Abstract

Blockade of the renin–angiotensin–aldosterone system (RAAS) with angiotensin-converting enzyme inhibitors or Ang II-receptor blockers has been demonstrated to lower blood pressure and to be effective in heart failure and postmyocardial infarction. It is also beneficial in renal disease. These RAAS blockers further activate the RAAS, leading to an increase of plasma renin activity and plasma renin concentration. Aliskiren, the first orally active direct renin inhibitor, is an effective and well-tolerated antihypertensive agent when used as monotherapy or in combination with other antihypertensive agents in patients with mild-to-moderate hypertension. In contrast with angiotensin-converting enzyme inhibitors and Ang II-receptor blockers, aliskiren reduces plasma renin activity. A number of clinical trials with aliskiren are ongoing or completed and provide us with objective evidence regarding the clinical importance of direct renin inhibition in the treatment of cardiovascular disease.

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