eptifibatide

Decreases platelet aggregation by reversibly antagonizing the binding of fibrinogen to the glycoprotein IIb/IIIa binding site on platelet surfaces.

Therapeutic effects:

Reduction in risk of death or new MI in patients with acute coronary syndrome.
Reduction in risk of death, new MI, or need for urgent intervention in patients undergoing PCI.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: 50% excreted by the kidneys.

Half-Life: 2.5 hr.

Time/Action Profile ⬆ ⬇

(effects on platelet function)

ROUTE	ONSET	PEAK	DURATION
IV	immediate	following bolus	brief‡

‡Inhibition is reversible following cessation of infusion.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Active internal bleeding or history of bleeding within previous 30 days;
Severe uncontrolled hypertension (systolic BP >200 mm Hg and/or diastolic BP >110 mm Hg);
Major surgical procedure within 6 wk;
History of hemorrhagic stroke or other stroke within 30 days;
Concurrent use of other glycoprotein IIb/IIIa receptor antagonists;
Platelet count <100,000/mm³;
Severe renal impairment (serum creatinine ≥4 mg/dL) or dependency on renal dialysis.

Use Cautiously in:

Renal impairment (↓ infusion rate if CCr <50 mL/min);
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: risk of bleeding in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Noted for patients receiving heparin and aspirin in addition to eptifibatide

CV: hypotension

Hemat: BLEEDING (INCLUDING GI AND INTRACRANIAL BLEEDING, HEMATURIA, AND HEMATOMAS), thrombocytopenia

Interactions ⬆ ⬇

Drug-drug:

↑risk of bleeding with other drugs that affect hemostasis (heparins, warfarin, NSAIDs, thrombolytic agents, dipyridamole, clopidogrel, some cephalosporins, valproates).

Drug-Natural Products:

↑bleeding risk with arnica, chamomile, clove, dong quai, feverfew, garlic, ginger, ginkgo, and Panax ginseng.

Route/Dosage ⬆ ⬇

Acute Coronary Syndrome

Percutaneous Coronary Intervention

IV (Adults ): 180 mcg/kg (max = 22.6 mg) as a bolus dose, followed by 2 mcg/kg/min (max = 15 mg/hr) infusion until hospital discharge or initiation of coronary artery bypass graft surgery (up to 72 hr). If a patient is to undergo PCI, the infusion should be continued until hospital discharge or for up to 18–24 hr after the PCI, whichever comes first, allowing for up to 96 hr of therapy.

Renal Impairment

IV (Adults ): CrCl <50 mL/min: 180 mcg/kg (max = 22.6 mg) as a bolus dose, followed by 1 mcg/kg/min (max = 7.4 mg/hr) infusion until hospital discharge or initiation of coronary artery bypass graft surgery (up to 72 hr). If a patient is to undergo PCI, the infusion should be continued until hospital discharge or for up to 18–24 hr after the PCI, whichever comes first, allowing for up to 96 hr of therapy.
IV (Adults ): 180 mcg/kg (max = 22.6 mg) as a bolus dose, immediately before PCI, followed by 2 mcg/kg/min (max = 15 mg/hr) infusion; a 2nd bolus of 180 mcg/kg (max = 22.6 mg) is given 10 min after 1st bolus. Infusion should be continued until hospital discharge, or for up to 18 to 24 hr, whichever comes first (minimum of 12 hr).

Renal Impairment

(Adults ): CrCl <50 mL/min: 180 mcg/kg (max = 22.6 mg) bolus followed by 1 mcg/kg/min (max = 7.4 mg/hr) infusion; a 2nd bolus of 180 mcg/kg (max = 22.6 mg) is given 10 min after 1st bolus.

Availability ⬆ ⬇

(Generic available)

Solution for injection: 20 mg/10 mL; 75 mg/100 mL; 200 mg/100 mL

Assessment ⬆ ⬇

Assess for bleeding. Most common sites are arterial access site for cardiac catheterization or GI or GU tract. Minimize arterial and venous punctures, IM injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes. Avoid noncompressible sites for IV access. If bleeding cannot be controlled with pressure, discontinue eptifibatide and heparin immediately.

Lab Test Considerations:

Prior to eptifibatide therapy, assess hemoglobin or hematocrit, platelet count, serum creatinine, and PT/aPTT. Activated clotting time (ACT) should also be measured in patients undergoing PCI.
- Maintain the aPTT between 50 and 70 sec unless PCI is to be performed. Maintain ACT between 300 and 350 sec during PCI.
- Arterial sheath should not be removed unless aPTT <45 sec.
- If platelet count decreases to <100,000 and is confirmed, discontinue eptifibatide and heparin and monitor and treat condition.

Implementation ⬆ ⬇

Accidental overdose of antiplatelet medications has resulted in patient harm or death from internal hemorrhage or intracranial bleeding. Have second practitioner independently check original order, dose calculations, and infusion pump settings.
Most patients receive heparin and aspirin concurrently with eptifibatide.
- After PCI, femoral artery sheath may be removed during eptifibatide treatment only after heparin has been discontinued and its effects mostly reversed.
- Do not administer solutions that are discolored or contain particulate matter. Discard unused portion.

IV Administration:

Diluent: Withdraw appropriate loading dose from bolus vial (20 mg/10-mL vial) into a syringe. Administer undiluted.
Concentration: 2 mg/mL.
Rate: Administer over 1–2 min.
Diluent: Administer undiluted directly from the 100-mL vial via an infusion pump.Concentration: 0.75 mg/mL or 2 mg/mL (depends on vial used).
Rate: Based on patient's weight (see Route/Dosage section).

Patient/Family Teaching ⬆ ⬇

Inform patient of the purpose of eptifibatide.
Instruct patient to notify health care professional immediately if any bleeding is noted.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇