What is Tekturna (Aliskiren)? (Part 1)

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A comment by a physician friend about Tekturna:
As a cardiologist, clinical researcher and vascular biologist, I am salivating at the arrival of this new medication.

The effects that renin inhibition has with regard to long term treatment of ACE intolerant subjects with regard to nephropathy, heart failure and endothelial function will be an interesting investigational opportunity...
Here are a few quick facts about Tekturna:
  1. It is the first new type of blood pressure medication in over a decade.
  2. It was initially called Rasilez. (Perhaps as a reference to the Renin Angiotension System.) The name change to Tekturna caught many drug representatives off guard.
  3. It's produced by the Swiss pharmaceutical maker Novartis.
  4. It works by blocking the enzyme renin. (Tekturna is a "renin inhibitor.")
  5. The name (and logo) are probably references to the "turning" of the feedback cycle of the renin-angiotensin-aldosterone system.
(Diagram reproduced under the GNU Free Documentation License.)

The renin-angiotensin-aldosterone system is a complex, interlocking system of hormones and enzymes critical for regulating blood pressure in the body. Briefly, renin is an enzyme produced by the kidney, which leads to a cascade of events (outlined above) which eventually produces angiotensin II, a powerful constrictor of blood vessels -- and angiotensin II raises blood pressure.

Many drugs already exist that block this system at different sites. Physicians use these medications routinely to control blood pressure (and to treat congestive heart failure and kidney disease -- more on that later). Some of these medications include angiotensin converting enzyme inhibitors, like lisinopril and ramipril (Altace), which prevent the formation of angiotensin II from angiotensin I; angiotensin receptor blockers like losartan (Cozaar) and irbesartan (Avapro), which block the blood vessel-constricting effect of angiotensin II; and aldosterone blockers like spironolactone and eplerenone (Inspra).

So why are physicians and researchers (like the cardiologist quoted above) excited about Aliskiren? This is the first medication that actually blocks renin, which is the critical first agent acting on the entire renin-angiotensin-aldosterone system.

More on the potential benefits of Tekturna in part 2.
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About the Author


MD, FACP, FASN

Dr. Schwimmer's blog explores the intersection of medicine, new technologies, and the Internet.

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