Drug Detail:Eptifibatide (Eptifibatide [ ep-ti-fye-ba-tide ])
Drug Class: Glycoprotein platelet inhibitors
Usual Adult Dose for Myocardial Infarction
Initial: 180 mcg/kg intravenous bolus administered as soon as possible following diagnosis
Maintenance: 2 mcg/kg/min continuous infusion (following the initial bolus) until hospital discharge or initiation of CABG surgery, up to 72 hours. If a patient is to undergo a percutaneous coronary intervention (PCI) while receiving eptifibatide, the infusion should be continued up to hospital discharge, or for up to 18 to 24 hours after the procedure, whichever comes first, allowing for up to 96 hours of therapy.
In patients who undergo coronary artery bypass graft surgery, eptifibatide infusion should be discontinued prior to surgery.
Usual Adult Dose for Angina Pectoris
Initial: 180 mcg/kg intravenous bolus administered as soon as possible following diagnosis
Maintenance: 2 mcg/kg/min continuous infusion (following the initial bolus) until hospital discharge or initiation of CABG surgery, up to 72 hours. If a patient is to undergo a percutaneous coronary intervention (PCI) while receiving eptifibatide, the infusion should be continued up to hospital discharge, or for up to 18 to 24 hours after the procedure, whichever comes first, allowing for up to 96 hours of therapy.
In patients who undergo coronary artery bypass graft surgery, eptifibatide infusion should be discontinued prior to surgery.
Usual Adult Dose for Acute Coronary Syndrome
Initial: 180 mcg/kg intravenous bolus administered as soon as possible following diagnosis
Maintenance: 2 mcg/kg/min continuous infusion (following the initial bolus) until hospital discharge or initiation of CABG surgery, up to 72 hours. If a patient is to undergo a percutaneous coronary intervention (PCI) while receiving eptifibatide, the infusion should be continued up to hospital discharge, or for up to 18 to 24 hours after the procedure, whichever comes first, allowing for up to 96 hours of therapy.
In patients who undergo coronary artery bypass graft surgery, eptifibatide infusion should be discontinued prior to surgery.
Usual Adult Dose for Percutaneous Coronary Intervention
Initial: 180 mcg/kg intravenous bolus administered immediately before the initiation of PCI followed by a continuous infusion of 2 mcg/kg/min and a second 180 mcg/kg bolus 10 minutes after the first bolus. Infusion should be continued until hospital discharge, or for up to 18 to 24 hours, whichever comes first. A minimum of 12 hours of infusion is recommended by the manufacturer. Alternatively, an infusion duration of 16 hours may be appropriate as noted in the ESPRIT substudy.
In patients who undergo coronary artery bypass graft surgery, eptifibatide infusion should be discontinued prior to surgery.
Renal Dose Adjustments
Acute Coronary Syndrome
CrCl less than 50 mL/min (or serum creatinine greater than 2.0 mg/dL if creatinine clearance is not available): 180 mcg/kg intravenous bolus as soon as possible following diagnosis, immediately followed by a continuous infusion of 1 mcg/kg/min.
Percutaneous Coronary Intervention (PCI)
CrCl less than 50 mL/min (or serum creatinine greater than 2.0 mg/dL if creatinine clearance is not available): 180 mcg/kg intravenous bolus administered immediately before the initiation of the procedure, immediately followed by a continuous infusion of 1 mcg/kg/min and a second 180 mcg/kg bolus administered 10 minutes after the first.
Liver Dose Adjustments
Data not available
Precautions
Eptifibatide is contraindicated in patients with a history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days, those with severe hypertension (systolic blood pressure greater than 200 mm Hg or diastolic blood pressure greater than 110 mm Hg) not adequately controlled on antihypertensive therapy, any patient having major surgery within the preceding 6 weeks, a history of stroke within 30 days or any history of hemorrhagic stroke, current or planned administration of another parenteral GP IIb/IIIa inhibitor, or in those with dependency on renal dialysis.
Risk factors for bleeding events in patients treated with glycoprotein (GP) IIb/IIIa inhibitors undergoing percutaneous coronary intervention have been identified and include advanced age, renal dysfunction, female gender, peripheral vascular disease, lower body weight, duration of GP IIb/IIIa infusion, baseline platelet count, lower baseline hemoglobin, diabetes, and elevated peak activated clotting time. According to one study (CRUSADE trial) involving patients with non ST segment elevation acute coronary syndrome treated with a GP IIb/IIIa inhibitor, women are at a greater risk of bleeding than men, primarily because of excessive dosing.
Safety and effectiveness have not been established in pediatric patients (less than 18 years of age).
Dialysis
Although there has been no clinical experience on the use of eptifibatide in patients on dialysis, in vitro studies suggest it is not extensively bound to plasma proteins and thus may be cleared from plasma by dialysis. Use of eptifibatide is considered contraindicated in patients who are dependent on renal dialysis.
Other Comments
In clinical trials, most patients received concomitant therapy with aspirin and heparin. The following are recommended dosages for aspirin and heparin in the treatment of ACS and PCI:
Acute Coronary Syndrome
Aspirin:
160 to 325 mg orally initially and daily thereafter
Heparin:
The target aPTT is 50 to 70 seconds during medical management.
If weight is greater than or equal to 70 kg, 5000 unit bolus is given followed by infusion of 1000 units/hr.
If weight is less than 70 kg, 60 units/kg bolus is given followed by infusion of 12 units/kg/hr.
The target ACT is 200 to 300 seconds during PCI.
If heparin is initiated prior to PCI, additional boluses during PCI to maintain an ACT target of 200 to 300 seconds may be given. Heparin infusion after the PCI is discouraged.
PCI
Aspirin:
160 to 325 mg orally 1 to 24 hours prior to PCI and daily thereafter
Heparin:
The target ACT is 200 to 300 seconds.
A 60 units/kg bolus is given initially in patients not treated with heparin within 6 hours prior to PCI. Additional boluses during PCI may be given to maintain ACT within target. Heparin infusion after the PCI is strongly discouraged.
Patients requiring thrombolytic therapy should have eptifibatide infusions stopped.
It has been suggested that in patients receiving any GP IIb/IIIa inhibitor, platelet counts should be monitored 2 to 4 hours after administration and at 24 hours or before discharge.
According to the results of one study (ICE trial), in patients undergoing percutaneous coronary intervention (i.e., coronary stent implantation), two intracoronary boluses of eptifibatide only (180 mcg/kg) may be safer (lower risk of bleeding) and produce better clinical outcomes (less rehospitalization, lower risk of death or MI) than two intravenous boluses and the continuous infusion may not be necessary. Additional studies are required to confirm these findings.