aliskiren (Rx)

Brand and Other Names:Tekturna
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 150mg
  • 300mg

oral pellets in capsules

  • 37.5mg

Hypertension

Indicated for treatment of hypertension in adults and children ≥6 years

150 mg PO qDay, may increase to 300 mg PO qDay based on response and tolerability

See also Administration

Dosage Modification

Hepatic impairment

  • No dose adjustment required

Renal impairment

  • CrCl ≥30 mL/min: No dose adjustment required
  • CrCl <30 mL/min: No dose adjustment required, but risk of hyperkalemia and renal dysfunction may occur; use caution
  • End-stage renal disease (ESRD): No dosage adjustment required

Dosage Forms & Strengths

tablet

  • 150mg
  • 300mg

oral pellets

  • 37.5mg

Hypertension

Indicated for treatment of hypertension in adults and children ≥6 years

See also Administration

<2 years: Contraindicated

2 to <6 years: Safety and efficacy not established

6 to 17 years

  • <20 kg: Not recommended
  • 20 to <50 kg: Starting dose is 75 mg PO qDay; not to exceed 150 mg PO qDay
  • ≥50 kg: 150 mg PO qDay; may increase to 300 mg PO qDay based on response and tolerability
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Interactions

Interaction Checker

and aliskiren

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Diarrhea (2.3%)

            Cough (1.1%)

            Rash (1%)

            Increase in serum creatinine (<7%)

            Hyperkalemia (<1%)

            <1%

            Angioedema

            Headache

            Gout

            Renal stones

            Seizure

            Severe hypotension

            Rhabomyolysis

            Toxic epidermal necrolysis

            Increase in uric acid

            Angina

            Postmarketing Reports

            Peripheral edema

            Increased serum creatinine

            Nausea/vomiting

            Hyponatremia

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            Warnings

            Black Box Warnings

            Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death

            Contraindications

            Hypersensitivity

            Coadministration with ARBs or ACE inhibitors in patients with diabetes mellitus

            Children <2 years

            Cautions

            Hypersensitivity reactions (eg, anaphylactic reactions and angioedema of the face, extremities, lips, tongue, glottis and/or larynx) have been reported in patients treated with aliskiren and has necessitated hospitalization and intubation; treat and discontinue therapy immediately in patients who develop anaphylactic reactions or angioedema, and do not readminister

            Patients whose renal function may depend in part on activity of renin-angiotensin–aldosterone system (RAAS) [eg, patients with renal artery stenosis, severe heart failure, postmyocardial infarction or volume depletion) or patients receiving ARB, ACE inhibitors or nonsteroidal anti-inflammatory drug (NSAID), including selective cyclooxygenase-2 inhibitors (COX-2 inhibitors)], therapy may be at particular risk of developing acute renal failure; monitor renal function periodically (see Black Box Warnings)

            Symptomatic hypotension may occur after initiation of treatment in patients with marked volume depletion, patients with salt depletion, or with combined use of aliskiren and other agents acting on the RAAS; volume or salt depletion should be corrected prior to administration, or initiate treatment under close medical supervision; a transient hypotensive response is not a contraindication to further treatment

            Drugs interactions overview

            • Cyclosporine or itraconazole increase aliskiren levels; avoid concomitant use
            • Oral coadministration of aliskiren and furosemide reduced exposure to furosemide
            • Coadministration of nonsteroidal anti-inflammatory drug (NSAIDs), including selective COX-2 inhibitors with aliskiren, may result in deterioration of renal function, including possible acute renal failure; effects are usually reversible; monitor renal function periodically in patients receiving aliskiren and NSAID therapy
            • Coadministration with ACE inhibitors or ARBs
              • Concomitant use of aliskiren with other agents acting on the RAAS (eg, ACEIs or ARBs) is associated with an increased risk of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared with monotherapy)
              • Coadministration of 2 drugs that inhibit the renin-angiotensin system do not obtain any additional benefit compared to monotherapy (see Contraindications)
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            Pregnancy & Lactation

            Pregnancy

            Fetal harm may occur 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

            Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (eg, need for cesarean section, and post-partum hemorrhage); hypertension increases the fetal risk for intrauterine growth restriction and intrauterine death

            Fetal or neonatal adverse reactions

            • Use of drugs that act on the renin-angiotensin system in the second and third trimesters of pregnancy can result in the following: reduced fetal renal function leading to anuria and renal failure, oligohydramnios, fetal lung hypoplasia and skeletal deformations, including skull hypoplasia, hypotension, and death
            • Perform serial ultrasound examinations to assess the intra-amniotic environment
            • Observe infants with histories of in utero exposure to aliskiren for hypotension, oliguria, and hyperkalemia; if oliguria or hypotension occur in neonates with a history of in utero exposure to aliskiren, support blood pressure and renal perfusion

            Lactation

            There is no information regarding the presence of aliskiren in human milk, the effects on the breastfed infant, or the effects on milk production

            Owing to the potential for serious adverse reactions, including hypotension, hyperkalemia and renal impairment in nursing infants

            Advise a nursing woman that breastfeeding is not recommended during therapy

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Renin inhibitor that inhibits the conversion of angiotensinogen to angiotensin I. The decrease in antiotensin I causes a decrease in angiotensin II, a potent blood pressure elevating peptide

            Absorption

            Bioavailability: ~3%

            Peak Plasma Time: 1-3 hr

            Onset of action: Optimum effect achieved within 2 weeks

            Mean AUC and Cmax of aliskiren are decreased by 71% and 85% when taken with a high fat meal

            Metabolism

            Metabolism: CYP3A4

            In preclinical studies, P-gp was found to be the major efflux system involved in intestinal absorption and elimination via biliary excretion of aliskiren

            Excretion

            Half-life: 24 hr

            Excretion: Urine (~25%)

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            Administration

            Oral administration

            Tablets: Establish a routine pattern for taking aliskiren with regard to meals; high-fat meals decrease absorption substantially

            Oral pellets

            • Use for patients unable to swallow tablets
            • Oral pellets are available in a dispensing capsule; do not swallow the capsules containing oral pellets
            • Do not empty contents of capsule directly into mouth; do not chew or crush the contents of the capsule
            • Hold capsule upright with the imprint NVR12 at the top; carefully open capsule and ensure no pellets remain in the dispensing capsule
            • Pour entire contents in milk (dairy or soy-based) or water immediately without chewing or crushing
            • Alternatively, oral pellets may be mixed with 1 or more teaspoons of vanilla pudding (milk or soy-based), or vanilla ice cream (milk or soy based)
            • Establish a routine pattern for taking aliskiren with regard to meals; high-fat meals decrease absorption substantially

            Storage

            Oral pellets and tablets

            • Store at room temperature between 68-77°F (20-25°C)
            • Keep in the blister packages in the original container; protect from moisture
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.