A blood pressure medication that inhibits renin - Aliskiren

Aliskiren is a renin inhibitor and is the first of this class of blood pressure medication to become commercially available. It has been approved for use in primary hypertension by the FDA. It's brand name is Tekturna (Novartis).

If you have read about the drugs that affect angiontensin (ACE inhibitors and Angiotensin receptor blockers) you will easily understand how aliskiren works - it exerts its effects further back in the chain of events leading to the production of angiotensin. In other words by blocking renin's activity it effectively blocks angiotensin and thus its blood pressure raising effect. (Angiotensin causes blood vessels to constrict thus raising blood pressure - it also causes the production of alsosterone that causes the kidneys to retain sodium which as we know also causes a rise in blood pressure through expansion of plasma volume).

Aliskiren is relatively new (it was licensed by the FDA in 1997) so information on longer term use is not yet available but it is thought that it may have beneficial effects on the kidneys.

Aliskiren appears to be well tolerated with a few side effects that occur infrequently, such as raised potassium levels, low blood pressure (caution if you are on a low salt diet), diarrhoea, heartburn, headache, cough, allergic reaction (angioedema) and raised uric acid which could precipitate gout.

Aliskiren should NOT be taken in pregnancy or if you are planning for children as it could harm the fetus.

The dosage is once daily between 150 to 300 mg. Some preparations of aliskiren are also available where it is combined with another blood pressure medication such as the thiazide diuretic hydrochlorthiazide (Tekturna HCT); the calcium antagonist amlodipine (one study has recommended this combination as a first line-treatment) and with the angiotensin receptor blocker valsartan (Valturna).

Some scientists have voiced concern that a blood pressure medication that blocks renin production might cause a rebound effect in which the body reacts to produce even more but so far this has not yet been shown to happen.


Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). "Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients". Circulation 111 (8): 1012–8.

Parving HH, Persson F, Lewis JB, Lewis EJ, Hollenberg NK. "Aliskiren Combined with Losartan in Type 2 Diabetes and Nephropathy," N Engl J Med 2008;358:2433-46.

Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet 368 (9545): 1449–56. doi:10.1016/S0140-6736(06)69442-7. PMID 17055947

Sealey JE and Laragh JH. Aliskiren, the first renin inhibitor for treating hypertension: Reactive renin secretion may limit its effectiveness. Am J Hypertens 2007; 20:587-597.

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This page was last modified on : May 12, 2011.