Antiplatelet · GP IIb/IIIa inhibitor

Eptifibatide (Integrilin)

Also called Integrilin

Reviewed by Alex G, BSN, RN, CEN, CCRN, CMC, NREMT-P · From the Reference tab of the app

Indications

Unstable angina or NSTEMI, managed medically or heading to PCI, with aspirin and heparin (label)
PCI, including stenting, started just before the procedure (label)
Bailout during PCI for large thrombus, no-reflow or slow flow, now its main use (ACC/AHA 2025)
Bridging a recent stent when oral P2Y12 inhibitors stop before surgery (off-label)

Dosing

Eptifibatide drip card and mL/h converterStart: 180 mcg/kg IV bolus from the 2 mg/mL vial, then 2 mcg/kg/min; PCI adds a second 180 mcg/kg bolus 10 minutes after the first. CrCl under 50 mL/min (Cockcroft-Gault): same bolus, then 1 mcg/kg/min

Mechanism of action

Eptifibatide is a cyclic heptapeptide that reversibly blocks glycoprotein IIb/IIIa (integrin αIIbβ3), the receptor activated platelets use to bind fibrinogen and von Willebrand factor and link to each other. Its homoarginine–glycine–aspartate sequence mimics the KGD motif of barbourin, a snake venom disintegrin, which makes it selective for αIIbβ3. Blocking this final common pathway stops aggregation whatever the trigger, and because the drug dissociates quickly, platelet function returns within hours of stopping.

Pharmacology

Hematologic: inhibits more than 80% of platelet aggregation within 15 min of the bolus; 4 h after stopping, inhibition is under 50% (label)
Hematologic: prolongs bleeding time; PT and aPTT change little, so the aPTT and ACT mostly track the heparin given with it
Cardiovascular: no direct effect on heart rate or contractility; hypotension usually means bleeding
Immune: drug-dependent antibodies can cause acute profound thrombocytopenia within hours (label)

Pharmacokinetics

Onset	Platelet inhibition within 15 min of the bolus (label)
Steady state	4–6 h without the second bolus, which fills the early dip in levels (label)
Duration	Platelet function recovers over about 4–8 h after stopping
Half-life	About 2.5 h (label)
Protein binding	About 25% (label)
Metabolism	Limited: deaminated and more polar metabolites in urine, none major in plasma (label)
Clearance	About 55 mL/kg/h in coronary disease, half of it renal (label)
Organ failure	CrCl under 50 mL/min: infusion halved; contraindicated on dialysis, though dialysis can clear it in overdose (label)

Chemistry

Cyclic heptapeptide of six amino acids and a mercaptopropionyl residue joined by a disulfide bridge; C₃₅H₄₉N₁₁O₉S₂, MW 832 (label)
Modeled on barbourin from southeastern pygmy rattlesnake venom, with homoarginine in place of its lysine
Water-soluble: 2 mg/mL bolus vials and 0.75 or 2 mg/mL infusion vials (or a 75 mg/100 mL bag) with citric acid, pH 5.35; refrigerate, or keep up to 2 months at room temperature (label)

Adverse effects and cautions

Safety

Bleeding: major bleeding 10.8% vs 9.3% with placebo in PURSUIT and 1.3% vs 0.4% in ESPRIT (label), mostly at the femoral site or in the GI and GU tracts
Contraindicated with bleeding or stroke in the past 30 days, any hemorrhagic stroke, SBP over 200 or DBP over 110, major surgery within 6 weeks, another GP IIb/IIIa inhibitor or dialysis (label)
Thrombocytopenia in 1.2% vs 0.6% with placebo (ESPRIT): stop eptifibatide and heparin if platelets fall below 100,000 (label)
Pull the sheath only after heparin has been off 3–4 h and the aPTT is under 45 s or ACT under 150 s (label)
Bleeding adds up with heparin, thrombolytics, P2Y12 inhibitors and anticoagulants
No antidote: function returns within hours of stopping; transfused platelets may help less than after abciximab because free drug binds them

In the one-pagers

ACS and STEMIAntiplatelet and anticoagulant choices: Eptifibatide, tirofiban: Weight-based IV infusion: Minutes; 4–8 h: Bailout for thrombus; watch platelets

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Sources

FDA label: Eptifibatide (Mylan, 2021)
FDA label: Eptifibatide in Galaxy container (Baxter, 2024)
PURSUIT 1998 and ESPRIT 2000 trials
ACC/AHA ACS guideline (2025)

For education and exam preparation only. Follow your institution’s protocols. Typical adult values for study. Follow your local protocols and medical direction.