{"title":"鲁拉西酮:精神分裂症的新治疗选择。","authors":"R T Owen","doi":"10.1358/dot.2011.47.11.1708832","DOIUrl":null,"url":null,"abstract":"<p><p>Lurasidone is a novel benzoisothiazol antipsychotic that has recently been approved for the treatment of schizophrenia in the U.S. Like many other second-generation antipsychotics, it has a high affinity for dopamine D(2) and serotonin 5-HT(2A) receptors as well as a high affinity for 5-HT(7) receptors. It has negligible affinity for α(1)-adrenoceptors, histamine H(1) receptors or muscarinic acetylcholine M(1) receptors. It has demonstrated efficacy in short-term trials versus placebo, two of which included an active comparator (olanzapine, quetiapine) assay arm. A short-term, head-to-head trial of lurasidone versus ziprasidone in chronic stable schizophrenia was also conducted. A long-term, 12-month risperidone-controlled study and open-label studies primarily investigated the safety and tolerability of lurasidone. Limited evidence of procognitive and antidepressant effects was seen although these need further corroboration. The incidence of extrapyramidal symptoms (excluding akathisia/restlessness) was greater with lurasidone (14.7%) than placebo (5.1%). Akathisia and somnolence were dose-related adverse events. Lurasidone appears to have relatively little effect on weight, plasma glucose or lipids to date. No evidence of QTc prolongation was seen and orthostatic hypotension was uncommon. Raised prolactin levels in short-term studies were dose-dependent, greater in females and occurred overall in 3.7 and 0.7% of lurasidone and placebo recipients, respectively.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":" ","pages":"807-16"},"PeriodicalIF":1.8000,"publicationDate":"2011-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"4","resultStr":"{\"title\":\"Lurasidone: a new treatment option for schizophrenia.\",\"authors\":\"R T Owen\",\"doi\":\"10.1358/dot.2011.47.11.1708832\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Lurasidone is a novel benzoisothiazol antipsychotic that has recently been approved for the treatment of schizophrenia in the U.S. Like many other second-generation antipsychotics, it has a high affinity for dopamine D(2) and serotonin 5-HT(2A) receptors as well as a high affinity for 5-HT(7) receptors. It has negligible affinity for α(1)-adrenoceptors, histamine H(1) receptors or muscarinic acetylcholine M(1) receptors. It has demonstrated efficacy in short-term trials versus placebo, two of which included an active comparator (olanzapine, quetiapine) assay arm. A short-term, head-to-head trial of lurasidone versus ziprasidone in chronic stable schizophrenia was also conducted. A long-term, 12-month risperidone-controlled study and open-label studies primarily investigated the safety and tolerability of lurasidone. Limited evidence of procognitive and antidepressant effects was seen although these need further corroboration. The incidence of extrapyramidal symptoms (excluding akathisia/restlessness) was greater with lurasidone (14.7%) than placebo (5.1%). Akathisia and somnolence were dose-related adverse events. Lurasidone appears to have relatively little effect on weight, plasma glucose or lipids to date. No evidence of QTc prolongation was seen and orthostatic hypotension was uncommon. Raised prolactin levels in short-term studies were dose-dependent, greater in females and occurred overall in 3.7 and 0.7% of lurasidone and placebo recipients, respectively.</p>\",\"PeriodicalId\":11397,\"journal\":{\"name\":\"Drugs of today\",\"volume\":\" \",\"pages\":\"807-16\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2011-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drugs of today\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1358/dot.2011.47.11.1708832\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drugs of today","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1358/dot.2011.47.11.1708832","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Medicine","Score":null,"Total":0}
Lurasidone: a new treatment option for schizophrenia.
Lurasidone is a novel benzoisothiazol antipsychotic that has recently been approved for the treatment of schizophrenia in the U.S. Like many other second-generation antipsychotics, it has a high affinity for dopamine D(2) and serotonin 5-HT(2A) receptors as well as a high affinity for 5-HT(7) receptors. It has negligible affinity for α(1)-adrenoceptors, histamine H(1) receptors or muscarinic acetylcholine M(1) receptors. It has demonstrated efficacy in short-term trials versus placebo, two of which included an active comparator (olanzapine, quetiapine) assay arm. A short-term, head-to-head trial of lurasidone versus ziprasidone in chronic stable schizophrenia was also conducted. A long-term, 12-month risperidone-controlled study and open-label studies primarily investigated the safety and tolerability of lurasidone. Limited evidence of procognitive and antidepressant effects was seen although these need further corroboration. The incidence of extrapyramidal symptoms (excluding akathisia/restlessness) was greater with lurasidone (14.7%) than placebo (5.1%). Akathisia and somnolence were dose-related adverse events. Lurasidone appears to have relatively little effect on weight, plasma glucose or lipids to date. No evidence of QTc prolongation was seen and orthostatic hypotension was uncommon. Raised prolactin levels in short-term studies were dose-dependent, greater in females and occurred overall in 3.7 and 0.7% of lurasidone and placebo recipients, respectively.
期刊介绍:
An international, peer-reviewed journal publishing monographs on new products entering the market and review articles.
Since its inception in 1965, Drugs of Today has established a reputation for excellence in providing physicians and other key healthcare professionals with practical, up-to-date monographs on recently approved and launched drugs.