cangrelor (Rx)

Brand and Other Names:Kengreal
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, lyophilized powder for reconstitution

  • 50mg/vial

Percutaneous Coronary Intervention

Indicated as an adjunct to percutaneous coronary intervention (PCI) to reduce the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor

30 mcg/kg IV bolus infused over 1 minute before PCI, THEN

Immediately follow bolus injection with 4 mcg/kg/min IV infusion; continue for at least 2 hr or duration of PCI, whichever is longer

Transition patients to oral P2Y12 platelet inhibitor

  • Choose from 1 of the loading-dose regimens described below to initiate oral therapy:
  • Ticagrelor: 180 mg PO at any time during cangrelor infusion or immediately after discontinuation
  • Prasugrel: 60 mg PO immediately after discontinuing cangrelor; do not administer prasugrel prior to cangrelor discontinuation because of drug interaction
  • Clopidogrel: 600 mg PO immediately after discontinuing cangrelor; do not administer clopidogrel prior to cangrelor discontinuation because of drug interaction

Safety and efficacy not established

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Interactions

Interaction Checker

and cangrelor

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Bleeding

            GUSTO trial data

            • Mild (14.9%)
            • Moderate (0.4%)
            • Severe/life-threatening (0.2%)

            TIMI trial data

            • Minor (0.6%)
            • Major (0.2%)

            1-10%

            Worsening renal function in patients with CrCl <30 mL/min (3.2%)

            <1%

            Hypersensitivity

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            Warnings

            Contraindications

            Significant active bleeding

            Hypersensitivity

            Cautions

            Increased risk of bleeding; bleeding events of all severities were more common with cangrelor than with clopidogrel

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            Pregnancy

            Pregnancy

            There are no available data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; untreated myocardial infarction can be fatal to pregnant women and fetus

            Disease-associated maternal and/or embryo/fetal risk

            • Myocardial infarction is a medical emergency in pregnancy which can be fatal to pregnant woman and fetus if left untreated; life-sustaining therapy for the pregnant woman should not be withheld due to potential concerns regarding the effects of the drug on the fetus

            Animal data

            • In animal reproduction studies, continuous infusion of drug in pregnant rats and rabbits throughout organogenesis at dose approximately 2-times maximum recommended human dose (MRHD) did not result in fetal malformations

            Labor or delivery

            • Drug use during labor and delivery may increase risk for maternal bleeding and hemorrhage; performance of neuraxial blockade procedures is not advised during drug use due to potential risk of spinal hematoma; when possible, discontinue drug 1 hour prior to labor, delivery, or neuraxial blockade

            Lactation

            There are no data on presence of drug in human milk or animal milk, effects on breastfed infant, or on milk production; due to its short-half life, drug exposure is expected to be very low in breastfed infant

            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

            P2Y12 platelet inhibitor that blocks ADP-induced platelet activation and aggregation; it binds selectively and reversibly to the P2Y12 receptor to prevent further signaling and platelet activation

            Absorption

            Peak plasma concentration: 2 minutes

            Onset of action: Within 2 minutes following 30 mcg/kg IV bolus followed by 4 mcg/kg/min IV infusion

            After discontinuation of the infusion, the antiplatelet effect decreases rapidly and platelet function returns to normal within 1 hr

            Distribution

            Protein bound 97-98%

            Vd: 3.9 L

            Metabolism

            Deactivated rapidly in the circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible antiplatelet activity

            Metabolism is independent of hepatic function and it does not interfere with other drugs metabolized by hepatic enzymes

            Elimination

            Half-life: 3-6 minutes

            Excretion: 58% urine; 35% feces

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            Administration

            IV Preparation

            For each 50 mg/vial, reconstitute by adding 5 mL of sterile water for injection

            Swirl gently until all material is dissolved; avoid vigorous mixing

            Allow any foam to settle

            Ensure that vial contents are fully dissolved and the reconstituted material is a clear, colorless to pale yellow solution

            Do not use without dilution

            Before administration, each reconstituted vial must be diluted further with 0.9% NaCl or D5W

            Withdraw the contents from 1 reconstituted vial and add to 250-mL bag of 0.9% NaCl or D5W

            Mix the bag thoroughly

            This dilution results in a concentration of 200 mcg/mL and should be sufficient for at least 2 hr of dosing

            Patients who weigh ≥100 kg require a minimum of 2 bags

            IV Administration

            Administer via a dedicated IV line

            Administer the bolus volume rapidly (<1 minute), from the diluted bag via manual IV push or pump

            Ensure the bolus is completely administered before the start of PCI

            Start the IV infusion immediately after the bolus administration

            Storage

            Store at controlled room temperature (20-25°C [68-77°F]), with excursions between 15-30°C (59-86°F) permitted

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            Formulary

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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.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            Code Definition
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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.