eptifibatide (Rx)

Brand and Other Names:Integrilin
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injection solution

  • 2mg/mL
  • 0.75mg/mL

Acute Coronary Syndromes

180 mcg/kg IV bolus over 1-2 min, THEN  

2 mcg/kg/min IV continuous infusion; continue infusion until hospital discharge or initiation of coronary artery bypass graft surgery (CABG), up to 72 hours

Patient to undergo PCI: infusion should be continued until hospital discharge or for up to 18- 24 hr after procedure, whichever comes first, allowing for up to 96 hr of therapy

Administer aspirin (160-325 mg) daily

Dosing considerations

  • Administer concomitantly with heparin dosed to achieve the following parameters:
    • During medical management
      • Target aPTT 50 - 70 seconds
      • If weight greater than or equal to 70 kg, 5000-unit bolus followed by infusion of 1000 units/h
      • If weight less than 70 kg, 60-units/kg bolus followed by infusion of 12 units/kg/h
    • During PCI
      • Target ACT 200 to 300 seconds
      • If heparin is initiated prior to PCI, additional boluses during PCI to maintain an ACT target of
      • 200 to 300 seconds.
      • Heparin infusion after the PCI is discouraged

Percutaneous Coronary Intervention

180 mcg/kg IV bolus immediately, THEN  

Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st bolus

Continue infusion until hospital discharge, or for up to 18 to 24 hours, whichever comes first; minimum 12 hr infusion recommended

In patients who undergo CABG surgery, drug infusion should be discontinued prior to surgery

Administer aspirin, 160 to 325 mg, 1 to 24 hours prior to PCI and daily thereafter

  • Dosing considerations

    • Administer concomitantly with heparin to achieve a target ACT of 200 to 300 seconds
    • Administer 60-units/kg bolus initially in patients not treated with heparin within 6 hours prior to PCI.
    • Additional boluses during PCI to maintain ACT within target.
    • Heparin infusion after the PCI is strongly discouraged

Discontinue administration in patients requiring thrombolytic therapy

Renal Impairment

(CrCl <50 mL/min)

ACS: 180 mcg/kg IV bolus as soon as possible, THEN continuous infusion 1 mcg/kg/min  

PCI: 180 mcg/kg IV immediately before PCI, THEN continuous infusion 1 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st bolus

Hemodialysis: Safety and using during hemodialysis not established

Safety & efficacy not established

In clinical trials, incidence of bleeding complications was higher in the elderly in both placebo and eptifibatide groups, and the incremental risk of eptifibatide-associated bleeding was greater in the older patients. Adjust dose to renal function

Acute Coronary Syndromes

180 mcg/kg IV bolus over 1-2 min, THEN  

2 mcg/kg/min IV for up to 72 hr

Percutaneous Coronary Intervention

180 mcg/kg IV, THEN

Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one

Continue infusion for at least 12 hours

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Interactions

Interaction Checker

and eptifibatide

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            1-10%

            Bleeding (8%)

            Hypotension (7%)

            Thrombocytopenia (2.3%)

            Injection site reaction

            <1%

            Hypersensitivity

            Intracranial hemorrhage

            Pulmonary hemorrhage

            Thrombocytopenia

            GI hemorrhage

            Postmarketing Reports

            Immune-mediated thrombocytopenia (thought to be caused by antibodies that react with GP IIb/IIIa complex)

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            Warnings

            Contraindications

            Hypersensitivity

            History of internal bleeding, intracranial hemorrhage or neoplasm, CVA, thrombocytopenia

            AV malformation or aneurysm, aortic dissection, severe HTN, acute pericarditis

            Other parenteral glycoprotein IIb/IIIa inhibitors

            Cautions

            Bleeding

            • At the site of arterial sheath placement bleeding is the most common complication; minimize use of arterial and venous punctures, intramuscular injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes; when obtaining intravenous access, avoid non-compressible sites (eg, subclavian or jugular veins)
            • Risk factors for bleeding include older age, a history of bleeding disorders, and concomitant use of drugs that increase risk of bleeding (thrombolytics, oral anticoagulants, nonsteroidal anti-inflammatory drugs, and P2Y12 inhibitors); concomitant treatment with other inhibitors of platelet receptor glycoprotein (GP) IIb/IIIa should be avoided; in patients treated with heparin, bleeding can be minimized by close monitoring of aPTT and ACT
            • In patients undergoing PCI, treatment may increase in major and minor bleeding at site of arterial sheath placement; after PCI, infusion should be continued until hospital discharge or up to 18 - 24 hours, whichever comes first;
            • Heparin use is discouraged after PCI procedure; early sheath removal is encouraged while drug is being infused; prior to removing the sheath, it is recommended that heparin be discontinued for 3 to 4 hours and an aPTT of <45 seconds or ACT <150 seconds be achieved; in any case, both drugs should be discontinued and sheath hemostasis achieved at least 2 to 4 hours before hospital discharge; if bleeding at access site cannot be controlled with pressure, infusion of both drugs should be discontinued immediately

            Thrombocytopenia

            • There have been reports of acute, profound thrombocytopenia (immune-mediated and non-immune mediated); in the event of acute profound thrombocytopenia or a confirmed platelet decrease to <100,000/mm3, discontinue drug and heparin (unfractionated or low-molecular weight); monitor serial platelet counts, assess presence of drug-dependent antibodies, and treat as appropriate
            • There has been no clinical experience with therapy initiated in patients with a baseline platelet count <100,000/mm3; if a patient with low platelet counts is receiving drug, their platelet count should be monitored closely
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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: excretion in milk unknown; use with caution

            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

            Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface

            Pharmacokinetics

            Half-life, elimination: 2.5 hr

            Onset: 1 hr

            Duration: 4 hr

            Protein bound: 25%

            Vd: 185-260 mL/kg

            Metabolites: Deaminated eptifibatide, other more polar metabolites detected in urine, no metabolites detected in plasma

            Clearance: 55-58 mL/kg/hr

            Excretion: Urine

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            Administration

            IV Incompatibilities

            Y-site, additive, syringe: furosemide

            IV Compatibilities

            Y-site: alteplase, amiodarone, atropine, bivalirudin, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine sulfate, nitroglycerin, verapamil

            IV Preparation

            Bolus injection: withdraw from 10 mL vial (2 mg/mL; 10, 100 mL)

            Infusion: no prep needed; spike 100 ml vial with vented infusion set (0.75 mg/mL; 100 mL)

            IV Administration

            Inspect for particulate matter and discoloration prior to administration, whenever solution and container permit

            May administer in the same intravenous line as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil

            Do not administer through the same intravenous line as furosemide

            May administer in the same IV line with 0.9% NaCl or 0.9% NaCl/5% dextrose; with either vehicle, the infusion may also contain up to 60 mEq/L of potassium chloride

            Withdraw bolus dose(s) from the 10-mL vial into a syringe; administer bolus dose(s) by IV push

            Immediately following bolus dose administration, initiate a continuous infusion

            When using an intravenous infusion pump, administer undiluted directly from 100-mL vial

            Spike the 100-mL vial with a vented infusion set; center the spike within the circle on the stopper top

            Discard any unused portion left in the vial

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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.
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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.