title: Efficacy and safety profile of aliskiren: practical implications for clinicians.
abstract: Renin-angiotensin-system (RAS) is an enzymatic cascade that plays a pivotal role in the development of arterial hypertension, kidney disease and cardiovascular disease. Inhibition of the RAS with angiotensin converting enzyme (ACE) inhibitors (ACE-Is) or angiotensin receptor blockers (ARBs) has proved to be a successful strategy for the treatment of hypertension and related cardiovascular disorders. However, by reducing feedback inhibition of renin release, the effects of ACE-Is and ARBs lead to an increase in plasma renin concentration (PRC) and activity (PRA), limiting a complete inhibition of the RAS. Consequently the effects of a different pharmacological strategy that completely blocks the RAS upstream has been assessed in the last years. In this context, aliskiren is the first representative of a new class of non-peptide orally active renin inhibitor that blocks the RAS at its rate-limiting step and induces a net reduction in PRA, angiotensin II and aldosterone levels. Aliskiren effectively reduces blood pressure as a monotherapy as well in combination therapy. In addition, aliskiren has a placebo-like tolerability profile at the licensed doses of 150 mg and 300 mg. Aliskiren also exhibits additive effects on blood pressure reduction when combined with drugs that lead to a reactive increase in the PRA, such as diuretics, ACE-Is or ARBs. In previous studies, aliskiren showed beneficial effects in patients with arterial hypertension and associated clinical conditions. However, later trials indicated that the use of aliskiren should be avoided in patients with renal failure or receiving ACE-Is or ARBs. The main aim of this review is to summarize the available data on its efficacy and safety profile, highlighting clinical implications from recent trials.
authors: Fabio
authors: F
authors: Angeli
authors: Gianpaolo
authors: G
authors: Reboldi
authors: Cristina
authors: C
authors: Poltronieri
authors: Enrica
authors: E
authors: Angeli
authors: Valentina
authors: V
authors: De Filippo
authors: Alessandra
authors: A
authors: Crocetti
authors: Claudia
authors: C
authors: Bartolini
authors: Cinzia
authors: C
authors: D'Ambrosio
authors: Division of Cardiology and Cardiovascular Pathophysiology, University Hospital "S.M. della Misericordia", Perugia, Italy. fangeli@cardionet.it.
authors: Paolo
authors: P
authors: Verdecchia
mesh_terms: D000577:Amides / Q000009:adverse effects / Q000627:therapeutic use*; D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000627:therapeutic use*; D050197:Atherosclerosis / Q000188:drug therapy; D001794:Blood Pressure / Q000187:drug effects; D004359:Drug Therapy, Combination; D005650:Fumarates / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D017379:Hypertrophy, Left Ventricular / Q000188:drug therapy; D000092502:Renin Inhibitors
chemical_list: D000577:Amides; D000959:Antihypertensive Agents; D005650:Fumarates; D000092502:Renin Inhibitors; C446481:aliskiren