration occurs in 2 - 4 h but elimination half-life is 18 h for extensive CYP2D6 metabolizers and 33 h for poor CYP2D6 metabolizers, suggesting that once or twice daily dosing would be feasible. Dizziness and/or postural hypotension are the limiting factors for how fast iloperidone can be titrated, and is explained by iloperidone and its metabolites' norepinephrine alpha 1 antagonism. Efficacy of iloperidone appears similar to that for ziprasidone and haloperidol, but iloperidone may be inferior in efficacy to risperidone. Iloperidone can prolong the ECG QT interval. The tolerability profile of iloperidone is noteworthy in terms of modest weight gain, no medically important changes in lipid and glucose, little in the way of prolactin elevation, and an absence of extrapyramidal adverse effects, including akathisia.
依匹哌唑是一种新商业化的第二代（非典型）抗精神病药，批准用于成人精神分裂症的急性治疗。
本综述的目的是描述依匹哌唑的药代动力学特征及其在精神分裂症治疗中的临床意义。还提供了有关化学、药效学、临床疗效和安全性数据以及监管事务的背景信息。
读者将了解依匹哌唑在疗效和安全性方面的药代动力学和整体代谢情况。
对于广泛的 CYP2D6 代谢者，达峰血浆浓度时间发生在 2-4 小时，但消除半衰期为 18 小时，对于 CYP2D6 差代谢者为 33 小时，这表明每天一次或两次给药是可行的。头晕和/或体位性低血压是依匹哌唑能够快速滴定的限制因素，这可以用依匹哌唑及其代谢物的去甲肾上腺素α1拮抗作用来解释。依匹哌唑的疗效似乎与齐拉西酮和氟哌啶醇相似，但依匹哌唑的疗效可能不如利培酮。依匹哌唑可延长心电图 QT 间期。依匹哌唑的耐受性特征值得注意，包括适度的体重增加、血脂和血糖无重要变化、催乳素升高很少，以及没有锥体外系不良反应，包括静坐不能。
