Aliskiren as a novel therapeutic agent for hypertension and cardio-renal diseases

• Published in: Journal of pharmacy and pharmacology 2012-04, Vol.64 (4), p.470-481
• Main Authors: Rashikh, Azhar, Ahmad, Shibli Jameel, Pillai, Krishna Kolappa, Najmi, Abul Kalam
• Format: Article
• Language: English
• Subjects: aliskiren; Amides - pharmacokinetics; Amides - pharmacology; Amides - therapeutic use; Animals; Antihypertensive Agents - pharmacokinetics; Antihypertensive Agents - pharmacology; Antihypertensive Agents - therapeutic use; Blood Pressure - drug effects; Cardiovascular Diseases - etiology; Cardiovascular Diseases - prevention & control; Fumarates - pharmacokinetics; Fumarates - pharmacology; Fumarates - therapeutic use; Humans; hypertension; Hypertension - complications; Hypertension - drug therapy; Hypertension - physiopathology; Kidney Diseases - etiology; Kidney Diseases - prevention & control; plasma renin activity; Renin - antagonists & inhibitors; renin angiotensin aldosterone system; Renin-Angiotensin System - drug effects
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1111/j.2042-7158.2011.01414.x

Objectives  High blood pressure (BP) is a major risk factor for cardiovascular and renal complications. A majority of treated hypertensive patients still complain of high BP. The renin‐angiotensin aldosterone system (RAAS) has been a centre‐stage target for all the cardiovascular and cardio‐renal complications. Aliskiren, is the first direct renin inhibitor (DRI) to be approved by the US FDA. Renin controls the rate‐limiting step in the RAAS cascade and hence is the most favorable target for RAAS suppression. Key findings  This review article strives to summarize the pharmacokinetic, preclinical and clinical studies done so far pertaining to the efficacy of aliskiren. Further, the pharmacology of aliskiren has been comprehensively dealt with to enhance understanding so as to further research in this unfathomed area in the multitude of cardiovascular disorders and renal diseases. Summary  Aliskiren has been shown to have comparable BP‐lowering effects to other RAAS inhibitors. Recent clinical trials have indicated that it might contribute significantly in combination with other agents for the protection of end‐organ diseases.