Ovaert P, Elliott J, Bernay F, Guillot E, Bardon T
DVM, CEVA Santé Animale, Research and Development, Libourne Cedex, France.
J Vet Pharmacol Ther. 2010 Apr;33(2):109-17. doi: 10.1111/j.1365-2885.2009.01122.x.
Historically, aldosterone receptor antagonists (ARA) have been classified as 'potassium sparing diuretics'. However, the positive effect of spironolactone, the most extensively studied ARA, on morbidity and mortality observed in humans suffering cardiac insufficiency could not be explained by the renal effect of the drug alone, and a pivotal clinical study has led to extensive research. Many experimental studies have demonstrated that ARA have previously unexpected beneficial effects on the cardiovascular system including reduction in remodelling of the vascular smooth muscle cells and myocytes and improvement of endothelial cell dysfunction in heart failure. These effects improve vascular compliance and slow down the progression of left ventricular dysfunction and end-organ damage. Furthermore, aldosterone receptor blockade also restores the baroreceptor reflex, improving heart rate variability in heart failure in humans. Some of these effects have been demonstrated in dog models of cardiac disease and so justified further investigation of the potential benefit of ARA in dogs with congestive heart failure (CHF). Positive effects of spironolactone on morbidity and mortality appear to have been seen in studies conducted in dogs suffering from naturally occurring CHF. In addition, eplerenone has been shown to have benefits in canine models of heart failure. The precise mechanisms by which ARA produce these beneficial effects in dogs remain to be determined but this group of drugs clearly provide therapeutic actions out-with their diuretic effects.
从历史上看,醛固酮受体拮抗剂(ARA)一直被归类为“保钾利尿剂”。然而,螺内酯(研究最广泛的ARA)对心力衰竭患者发病率和死亡率的积极影响,无法仅用该药物的肾脏效应来解释,一项关键的临床研究引发了广泛的研究。许多实验研究表明,ARA对心血管系统具有先前未预料到的有益作用,包括减少血管平滑肌细胞和心肌细胞的重塑,以及改善心力衰竭时的内皮细胞功能障碍。这些作用可改善血管顺应性,减缓左心室功能障碍和终末器官损伤的进展。此外,醛固酮受体阻断还可恢复压力感受器反射,改善人类心力衰竭时的心率变异性。其中一些作用已在犬类心脏病模型中得到证实,因此有理由进一步研究ARA对充血性心力衰竭(CHF)犬的潜在益处。螺内酯对发病率和死亡率的积极影响似乎已在患有自然发生的CHF的犬类研究中得到体现。此外,依普利酮已被证明对犬类心力衰竭模型有益。ARA在犬类中产生这些有益作用的确切机制仍有待确定,但这组药物显然具有利尿作用之外的治疗作用。