Active Ingredients

Aliskiren – Effect, Application & Risks


Aliskiren , a drug that acts as a renin inhibitor, is available for the treatment of arterial hypertension . It is sold under various trade names as a single and combination drug, and requires a prescription. The drug was approved in March 2007 in the USA, in June in Switzerland and in August in Germany.

What is Aliskiren?

Aliskiren is a drug used to regulate high blood pressure . It inhibits the enzyme renin, thereby interfering with the blood pressure -regulating renin-angiotensin-aldosterone system. Among the known renin inhibitors, aliskiren is the only drug that has been approved so far. Two other preparations – Zankiren and Remikiren – are still awaiting approval.

The first renin inhibitors were antibodies that were directed against the enzyme renin. What lowered blood pressure in animal experiments was not further developed, especially since these first renin inhibitors could only be administered by injection. Further intermediate steps finally led to Aliskiren being ready for the market, which well met expectations.

Pharmacological action

By interfering with the renin-angiotension-aldosterone system, aliskiren binds the enzyme renin, triggering subsequent biochemical processes.Namely, renin as a protease, a protein-splitting enzyme, converts angiotensinogen into angiotensin I, which in turn is converted into angiotensin II by an angiotensin-converting enzyme. This can then independently trigger vasoconstriction and cause an additional release of aldosterone. This results in a higher reabsorption of sodium ions and water in the renal collecting ducts, which causes the blood pressure to rise.

Aliskiren binds to renin, effectively blocking its complex function. The processes described do not occur and the blood pressure can drop.

Aliskiren is taken by mouth once a day. Since it influences blood pressure by releasing renin, it takes about one to two weeks after the start of treatment until the first measurable therapeutic success. Aliskiren is almost always given in combination with other antihypertensive drugs. These can be, for example, diuretics prescribed to treat high blood pressure .

Medical Application & Use

The renin inhibitor aliskiren is a novel and effective drug available for the treatment of high blood pressure. The producer Novartis even speaks of “a new dimension in the treatment of hypertension”.

Since the renin inhibitor aliskiren intervenes very early in the renin-angiotensin-aldosterone system, it completely prevents the production of angiotensin II. This distinguishes the drug from others that have often been used to date, such as ACE inhibitors . These only inhibit ACE (angiotensin converting enzyme), which converts angiotensin I to angiotensin II, but not the enzyme chymase. As a result, the renin-angiotensin system is only partially inhibited.

In addition, renin inhibitors such as aliskiren do not slow down the breakdown of bradykinin, an inflammatory mediator. When ACE inhibitors are used, the bradykinin then present causes the well-known kinin cough, the typical side effect of ACE inhibitor medication. Nevertheless, it is unclear whether the still new drug Aliskiren is therapeutically superior to the more conventional ACE inhibitors.

When taking aliskiren, it should be noted that an increased fat content in food negatively affects the absorption of the active ingredient. It is therefore not always so easy to control Aliskiren in terms of its individual efficiency. Added to this is the generally poor absorption of renin inhibitors, which is often less than 2% with oral medication.

Due to the lack of long-term results, the administration of aliskiren to children and adolescents is not recommended. Pregnant and breastfeeding women should also avoid it.

Risks & side effects

Aliskiren therapy can cause undesirable side effects:

In the case of numerous chronic or acute diseases and the corresponding medication, a detailed consultation between the doctor and the patient is essential before treatment with aliskiren begins.

The administration of aliskiren is contraindicated in the following diseases:

Aliskiren is also contraindicated in medication with:

A responsible doctor will therefore check blood pressure, electrolyte values, laboratory values ​​and kidney functions regularly in the run-up to a planned therapy with Aliskiren and, if necessary, during the treatment period.

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.