eptifibatide (Rx)

1-10%

Bleeding (8%)

Hypotension (7%)

Thrombocytopenia (2.3%)

Injection site reaction

<1%

Hypersensitivity

Intracranial hemorrhage

Pulmonary hemorrhage

Thrombocytopenia

GI hemorrhage

Postmarketing Reports

Immune-mediated thrombocytopenia (thought to be caused by antibodies that react with GP IIb/IIIa complex)

Contraindications

Hypersensitivity

History of internal bleeding, intracranial hemorrhage or neoplasm, CVA, thrombocytopenia

AV malformation or aneurysm, aortic dissection, severe HTN, acute pericarditis

Other parenteral glycoprotein IIb/IIIa inhibitors

Cautions

Bleeding

• At the site of arterial sheath placement bleeding is the most common complication; minimize use of arterial and venous punctures, intramuscular injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes; when obtaining intravenous access, avoid non-compressible sites (eg, subclavian or jugular veins)
• Risk factors for bleeding include older age, a history of bleeding disorders, and concomitant use of drugs that increase risk of bleeding (thrombolytics, oral anticoagulants, nonsteroidal anti-inflammatory drugs, and P2Y12 inhibitors); concomitant treatment with other inhibitors of platelet receptor glycoprotein (GP) IIb/IIIa should be avoided; in patients treated with heparin, bleeding can be minimized by close monitoring of aPTT and ACT
• In patients undergoing PCI, treatment may increase in major and minor bleeding at site of arterial sheath placement; after PCI, infusion should be continued until hospital discharge or up to 18 - 24 hours, whichever comes first;
• Heparin use is discouraged after PCI procedure; early sheath removal is encouraged while drug is being infused; prior to removing the sheath, it is recommended that heparin be discontinued for 3 to 4 hours and an aPTT of <45 seconds or ACT <150 seconds be achieved; in any case, both drugs should be discontinued and sheath hemostasis achieved at least 2 to 4 hours before hospital discharge; if bleeding at access site cannot be controlled with pressure, infusion of both drugs should be discontinued immediately

Thrombocytopenia

• There have been reports of acute, profound thrombocytopenia (immune-mediated and non-immune mediated); in the event of acute profound thrombocytopenia or a confirmed platelet decrease to <100,000/mm³, discontinue drug and heparin (unfractionated or low-molecular weight); monitor serial platelet counts, assess presence of drug-dependent antibodies, and treat as appropriate
• There has been no clinical experience with therapy initiated in patients with a baseline platelet count <100,000/mm³; if a patient with low platelet counts is receiving drug, their platelet count should be monitored closely

Pregnancy Category: B

Lactation: excretion in milk unknown; use with caution

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface

Pharmacokinetics

Half-life, elimination: 2.5 hr

Onset: 1 hr

Duration: 4 hr

Protein bound: 25%

Vd: 185-260 mL/kg

Metabolites: Deaminated eptifibatide, other more polar metabolites detected in urine, no metabolites detected in plasma

Clearance: 55-58 mL/kg/hr

Excretion: Urine

IV Incompatibilities

Y-site, additive, syringe: furosemide

IV Compatibilities

Y-site: alteplase, amiodarone, atropine, bivalirudin, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine sulfate, nitroglycerin, verapamil

IV Preparation

Bolus injection: withdraw from 10 mL vial (2 mg/mL; 10, 100 mL)

Infusion: no prep needed; spike 100 ml vial with vented infusion set (0.75 mg/mL; 100 mL)

IV Administration

Inspect for particulate matter and discoloration prior to administration, whenever solution and container permit

May administer in the same intravenous line as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil

Do not administer through the same intravenous line as furosemide

May administer 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 bolus dose(s) from the 10-mL vial into a syringe; administer bolus dose(s) by IV push

Immediately following bolus dose administration, initiate a continuous infusion

When using an intravenous infusion pump, administer undiluted directly from 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