Overview
Eptifibatide (Integrilin) is an FDA-approved cyclic heptapeptide antiplatelet agent derived from a disintegrin protein found in the venom of the southeastern pygmy rattlesnake. It is used intravenously in the management of acute coronary syndrome and as an adjunct to percutaneous coronary intervention (PCI) to reduce the risk of cardiac ischemic events.
Mechanism of action
Eptifibatide reversibly inhibits platelet aggregation by selectively blocking the glycoprotein IIb/IIIa (GPIIb/IIIa) receptor on the platelet surface. GPIIb/IIIa is the predominant receptor mediating platelet aggregation; it binds fibrinogen and von Willebrand factor, enabling platelets to cross-link and form a thrombus. Eptifibatide's RGD-mimetic KGD sequence occupies the fibrinogen-binding pocket of GPIIb/IIIa with high affinity, competitively displacing these ligands. Because inhibition is reversible, platelet function recovers within 4–8 hours of discontinuation as drug dissociates and plasma levels fall. The cyclic peptide structure confers selectivity over RGD-binding integrins on other cell types, reducing off-target effects compared to non-cyclic RGD peptides.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| acute coronary syndrome | intravenous | 180–180 mcg/kg | IV bolus, then 2 mcg/kg/min infusion for up to 72 hours | Initial 180 mcg/kg bolus followed by continuous infusion. Dose-adjust in renal impairment (CrCl <50 mL/min). Monitor for bleeding. |
| percutaneous coronary intervention adjunct | intravenous | 180–180 mcg/kg | Double bolus 10 min apart, then 2 mcg/kg/min infusion for 18–24 hours | Two 180 mcg/kg boluses 10 minutes apart at time of PCI per ESPRIT protocol. Maintain infusion through procedure and 18–24 hours post-PCI. |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
Eptifibatide received FDA approval in 1998 based on the PURSUIT and ESPRIT clinical trials. PURSUIT (10,948 patients) demonstrated a significant reduction in the composite endpoint of death or myocardial infarction at 30 days compared to placebo in ACS patients. ESPRIT confirmed benefit as a PCI adjunct. Post-approval research has evaluated eptifibatide in combination with thrombolytics and in specific high-risk PCI subgroups. Its short half-life and reversibility make it preferable to abciximab when rapid offset is desired.
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Legal status
FDA-approved since 1998 for ACS and PCI adjunct therapy. Available as an intravenous injection for hospital and procedural suite use only. Schedule: not a controlled substance. Requires medical supervision and cardiac monitoring during infusion.
Where to get it
Prescription required
Eptifibatide is a prescription medication. Consult your healthcare provider or a licensed telehealth platform for access.