INTEGRILIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INTEGRILIN (INTEGRILIN).
Reversible antagonist of the platelet glycoprotein IIb/IIIa receptor, inhibiting platelet aggregation by preventing fibrinogen binding.
| Metabolism | Minimal metabolism; primarily excreted unchanged in urine (approximately 50% as epitifibatide and metabolites). Not extensively metabolized by cytochrome P450. |
| Excretion | Renal: ~50% as unchanged drug and metabolites, Biliary/fecal: minimal; total clearance approximately 55-58% renal. |
| Half-life | Terminal elimination half-life: ~2.5 hours (2-3 hours) after intravenous administration; clinical context: rapid clearance allows return of platelet function within 4 hours after infusion cessation. |
| Protein binding | ~25% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Vd approximately 0.2-0.3 L/kg; indicates distribution mainly in extracellular fluid and blood. |
| Bioavailability | Only available intravenously; bioavailability is 100% by IV route. Not administered orally. |
| Onset of Action | Intravenous bolus: within 15 minutes (inhibition of platelet aggregation reaches peak at ~15 min). |
| Duration of Action | Platelet function returns to normal within 4 hours after stopping infusion; clinical effect lasts for the duration of infusion (bolus + continuous infusion). |
| Action Class | Glycoprotein IIb/IIIa inhibitors |
| Brand Substitutes | Eptide 0.75mg/ml Infusion, Eptiflo 0.75mg/ml Infusion, Eptibind 0.75mg/ml Infusion, Clotide 0.75mg/ml Infusion, Eptiba Infusion |
Acute coronary syndrome: IV bolus of 180 mcg/kg, followed by continuous IV infusion of 2 mcg/kg/min for up to 72 hours. Percutaneous coronary intervention: IV bolus of 180 mcg/kg immediately before PCI, followed by continuous IV infusion of 2 mcg/kg/min for up to 18-24 hours, with a second 180 mcg/kg bolus 10 minutes after the first.
| Dosage form | INJECTABLE |
| Renal impairment | For CrCl <50 mL/min: Reduce infusion rate to 1 mcg/kg/min. No bolus dose adjustment required. Use is contraindicated in patients on dialysis. |
| Liver impairment | No specific hepatic dose adjustments provided in manufacturer labeling; caution advised due to increased bleeding risk in severe hepatic impairment. No Child-Pugh based guidelines. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; no specific dosing recommendations. |
| Geriatric use | No specific dose adjustment based solely on age, but due to higher risk of bleeding, consider lower initial infusion rate (1 mcg/kg/min) in elderly patients, especially those with low body weight or renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for INTEGRILIN (INTEGRILIN).
| Breastfeeding | It is unknown whether eptifibatide is excreted in human milk. Due to the high molecular weight of the peptide, excretion is unlikely. Caution should be exercised when administered to a nursing woman. No M/P ratio is available. |
| Teratogenic Risk | Integrilin (eptifibatide) is a pregnancy category B drug. No adequate and well-controlled studies in pregnant women. In animal studies, no evidence of fetal harm was observed at doses up to 8 times the human exposure. However, because of the risk of maternal hemorrhage and potential for fetal bleeding, use only if clearly needed. Risks are theoretical and not well-defined per trimester. |
■ FDA Black Box Warning
Integrilin increases the risk of bleeding, including major bleeding and intracranial hemorrhage. It is contraindicated in patients with active bleeding or recent major bleeding, history of stroke within 30 days, major surgery or severe trauma within 6 weeks, bleeding diathesis, severe hypertension, or use of other GP IIb/IIIa inhibitors.
| Serious Effects |
Active bleeding or recent major bleeding (within 30 days), history of stroke within 30 days or any hemorrhagic stroke, major surgery or severe trauma within 6 weeks, bleeding diathesis (e.g., INR >2, platelet count <100,000/µL), severe hypertension (systolic >200 mmHg or diastolic >110 mmHg), concurrent use of another GP IIb/IIIa inhibitor, hypersensitivity to epitifibatide or any component.
| Precautions | Risk of bleeding, especially in patients with renal impairment (reduce dose if CrCl <50 mL/min); thrombocytopenia (monitor platelet counts); concomitant use with other anticoagulants increases bleeding risk; use caution in patients with recent bleeding or surgery. |
| Food/Dietary |
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| Fetal Monitoring | Monitor for signs of bleeding (e.g., hematoma, hemorrhage, hematuria). Monitor platelet count regularly during infusion. Assess for hypersensitivity reactions. Fetal monitoring should be considered if used near term due to risk of fetal hemorrhage. |
| Fertility Effects | No studies on fertility effects in humans. Animal studies with eptifibatide showed no impairment of fertility at doses up to 8 times the human dose. No specific data on reproductive function. |
| No specific food interactions. However, patients should avoid alcohol and grapefruit juice as they may affect bleeding risk |
| Clinical Pearls | Integrilin (eptifibatide) is a glycoprotein IIb/IIIa inhibitor used in acute coronary syndrome (ACS) and during percutaneous coronary intervention (PCI). It has a short half-life (2.5 hours) and renal clearance; dose adjustment is needed for creatinine clearance <50 mL/min. Contraindicated in severe hypertension (systolic >200 mmHg or diastolic >110 mmHg), recent major surgery, active bleeding, or history of intracranial hemorrhage. Abrupt discontinuation may increase thrombotic risk; maintain for 18-24 hours after PCI. |
| Patient Advice | This medication is given to prevent blood clots during a heart attack or stent procedure. · You will be closely monitored for bleeding, including at catheter sites, gums, and urine. · Report any unusual bruising, black or tarry stools, or blood in urine immediately. · Avoid aspirin or other NSAIDs unless prescribed by your doctor, as they increase bleeding risk. · Do not discontinue the infusion without your doctor's approval, as it may increase clot risk. |