房颤急性转化期的新型药物:以vernakalant为重点。

Pio Cialdella, Daniela Pedicino, Pasquale Santangeli
{"title":"房颤急性转化期的新型药物:以vernakalant为重点。","authors":"Pio Cialdella,&nbsp;Daniela Pedicino,&nbsp;Pasquale Santangeli","doi":"10.2174/157489011794578428","DOIUrl":null,"url":null,"abstract":"<p><p>Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. Its action is mainly due to the blockade of atrial-selective channels responsible of the ultra-rapid delayed rectifier current I(Kur), but has also important interactions with other channels and currents, such as I(Na) (inward sodium current), and I(KACh) (acetylcholine-regulated potassium current). Due to the relatively selective blockade of the I(Kur), vernakalant prolongs the effective refractory period of the atria with minimal effects on the ventricles, thus minimizing the risk of proarrhythmia. Thus far vernakalant has been tested in three placebo-controlled trials (ACT I, ACT II and ACT III) and in one amiodarone-controlled study (AVRO). Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events. This article will review the recent patents on this novel atrial-selective agent, discussing its mechanisms of action and possible clinical applications in the real-world practice.</p>","PeriodicalId":20905,"journal":{"name":"Recent patents on cardiovascular drug discovery","volume":"6 1","pages":"1-8"},"PeriodicalIF":0.0000,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/157489011794578428","citationCount":"6","resultStr":"{\"title\":\"Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.\",\"authors\":\"Pio Cialdella,&nbsp;Daniela Pedicino,&nbsp;Pasquale Santangeli\",\"doi\":\"10.2174/157489011794578428\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. Its action is mainly due to the blockade of atrial-selective channels responsible of the ultra-rapid delayed rectifier current I(Kur), but has also important interactions with other channels and currents, such as I(Na) (inward sodium current), and I(KACh) (acetylcholine-regulated potassium current). Due to the relatively selective blockade of the I(Kur), vernakalant prolongs the effective refractory period of the atria with minimal effects on the ventricles, thus minimizing the risk of proarrhythmia. Thus far vernakalant has been tested in three placebo-controlled trials (ACT I, ACT II and ACT III) and in one amiodarone-controlled study (AVRO). Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events. This article will review the recent patents on this novel atrial-selective agent, discussing its mechanisms of action and possible clinical applications in the real-world practice.</p>\",\"PeriodicalId\":20905,\"journal\":{\"name\":\"Recent patents on cardiovascular drug discovery\",\"volume\":\"6 1\",\"pages\":\"1-8\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2011-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.2174/157489011794578428\",\"citationCount\":\"6\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Recent patents on cardiovascular drug discovery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/157489011794578428\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Recent patents on cardiovascular drug discovery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/157489011794578428","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 6

摘要

Vernakalant是一种新型抗心律失常药物,最近被批准用于近期发作的心房颤动的心律转复。它的作用主要是由于阻断了负责超快速延迟整流电流I(Kur)的心房选择性通道,但也与其他通道和电流有重要的相互作用,如I(Na)(向内钠电流)和I(KACh)(乙酰胆碱调节的钾电流)。由于相对选择性地阻断I(Kur),维那卡兰特延长了心房的有效不应期,而对心室的影响最小,从而将心律失常的风险降至最低。迄今为止,vernakalant已在三个安慰剂对照试验(ACT I、ACT II和ACT III)和一个胺碘酮对照研究(AVRO)中进行了测试。Vernakalant已被证明比安慰剂和胺碘酮对房颤的快速转化更有效,没有明显的不良事件。本文将对这种新型心房选择性药物的最新专利进行综述,讨论其作用机制和可能的临床应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.

Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. Its action is mainly due to the blockade of atrial-selective channels responsible of the ultra-rapid delayed rectifier current I(Kur), but has also important interactions with other channels and currents, such as I(Na) (inward sodium current), and I(KACh) (acetylcholine-regulated potassium current). Due to the relatively selective blockade of the I(Kur), vernakalant prolongs the effective refractory period of the atria with minimal effects on the ventricles, thus minimizing the risk of proarrhythmia. Thus far vernakalant has been tested in three placebo-controlled trials (ACT I, ACT II and ACT III) and in one amiodarone-controlled study (AVRO). Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events. This article will review the recent patents on this novel atrial-selective agent, discussing its mechanisms of action and possible clinical applications in the real-world practice.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
Patents and Heart Valve Surgery - III: Percutaneous Heart Valves. Patents and Heart Valve Surgery - III: Percutaneous Heart Valves. New frontiers in the management of acute coronary syndromes: cangrelor and elinogrel. Blockade of renin angiotensin system in heart failure post-myocardial infarction: what is the best therapy? Ticagrelor: a novel drug for an old problem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1