Mollace Vincenzo, Gliozzi Micaela, Capuano Annalisa, Rossi Francesco
Institute of Research for Food Safety & Health (IRC-FSH), University "Magna Graecia" of Catanzaro, Italy.
Institute of Research for Food Safety & Health (IRC-FSH), University "Magna Graecia" of Catanzaro, Italy.
Int J Cardiol. 2017 Jan 1;226:126-131. doi: 10.1016/j.ijcard.2016.03.085. Epub 2016 Mar 24.
The use of renin-angiotensin-aldosterone system (RAAS) inhibitors in the treatment of chronic heart failure (HF) and arterial hypertension is recommended by the European Society of Cardiology Guidelines on the basis of consolidated evidence supporting their efficacy in the development of such a disease. However, the high incidence of re-hospitalization and mortality in patients undergoing chronic HF, leads to the need for the development of novel RAAS inhibitors possessing a better pharmacokinetic/pharmacodynamics profile in approaching hemodynamic imbalance and myocardial dysfunction associated with the development of chronic HF. Here we summarize some of the recent advances in the area of RAAS-modulators, including novel renin inhibitors, mineralcorticoid receptor antagonists and novel AT1 and AT2-receptor modulators. In addition, the pharmacology of a new class of compounds which display both AT1-receptor blocking properties combined with inhibition of neprilysin, the vasopeptidase enzyme degradating natriuretic peptide (ARNi), will be reviewed, alongside with their impact in the pathophysiology of chronic HF.
欧洲心脏病学会指南推荐使用肾素 - 血管紧张素 - 醛固酮系统(RAAS)抑制剂治疗慢性心力衰竭(HF)和动脉高血压,这是基于支持其在此类疾病发展中疗效的确凿证据。然而,慢性HF患者再次住院和死亡率较高,因此需要开发新型RAAS抑制剂,这些抑制剂在应对与慢性HF发展相关的血流动力学失衡和心肌功能障碍方面具有更好的药代动力学/药效学特征。在此,我们总结RAAS调节剂领域的一些最新进展,包括新型肾素抑制剂、盐皮质激素受体拮抗剂以及新型AT1和AT2受体调节剂。此外,还将综述一类新型化合物的药理学,这类化合物兼具AT1受体阻断特性以及抑制中性肽链内切酶(一种降解利钠肽的血管肽酶)的作用(ARNi),以及它们对慢性HF病理生理学的影响。