Integrilin (eptifibatide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Eptifibatide, a selective platelet-aggregation inhibitor, is a platelet glycoprotein (GP) IIb/IIIa-receptor inhibitor.
Eptifibatide is a selective, competitive, reversible inhibitor of platelet aggregation. Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand's factor, and other adhesive ligands to resting and active glycoprotein (GP) IIb/IIIa receptors.
Eptifibatide is composed of 6 amino acids and a mercaptopropionyl (desamino cysteinyl) residue with an interchain disulfide bridge between the cysteine amide and the mercaptopropionyl moieties. The active domain of eptifibatide contains a modified lysine-glycine-aspartate (KGD) amino acid sequence similar to the physiologic arginine-glycine-aspartate (RGD) sequence in von Willebrand's factor, vitronectin, fibrinogen, and fibronectin, adhesive ligands that bind to platelet GP IIb/IIIa receptors on activated platelets and cause platelet aggregation. The substitution of lysine for arginine on the binding site in eptifibatide increases the selectivity of binding to the GP IIb/IIIa receptor.
Inhibition of platelet aggregation by eptifibatide occurs in a dose- and concentration-dependent manner via an increase in GP IIb/IIIa-receptor occupancy (as determined by ex vivo platelet aggregation assay with the direct thrombin inhibitor d-phenylalanyl-l-propyl-l-arginyl chloromethyl ketone (PPACK)). Since the effect of eptifibatide on platelet aggregation is rapidly reversible following cessation of the infusion, the drug has a modest effect on hemostatic indices (e.g., bleeding times) and platelet function. The pharmacokinetics of eptifibatide are linear, and plasma concentrations are proportional to dose following IV loading doses of 90-250 mcg/kg and IV infusion rates of 0.5-3 mcg/kg per minute.
The plasma half-life of eptifibatide is around 2.5 hours. A single 180 mcg/kg bolus followed by an infusion produces an initial peak concentration, which then slightly decreases before reaching steady state within 4-6 hours; this small decline can be avoided by giving a second 180 mcg/kg bolus 10 minutes after the first. Approximately 25% of eptifibatide binds to human plasma proteins.
In healthy individuals, renal clearance accounts for roughly half of the total body clearance, with most of the drug excreted in urine as eptifibatide, deaminated eptifibatide, and other, more polar metabolites. No major metabolites have been detected in human plasma.
Generic name: eptifibatide
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Integrilin:
- Acute Coronary Syndrome
- Percutaneous Coronary Intervention Adjunct For Thrombosis Prevention
Dosing
No dosing information is available for this tab.
Eptifibatide is administered by IV bolus followed by IV infusion using a controlled-infusion device (e.g., IV infusion pump). For IV injection, the appropriate bolus dose of eptifibatide is withdrawn from the 10-mL vial containing the drug solution and administered undiluted IV push. The solution for continuous IV infusion should be administered directly from the 100-mL vial after spiking the vial with a vented infusion set. Care should be taken to center the spike within the circle on the stopper top. Any drug solution remaining after IV injection or infusion of the appropriate dose of eptifibatide should be discarded.
Eptifibatide may be delivered through the same IV line as compatible agents such as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil. Eptifibatide should not be co-administered in the same IV line as furosemide. Eptifibatide may be administered through the same IV line with 0.9% sodium chloride or 0.9% sodium chloride with 5% dextrose. Either solution may also contain up to 60 mEq/L of potassium chloride.
Store vials refrigerated at 2-8degreesC. Vials may be transferred to room temperature (20-25degreesC) for up to 2 months. Protect from light until administration.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Hypersensitivity to eptifibatide or any component of the product.
*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 glycoprotein IIb/IIIa inhibitor.
*Dependency on renal dialysis.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions reported are bleeding and hypotension.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and effectiveness in pediatric patients have not been established.
Available human data on eptifibatide use during pregnancy are insufficient to determine whether there is an associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal studies with rats and rabbits, no adverse effects on maternal health or fetal development were observed at exposures up to 4 times the maximum recommended human dose. Clinically, untreated myocardial infarction can be life-threatening for both the pregnant patient and the fetus.
There is no information on the presence of eptifibatide in human milk, its effects on a breast-fed infant, or its effects on milk production. Since eptifibatide is a peptide, it is likely to be destroyed in the infant's GI tract and not absorbed orally by the breast-fed infant.
The manufacturer makes no recommendations for dosage adjustment in geriatric patients.
In clinical trials of eptifibatide, patients ranged in age from 20--94 years, representing an older population than those enrolled in clinical pharmacology trials. Plasma concentrations of eptifibatide were higher and total body clearance was lower among geriatric patients with coronary artery disease compared to younger patients receiving the same dose.
In the PURSUIT and IMPACT II clinical trials, there were no overall differences in effectiveness observed between geriatric and younger patients. However, geriatric patients had a higher incidence of bleeding complications than younger patients in both the placebo and eptifibatide groups, and the incremental risk of eptifibatide-associated bleeding was greater among older patients. No dosage adjustment was made for geriatric patients in the principal clinical trials (PURSUIT, IMPACT II), but patients >75 years of age had to weigh >=50 kg to be enrolled in the PURSUIT study because of a concern for an increased risk of bleeding in those weighing less than 50 kg. Data are limited for patients >75 years of age who weigh <50 kg.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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