Aliskiren

Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin I (Ang I).

• Aliskiren tablets are a renin inhibitor (RI) 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, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.ICD-10: I10

• Do not use aliskiren with ARBs or ACEIs in patients with diabetes [see Warnings and Precautions (5.2) and Clinical Studies (14.3) ]. Aliskiren tablets are contraindicated in patients with known hypersensitivity to any of the components [see Warnings and Precautions (5.3) ].contraindicated

Starting dose (adults and pediatric patients): 150 mg once daily with a routine pattern with regard to meals. If blood pressure remains uncontrolled titrate up to 300 mg daily. ( 2.1 ) Majority of effect of given dose attained in 2 weeks ( 2.1 ) 2.1 Recommended Dosage In adult patients and in pediatric patients weighing 50 kg or greater who are at least 6 years of age, the recommended starting dose of aliskiren tablets is 150 mg once daily. In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 300 mg once daily. Doses above 300 mg did not give an increased blood pressure response but resulted in an increased rate of diarrhea. The antihypertensive effect of a given dosage is substantially attained (85% to 90%) by 2 weeks. 2.2 Relationship to Meals Patients should establish a routine pattern for taking aliskiren tablets with regard to meals. High-fat meals decrease absorption substantially [ see Clinical Pharmacology (12.3) ].

Avoid concomitant use with ARBs or ACEIs particularly in patients with renal impairment [creatinine clearance (CrCl) <60 mL/min]. ( 5.2 , 5.4 ) Anaphylactic Reactions and Head and Neck Angioedema. ( 5.3 ) Hypotension: Correct imbalances in volume and/or salt depleted patients. ( 5.4 ) Impaired Renal Function: Monitor serum creatinine periodically. ( 5.5 ) Hyperkalemia: Monitor potassium levels periodically. ( 5.6 ) 5.1 Fetal Toxicity Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue aliskiren tablets as soon as possible [ see Use in Specific Populations (8.1) ]. 5.2 Renal Impairment/Hyperkalemia/Hypotension when Aliskiren Tablets are Given in Combination with ARBs or ACEIs Aliskiren tablets are contraindicated in patients with diabetes who are receiving ARBs or ACEIs because of the increased risk of renal impairment, hyperkalemia, and hypotension. In general, avoid combined use of aliskiren with ACE inhibitors or ARBs, particularly in patients with creatinine clearance (CrCl) less than 60 mL/min [see Contraindications (4) , Drug Interactions (7) and Clinical Studies (14.3) ] .

Most common adverse reaction: diarrhea (incidence 2.3%) (6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Endo at 1-800-828-9393 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience The following serious adverse reactions are discussed in greater detail in other sections of the label: Fetal Toxicity [ see Warnings and Precautions (5.1) ] Anaphylactic Reactions and Head and Neck Angioedema [ see Warnings and Precautions (5.3) ] Hypotension [ see Warnings and Precautions (5.4) ] Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in clinical trials of another drug and may not reflect the rates observed in practice. Adult Hypertension Data described below reflect the evaluation of the safety of aliskiren tablets in more than 6,460 patients, including over 1,740 treated for longer than 6 months, and more than 1,250 patients for longer than 1 year. In placebo-controlled clinical trials, discontinuation of therapy due to a clinical adverse event, including uncontrolled hypertension, occurred in 2.2% of patients treated with aliskiren tablets versus 3.5% of patients given placebo. These data do not include information from the ALTITUDE study which evaluated the use of aliskiren in combination with ARBs or ACEIs [see Contraindications (4) , Warnings and Precautions (5.2) , and Clinical Studies (14.3) ]. Angioedema: Two cases of angioedema with respiratory symptoms were reported with aliskiren tablets use in the clinical studies.

Lactation: Breastfeeding not recommended. ( 8.2 ) 8.1 Pregnancy Risk Summary Aliskiren can cause fetal harm when administered to a pregnant woman. Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death [see Clinical Considerations ] . Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents. When pregnancy is detected, discontinue aliskiren as soon as possible. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major malformations and miscarriage in clinically recognized pregnancies is 2 to 4%, and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage).

Metabolism

Aliskiren is poorly absorbed (bioavailability about 2.5%) with an approximate accumulation half-life of 24 hours. Steady state blood levels are reached in about 7 to 8 days.

Limited data are available related to overdosage in humans. The most likely manifestation of overdosage would be hypotension. If symptomatic hypotension occurs, supportive treatment should be initiated. Aliskiren is poorly dialyzed. Therefore, hemodialysis is not adequate to treat aliskiren overexposure [ see Clinical Pharmacology (12.3) ] .

• Mar 5, 2007NDANDA021985Lxo Ireland
• Mar 22, 2019ANDAANDA206665Ph Health

1. 1Nausea64411%
2. 2Blood Pressure Increased60610%
3. 3Headache59610%
4. 4Fatigue59410.0%
5. 5Fall5769.7%
6. 6Asthenia5709.6%
7. 7Dizziness5288.9%
8. 8Cough5238.8%
9. 9Dyspnoea5188.7%
10. 10Malaise5098.6%
11. 11Diarrhoea4607.7%
12. 12Vomiting4557.6%
13. 13Pyrexia4116.9%
14. 14Cerebrovascular Accident3986.7%
15. 15Drug Ineffective3556.0%

The 10 most recently updated of 160 ClinicalTrials.gov registrations naming Aliskiren as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Evaluation of a Renin Inhibitor, Aliskiren, Compared to Enalapril, in C3 Glomerulopathy
  Recruiting · Phase 2 · Interventional · 30 enrolled · Region Skane
  NCT04183101updated 2025-06-22
• Non-Inferiority Study of Aliskiren vs Losartan in the Treatment of Hypertension With Hyperuricemia
  Completed · Phase 4 · Interventional · 66 enrolled · Hansung University
  NCT06718062updated 2024-12-05
• A Long Term Safety Study to Test the Combination of Aliskiren/ Amlodipine / Hydrochlorothiazide in Participants With Essential Hypertension
  Completed · Phase 3 · Interventional · 564 enrolled · Novartis
  NCT00667719updated 2021-06-07
• ACEI or ARB and COVID-19 Severity and Mortality in US Veterans
  Completed · Observational · 22,213 enrolled · University of Utah
  NCT04467931updated 2021-04-28
• Pharmacokinetic and Pharmacodynamic Profiles of Aliskiren in Japanese Patients With Mild to Moderate Essential Hypertension
  Completed · Phase 1 · Interventional · 34 enrolled · Novartis
  NCT00424541updated 2020-12-21
• Effect of Light Meal on Pharmacokinetic and Pharmacodynamics of Aliskiren in Patients With Mild to Moderate Hypertension
  Completed · Phase 1 · Interventional · 124 enrolled · Novartis Pharmaceuticals
  NCT00933920updated 2020-12-21
• Efficacy and Tolerability of an Aliskiren-based Treatment Algorithm in Patients With Mild to Moderate Hypertension
  Completed · Phase 4 · Interventional · 256 enrolled · Novartis
  NCT00765947updated 2020-08-06
• Effect of Aliskiren and Hydrochlorothiazide on Kidney Oxygenation in Patients With Hypertension
  Completed · Phase 4 · Interventional · 24 enrolled · Centre Hospitalier Universitaire Vaudois
  NCT01519635updated 2020-03-17
• A Clinical Study to Evaluate Safety & Efficacy of the Combination of Aliskiren, Valsartan & Hydrochlorothiazide in Diabetic Hypertensive Nonresponder Patients
  Completed · Phase 3 · Interventional · 336 enrolled · Novartis
  NCT00219102updated 2020-02-11
• 52-104 Week Off-therapy Second Extension to Study CSPP100A2365
  Completed · Observational · 106 enrolled · Noden Pharma
  NCT01420068updated 2019-03-19

Frequently asked questions

How does Aliskiren work?

Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin I (Ang I).

What is Aliskiren used for?

According to FDA labeling, Aliskiren carries indications including: Aliskiren tablets are a renin inhibitor (RI) 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, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Aliskiren?

Aliskiren is classified as Renin-inhibitors, Renin Inhibitor, Angiotensin-converting Enzyme Inhibitors, Renin Inhibitors, Decreased Blood Pressure.

What are the brand names for Aliskiren?

Aliskiren is marketed under brand names including Tekturna, Tekturna HCT.

What are the contraindications for Aliskiren?

Aliskiren labeling lists contraindications including: Do not use aliskiren with ARBs or ACEIs in patients with diabetes [see Warnings and Precautions (5.2) and Clinical Studies (14.3) ]. Aliskiren tablets are contraindicated in patients with known hypersensitivity to any of the components [see Warnings and Precautions (5.3) ].. Always consult the full prescribing information and a clinician.