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Aliskiren (brand names Tekturna and Rasilez) is the first in a class of drugs called direct renin inhibitors. It is used for essential (primary) hypertension. While used for high blood pressure, other better studied medications are typically recommended due to concerns of higher side effects and less evidence of benefit.
In December 2011, Novartis halted a trial of the drug after discovering increased nonfatal stroke, kidney complications, high blood potassium, and low blood pressure in people with diabetes and kidney problems.
As a result, in 2012:

A new contraindication was added to the product label concerning the use of aliskiren with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes because of the risk of kidney impairment, low blood pressure, and high levels of potassium in the blood.
A warning to avoid use of aliskiren with ARBs or ACEIs was also added for patients with moderate to severe kidney impairment (i.e., where glomerular filtration rate is less than 60 ml/min).
Novartis decided to stop marketing Valturna (aliskiren/valsartan).
Aliskiren was co-developed by the Swiss pharmaceutical companies Novartis and Speedel.




Medical uses


While used for high blood pressure, other better-studied medications are typically recommended. Prescrire has stated that aliskiren is potentially more harmful than beneficial and thus list it as a drug to avoid (as of 2014).




Adverse effects


Angioedema - The ADE of angioedema found in patients using Aliskiren is due to the inhibition of bradykinin degradation which occurs within the Renin-Angiotensin System (RAAS)
High blood potassium level (particularly when used with ACE inhibitors in diabetic patients)
Low blood pressure (particularly in volume-depleted patients)
Diarrhea and other GI symptoms
Headache
Dizziness
Cough




Contraindications


Pregnancy: Other drugs such as ACE inhibitors, also acting on the renin–angiotensin system, have been associated with fetal malformations and neonatal death. Angiotensin cannot be used in patients who are pregnant because it will result in disruption of normal fetal kidney development.
Breastfeeding: During animal studies, the drug has been found present in milk.
Aliskiren has been shown to increase the likelihood of adverse cardiovascular outcomes in patients with diabetes and kidney or heart disease.




Drug interactions


Aliskiren is a minor inhibitor of substrate CYP3A4 and, more importantly, P-glycoprotein:

It reduces furosemide blood concentration.
Atorvastatin may increase aliskiren's blood concentration, but no dose adjustment is needed.
Due to possible interaction with ciclosporin, the use of ciclosporin and aliskiren at the same time is contraindicated.
Caution should be exercised when aliskiren is administered with ketoconazole and other moderate P-glycoprotein inhibitors such as itraconazole, clarithromycin, telithromycin, erythromycin, or amiodarone.
Recommendations have been made to stop prescribing aliskiren-containing medicines to patients with diabetes (type 1 or type 2) or with moderate to severe kidney impairment who are also taking an ACE inhibitor or ARB. Such patients should consider alternative antihypertensive treatment as necessary.




Mechanism of action


Aliskiren is an inhibitor of renin. Renin, the first enzyme in the renin–angiotensin–aldosterone system, plays a role in blood pressure control. It cleaves angiotensinogen to angiotensin I, which is in turn converted by angiotensin-converting enzyme (ACE) to angiotensin II. Angiotensin II has both direct and indirect effects on blood pressure. It directly causes arterial smooth muscle to contract, leading to vasoconstriction and increased blood pressure. Angiotensin II also stimulates the production of aldosterone from the adrenal cortex, which causes the tubules of the kidneys to increase reabsorption of sodium, with water following, thereby increasing plasma volume, and thus blood pressure. Aliskiren binds to the S3bp binding site of renin, essential for its activity. Binding to this pocket prevents the conversion of angiotensinogen to angiotensin I.
Aliskiren is also available as combination therapy with hydrochlorothiazide.




Chemistry


The chemical name for aliskiren is (2 S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[ 4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide.




Rationale for design


Many drugs control blood pressure by interfering with angiotensin or aldosterone. However, when these drugs are used chronically, the body increases renin production, which drives blood pressure up again. Therefore, pharmacologists have been looking for a drug to inhibit renin directly. Aliskiren is the first drug to do so.




References






External links


"Aliskiren". Drug Information Portal. U.S. National Library of Medicine.
Aliskiren at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

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• Amlodipine
• Renin–angiotensin system
• Novartis
• Aliskiren/hydrochlorothiazide
• Lisinopril
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Aliskiren — Medlibes: Online Medical Library

APExBIO - Aliskiren|Direct renin inhibitor|CAS# 173334-57-1

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Daftar Isi

• Aliskiren Uses, Side Effects & Warnings - Drugs.com
• Aliskiren - Wikipedia
• Aliskiren (oral route) - Mayo Clinic
• Aliskiren Side Effects: Common, Severe, Long Term - Drugs.com
• Aliskiren (Tekturna) - Uses, Side Effects, and More - WebMD
• Aliskiren: MedlinePlus Drug Information
• Tekturna: Uses, Dosage & Side Effects - Drugs.com
• ALISKIREN- aliskiren hemifumarate tablet, film coated - DailyMed
• Aliskiren (Tekturna): Uses, Side Effects, Alternatives & More - GoodRx
• Aliskiren - PMC

Aliskiren Uses, Side Effects & Warnings - Drugs.com

Jun 27, 2023 · Aliskiren is used to treat high blood pressure (hypertension) in people who are at least 6 years old and weigh at least 110 pounds (50 kg). Aliskiren may also be used for purposes not listed in this medication guide.

Aliskiren - Wikipedia

Aliskiren (brand names Tekturna and Rasilez) is the first in a class of drugs called direct renin inhibitors. It is used for essential (primary) hypertension. [2] While used for high blood pressure, other better studied medications are typically recommended due to concerns of higher side effects and less evidence of benefit. [3]

Aliskiren (oral route) - Mayo Clinic

Aliskiren is a renin inhibitor. It works by blocking an enzyme in the body that is necessary to produce a substance that causes blood vessels to tighten. As a result, the blood vessels relax and this decreases the blood pressure.

Aliskiren Side Effects: Common, Severe, Long Term - Drugs.com

Oct 5, 2024 · Learn about the side effects of aliskiren, from common to rare, for consumers and healthcare professionals.

Aliskiren (Tekturna) - Uses, Side Effects, and More - WebMD

What is aliskiren used for? Aliskiren is commonly used to lower high blood pressure (hypertension). Aliskiren may also be used for other conditions as determined by your healthcare provider....

Aliskiren: MedlinePlus Drug Information

Aliskiren is in a class of medications called direct renin inhibitors. It works by decreasing certain natural chemicals that tighten the blood vessels, so blood vessels relax and the heart can pump blood more efficiently.

Tekturna: Uses, Dosage & Side Effects - Drugs.com

Jul 5, 2023 · Tekturna (aliskiren) is used alone or in combination with some medications to treat high blood pressure (hypertension) in people who are at least 6 years old and weigh at least 110 pounds (50 kg). Tekturna belongs to a class of medications called direct renin inhibitors.

ALISKIREN- aliskiren hemifumarate tablet, film coated - DailyMed

May 1, 2023 · Aliskiren is indicated for the treatment of hypertension in adults and in pediatric patients weighing 50 kg or greater who are at least 6 years of age and older to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.

Aliskiren (Tekturna): Uses, Side Effects, Alternatives & More - GoodRx

May 11, 2023 · Aliskiren (Tekturna) is a direct renin inhibitor. It blocks renin, an enzyme (protein) in your body that plays a role in tightening your blood vessels and raising blood pressure. By blocking renin, aliskiren (Tekturna) allows your blood vessels to relax, which helps lower your blood pressure. What are the side effects of Aliskiren (Tekturna)?

Aliskiren - PMC

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).