Eptifibatide

What it is and how it works

Mechanism of Action Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands to GP IIb/IIIa. When administered intravenously, eptifibatide inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. Platelet aggregation inhibition is reversible following cessation of the eptifibatide infusion; this is thought to result from dissociation of eptifibatide from the platelet.

Indications

Eptifibatide injection is a platelet aggregation inhibitor indicated for: • Treatment of acute coronary syndrome (ACS) managed medically or with percutaneous coronary intervention (PCI) • Treatment of patients undergoing PCI (including intracoronary stenting) Acute Coronary Syndrome (ACS) Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death or new myocardial infarction (MI) in patients with ACS (unstable angina [UA]/non-ST- elevation myocardial infarction [NSTEMI]), including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI). Percutaneous Coronary Intervention (PCI) Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death, new MI, or need for urgent intervention in patients undergoing PCI, including those undergoing intracoronary stenting .

Dosage and administration (summary)

Before infusion of eptifibatide injection, the following laboratory tests should be performed to identify pre-existing hemostatic abnormalities: hematocrit or hemoglobin, platelet count, serum creatinine, and PT/aPTT. In patients undergoing PCI, the activated clotting time (ACT) should also be measured. The activated partial thromboplastin time (aPTT) should be maintained between 50 and 70 seconds unless PCI is to be performed. In patients treated with heparin, bleeding can be minimized by close monitoring of the aPTT and ACT. ACS or PCI: 180 mcg/kg IV bolus as soon as possible after diagnosis followed by infusion at 2 mcg/kg/min.

Contraindications

Treatment with eptifibatide is contraindicated in patients with: • A history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days • Severe hypertension (systolic blood pressure >200 mm Hg or diastolic blood pressure >110 mm Hg) not adequately controlled on antihypertensive therapy • Major surgery within the preceding 6 weeks • History of stroke within 30 days or any history of hemorrhagic stroke • Current or planned administration of another parenteral GP II…

Warnings and precautions

• Eptifibatide can cause serious bleeding. If bleeding cannot be controlled, discontinue eptifibatide immediately. Minimize vascular and other traumas. If heparin is given concomitantly, monitor aPTT or ACT. • Thrombocytopenia: Discontinue eptifibatide and heparin. Monitor and treat condition appropriately. Bleeding Bleeding is the most common complication encountered during eptifibatide therapy. Administration of eptifibatide is associated with an increase in major and minor bleeding, as classified by the criteria of the Thrombolysis in Myocardial Infarction Study group (TIMI) .

Pregnancy

Pregnancy Risk Summary Available data on eptifibatide use in pregnant women from published literature and the pharmacovigilance database are insufficient to establish a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

Storage and supply

How Supplied Eptifibatide injection is supplied as a sterile solution as follows: NDC Eptifibatide Injection Package Factor 67457-629-10 20 mg/10 mL vial 1’s 67457-630-10 200 mg/100 mL vial 1’s 67457-631-10 75 mg/100 mL vial 1’s Storage Vials should be stored refrigerated at 2° to 8°C (36° to 46°F).

Source: Eptifibatide (Eptifibatide) — US FDA prescribing information, 2021-05-28, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.