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阿利吉仑在心血管肾保护中的作用及其在伴有多种危险因素的高血压患者中的应用。

Role of aliskiren in cardio-renal protection and use in hypertensives with multiple risk factors.

机构信息

Endocrine Hypertension Research Centre and Clinical Centre of Research Excellence in Cardiovascular Disease and Metabolic Disorders, University of Queensland School of Medicine, Greenslopes Princess Alexandra Hospitals, Brisbane, QLD, Australia;

出版信息

Ther Clin Risk Manag. 2009 Jun;5(3):459-64. doi: 10.2147/tcrm.s5702. Epub 2009 Jun 22.

DOI:10.2147/tcrm.s5702
PMID:19707255
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2701487/
Abstract

The renin-angiotensin-aldosterone system (RAAS) is a key mediator of blood pressure (BP) and volume regulation in both normotensive and hypertensive persons. Stimulation of RAAS also contributes to hypertension-related target organ damage. The renin-angiotensinogen reaction is the first and rate-limiting step in the generation of angiotensin II (Ang II) and has been a target of antihypertensive drug development for decades. Aliskiren is the first in a new class of orally effective direct renin inhibitors (DRIs) and is approved for the treatment of hypertension in humans. It effectively reduces BP in the general population of hypertensive patients and has a tolerability and safety profile similar to placebo. Aliskiren has favorable effects on vascular inflammation and remodeling, on neurohumoral mediators of various forms of cardiovascular disease, including heart failure, and on proteinuria in diabetic patients. Additional outcome trials are needed to establish the role of this novel class of antihypertensive medication in preventing cardiovascular disease morbidity and mortality.

摘要

肾素-血管紧张素-醛固酮系统(RAAS)是调节血压(BP)和容量的关键介质,在正常血压和高血压人群中均如此。RAAS 的刺激也有助于与高血压相关的靶器官损伤。肾素-血管紧张素原反应是生成血管紧张素 II(Ang II)的第一步和限速步骤,并且几十年来一直是降压药物开发的靶点。阿利克仑是新型口服有效直接肾素抑制剂(DRI)类药物中的第一种,已被批准用于人类高血压的治疗。它可有效降低一般高血压患者的血压,且耐受性和安全性与安慰剂相似。阿利克仑对血管炎症和重塑、心力衰竭等各种形式心血管疾病的神经激素介质以及糖尿病患者的蛋白尿均有有利影响。需要进一步的结局试验来确定这种新型降压药物在预防心血管疾病发病率和死亡率方面的作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bc2/2701487/130526182a46/tcrm-5-459f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bc2/2701487/ebd6d54c718e/tcrm-5-459f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bc2/2701487/130526182a46/tcrm-5-459f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bc2/2701487/ebd6d54c718e/tcrm-5-459f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bc2/2701487/130526182a46/tcrm-5-459f2.jpg

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Circ Heart Fail. 2008 May;1(1):17-24. doi: 10.1161/CIRCHEARTFAILURE.107.740704.
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Chronic increases in circulating prorenin are not associated with renal or cardiac pathologies.循环中肾素原的慢性升高与肾脏或心脏病变无关。
Hypertension. 2009 Jun;53(6):1062-9. doi: 10.1161/HYPERTENSIONAHA.108.115444. Epub 2009 Apr 13.
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Efficacy of aliskiren/hydrochlorothiazide single-pill combinations in aliskiren non-responders.
Kidney Int Suppl (2011). 2022 Apr;12(1):36-47. doi: 10.1016/j.kisu.2021.11.002. Epub 2022 Mar 18.
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Aliskiren Reduces the Adrenal Zona Glomerulosa Apoptosis and Autophagy in Wistar Rats with 2K1C Hypertension.阿利吉仑减少2K1C高血压Wistar大鼠肾上腺球状带细胞凋亡和自噬
Int J Hypertens. 2020 Oct 21;2020:7684849. doi: 10.1155/2020/7684849. eCollection 2020.
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The Anti-Inflammatory Effect of Different Doses of Aliskiren in Rat Models of Inflammation.不同剂量阿利吉仑在大鼠炎症模型中的抗炎作用
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Exp Diabetes Res. 2011;2011:489708. doi: 10.1155/2011/489708. Epub 2011 Jun 4.
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Pleiotropic effects of inhibitors of the RAAS in the diabetic population: above and beyond blood pressure lowering.RAAS 抑制剂在糖尿病患者中的多效作用:超越降压作用。
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Aliskiren fails to lower blood pressure in patients who have either low PRA levels or whose PRA falls insufficiently or reactively rises.阿利吉仑对原发性肾素活性(PRA)水平低、PRA下降不足或反应性升高的患者无效。
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