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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.

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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