Safety and Efficacy of Eplerenone in the Management of Essential Hypertension

F. McManus, J. Connell
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引用次数: 1

Abstract

Suppression of the Renin-Angiotensin-Aldosterone system (RAAS) is an established intervention in the management of cardiovascular disease. Large, randomized controlled trials have provided a sound evidence base for the use of mineralocorticoid receptor antagonists to block the end product of the RAAS in the treatment of heart failure. However, the place for mineralocorticoid blockade in the treatment of hypertension is less well defined and lacking a strong evidence base. The main indication for the use of this strategy in hypertension is as a third line agent in the treatment of refractory hypertension. The most widely used mineralocorticoid receptor antagonist, spironolactone, is associated with dose related sexual side effects, limiting its use in clinical practice. Eplerenone, the selective mineralocorticoid receptor antagonist, is a promising cardiovascular drug licensed for the treatment of heart failure in Europe and heart failure and hypertension in the USA. It effectively blocks the mineralocorticoid receptor without the unpleasant sexual side effect profile of spironolactone. We review the use of eplerenone, a selective mineralocorticoid receptor antagonist in the treatment of hypertension; discuss its mechanism of action, safety profile as well as its current place in therapy.
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依普利酮治疗原发性高血压的安全性和有效性
抑制肾素-血管紧张素-醛固酮系统(RAAS)是心血管疾病管理的既定干预措施。大型随机对照试验为使用矿皮质激素受体拮抗剂阻断RAAS治疗心力衰竭的最终产物提供了可靠的证据基础。然而,矿皮质激素阻断在高血压治疗中的地位尚不明确,缺乏强有力的证据基础。在高血压中使用这种策略的主要适应症是作为治疗难治性高血压的三线药物。最广泛使用的矿物皮质激素受体拮抗剂螺内酯与剂量相关的性副作用有关,限制了其在临床实践中的应用。Eplerenone是一种选择性矿皮质激素受体拮抗剂,是一种很有前途的心血管药物,在欧洲被批准用于治疗心力衰竭和美国的心力衰竭和高血压。它有效地阻断了矿物皮质激素受体,而没有螺内酯令人不快的性副作用。我们回顾了选择性矿皮质激素受体拮抗剂eplerenone在高血压治疗中的应用;讨论其作用机制、安全性以及目前在治疗中的地位。
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