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(Hypertension. 2002;39:189.)
© 2002 American Heart Association, Inc.
Hypertension Electronic Pages |
Angiotensin II Suppression in Humans by the Orally Active Renin Inhibitor Aliskiren (SPP100)
Comparison With Enalapril
Juerg Nussberger
Grégoire Wuerzner
Chris Jensen
Hans R. Brunner
Abstract
Renin is the main determinant of angiotensin (Ang) II levels. It, therefore, always appeared desirable to reduce Ang II levels by direct inhibition of renin. So far, specific renin inhibitors lacked potency and/or oral availability. We tested the new orally active nonpeptidic renin inhibitor SPP100 (Aliskiren, an octanamide with a 50% inhibitory concentration [IC50] in the low nanomolar range) in 18 healthy volunteers on a constant 100 mmol/d sodium diet using a double-blind, 3-way crossover protocol. In 3 periods of 8 days, separated by wash-outs of 6 days, each volunteer received 2 dosage levels of Aliskiren (low before high; 40 and 80 or 160 and 640 mg/d) and randomized placebo or 20 mg enalapril. Aliskiren was well tolerated. Not surprisingly, blood pressure and heart rate remained unchanged in
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