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ranolazine (Rx)Brand and Other Names:Ranexa

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, extended-release

  • 500mg
  • 1,000mg
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Angina

Chronic angina

500 mg PO BID initially; may increase to 1,000 mg PO BID, if needed

Dosage Considerations

May be used concomitantly with beta blockers, nitrates, calcium channel blockers, antiplatelet therapy, lipid-lowering therapy, ACE inhibitors, and ARBs

Strong CYP3A4 inhibitors of inducers: Contraindicated

Coadministration with moderate CYP3A4 inhibitors: Not to exceed 500 mg PO BID

Coadministration with P-gp inhibitors (eg, cyclosporine): May require downward titration

Dosing Modifications

Renal impairment: Cmax increases between 40-50% in patients with mild, moderate, or severe renal impairment

Hepatic impairment

  • Contraindicated for all degrees of hepatic impairment, due to 3-fold increased risk of QT prolongation
  • Mild (Child-Pugh A): Cmax increases 30%
  • Moderate (Child Pugh B): Cmax increases 80%

Administration

Swallow tablets whole; do not crush, chew, or split

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

ranolazine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dizziness (5-13%)

            1-10%

            Nausea (4-9%)

            Constipation (5-8%)

            Headache (3-6%)

            Syncope (3%)

            Frequency Not Defined

            Palpitations

            Bradycardia

            Peripheral edema

            Prolonged QT interval

            Abdominal pain

            Dry mouth

            Dyspepsia

            Anorexia

            Vomiting

            Hematuria

            Dyspnea

            Tinnitus

            Vertigo

            Blurred vision

            Vasovagal syncope

            Confusional state

            Hematuria

            Hyperhidrosis

            Postmarketing Reports

            Neurologic: Tremor, paresthesia, hypoesthesia

            Psychiatric: Hallucination

            Angioedema

            Rash

            Pruritus

            Orthostatic hypotension

            Hypoglycemia (in diabetic patients on antidiabetic medication)

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            Warnings

            Contraindications

            Hepatic cirrhosis, including Child-Pugh class A (mild), B (moderate), and C (severe)

            Strong CYP3A inhibitors (eg, ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, saquinavir)

            CYP3A inducers (eg, carbamazepine, phenobarbital, phenytoin, rifampin, rifabutin, rifapentine, St. John’s wort)

            Cautions

            Not for acute anginal episodes

            While ACS patients appear not to be at increased risk for proarrhythmia or sudden death, ranolazine has been shown to block I-Kr and cause dose-related QTc-interval prolongation

            Little data available on high doses (ie, >1000 mg BID), long exposure, concomitant use with QT interval-prolonging drugs, or potassium channel variants causing prolonged QT interval

            Increased risk of QTc prolongation in patients with mild or moderate hepatic impairment

            Acute renal failure reported in some patients with severe renal impairment (CrCl <30 mL/min); discontinue if marked increase in creatinine occurs with increased BUN

            Individuals >75 years have higher incidence of adverse effects

            Causes small reductions in HbA1c in patients with diabetes; must not be considered a treatment for diabetes

            Avoid grapefruit products

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Unknown if excreted in breast milk; discontinue or do not nurse

            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

            Antianginal effects not determined, but does not depend on HR or BP reduction; no effect on rate-pressure product at maximal exercise; shown to inhibit cardiac late sodium current (INA) at therapeutic levels

            Absorption

            Bioavailability: 76%; absorption is highly variable but is unaffected by food

            Peak plasma time: 2-5 hr

            Distribution

            Protein bound: 62%

            Metabolism

            Intestine and liver (CYP3A4 and CYP2D6)

            Enzymes inhibited: CYP3A4 (weak); CYP2D6 (moderate); both in vitro

            Elimination

            Half-life: 7 hr

            Excretion: Urine (75%), feces (25%)

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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