Τόμος 23 (2009) – Τεύχος 2 – Άρθρο 3 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 23 (2009) – Issue 2 – Article 3 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Aliskiren: a direct renin inhibitor for the treatment of hypertension and for end organ protection
Authors P.K. Panagopoulos and M. Mironidou-Tzouveleki

A’ Department of Pharmacology, Medical School, Aristotle University of Thessaloniki, Greece

Citation Panagopoulos, P.K., Mironidou-Tzouveleki, M.: Aliskiren: a direct renin inhibitor for the treatment of hypertension and for end organ protection, Epitheorese Klin. Farmakol. Farmakokinet. 23(2): 67-72 (2009)
Publication Date Accepted for publication (Final Version): July 1, 2009
Full Text Language English
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Keywords Renin-angiotensin-aldosterone system, direct renin inhibitors, aliskiren, pharmacology, hypertension, cardiovascular diseases, renal diseases.
Other Terms review article
Summary Aliskiren is the first oral direct renin inhibitor (DRI) approved by the US FDA in March 2007 for the treatment of hypertension. Direct renin inhibitors inhibit the cleavage of angiotensinogen by renin, which is the first step of the renin-angiotensin-aldosterone system (RAAS). Increased activity of the RAAS system is a key factor in the pathophysiology and development of increased blood pressure, renal disease, atherosclerosis, diabetes and heart failure. Therefore, its inhibition by DRIs is expected to be effective not only in treating arterial hypertension, but also in preventing end-organ damage. Other RAAS inhibitors do exist, but they inhibit downstream components of the RAAS, whereas DRIs shut down the entire downstream RAAS cascade. Furthermore, since other anti-hypertensive drugs cause a reactive increase in renin activity, DRIs could be combined with them for better results. Clinical trials have shown that aliskiren lowers blood pressure as effectively as other anti-hypertensive drugs and its combination with any of them is more effective than monotherapy. Both monotherapy and combinations have been shown to be safe and tolerable. Concerning end-organ protection, only surrogate parameter studies are available. Their results show that aliskiren improves the prognosis of cardiovascular and renal diseases, but outcome studies are needed. Large outcome studies are currently underway and will eventually assess the effect of aliskiren on cardiovascular and renal endpoints.
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