No

Antiplatelet Agent

Treatment of patients with acute coronary syndrome (UA/NQMI), including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI including PTCA)

B

Hypersensitivity to eptifibatide or any component of the product; active abnormal bleeding or a history of bleeding diathesis within the previous 30 days; history of CVA within 30 days or a history of hemorrhagic stroke; 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; current or planned administration of another parenteral GP IIb/IIIa inhibitor; thrombocytopenia; serum creatinine greater than or equal to 4 mg/dL; dependency on renal dialysis

Bleeding is the most common complication. Most major bleeding occurs at the arterial access site where the cardiac catheterization was done. When bleeding can not be controlled with pressure, discontinue infusion and heparin. Use caution in patients with platelet counts <150,000/mm³, hemorrhagic retinopathy, or with other drugs that affect hemostasis. Concurrent use with thrombolytics has not been established as safe. Minimize other procedures including arterial and venous punctures, I.M. injections, nasogastric tubes, etc. Sheath should not be removed unless the aPTT < 45 sec or the ACT < 150 sec.

Bleeding is the major drug-related adverse effect. Major bleeding was reported in 4.4% to 10.5%; minor bleeding was reported in 10.5% to 14.2%; requirement for transfusion was reported in 5.5% to 12.8%.

Local: Injection site reaction

Neuromuscular & skeletal: Back pain

1% to 10%: Hematologic: Thrombocytopenia (2.8% to 3.2%)

<1% (Limited to important or life-threatening symptoms): Intracranial hemorrhage (0.5% to 0.7%), anaphylaxis (0.4% to 0.6%)

Two cases of human overdosage have been reported; neither case was eventful and these were not associated with major bleeding. Symptoms of overdose in animal studies include loss of righting reflex, dyspnea, ptosis, decreased muscle tone, and petechial hemorrhages.

Cephalosporins which contain the MTT side chain may theoretically increase the risk of hemorrhage

Drugs which affect platelet function (eg, aspirin, NSAIDs, dipyridamole, ticlopidine, clopidogrel) may potentiate the risk of hemorrhage; use with caution

Heparin and aspirin: Use with aspirin and heparin may increase bleeding over aspirin and heparin alone. However, aspirin and heparin were used concurrently in the majority of patients in the major clinical studies of eptifibatide

Thrombolytic agents theoretically may increase the risk of hemorrhage; use with caution

Warfarin and oral anticoagulants: Risk of bleeding may be increased during concurrent therapy

Other IIb/IIIa antagonists: Avoid concomitant use of other glycoprotein IIb/IIIa antagonists (see Contraindications)

Vials should be stored refrigerated at 2°C to 8°C (36°F to 46°F). Vials can be kept at room temperature for 2 months. Protect from light until administration. Do not use beyond the expiration date. Discard any unused portion left in the vial.

Eptifibatide is a cyclic heptapeptide which blocks the platelet glycoprotein IIb/IIIa receptor, the binding site for fibrinogen, von Willebrand factor, and other ligands. Inhibition of binding at this final common receptor reversibly blocks platelet aggregation and prevents thrombosis.

Onset of action: Within 1 hour

Half-life: 2.5 hours

Metabolism: Total body clearance: 55-58 mL/kg/hour; renal clearance is ~50% of total in healthy subjects

Protein binding: ~25%

Elimination: Renal excretion of eptifibatide and metabolites accounts for majority of drug elimination; significant renal impairment is expected to alter the disposition of this compound

Reversibility: Platelet function is restored in about 4 hours following discontinuation

Adults: I.V.:

Percutaneous coronary intervention (PCI) in patients not presenting with an acute coronary syndrome: Bolus of 135 mcg/kg administered immediately before the initiation of PCI followed by a continuous infusion of 0.5 mcg/kg/minute for 20-24 hours.

Dosing adjustment in renal impairment: Adults: S_Cr >2 mg/dL and <4 mg/dL: Use 135 mcg/kg bolus and 0.5 mcg/kg/minute infusion.

Coagulation parameters, signs/symptoms of excessive bleeding. Laboratory tests at baseline and monitoring during therapy: hematocrit and hemoglobin, platelet count, serum creatinine, PT/APTT, and ACT with PCI (maintain ACT between 300-350 seconds).

Eptifibatide and other IIb/IIIa inhibitors appear to have a beneficial effect in decreasing cardiovascular death and the need for revascularization when used in patients with coronary artery disease. This is not necessarily a class effect. Some IIb/IIIa inhibitors (eg, sibrafiban) have not demonstrated clear cardiovascular benefit. Specifically, the benefits of IIb/IIIa inhibitors are evident when used with aspirin either with or in comparison to heparin in patients with unstable angina. IIb/IIIa inhibitors also decrease the frequency of cardiovascular presentations when used prior to angioplasty or arthrectomy. The benefits in terms of cardiovascular event reduction need to be balanced against a small but significantly increased risk of bleeding.

None reported

Contraindicated in patients with a recent stroke (within 30 days)

No information available to require special precautions

Bleeding may occur while patient is medicated with eptifibatide. Platelet function is restored in about 4 hours following discontinuation.

Emergency use may dictate depth of patient education. This medication can only be administered I.V. You will have a tendency to bleed easily following this medication. Use caution to prevent injury (use electric razor, use soft toothbrush, use caution with sharps). If bleeding occurs, apply pressure to bleeding spot until bleeding stops completely. Report unusual bruising or bleeding (eg, blood in urine, stool, or vomitus, bleeding gums), dizziness or changes in vision, or back pain. Breast-feeding precautions: Breast-feeding is not recommended.

Do not shake the vial; maintain bleeding precautions, avoid unnecessary arterial and venous punctures, use saline or heparin lock for blood drawing, assess sheath insertion site and distal pulses of affected leg every 15 minutes for the first hour and then every 1 hour for the next 6 hours. Arterial access site care is important to prevent bleeding. Care should be taken when attempting vascular access that only the anterior wall of the femoral artery is punctured, avoiding a Seldinger (through and through) technique for obtaining sheath access. Femoral vein sheath placement should be avoided unless needed. While the vascular sheath is in place, patients should be maintained on complete bed rest with the head of the bed at a 30° angle and the affected limb restrained in a straight position.

Injection: 0.75 mg/mL (100 mL); 2 mg/mL (10 mL)