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阿朴西汀在高血压管理中的应用:临床疗效、安全性及未来前景

Aprocitentan in hypertension management: clinical efficacy, safety, and future prospects.

作者信息

Riaz Rumaisa, Ahmed Usaid, Naqi Unaiza, Afaq Laiba, Shaukat Ayesha, Khan Yalnaz, Akilimali Aymar

机构信息

Internal Medicine, Dow University of Health Sciences (DUHS), Karachi, Pakistan.

Department of Research, Medical Research Circle (MedReC), Goma, DR Congo.

出版信息

Ann Med Surg (Lond). 2025 Feb 7;87(3):1472-1478. doi: 10.1097/MS9.0000000000003028. eCollection 2025 Mar.

Abstract

Hypertension (HTN) is a prevalent medical condition characterized by systolic blood pressure ≥ 130 mm Hg and diastolic blood pressure ≥ 80 mm Hg. In 2010, the global prevalence of HTN was 31.1%, with higher rates in men and low- and middle-income countries (LMICs). The etiology of primary HTN involves neurohumoral, renal, metabolic, genetic, and environmental factors, with the kidneys playing a significant role in long-term blood pressure regulation. Endothelin-1 (ET-1), a potent vasoconstrictor, contributes to HTN by affecting salt-water balance and promoting vascular remodeling. HTN often presents without symptoms, leading to complications such as heart failure, stroke, and renal failure if untreated. Common treatment options include angiotensin-converting enzyme inhibitors, angiotensin-receptor blockers, calcium channel blockers, and diuretics. Aprocitentan, a novel dual endothelin receptor antagonist, has shown promise in reducing blood pressure in patients with resistant HTN. Clinical trials, including the Phase 3 PRECISION study, demonstrated its efficacy and long-term control. However, Aprocitentan's use is associated with safety concerns, such as hepatotoxicity, fluid retention, and embryo-fetal toxicity, necessitating careful monitoring. Aprocitentan represents a significant advancement in HTN management, offering a new therapeutic option for patients with uncontrolled HTN, although vigilant monitoring and informed decision-making are essential to mitigate potential risks and ensure optimal outcomes.

摘要

高血压(HTN)是一种常见的医学病症,其特征为收缩压≥130毫米汞柱且舒张压≥80毫米汞柱。2010年,全球高血压患病率为31.1%,男性以及低收入和中等收入国家(LMICs)的患病率更高。原发性高血压的病因涉及神经体液、肾脏、代谢、遗传和环境因素,其中肾脏在长期血压调节中起着重要作用。内皮素-1(ET-1)是一种强效血管收缩剂,通过影响水盐平衡和促进血管重塑导致高血压。高血压通常没有症状,如果不治疗会导致心力衰竭、中风和肾衰竭等并发症。常见的治疗选择包括血管紧张素转换酶抑制剂、血管紧张素受体阻滞剂、钙通道阻滞剂和利尿剂。阿朴生坦是一种新型双重内皮素受体拮抗剂,在降低顽固性高血压患者的血压方面显示出前景。包括3期PRECISION研究在内的临床试验证明了其疗效和长期控制效果。然而,阿朴生坦的使用存在安全问题,如肝毒性、液体潴留和胚胎-胎儿毒性,因此需要仔细监测。阿朴生坦代表了高血压管理方面的重大进展,为未控制的高血压患者提供了一种新的治疗选择,尽管密切监测和明智决策对于减轻潜在风险和确保最佳结果至关重要。

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