EPTIFIBATIDE
Clinical safety rating: safe
Animal studies have demonstrated safety
Competitive antagonist of the glycoprotein IIb/IIIa receptor on platelets, preventing fibrinogen and von Willebrand factor binding and thereby inhibiting platelet aggregation.
| Metabolism | Primarily eliminated renally (approximately 50% excreted unchanged in urine). Not significantly metabolized by cytochrome P450 enzymes; undergoes some proteolysis. |
| Excretion | Renal excretion accounts for approximately 50% of total clearance, with about 30% excreted unchanged in urine. The remainder is metabolized and eliminated via biliary/fecal routes (~50%). |
| Half-life | Terminal elimination half-life is approximately 2.5 hours. In patients with moderate to severe renal impairment (CrCl <50 mL/min), half-life is prolonged to about 4.2 hours, necessitating dose adjustment. |
| Protein binding | Approximately 25% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is about 0.2 L/kg, indicating limited extravascular distribution, consistent with its peptide nature and low lipophilicity. |
| Bioavailability | Only administered intravenously; bioavailability is 100% for the IV route. |
| Onset of Action | Intravenous bolus: Onset of platelet inhibition occurs within minutes, with maximal effect achieved within 15 minutes. |
| Duration of Action | Platelet function returns to near baseline within 4-8 hours after discontinuation of infusion. The infusion is typically continued for 18-24 hours after PCI or until hospital discharge, up to 72 hours. |
Intravenous bolus of 180 mcg/kg followed by continuous infusion of 2 mcg/kg/min for up to 18 hours. For patients undergoing PCI, an additional 180 mcg/kg bolus 10 minutes after the first bolus is given.
| Dosage form | INJECTABLE |
| Renal impairment | If CrCl <50 mL/min: reduce infusion to 1 mcg/kg/min. No dose adjustment for bolus. Contraindicated if CrCl <10 mL/min or on dialysis. |
| Liver impairment | No specific dose adjustment for hepatic impairment. Use with caution in severe hepatic disease due to increased bleeding risk. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no approved dosing. |
| Geriatric use | Elderly patients have increased risk of bleeding; monitor renal function closely. No specific dose adjustment, but CrCl should be assessed and renal adjustment applied if CrCl <50 mL/min. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that affect hemostasis increase bleeding risk Can cause serious bleeding and thrombocytopenia.
| Breastfeeding | It is not known whether eptifibatide is excreted in human milk. However, eptifibatide is a protein and likely present in milk only in trace amounts. Due to low oral bioavailability, absorption by the infant is minimal. Caution is advised; the M/P ratio is not established. |
| Teratogenic Risk | Pregnancy Category B. Animal studies at doses up to 0.7 mg/kg/day IV (0.2 times the maximum human daily dose on a mg/m² basis) revealed no evidence of fetal harm. However, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, use only if clearly needed. Eptifibatide is a glycoprotein IIb/IIIa inhibitor; bleeding risk during labor/delivery must be considered. |
■ FDA Black Box Warning
Bleeding: Eptifibatide increases the risk of bleeding, including major bleeding (e.g., intracranial hemorrhage, retroperitoneal bleeding, and bleeding requiring transfusion). Risk is increased with invasive procedures, concomitant use of anticoagulants, thrombolytics, or NSAIDs, and in patients with renal insufficiency.
| Common Effects | Bleeding |
| Serious Effects |
["Active internal bleeding or recent bleeding (within 30 days) such as GI or GU bleeding","History of hemorrhagic stroke or intracranial hemorrhage at any time","Major surgery or severe trauma within the prior 6 weeks","Intracranial neoplasm, arteriovenous malformation, or aneurysm","History of thrombocytopenia with prior eptifibatide therapy","Severe renal impairment (creatinine clearance <10 mL/min) or dialysis dependence","Hypersensitivity to eptifibatide or any component"]
| Precautions | ["Bleeding: Monitor for bleeding, especially at arterial puncture sites. Use with caution in patients with active bleeding or recent surgery/trauma.","Thrombocytopenia: May cause acute profound thrombocytopenia; monitor platelet counts within 6 hours after start and daily thereafter.","Renal impairment: Dose adjustment required for creatinine clearance <50 mL/min; contraindicated in severe renal impairment (CrCl <10 mL/min) or dialysis.","Concomitant therapy: Increased bleeding risk with anticoagulants, thrombolytics, or antiplatelet agents; use with caution."] |
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| Fetal Monitoring | Monitor for signs of bleeding, including unexplained decreases in hemoglobin/hematocrit, hematuria, gastrointestinal bleeding, or intracranial hemorrhage. Assess platelet count within 6 hours of loading dose and daily during infusion. Monitor activated clotting time (ACT) or activated partial thromboplastin time (aPTT) during concurrent heparin use. Fetal heart rate monitoring during labor. |
| Fertility Effects | No human data on fertility effects. In animal studies, no impairment of fertility was observed in male and female rats at doses up to 0.7 mg/kg/day IV (0.2 times the clinical dose on a mg/m² basis). |