Edoxabán. Propiedades farmacocinéticas y farmacodinámicas

Juan Tamargo
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引用次数: 1

Abstract

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.

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爱德华。药代动力学和药效学特性
依多沙班是一种有效的、选择性的、直接的、可逆的凝血因子Xa抑制剂。由于其作用机制,依多沙班可延长凝血酶原时间和活化部分凝血活酶时间,降低抗因子xa活性。在体外和体内模型中,依多沙班是一种比氟达肝素更有效的抗血栓药。口服后,药物迅速(即在1-2小时内)达到血药浓度峰值,并对各种抗血栓生物标志物(如凝血酶原时间、活化的部分凝血活酶时间和抗xa因子活性)达到最大效果。依多沙班(15 - 150mg,每日一次)具有线性药代动力学特征。口服时很容易吸收(生物利用度为62%),但与其他因子xa抑制剂不同,它与血浆蛋白的结合较差,不能通过CYP3A4进行生物转化。它通过胆道和肾脏途径消除,半衰期为10-14小时,因此可以每天给药一次。药物暴露与年龄、性别和种族无关,但随着患者体重和肾功能下降而增加。
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来源期刊
Revista Espanola de Cardiologia Suplementos
Revista Espanola de Cardiologia Suplementos Medicine-Cardiology and Cardiovascular Medicine
CiteScore
1.20
自引率
0.00%
发文量
1
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.
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