Eptifibatide

Summary

Eptifibatide is a synthetic cyclic heptapeptide antiplatelet agent that inhibits the platelet glycoprotein IIb/IIIa receptor. It is used to reduce the risk of acute cardiac ischemic events in patients with acute coronary syndrome (ACS) or undergoing percutaneous coronary intervention (PCI).

Mechanism of Action

Reversibly binds to the glycoprotein IIb/IIIa receptor on platelet surfaces, blocking fibrinogen, von Willebrand factor, and other ligands from binding, thereby inhibiting platelet aggregation.

Routes of Administration

Goals & Uses

• Prevention of abrupt vessel closure post-PCICardiovascular / Thrombosis PreventionHigh
• Percutaneous Coronary Intervention (PCI) adjunctCardiovascular / AntiplateletHigh
• Acute Coronary Syndrome (ACS) managementCardiovascular / AntiplateletHigh

Contraindications

• Thrombocytopenia (platelet count <100,000/mm³)HematologicalHigh
• Major surgery or trauma within 6 weeksSurgicalHigh
• Severe renal impairment (creatinine ≥4 mg/dL or dialysis dependency)RenalHigh
• History of stroke within 30 days or hemorrhagic stroke at any timeNeurologicalHigh
• Active internal bleeding or bleeding diathesis within 30 daysBleeding RiskHigh
• Severe hypertension (uncontrolled, systolic >200 mmHg or diastolic >110 mmHg)CardiovascularHigh

Adverse Effects

• ThrombocytopeniaHematologicUncommonLow platelet count
• HypotensionCardiovascularUncommonLow blood pressure
• Allergic/hypersensitivity reactionsImmunologicalRare
• Bleeding (minor and major)HemorrhagicCommon

Drug Interactions

• Heparin / Low-molecular-weight heparinsModerate
• Thienopyridines (clopidogrel, ticagrelor)Moderate
• Aspirin / NSAIDsModerate
• Other GPIIb/IIIa inhibitors (abciximab, tirofiban)High
• Warfarin / oral anticoagulantsHigh

Population Constraints

• PregnancyReproductive SafetyRelative
• Renal impairment (moderate: CrCl <50 mL/min)RenalRelative
• Low body weight patients (<60 kg)AnthropometricRelative
• Pediatric patientsAgeRelative
• Elderly patients (≥75 years)AgeRelative

Regulatory Status

• European UnionApprovedApproved: Prevention of early myocardial infarction in patients presenting with NSTEMI-ACS, Adjunct to PCIApproved by EMA. Available in EU member states; regulatory review conducted by EMA.
• United StatesApprovedApproved: Acute coronary syndrome (unstable angina/NSTEMI) managed medically or with PCI, Percutaneous coronary intervention (PCI) to reduce ischemic complicationsFDA-approved in 1998. Marketed as Integrilin by Millennium Pharmaceuticals/Schering-Plough. Generic versions available.
• United KingdomApprovedApproved: Acute coronary syndrome, Percutaneous coronary interventionApproved by MHRA. Remains available in the UK post-Brexit under MHRA oversight.

FDA-approved since 1998. Marketed as Integrilin. Used in hospital settings under medical supervision. Generic versions are available.

Evidence & Sources

No sources recorded yet.