Aliskiren – first in the new class of antihypertensives
Katarzyna Jobs, Anna Jung
Aliskiren is the first in a new class of antihypertensives – the direct renin inhibitors. It took a long time to discover it, mainly because of difficulties with creating an oral form with good bioavailability. It has been approved for the treatment of primary hypertension in United States and Europe in 2007. It provides good blood pressure efficacy, has good tolerability and small amount of undesirable side effects. Blocking renin, it prevents conversion of angiotensinogen to angiotensin I. First clinical trials concerning its use alone or in combination with ACEI or ARB give hope for greater reduction in blood pressure and more renal and cardiovascular protection that provided by ACEIs and ARBs. The ongoing clinical trial programme ASPIRE HIGHER will investigate the potential of aliskiren in improvement of renal and cardiovascular protection. Preliminary results are very promising. Aliskiren diminishes plasma renin activity from 50 to 80% in hypertensive patients after oral administration. It diminishes systolic and diastolic blood pressure. After single dose the effect of the drug lasts for 24 hours. Whole therapeutic effect is observed after two weeks.