Eptifibatide (2 brand names, 1 dosage form, 1 route)
Available dosage forms: INJECTABLE.
Routes of administration: INJECTION.
Brand Names
- EPTIFIBATIDE
- INTEGRILIN
Dosage and Administration
Eptifibatide injection in Galaxy container is for intravenous infusion only, not for intravenous bolus use. 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.
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 IIb/IIIa inhibitor •Dependency on renal dialysis •Hypersensitivity to eptifibatide or any component of the product (hypersensitivity reactions that occurred included anaphylaxis and urticaria)
Adverse Reactions
The following serious adverse reaction is also discussed elsewhere in the labeling: •Bleeding [see Contraindications (4) and Warnings and Precautions (5.1)]
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.
Overdosage
There has been only limited experience with overdosage of eptifibatide. There were 8 patients in the IMPACT II study, 9 patients in the PURSUIT study, and no patients in the ESPRIT study who received bolus doses and/or infusion doses more than double those called for in the protocols. None of these patients experienced an intracranial bleed or other major bleeding. Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis). Symptoms of acute toxicity were loss of righting reflex, dyspnea, ptosis, and decreased muscle tone in rabbits and petechial hemorrhages in the femoral and abdominal areas of monkeys. From in vitro studies, eptifibatide is not extensively bound to plasma proteins and thus may be cleared from plasma by dialysis.