BLACK BOX WARNING
- serious bleeding risk
eptifibatide
Brand: Integrilin
⚠ BBW ISMP High Alert Prototype: abciximab
Drug Class: glycoprotein IIb/IIIa inhibitor
Drug Family: antiplatelet
Subclass: cyclic heptapeptide GP IIb/IIIa inhibitor
Organ Systems: cardiovascularhematology-oncology
Mechanism of Action
Cyclic heptapeptide derived from the disintegrin barbourin; competitively inhibits fibrinogen binding to GP IIb/IIIa receptors via an RGD-mimetic sequence, blocking platelet aggregation; reversible binding allows platelet function recovery within 2-4 hours of discontinuation.
glycoprotein IIb/IIIa receptor (integrin alphaIIb-beta3)
Indications
- acute coronary syndromes (NSTEMI/unstable angina) managed medically or with PCI
- adjunct to PCI (elective or urgent)
Contraindications
- history of stroke within 30 days or any hemorrhagic stroke
- severe hypertension (SBP >200 mmHg or DBP >110 mmHg)
- major surgery or severe trauma within 6 weeks
- current or planned parenteral GP IIb/IIIa inhibitor
- thrombocytopenia <100,000 cells/mcL
- renal dialysis
Adverse Effects
Common
- bleeding (access site, GI)
- thrombocytopenia
- hypotension
Serious
- major hemorrhage
- intracranial hemorrhage
- severe thrombocytopenia
Pharmacokinetics (ADME)
| Absorption | IV administration only |
| Distribution | Vd approximately 185-260 mL/kg; minimal protein binding |
| Metabolism | minimal hepatic metabolism; primarily excreted unchanged |
| Excretion | renal (approximately 50% unchanged); dose reduction required when CrCl <50 mL/min |
| Half-life | approximately 2.5 hours |
| Onset | within minutes of bolus |
| Peak | end of initial bolus |
| Duration | platelet function recovers within 2-4 hours of stopping infusion |
| Protein Binding | approximately 25% |
| Vd | 185-260 mL/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| heparin and other anticoagulants | additive anticoagulant/antiplatelet effect increases bleeding risk | major |
| other GP IIb/IIIa inhibitors | additive receptor blockade; concurrent use not recommended | major |
| thrombolytics | markedly increased hemorrhagic risk | major |
Nursing Considerations
- Dose must be reduced to 1 mcg/kg/min infusion (from 2 mcg/kg/min) when CrCl is less than 50 mL/min; always verify renal function and confirm correct infusion rate per renal function.
- Monitor platelet count at baseline, 6 hours after initiation, and daily; if platelets fall below 100,000, discontinue eptifibatide and heparin and notify physician.
- Platelet function recovers within 2-4 hours of discontinuation (compared with 24-48 hours for abciximab) — this faster reversal makes eptifibatide preferable when urgent surgical intervention may be needed.
- Minimize vascular access sites; compress femoral artery access sites for 30 minutes after sheath removal; maintain patient supine as per institutional PCI post-procedure protocol.
Clinical Pearls
- Eptifibatide's reversible, competitive binding means that in the event of life-threatening bleeding, discontinuing the infusion will restore platelet function within 2-4 hours without the need for platelet transfusion in most cases.
- Renal dosing adjustments are critical; CrCl-based dose modification (infusion rate reduction, not bolus change) prevents drug accumulation and excess bleeding in patients with renal impairment — a common oversight in clinical settings.
Safety Profile
Pregnancy generally-safe
Lactation insufficient-data
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.