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临床实践中的口服肾素抑制剂:观点综述。

Oral renin inhibitors in clinical practice: a perspective review.

机构信息

Department of Internal Medicine, Ospedale dell'Angelo-General Hospital, Mestre-Venezia, Italy.

出版信息

Ther Adv Chronic Dis. 2012 Jul;3(4):173-81. doi: 10.1177/2040622312446244.

DOI:10.1177/2040622312446244
PMID:23342233
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3539287/
Abstract

Hypertension is an important risk factor for cardiovascular morbidity and mortality. The importance of the renin-angiotensin-aldosterone system (RAAS) in cardiovascular and renal diseases has long been recognized: for this reason the conventional therapies, such as angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), β-blockers, and aldosterone antagonists represent the backbone of current antihypertensive therapy. Aliskiren is the first direct renin inhibitor (DRI) suitable for oral administration. By achieving more complete renin-angiotensin system inhibition, direct renin inhibitors may afford greater protection from hypertensive complications. Present evidence indicates that aliskiren reduces baseline systolic and diastolic blood pressure greater than placebo and that it is as effective as other first-line antihypertensive agents. Extra advantages can be reached when it is used in combination therapy. Clinical trials and in vitro studies also suggest that aliskiren has several cardioprotective and renoprotective effects. Therapy with aliskiren is well tolerated, but recently some concerns have arisen because of the early termination of the ALTITUDE study due to an increased incidence of adverse effects.

摘要

高血压是心血管发病率和死亡率的重要危险因素。肾素-血管紧张素-醛固酮系统(RAAS)在心血管和肾脏疾病中的重要性早已得到认可:因此,传统的治疗方法,如血管紧张素转换酶(ACE)抑制剂和血管紧张素受体阻滞剂(ARB)、β受体阻滞剂和醛固酮拮抗剂,构成了当前抗高血压治疗的基础。阿利克仑是第一个适合口服的直接肾素抑制剂(DRI)。通过实现更完全的肾素-血管紧张素系统抑制,直接肾素抑制剂可能提供更大的高血压并发症保护。目前的证据表明,阿利克仑降低基线收缩压和舒张压的效果大于安慰剂,并且与其他一线抗高血压药物一样有效。当与联合治疗联合使用时,可以达到额外的优势。临床试验和体外研究还表明,阿利克仑具有几种心脏保护和肾脏保护作用。阿利克仑治疗耐受性良好,但最近由于 ALTITUDE 研究因不良反应发生率增加而提前终止,引起了一些关注。

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本文引用的文献

1
Aliskiren and the calcium channel blocker amlodipine combination as an initial treatment strategy for hypertension control (ACCELERATE): a randomised, parallel-group trial.阿利克仑与钙通道阻滞剂氨氯地平联合作为高血压控制的初始治疗策略(ACCELERATE):一项随机、平行组试验。
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Aliskiren alone or in combination with hydrochlorothiazide in patients with the lower ranges of stage 2 hypertension: The ACQUIRE randomized double-blind study.阿利吉仑单药治疗或与氢氯噻嗪联合治疗 2 期高血压低危患者的效果:ACQUIRE 随机双盲研究。
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Aliskiren: a review of its use as monotherapy and as combination therapy in the management of hypertension.阿利克仑:在高血压治疗中单药治疗和联合治疗中的应用评价。
Drugs. 2010 Oct 22;70(15):2011-49. doi: 10.2165/11204360-000000000-00000.
4
Renin inhibitors in chronic heart failure: the Aliskiren Observation of Heart Failure Treatment study in context.肾素抑制剂在慢性心力衰竭中的应用:阿利克仑心力衰竭治疗观察研究的背景。
Clin Cardiol. 2010 Sep;33(9):536-41. doi: 10.1002/clc.20828.
5
Impact of baseline renal function on the efficacy and safety of aliskiren added to losartan in patients with type 2 diabetes and nephropathy.基线肾功能对阿利克仑联合氯沙坦治疗 2 型糖尿病肾病患者疗效和安全性的影响。
Diabetes Care. 2010 Nov;33(11):2304-9. doi: 10.2337/dc10-0833. Epub 2010 Aug 6.
6
Patients with acute coronary syndromes and elevated levels of natriuretic peptides: the results of the AVANT GARDE-TIMI 43 Trial.急性冠状动脉综合征伴利钠肽升高的患者:AVANT GARDE-TIMI 43 试验的结果。
Eur Heart J. 2010 Aug;31(16):1993-2005. doi: 10.1093/eurheartj/ehq190. Epub 2010 Jun 17.
7
Antihypertensive efficacy, safety, and tolerability of the oral direct renin inhibitor aliskiren in patients with hypertension: a pooled analysis.口服直接肾素抑制剂阿利吉仑治疗高血压患者的降压疗效、安全性及耐受性:一项汇总分析
J Am Soc Hypertens. 2007 Jul-Aug;1(4):264-77. doi: 10.1016/j.jash.2007.04.004.
8
Effect of the direct Renin inhibitor aliskiren, the Angiotensin receptor blocker losartan, or both on left ventricular mass in patients with hypertension and left ventricular hypertrophy.直接肾素抑制剂阿利吉仑、血管紧张素受体阻滞剂氯沙坦或两者联用对高血压合并左心室肥厚患者左心室质量的影响。
Circulation. 2009 Feb 3;119(4):530-7. doi: 10.1161/CIRCULATIONAHA.108.826214. Epub 2009 Jan 19.
9
Effects of the direct renin inhibitor aliskiren and atenolol alone or in combination in patients with hypertension.直接肾素抑制剂阿利克仑与阿替洛尔单用或联合用于高血压患者的效果。
J Renin Angiotensin Aldosterone Syst. 2008 Sep;9(3):163-75. doi: 10.1177/1470320308096411.
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Pharmacokinetics of the oral direct renin inhibitor aliskiren in combination with digoxin, atorvastatin, and ketoconazole in healthy subjects: the role of P-glycoprotein in the disposition of aliskiren.健康受试者中口服直接肾素抑制剂阿利吉仑与地高辛、阿托伐他汀及酮康唑联合应用的药代动力学:P-糖蛋白在阿利吉仑处置中的作用
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