{"title":"爱德华。药代动力学和药效学特性","authors":"Juan Tamargo","doi":"10.1016/S1131-3587(16)30017-6","DOIUrl":null,"url":null,"abstract":"<div><p>Edoxaban is a potent, selective, direct, reversible inhibitor of coagulation factor Xa. Because of its mechanism of action, edoxaban prolongs the prothrombin time and the activated partial thromboplastin time and reduces anti-factor-Xa activity. In both in vitro and in vivo models, edoxaban is a more effective antithrombotic than fondaparinux. Given orally, the drug rapidly (i.e. in 1–2 hours) reaches its peak plasma concentration and achieves its maximum effect on various antithrombotic biomarkers (e.g. prothrombin time, activated partial thromboplastin time and anti-factor-Xa activity). Edoxaban (15–150 mg once daily) has a linear pharmacokinetic profile. It is readily absorbed when given orally (the bioavailability is 62%), but, unlike other factor-Xa inhibitors, it exhibits only poor binding to plasma proteins and is not biotransformed via CYP3A4. It is eliminated by biliary and renal routes and has a half-life of 10–14 hours, which enables edoxaban to be administered once daily. Exposure to the drug is independent of age, sex and ethnicity, but increases as the patient's weight and renal function decrease.</p></div>","PeriodicalId":34926,"journal":{"name":"Revista Espanola de Cardiologia Suplementos","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S1131-3587(16)30017-6","citationCount":"1","resultStr":"{\"title\":\"Edoxabán. Propiedades farmacocinéticas y farmacodinámicas\",\"authors\":\"Juan Tamargo\",\"doi\":\"10.1016/S1131-3587(16)30017-6\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Edoxaban is a potent, selective, direct, reversible inhibitor of coagulation factor Xa. Because of its mechanism of action, edoxaban prolongs the prothrombin time and the activated partial thromboplastin time and reduces anti-factor-Xa activity. In both in vitro and in vivo models, edoxaban is a more effective antithrombotic than fondaparinux. Given orally, the drug rapidly (i.e. in 1–2 hours) reaches its peak plasma concentration and achieves its maximum effect on various antithrombotic biomarkers (e.g. prothrombin time, activated partial thromboplastin time and anti-factor-Xa activity). Edoxaban (15–150 mg once daily) has a linear pharmacokinetic profile. It is readily absorbed when given orally (the bioavailability is 62%), but, unlike other factor-Xa inhibitors, it exhibits only poor binding to plasma proteins and is not biotransformed via CYP3A4. It is eliminated by biliary and renal routes and has a half-life of 10–14 hours, which enables edoxaban to be administered once daily. Exposure to the drug is independent of age, sex and ethnicity, but increases as the patient's weight and renal function decrease.</p></div>\",\"PeriodicalId\":34926,\"journal\":{\"name\":\"Revista Espanola de Cardiologia Suplementos\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2016-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S1131-3587(16)30017-6\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Revista Espanola de Cardiologia Suplementos\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1131358716300176\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Revista Espanola de Cardiologia Suplementos","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1131358716300176","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Medicine","Score":null,"Total":0}
Edoxabán. Propiedades farmacocinéticas y farmacodinámicas
Edoxaban is a potent, selective, direct, reversible inhibitor of coagulation factor Xa. Because of its mechanism of action, edoxaban prolongs the prothrombin time and the activated partial thromboplastin time and reduces anti-factor-Xa activity. In both in vitro and in vivo models, edoxaban is a more effective antithrombotic than fondaparinux. Given orally, the drug rapidly (i.e. in 1–2 hours) reaches its peak plasma concentration and achieves its maximum effect on various antithrombotic biomarkers (e.g. prothrombin time, activated partial thromboplastin time and anti-factor-Xa activity). Edoxaban (15–150 mg once daily) has a linear pharmacokinetic profile. It is readily absorbed when given orally (the bioavailability is 62%), but, unlike other factor-Xa inhibitors, it exhibits only poor binding to plasma proteins and is not biotransformed via CYP3A4. It is eliminated by biliary and renal routes and has a half-life of 10–14 hours, which enables edoxaban to be administered once daily. Exposure to the drug is independent of age, sex and ethnicity, but increases as the patient's weight and renal function decrease.
期刊介绍:
Revista Española de Cardiología, is an international scientific journal dealing with cardiovascular medicine. Revista Española de Cardiología, the official publication of the Spanish Society of Cardiology, publishes research articles related to cardiovascular diseases. Articles are published in Spanish for the paper edition and in both Spanish and English in the electronic edition, which is available on the Internet. Regular sections include original articles reporting clinical or basic research, brief reports, review articles, editorials and letters to the Editor.