Stier Charles T, Chander Praveen N, Rocha Ricardo
Department of Pharmacology, New York Medical College, Valhalla, New York 10595, USA.
Cardiol Rev. 2002 Mar-Apr;10(2):97-107. doi: 10.1097/00045415-200203000-00008.
The renin-angiotensin-aldosterone system plays a central role in the development of hypertension and the progression of end-organ damage. Although angiotensin-converting enzyme inhibitors and angiotensin II receptor antagonists can initially suppress plasma aldosterone, it is now well established that aldosterone escape may occur, whereby aldosterone levels return to or exceed baseline levels. The classic effects of aldosterone relate mainly to its action on epithelial cells to regulate water and electrolyte balance. However, blood pressure reduction or fluid loss could not account for the results of the Randomized Aldactone Evaluation Study, which showed that a low dose of spironolactone in addition to conventional therapy could decrease the overall risk of mortality by 30% among patients with severe congestive heart failure. The action of aldosterone at nonepithelial sites in the brain, heart, and vasculature is consistent with the presence of mineralocorticoid receptors in these tissues. Aldosterone has a number of deleterious effects on the cardiovascular system, including myocardial necrosis and fibrosis, vascular stiffening and injury, reduced fibrinolysis, endothelial dysfunction, catecholamine release, and production of cardiac arrhythmias. Several studies have now shown vascular and target-organ protective effects of aldosterone receptor antagonism in the absence of significant blood pressure lowering, consistent with a major role for endogenous mineralocorticoids as mediators of cardiovascular injury. The advent of selective aldosterone receptor antagonists such as eplerenone should prove of great therapeutic value in the prevention of cardiovascular disease and associated end-organ damage.
肾素-血管紧张素-醛固酮系统在高血压的发生及靶器官损害的进展中起核心作用。虽然血管紧张素转换酶抑制剂和血管紧张素II受体拮抗剂最初可抑制血浆醛固酮,但现已明确醛固酮逃逸可能会发生,即醛固酮水平恢复至或超过基线水平。醛固酮的经典作用主要涉及其对上皮细胞的作用,以调节水和电解质平衡。然而,血压降低或液体丢失并不能解释随机醛固酮评估研究的结果,该研究表明,在常规治疗基础上加用低剂量螺内酯可使重度充血性心力衰竭患者的总体死亡风险降低30%。醛固酮在脑、心脏和血管系统的非上皮部位的作用与这些组织中盐皮质激素受体的存在相一致。醛固酮对心血管系统有许多有害作用,包括心肌坏死和纤维化、血管硬化和损伤、纤溶降低、内皮功能障碍、儿茶酚胺释放以及心律失常的产生。现在有几项研究表明,在未显著降低血压的情况下,醛固酮受体拮抗具有血管和靶器官保护作用,这与内源性盐皮质激素作为心血管损伤介质的主要作用相一致。依普利酮等选择性醛固酮受体拮抗剂的出现应在预防心血管疾病及相关靶器官损害方面具有巨大的治疗价值。