eptifibatide (Integrilin)
Classes: Antiplatelet Agents, Cardiovascular; Glycoprotein IIb/IIIa Inhibitors
Dosing and uses of Integrilin (eptifibatide)
Adult dosage forms and strengths
injection solution
- 2mg/mL
- 0.75mg
Acute Coronary Syndromes
180 mcg/kg IV bolus over 1-2 min, THEn
2 mcg/kg/min IV for up to 72 hr
Percutaneous Coronary Intervention
180 mcg/kg IV, THEn
Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one
Continue infusion for at least 12 hours
Renal Impairment
(CrCl <50 mL/min)
ACS: 180 mcg/kg IV, THEN continuous infusion 1 mcg/kg/min
PCI: 180 mcg/kg IV, THEN continuous infusion 1 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one
Hemodialysis: Safety and using during hemodialysis not established
Pediatric dosage forms and strengths
Safety & efficacy not established
Geriatric dosage forms and strengths
In clinical trials, incidence of bleeding complications was higher in the elderly in both placebo and eptifibatide groups, and the incremental risk of eptifibatide-associated bleeding was greater in the older patients. Adjust dose to renal function
Acute Coronary Syndromes
180 mcg/kg IV bolus over 1-2 min, THEn
2 mcg/kg/min IV for up to 72 hr
Percutaneous Coronary Intervention
180 mcg/kg IV, THEn
Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one
Continue infusion for at least 12 hours
Integrilin (eptifibatide) adverse (side) effects
1-10%
Bleeding (8%)
Hypotension (7%)
Thrombocytopenia (2.3%)
Injection site reaction
<1%
Hypersensitivity
Intracranial hemorrhage
Pulmonary hemorrhage
Thrombocytopenia
GI hemorrhage
Postmarketing Reports
Immune-mediated thrombocytopenia (thought to be caused by antibodies that react with GP IIb/IIIa complex)
Warnings
Contraindications
Hypersensitivity
History of internal bleeding, intracranial hemorrhage or neoplasm, CVA, thrombocytopenia
AV malformation or aneurysm, aortic dissection, severe HTN, acute pericarditis
Other parenteral glycoprotein IIb/IIIa inhibitors
Cautions
Bleeding at the site of arterial sheath placement is the most common complication
Early sheath removal is encouraged while eptifibatide is being infused; prior to removing the sheath, it is recommended that heparin be discontinued for 3-4 hr and an aPTT of <45 seconds or ACT <150 seconds be achieved
Thrombocytopenia: Discontinue if platelet levels <100,000 mm/cu.mm
Pregnancy and lactation
Pregnancy category: B
Lactation: excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Integrilin (eptifibatide)
Mechanism of action
Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface
Pharmacokinetics
Half-life, elimination: 2.5 hr
Onset: 1 hr
Duration: 4 hr
Protein bound: 25%
Vd: 185-260 mL/kg
Metabolites: Deaminated eptifibatide, other more polar metabolites detected in urine, no metabolites detected in plasma
Clearance: 55-58 mL/kg/hr
Excretion: Urine
Administration
IV Incompatibilities
Y-site, additive, syringe: furosemide
IV Compatibilities
Y-site: alteplase, amiodarone, atropine, bivalirudin, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine sulfate, nitroglycerin, verapamiL
IV Preparation
Bolus injection: withdraw from 10 mL vial (2 mg/mL; 10, 100 mL)
Infusion: no prep needed; spike 100 ml vial with vented infusion set (0.75 mg/mL; 100 mL)
IV Administration
Bolus: administer undiluted over 1-2 min
