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aliskiren (Rx)Brand and Other Names:Tekturna

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 150mg
  • 300mg
more...

Hypertension

150 mg PO qDay, may increase to 300 mg PO qDay

Administration: Use standard routine with regards to meals to ensure dosing consistency

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

Safety and efficacy not established

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Interactions

Interaction Checker

aliskiren and

No Results

     
     activity indicator 
    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

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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

            Cautions

            Hypersensitivity reactions such as 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; this may occur at any time during treatment and has occurred in patients with and without a history of angioedema with ACEIs or angiotensin receptor antagonists; patients who experience these effects, even without respiratory distress, require prolonged observation and appropriate monitoring measures; treatment with antihistamines and corticosteroids may not be sufficient to prevent respiratory involvement; prompt administration of subcutaneous epinephrine solution 1:1000 (0.3 mL to 0.5 mL) and measures to ensure a patent airway may be necessary; 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; e.g., 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; consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function

            High fat meal significantly reduces absorption

            Preclinical studies indicate a potential for substantial increase in exposure to aliskiren in pediatric patients

            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 renin-angiotensin‐ aldosterone system (RAAS); volume or salt depletion should be corrected prior to administration of therapy, or treatment should start under close medical supervision; a transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once blood pressure has stabilized

            Cyclosporine or itraconazole increase aliskiren levels; avoid concomitant use

            Coadministration with ACE inhibitors or ARBs

            • When aliskiren was prescribed with ACE inhibitors or angiotensin receptor blockers (ARBs) in the ALTITUDE study, an increased incidence of nonfatal stroke, renal complications, hyperkalemia, and hypotension was observed after 18-24 months
            • The ALTITUDE trial included patients with hypertension plus type 2 diabetes and renal impairment who were at high risk of cardiovascular and renal events
            • Coadministration of aliskiren with angiotensin converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) in patients with diabetes or kidney (renal) impairment; their use is contraindicated in patients with diabetes
            • Avoid use of aliskiren with ARBs or ACEIs in moderate to severe renal impairment (ie, GFR <60 mL/min)
            • Hyperkalemia: Increases in serum potassium >5.5 mEq/L were infrequent with aliskiren (0.9% compared to 0.6% with placebo); however, when used in combination with an ACE inhibitor in a diabetic population, increases in serum potassium were more frequent (5.5%); monitor potassium levels periodically
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            Pregnancy & Lactation

            Pregnancy Category: C (1st trimester); D (2nd & 3rd trimesters), see Boxed Warning

            Lactation: Excretion in milk unknown/not recommended

            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

            Pharmacokinetics

            Bioavailability: ~3%

            Peak Plasma Time: 1-3 hr

            Metabolism: CYP3A4

            Half-Life elimination: 24 hr

            Excretion: Urine (~25%)

            Onset of action: Optimum effect achieved within 2 weeks

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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.
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            ST Step Therapy
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            OR Other Restrictions
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