Eptifibatide
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From MedlinePlus, U.S. National Library of Medicine
Platelet Aggregation Inhibitor
Dosing in kidney impairment
Renal Impairment Approximately 50% of eptifibatide is cleared by the kidney in patients with normal renal function. Total drug clearance is decreased by approximately 50% and steady-state plasma eptifibatide injection concentrations are doubled in patients with an estimated CrCl <50 mL/min (using the Cockcroft-Gault equation).
Therefore, the infusion dose should be reduced to 1 mcg/kg/min in such patients [see Dosage and Administration] . The safety and efficacy of eptifibatide injection in patients dependent on dialysis has not been established.
| Indication | Normal Renal Function | Creatinine Clearance less than 50 mL/min |
| Patients with ACS | 180 mcg/kg intravenous (IV) bolus as soon as possible after diagnosis, followed by continuous infusion of 2 mcg/kg/min | 180 mcg/kg IV bolus as soon as possible after diagnosis, followed by continuous infusion of 1 mcg/kg/min |
| Infusion should continue until hospital discharge or initiation of coronary artery bypass graft surgery (CABG), up to 72 hours.If a patient is to undergo PCI, the infusion should be continued until hospital discharge or for up to 18 to 24 hours after the procedure, whichever comes first, allowing for up to 96 hours of therapy.Aspirin, 160 to 325 mg, should be given daily. | ||
| Indication | Normal Renal Function | Creatinine Clearance less than 50 mL/min |
| Patients with PCI | 180 mcg/kg IV bolus immediately before PCI followed by continuous infusion of2 mcg/kg/min and a second bolus of 180 mcg/kg (given 10 minutes after the first bolus) | 180 mcg/kg IV bolus immediately before PCI followed by continuous infusion of1 mcg/kg/min and a second bolus of 180 mcg/kg (given 10 minutes after the first bolus) |
| Infusion should be continued until hospital discharge, or for up to 18 to 24 hours, whichever comes first. A minimum of 12 hours of infusion is recommended.In patients who undergo CABG surgery, eptifibatide infusion should be discontinued prior to surgery.Aspirin, 160 to 325 mg, should be given 1 to 24 hours prior to PCI and daily thereafter. | ||
| Patient Weight | 180 mcg/kg Bolus Volume | 2 mcg/kg/min Infusion Volume (CrCl greater than or equal to 50 mL/min) | 1 mcg/kg/min Infusion Volume (CrCl less than 50 mL/min) | |||
| (kg) | (lb) | (from 2 mg/mL vial) | (from2 mg/mL100 mL vial) | (from0.75 mg/mL 100 mL vial) | (from2 mg/mL100 mL vial) | (from0.75 mg/mL 100 mL vial) |
| 37-41 | 81-91 | 3.4 mL | 2 mL/h | 6 mL/h | 1 mL/h | 3 mL/h |
| 42-46 | 92-102 | 4 mL | 2.5 mL/h | 7 mL/h | 1.3 mL/h | 3.5 mL/h |
| 47-53 | 103-117 | 4.5 mL | 3 mL/h | 8 mL/h | 1.5 mL/h | 4 mL/h |
| 54-59 | 118-130 | 5 mL | 3.5 mL/h | 9 mL/h | 1.8 mL/h | 4.5 mL/h |
| 60-65 | 131-143 | 5.6 mL | 3.8 mL/h | 10 mL/h | 1.9 mL/h | 5 mL/h |
| 66-71 | 144-157 | 6.2 mL | 4 mL/h | 11 mL/h | 2 mL/h | 5.5 mL/h |
| 72-78 | 158-172 | 6.8 mL | 4.5 mL/h | 12 mL/h | 2.3 mL/h | 6 mL/h |
| 79-84 | 173-185 | 7.3 mL | 5 mL/h | 13 mL/h | 2.5 mL/h | 6.5 mL/h |
| 85-90 | 186-198 | 7.9 mL | 5.3 mL/h | 14 mL/h | 2.7 mL/h | 7 mL/h |
| 91-96 | 199-212 | 8.5 mL | 5.6 mL/h | 15 mL/h | 2.8 mL/h | 7.5 mL/h |
| 97-103 | 213-227 | 9 mL | 6 mL/h | 16 mL/h | 3.0 mL/h | 8 mL/h |
| 104-109 | 228-240 | 9.5 mL | 6.4 mL/h | 17 mL/h | 3.2 mL/h | 8.5 mL/h |
| 110-115 | 241-253 | 10.2 mL | 6.8 mL/h | 18 mL/h | 3.4 mL/h | 9 mL/h |
| 116-121 | 254-267 | 10.7 mL | 7 mL/h | 19 mL/h | 3.5 mL/h | 9.5 mL/h |
| >121 | >267 | 11.3 mL | 7.5 mL/h | 20 mL/h | 3.7 mL/h | 10 mL/h |
Preparation and administration
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Important Administration Instructions Inspect eptifibatide injection for particulate matter and discoloration prior to administration, whenever solution and container permit. May administer eptifibatide injection in the same intravenous line as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil.
Do not administer eptifibatide injection through the same intravenous line as furosemide. May administer eptifibatide injection in the same IV line with 0.9% NaCl or 0.9% NaCl/5% dextrose. With either vehicle, the infusion may also contain up to 60 mEq/L of potassium chloride. Withdraw the bolus dose(s) of eptifibatide injection from the 10 mL vial into a syringe.
Administer the bolus dose(s) by IV push. Immediately following the bolus dose administration, initiate a continuous infusion of eptifibatide injection. When using an intravenous infusion pump, administer eptifibatide injection undiluted directly from the 100-mL vial. Spike the 100 mL vial with a vented infusion set. Center the spike within the circle on the stopper top.
Discard any unused portion left in the vial. Administer eptifibatide injection by volume according to patient weight (see Table 1 ). [See table below.] 1.9 mL/h 5 mL/h 66-71 144-157 6.2 mL 4 mL/h 11 mL/h 2 mL/h 5.5 mL/h 72-78 158-172 6.8 mL 4.5 mL/h 12 mL/h 2.3 mL/h 6 mL/h 79-84 173-185 7.3 mL 5 mL/h 13 mL/h 2.5 mL/h 6.5 mL/h 85-90 186-198 7.9 mL 5.3 mL/h 14 mL/h 2.7 mL/h 7 mL/h 91-96 199-212 8.5 mL 5.6 mL/h 15 mL/h 2.8 mL/h 7.5 mL/h 97-103 213-227 9 mL 6 mL/h 16 mL/h 3.0 mL/h 8 mL/h 104-109 228-240 9.5 mL 6.4 mL/h 17 mL/h 3.2 mL/h 8.5 mL/h 110-115 241-253 10.2 mL 6.8 mL/h 18 mL/h 3.4 mL/h 9 mL/h 116-121 254-267 10.7 mL 7 mL/h 19 mL/h 3.5 mL/h 9.5 mL/h >121 >267 11.3 mL 7.5 mL/h 20 mL/h 3.7 mL/h 10 mL/h
Drug interactions
Check eptifibatide against a medication listLabel text (2 paragraphs)
Coadministration of antiplatelet agents, thrombolytics, heparin, aspirin, and chronic NSAID use increases the risk of bleeding. Avoid concomitant use with other glycoprotein (GP) IIb/IIIa inhibitors. ( 7.1 )
7.1 Use of Thrombolytics, Anticoagulants, and Other Antiplatelet Agents Coadministration of antiplatelet agents, thrombolytics, heparin, aspirin, and chronic NSAID use increases the risk of bleeding. Concomitant treatment with other inhibitors of platelet receptor GP IIb/IIIa should be avoided.
Contraindications
Treatment with eptifibatide injection is contraindicated in patients with: A history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days Severe hypertension (systolic blood pressure >200 mm Hg or diastolic blood pressure >110 mm Hg) not adequately controlled on antihypertensive therapy Major surgery within the preceding 6 weeks History of stroke within 30 days or any history of hemorrhagic stroke Current or planned administration of another parenteral GP IIb/IIIa inhibitor Dependency on renal dialysis Hypersensitivity to eptifibatide injection or any component of the product (hypersensitivity reactions that occurred included anaphylaxis and urticaria).
Bleeding diathesis or bleeding within the previous 30 days. ( 4 ) Severe uncontrolled hypertension. ( 4 ) Major surgery within the preceding 6 weeks. ( 4 ) Stroke within 30 days or any history of hemorrhagic stroke. ( 4 ) Coadministration of another parenteral GP IIb/IIIa inhibitor. ( 4 ) Dependency on renal dialysis. ( 4 ) Known hypersensitivity to any component of the product. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
LiverTox has no chapter for eptifibatide. Check the label's hepatic warnings.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary Available data on eptifibatide use in pregnant women from published literature and the pharmacovigilance database are insufficient to establish a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Untreated myocardial infarction can be fatal to the pregnant woman and fetus [see Clinical Considerations ] . In animal reproduction studies, there was no evidence of adverse developmental effects when eptifibatide was administered intravenously to pregnant rats and rabbits at approximately 4 times the recommended maximum daily human dose.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk: Myocardial infarction is a medical emergency in pregnancy which can be fatal to the pregnant woman and fetus if left untreated.
Therapy for the pregnant woman should not be withheld because of potential concerns regarding the effects of eptifibatide injection on the fetus. Data Animal Data: Embryo-fetal development studies have been performed by continuous intravenous infusion of eptifibatide in pregnant rats during the period of organogenesis at total daily doses of up to 72 mg/kg/day (about 4 times the recommended maximum daily human dose on a body surface area basis) and in pregnant rabbits during the period of organogenesis at total daily doses of up to 36 mg/kg/day (also about 4 times the recommended maximum daily human dose on a body surface area basis).
These studies revealed no evidence of harm to the fetus due to eptifibatide.
Breastfeeding (LactMed)
No published information is available on the use of eptifibatide during breastfeeding. Because eptifibatide is a peptide, absorption by the infant is unlikely because it is probably destroyed in the infant's gastrointestinal tract. Until more data become available, eptifibatide should be used with caution during breastfeeding, especially while nursing a newborn or preterm infant. If it is used by a nursing mother, monitor the infant for bruising and bleeding.
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