Version May 2024
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.
Hypertension (alternative agent): Initial: 150 mg once daily; may increase to 300 mg once daily (maximum: 300 mg/day) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: No initial dosage adjustment necessary.
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, limited data suggests no dosage adjustment is necessary (Ref). Risk of hyperkalemia is increased and progressive renal impairment may occur; use with caution.
ESRD (requiring hemodialysis): No dosage adjustment necessary. Risk of hyperkalemia is increased with chronic therapy; use with extreme caution. Note: Hemodialysis eliminates a minimal fraction; does not significantly alter overall aliskiren exposure.
No initial dosage adjustment necessary.
Refer to adult dosing. No initial dosage adjustment required.
(For additional information see "Aliskiren: Pediatric drug information")
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 (Ref).
≥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.
Children ≥6 years and Adolescents: Oral:
CrCl ≥30 mL/minute: No initial dosage adjustment necessary
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, limited data in adults suggests no dosage adjustment is necessary (Ref). Risk of hyperkalemia is increased and progressive renal impairment may occur; use with caution, monitor serum potassium closely.
ESRD (requiring hemodialysis): No dosage adjustment necessary. Hemodialysis eliminates a minimal fraction; does not significantly alter overall aliskiren exposure. Risk of hyperkalemia is increased with chronic therapy; use with extreme caution, monitor serum potassium closely.
Children ≥6 years and Adolescents: Oral: No initial dosage adjustment necessary.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
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
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
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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
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.
Preclinical studies show increased exposure in pediatric patients compared to adults; use is not recommended in children <6 years of age and is contraindicated for use in children <2 years of age.
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
Yes
Tablets (Aliskiren Fumarate Oral)
150 mg (per each): $7.48 - $7.81
300 mg (per each): $9.44 - $9.86
Tablets (Tekturna Oral)
150 mg (per each): $12.67
300 mg (per each): $15.99
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Rasilez: 150 mg, 300 mg
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.
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.
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]).
Tekturna may be confused with Valturna
Substrate of CYP3A4 (minor), P-glycoprotein/ABCB1 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: 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. Risk D: 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. Risk D: Consider therapy modification
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Arginine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
CycloSPORINE (Systemic): May increase the serum concentration of Aliskiren. Risk X: Avoid combination
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Drospirenone-Containing Products: May enhance the hyperkalemic effect of Aliskiren. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Furosemide: Aliskiren may decrease the serum concentration of Furosemide. Risk C: Monitor therapy
Grapefruit Juice: May decrease the serum concentration of Aliskiren. Risk C: Monitor therapy
Heparins (Low Molecular Weight): May enhance the hyperkalemic effect of Aliskiren. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Indoramin: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Itraconazole: May increase the serum concentration of Aliskiren. Risk X: Avoid combination
Levodopa-Foslevodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Foslevodopa. Risk C: Monitor therapy
Loop Diuretics: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: 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). Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hyperkalemic effect of Aliskiren. Risk C: Monitor therapy
Nirmatrelvir and Ritonavir: May increase the serum concentration of Aliskiren. Risk X: Avoid combination
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Aliskiren. Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of Aliskiren. Risk C: 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. Risk D: Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of Aliskiren. Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Aliskiren. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Potassium Salts: May enhance the hyperkalemic effect of Aliskiren. Risk C: Monitor therapy
Prazosin: Antihypertensive Agents may enhance the hypotensive effect of Prazosin. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Silodosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Sparsentan: May enhance the adverse/toxic effect of Aliskiren. Risk X: Avoid combination
Terazosin: Antihypertensive Agents may enhance the hypotensive effect of Terazosin. Risk C: Monitor therapy
Urapidil: Antihypertensive Agents may enhance the hypotensive effect of Urapidil. Risk C: Monitor therapy
High-fat meals decrease absorption. Grapefruit juice may decrease the serum concentration of aliskiren. Management: Administer at the same time each day; administer with or without a meal, but consistent administration with regards to meals is recommended. Avoid concomitant use of aliskiren and grapefruit juice.
[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.
It is not known if aliskiren is present in breast milk. Due to the potential for serious adverse reactions in the breastfeeding infant, breastfeeding is not recommended by the manufacturer.
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
Decreases plasma renin activity and inhibits conversion of angiotensinogen to angiotensin I.
Note: Reported pharmacokinetic data in pediatric patients 6 to 17 years is similar to that of adults.
Onset of action: Maximum antihypertensive effect: Within 2 weeks
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
Bioavailability: ~3%
Half-life elimination: ~24 hours (range: 16 to 32 hours)
Time to peak, plasma: 1 to 3 hours
Excretion: Urine (~25% of absorbed dose excreted unchanged in urine); feces (unchanged via biliary excretion)
Older adult: AUC is increased in patients ≥65 years.
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