Zoccali Rocco A, Bruno Antonio, Muscatello Maria Rosaria Anna
From the Section of Psychiatry, Department of Neurosciences, University of Messina, Messina, Italy.
J Clin Psychopharmacol. 2015 Jun;35(3):286-95. doi: 10.1097/JCP.0000000000000305.
Sertindole is an atypical antipsychotic reintroduced into the European market in 2005 after a reevaluation of its risks and benefits, under the agreement that close electrocardiographic screening would be conducted. It has a high affinity for dopamine D2, serotonin 5-HT2A and 5-HT2C, and α1 adrenergic receptors. Moreover, sertindole shows modest affinity for H1-histaminergic and muscarinic receptors. The pharmacological properties, clinical efficacy, safety, and tolerability of sertindole are covered in this article based on a literature review from 1990 to 2014. Given current available findings, sertindole is at least effective as haloperidol, risperidone, and olanzapine on schizophrenia symptoms. Regarding its efficacy on cognitive symptoms, sertindole effect is supported by both preclinical and clinical studies versus haloperidol and olanzapine; however, its role on cognition needs further clarification. Concerning safety and tolerability issues, sertindole is characterized by a low potential to cause sedation and extrapyramidal symptoms, and by an acceptable metabolic profile; nevertheless, cardiac safety remains a major concern, and the electrocardiographic monitoring should be carried out during treatment to substantially reduce cardiovascular risk. In conclusion, although it has an equivalent profile compared to other antipsychotic drugs, sertindole actually remains a second-line choice for schizophrenic patients intolerant to at least one other antipsychotic agent.
塞汀多是一种非典型抗精神病药物,在对其风险和益处进行重新评估后,于2005年重新进入欧洲市场,协议规定要进行密切的心电图筛查。它对多巴胺D2、5-羟色胺5-HT2A和5-HT2C以及α1肾上腺素能受体具有高亲和力。此外,塞汀多对H1组胺能受体和毒蕈碱受体表现出适度的亲和力。本文基于1990年至2014年的文献综述,涵盖了塞汀多的药理特性、临床疗效、安全性和耐受性。根据目前可得的研究结果,塞汀多在治疗精神分裂症症状方面至少与氟哌啶醇、利培酮和奥氮平一样有效。关于其对认知症状的疗效,临床前和临床研究均支持塞汀多相对于氟哌啶醇和奥氮平的效果;然而,其在认知方面的作用仍需进一步阐明。关于安全性和耐受性问题,塞汀多的特点是引起镇静和锥体外系症状的可能性较低,且代谢情况可以接受;尽管如此,心脏安全性仍然是一个主要关注点,治疗期间应进行心电图监测以大幅降低心血管风险。总之,尽管塞汀多与其他抗精神病药物相比具有相当的特性,但实际上对于至少对一种其他抗精神病药物不耐受的精神分裂症患者,它仍然是二线选择。