PDF(Pubmed)
Abstract：
Pulmonary arterial hypertension (PAH) affects a wide range of people globally and has a poor prognosis despite many advancements in available treatment options. Among the available treatments, endothelin receptor antagonists (ERA) are among the most widely used drugs. These drugs have been evaluated in scientific trials. We included free full texts in the English language from the last ten years and reviewed them. We are writing this review to amalgamate the pharmacological aspects and the previous studies on ERAs to demonstrate a comprehensive overview of the current status of ERAs for PAH treatment. We focused on the structure, pharmacodynamics, pharmacokinetics, and efficacy and safety of the three most widely used ERAs: Bosentan, Ambrisentan, and Macitentan. These drugs have different receptor affinities, bioavailability, excretion routes, and different levels of safety profiles. There are three available studies, the RCT, the ARIES series, and the SERAPHIN studies, for assessing the safety and efficacy of Bosentan, Ambrisentan, and Macitentan, respectively. All the studies and some additional studies for combination therapy have proven all three drugs effective in treating PAH. The side effects (SE) varied from headache and hepatic enzyme elevation to worsening the PAH status of varied severities. Although these studies provided valuable insight into the role of ERAs, there is still enough scope for more studies on ERAs, both as monotherapy and combination therapy for PAH.
摘要：
肺动脉高压（PAH）在全球范围内影响广泛的人群，尽管在可用的治疗选择方面取得了许多进步，但预后较差。在现有的治疗方法中，内皮素受体拮抗剂（ERA）是最广泛使用的药物之一。这些药物已经在科学试验中进行了评估。我们包含了过去十年的免费英语全文，并对其进行了审查。我们正在撰写这篇综述，以合并药理学方面和先前对ERA的研究，以全面概述ERA用于PAH治疗的现状。我们专注于结构，药效学,药代动力学，以及三种最广泛使用的ERA的有效性和安全性：波生坦，Ambrisentan,还有Macitentan.这些药物有不同的受体亲和力，生物利用度，排泄途径,和不同级别的安全概况。有三个可用的研究，RCT,ARIES系列,和SERAPHIN研究，为了评估波生坦的安全性和有效性，Ambrisentan,还有Macitentan,分别。所有的研究和一些其他联合治疗的研究都证明了这三种药物都能有效治疗PAH。副作用（SE）从头痛和肝酶升高到严重程度不同的PAH状态恶化。尽管这些研究为电子逆向拍卖的作用提供了有价值的见解，仍然有足够的空间对电子逆向拍卖进行更多的研究，作为PAH的单药治疗和联合治疗。
