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Aliskiren

Medically reviewed by Drugs.com. Last updated on Sep 28, 2020.

Pronunciation

(a lis KYE ren)

Index Terms

  • Aliskiren Hemifumarate
  • SPP100

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Tekturna: 150 mg, 300 mg

Generic: 150 mg, 300 mg

Brand Names: U.S.

  • Tekturna

Pharmacologic Category

  • Renin Inhibitor

Pharmacology

Decreases plasma renin activity and inhibits conversion of angiotensinogen to angiotensin I.

Absorption

Poor; absorption decreased by high-fat meal. Aliskiren is a substrate of P-glycoprotein; concurrent use of P-glycoprotein inhibitors may increase absorption.

Metabolism

Extent of metabolism unknown; in vitro studies indicate metabolism via CYP3A4

Excretion

Urine (~25% of absorbed dose excreted unchanged in urine); feces (unchanged via biliary excretion)

Onset of Action

Maximum antihypertensive effect: Within 2 weeks

Time to Peak

1 to 3 hours

Half-Life Elimination

~24 hours (range: 16 to 32 hours)

Special Populations: Elderly

AUC is increased in patients ≥65 years.

Use: Labeled Indications

Hypertension: Management of hypertension in adults and pediatric patients ≥50 kg and ≥6 years of age.

Note: Not recommended for the initial treatment of hypertension (ACC/AHA [Whelton 2017]).

Contraindications

Hypersensitivity to aliskiren or any component of the formulation; concomitant use with an ACE inhibitor or ARB in patients with diabetes; children <2 years of age

Canadian labeling: Additional contraindications (not in US labeling): History of angioedema with aliskiren, ACE inhibitors, or ARBs; hereditary or idiopathic angioedema; pregnancy, breastfeeding; concomitant use with ACE inhibitors or ARBs in patients with GFR <60 mL/minute/1.73 m2

Dosing: Adult

Hypertension (alternative agent): Initial: 150 mg once daily; may increase to 300 mg once daily (maximum: 300 mg/day) (ACC/AHA [Whelton 2017]).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing. No initial dosage adjustment required.

Dosing: Pediatric

Note: Prior to initiation, correct hypovolemia and/or closely monitor volume status in patients on concurrent diuretics during treatment initiation.

Hypertension: Children ≥6 years and Adolescents: Oral:

20 to 50 kg: Limited data available: Initial: 75 mg once daily; if blood pressure not adequately controlled, may increase to 150 mg once daily; maximum daily dose: 150 mg/day (Tekturna prescribing information 2017).

≥50 kg: Initial: 150 mg once daily; if blood pressure not adequately controlled, may increase to 300 mg once daily; maximum daily dose: 300 mg/day.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Administration

Oral: Administer at the same time daily with or without a meal, but consistent administration with regards to meals is recommended; high-fat meal reduces absorption.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted to 15°C to 30°C (59°F to 86°F). Protect from moisture. Dispense blisters in the original container.

Drug Interactions

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification

Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Angiotensin II Receptor Blockers: Aliskiren may enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the hypotensive effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the nephrotoxic effect of Angiotensin II Receptor Blockers. Management: Aliskiren use with ACEIs or ARBs in patients with diabetes is contraindicated. Combined use in other patients should be avoided, particularly when CrCl is less than 60 mL/min. If combined, monitor potassium, creatinine, and blood pressure closely. Consider therapy modification

Angiotensin-Converting Enzyme Inhibitors: Aliskiren may enhance the hyperkalemic effect of Angiotensin-Converting Enzyme Inhibitors. Aliskiren may enhance the hypotensive effect of Angiotensin-Converting Enzyme Inhibitors. Aliskiren may enhance the nephrotoxic effect of Angiotensin-Converting Enzyme Inhibitors. Management: Aliskiren use with ACEIs or ARBs in patients with diabetes is contraindicated. Combined use in other patients should be avoided, particularly when CrCl is less than 60 mL/min. If combined, monitor potassium, creatinine, and blood pressure closely. Consider therapy modification

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

AtorvaSTATin: May increase the serum concentration of Aliskiren. Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Avoid combination

CycloSPORINE (Systemic): May increase the serum concentration of Aliskiren. Avoid combination

Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Drospirenone: May enhance the hyperkalemic effect of Aliskiren. Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy

Erdafitinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Monitor therapy

Furosemide: Aliskiren may decrease the serum concentration of Furosemide. Monitor therapy

Grapefruit Juice: May decrease the serum concentration of Aliskiren. Management: Avoid concomitant use of aliskiren and grapefruit juice. Separation of aliskiren and grapefruit juice administration by several hours may reduce the chance for interaction. Monitor for decreased aliskiren levels/effects. Consider therapy modification

Heparin: May enhance the hyperkalemic effect of Aliskiren. Monitor therapy

Heparins (Low Molecular Weight): May enhance the hyperkalemic effect of Aliskiren. Monitor therapy

Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Itraconazole: May increase the serum concentration of Aliskiren. Avoid combination

Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Avoid combination

Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Monitor therapy

Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Lumacaftor and Ivacaftor: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Monitor therapy

Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicorandil: May enhance the hyperkalemic effect of Aliskiren. Monitor therapy

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Aliskiren. Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Aliskiren. Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of Aliskiren. Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Aliskiren. Monitor therapy

Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Potassium Salts: May enhance the hyperkalemic effect of Aliskiren. Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Yohimbine: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Test Interactions

May lead to false-positive or false-negative aldosterone/renin ratio (ARR) (Funder 2016)

Adverse Reactions

1% to 10%:

Dermatologic: Skin rash (1%)

Gastrointestinal: Diarrhea (2%)

Neuromuscular & skeletal: Increased creatine phosphokinase (>300% increase: 1%)

Renal: Increased blood urea nitrogen (≤7%), increased serum creatinine (≤7%)

Respiratory: Cough (1%)

<1%, postmarketing, and/or case reports: Abdominal pain, anaphylaxis, anemia, angioedema, decreased hematocrit, decreased hemoglobin, dyspepsia, erythema, gastroesophageal reflux disease, gout, hepatic insufficiency, hyperkalemia, hyponatremia, increased liver enzymes, increased uric acid, myositis, nausea, nephrolithiasis, periorbital edema, peripheral edema, pruritus, rhabdomyolysis, seizure, severe hypotension, Stevens-Johnson syndrome, tonic-clonic seizures, toxic epidermal necrolysis, urticaria, vomiting

ALERT: U.S. Boxed Warning

Fetal toxicity

When pregnancy is detected, discontinue aliskiren as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus.

Warnings/Precautions

Concerns related to adverse effects:

• Hyperkalemia: May occur; risk increased in patients with renal impairment or diabetes, or concomitant use with ACE inhibitors, ARBs, NSAIDs, potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts.

• Hypersensitivity: Anaphylaxis and angioedema have been reported. Since the effect of aliskiren on bradykinin levels is unknown, the risk of kinin-mediated etiologies of angioedema occurring is also unknown. Use with caution in any patient with a history of angioedema (of any etiology) as angioedema, some cases necessitating hospitalization and intubation, has been observed with aliskiren use. Discontinue immediately following the occurrence of anaphylaxis or angioedema; do not readminister. Prolonged frequent monitoring may be required especially if tongue, glottis, or larynx are involved as they are associated with airway obstruction. Patients with a history of airway surgery may have a higher risk of airway obstruction. Early, aggressive, and appropriate management is critical.

• Hypotension: During the initiation of therapy, symptomatic hypotension may occur, particularly in volume or salt-depleted patients or with concomitant use of other agents acting on the renin-angiotensin-aldosterone system. Prior to initiation, correct hypovolemia or salt depletion, or closely monitor during treatment initiation. If hypotension does occur, this is not a contraindication for further use; once blood pressure has been stabilized, aliskiren usually can be continued without difficulty.

• Renal effects: Changes in renal function, including acute renal failure, may occur; risk is increased in patients with renal artery stenosis, severe heart failure, post-myocardial infarction, volume depletion, or patients receiving ARB, ACEI or NSAIDs. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function.

Disease-related concerns:

• Diabetes: Use in patients with diabetes has demonstrated an increased incidence of renal impairment, hypotension, and hyperkalemia; use is contraindicated in patients with diabetes who are taking an ACE inhibitor or ARB.

• Renal impairment: Use with caution in patients with renal impairment; risk of developing acute renal failure and hyperkalemia is increased. Avoid concomitant use with an ACE inhibitor or ARB in patients with CrCl <60 mL/minute.

Special populations:

• Pregnancy: [US Boxed Warning]: Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected.

Monitoring Parameters

Blood pressure; serum potassium, BUN, serum creatinine

The 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults (ACC/AHA [Whelton 2017]):

Confirmed hypertension and known CVD or 10-year ASCVD risk ≥10%: Target blood pressure <130/80 mm Hg is recommended

Confirmed hypertension without markers of increased ASCVD risk: Target blood pressure <130/80 mm Hg may be reasonable

Pregnancy Considerations

[US Boxed Warning]: Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected. The use of drugs which act on the renin-angiotensin system are associated with oligohydramnios. Oligohydramnios, due to decreased fetal renal function, may lead to fetal lung hypoplasia and skeletal malformations. Use is also associated with anuria, hypotension, renal failure, skull hypoplasia, and death in the fetus/neonate. The exposed fetus should be monitored for fetal growth, amniotic fluid volume, and organ formation. Infants exposed in utero should be monitored for hyperkalemia, hypotension, and oliguria.

Patient Education

What is this drug used for?

• It is used to treat high blood pressure.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Diarrhea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Kidney problems like unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain

• High potassium like abnormal heartbeat, confusion, dizziness, passing out, weakness, shortness of breath, numbness or tingling feeling

• Dizziness

• Passing out

• Abdominal pain

• Vomiting

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.