Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 2.08mg

Thromboembolism

Indicated to reduce thrombotic cardiovascular events in patients with a history of MI or with peripheral arterial disease

2.08 mg PO qDay in combination with either aspirin and/or clopidogrel (according to their indications or standard of care); there is limited clinical experience with other antiplatelet drugs and none with vorapaxar as the only antiplatelet agent

Dosage Modifications

Renal impairment: No dose adjustment required

Mild-to-moderate hepatic impairment: No dose adjustment required

Severe hepatic impairment: Not recommended; based on the increased inherent risk of bleeding in patients with severe hepatic impairment

Dosing Considerations

Results from clinical trials have shown vorapaxar reduces the rate of a combined endpoint of cardiovascular death, MI, stroke, and urgent coronary

Administration

May take with or without food

Safety and efficacy not established

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Interactions

Interaction Checker

and vorapaxar

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Bleeding

            Non-CABG-Related Bleeds in Post-MI or PAD Patients without a History of Stroke or TIA

            • Severe (1%)
            • Moderate or severe (3%)
            • Any bleeding (25%)
            • Fatal bleeding (0.2%)
            • Intracranial hemorrhage (0.4%)
            • Clinically significant bleeding (15.5%)
            • GI bleeding (4.7%)

            1-10%

            Anemia (5%)

            Depression (2.4%)

            Rashes, eruptions, exanthemas (2.2%)

            <1%

            Diplopia (0.2%)

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            Warnings

            Black Box Warnings

            Do not use in patients with a history of stroke, TIA, or intracranial hemorrhage (ICH)

            Increases risk of bleeding, including ICH and fatal bleeding

            Contraindications

            History of stroke, TIA, or ICH because of an increased risk of ICH in this population (see Black Box Warnings)

            Active pathologic bleeding

            Cautions

            Discontinue in patients who experience a stroke, TIA, or ICH

            Antiplatelet agents, including vorapaxar, increase the risk of bleeding, including ICH and fatal bleeding (see Black Box Warnings)

            Strong CYP3A inhibitors increase and inducers decrease vorapaxar exposure; avoid coadministration

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            Pregnancy & Lactation

            Pregnancy

            Based on potential for serious adverse reactions (such as maternal bleeding/hemorrhage) and long half-life which makes it effectively irreversible, discontinue therapy when pregnancy is detected and initiate alternative therapy with a shorter duration of action

            Available data from postmarketing experience with use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Animal data

            • In animal reproduction studies, no embryo/fetal toxicities, malformations or maternal toxicities were observed in rats and rabbits exposed during period of organogenesis at exposures 56 times and 26 times, respectively, human systemic exposure at recommended human dose (RHD)

            Lactation

            There are no data on presence of drug or metabolites in human milk, effects on breastfed infant, or on milk production; when drug was administered to lactating rats, drug was actively secreted in milk of rats; when a drug is present in animal milk, it is likely the drug will be present in human milk; because of potential for serious adverse reactions in breastfed infant, such as bleeding, advise patients that breastfeeding is not recommended during treatment

            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

            Reversible antagonist of the protease-activated receptor-1 (PAR-1) expressed on platelets, but its long half-life makes it effectively irreversible; inhibits thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation in in vitro studies

            Absorption

            Bioavailability: 100%

            Peak plasma time: 1 hr (fasting); 45 min (nonfasting)

            Distribution

            Protein bound: ≥99%; highly bound to albumin and does not preferentially distribute into RBCs

            Vd: 424 L

            Steady-state: 21 days

            Metabolism

            Metabolism via CYP3A4 and CYP2J2

            Major active circulating metabolite is M20 (monohydroxy metabolite) and the predominant metabolite identified in excreta is M19 (amine metabolite)

            Systemic exposure of M20 is ~20% of the exposure to vorapaxar

            Elimination

            Half-life: 3-4 days (disposition); 8 days (terminal elimination)

            Excretion (as metabolites): 58% feces; 25% urine

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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.
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            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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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each 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.