In this series we draw attention to recently licensed medicines with an entirely new mechanism of action. Publication does not imply endorsement of use in clinical practice. Copyright to the images belongs to Leiden University, but use of the images (available at http://coo.lumc.nl/trc) is free.
Article first published online: 21 JUL 2009
© 2009 The Authors. Journal compilation © 2009 The British Pharmacological Society
British Journal of Clinical Pharmacology
Volume 68, Issue 5, pages 653–654, November 2009
How to Cite
Dubois, E. A. and Cohen, A. F. (2009), Aliskiren. British Journal of Clinical Pharmacology, 68: 653–654. doi: 10.1111/j.1365-2125.2009.03504.x
- Issue published online: 6 NOV 2009
- Article first published online: 21 JUL 2009
Treatment of essential hypertension.
Aliskiren is the first renin inhibitor to be licensed in Europe. It selectively inhibits renin, the first enzyme in the renin–angiotensin system (RAS) cascade, thereby inhibiting the formation of angiotensin I from angiotensinogen (Figure 1). This reduces the production of vasoconstrictor angiotensin II and mineralocorticoid aldosterone, resulting in vasodilation, decreased sympathetic activity and increased excretion of sodium ions by the kidneys with a consequent decrease in blood pressure.
Other antihypertensive drugs, such as angiotensin converting enzyme inhibitors, angiotensin receptor blockers, and aldosterone antagonists exert their actions at later stages in the system. All drugs that block the RAS inhibit the negative feedback of angiotensin II on renin secretion, leading to a compensatory rise in renin concentration. Aliskiren is special because it inhibits the RAS at its origin. Furthermore, in contrast to other RAS-blocking agents, aliskiren decreases plasma renin activity despite the compensatory rise in renin concentration. Aliskiren does not interfere with the degradation of bradykinin (which is inhibited by angiotensin converting enzyme inhibitors but not by angiotensin receptor blockers).
Aliskiren causes only mild and transient adverse reactions, of which diarrhoea is the most common. Peripheral oedema, rash, and influenza-like symptoms have been reported.