Oral renin inhibitors in clinical practice: a perspective review

Abstract

Hypertension is an important risk factor for cardiovascular morbidity and mortality. The importance of the renin-angiotensin-aldosterone system (RAAS) in cardiovascular and renal diseases has long been recognized: for this reason the conventional therapies, such as angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), β-blockers, and aldosterone antagonists represent the backbone of current antihypertensive therapy. Aliskiren is the first direct renin inhibitor (DRI) suitable for oral administration. By achieving more complete renin-angiotensin system inhibition, direct renin inhibitors may afford greater protection from hypertensive complications. Present evidence indicates that aliskiren reduces baseline systolic and diastolic blood pressure greater than placebo and that it is as effective as other first-line antihypertensive agents. Extra advantages can be reached when it is used in combination therapy. Clinical trials and in vitro studies also suggest that aliskiren has several cardioprotective and renoprotective effects. Therapy with aliskiren is well tolerated, but recently some concerns have arisen because of the early termination of the ALTITUDE study due to an increased incidence of adverse effects.

Keywords: aliskiren; direct renin inhibition; hypertension; renin–angiotensin–aldosterone system.

Figure 1.

The renin–angiotensin–aldosterone system (RAAS) cascade and the drug classes developed to counteract its influence.