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Eptifibatide

Pronunciation: EP-ti-FIB-a-tide
Class: Glycoprotein IIb/IIIa inhibitor

Trade Names

Integrilin
- Injection, solution 0.75 mg/mL
- Injection, solution 2 mg/mL

Pharmacology

Reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands to glycoprotein IIb/IIIa.

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Pharmacokinetics

Distribution

Approximately 25% is protein bound.

Elimination

The plasma elimination half-life is approximately 2.5 h. The majority is excreted in the urine as eptifibatide and metabolites. Cl is 55 mL/kg/h. Renal Cl is approximately 50% of the total body Cl.

Special Populations

Renal Function Impairment

Cl reduced approximately 50% and steady-state plasma levels are approximately doubled in patients with moderate to severe renal function impairment (CrCl less than 50 mL/min).

Hepatic Function Impairment

No studies have been conducted.

Elderly

Higher plasma levels and lower total body Cl.

Gender

Males and females have not demonstrated any clinically significant differences.

Indications and Usage

Treatment of acute coronary syndrome (unstable angina/non–ST-segment elevation MI), including patients managed medically and those undergoing percutaneous coronary intervention (PCI); treatment of PCI, including patients undergoing intracoronary stenting.

Contraindications

History of bleeding diathesis; evidence of active abnormal bleeding within the previous 30 days; severe hypertension (systolic BP greater than 200 mm Hg or diastolic BP greater than 110 mm Hg); major surgery within the preceding 6 wk; history of stroke within 30 days; history of hemorrhagic stroke; current or planned administration of another parenteral glycoprotein IIb/IIIa inhibitor; dependence on renal dialysis; hypersensitivity to any component of the product.

Dosage and Administration

Acute Coronary Syndrome
Adults

IV bolus 180 mcg/kg as soon as possible after diagnosis followed immediately by continuous infusion of 2 mcg/kg/min until hospital discharge or initiation of coronary artery bypass graft (CABG) surgery, up to 72 h. If patient is to undergo PCI while receiving eptifibatide, continue infusion up to discharge, or up to 18 to 24 h after procedure, whichever occurs first, allowing for up to 96 h of therapy.

PCI
Adults

IV bolus 180 mcg/kg as IV bolus administered immediately before initiation of PCI followed immediately by continuous infusion of 2 mcg/kg/min and a second 180 mcg/kg bolus 10 min after first bolus. Continue infusion until hospital discharge, or for up to 18 to 24 h, whichever comes first. A minimum of 12 h of infusion is recommended.

Renal function impairment
CrCl less than 50 mL/min Acute coronary syndrome Adults

IV bolus 180 mcg/kg as soon as possible after diagnosis, followed by continuous infusion of 1 mcg/kg/min.

PCI Adults

IV bolus 180 mcg/kg administered immediately before initiation of PCI, followed immediately by continuous infusion of 1 mcg/kg/min and a second 180 mcg/kg bolus 10 min after the first bolus.

General Advice

  • For IV administration only.
  • Do not administer if particulate matter or discoloration is noted.
  • Withdraw bolus dose(s) from 10 mL vial into a syringe and administer by IV push.
  • Administer continuous infusion undiluted directly from 100 mL vial via IV infusion pump using vented infusion set.
  • Discard any unused portion left in vial.
  • May be administered through the same IV line with sodium chloride 0.9% or sodium chloride 0.9% with dextrose 5%. The infusion may also contain up to 60 mEq/L of potassium chloride.
  • May be administered in the same IV line with alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil.
  • Do not administer through the same IV line as furosemide.
  • Administer appropriate doses of aspirin and heparin if indicated.
  • Discontinue eptifibatide infusion in patients requiring thrombolytic therapy.
  • May also be dosed by weight.

Storage/Stability

Store vials in the refrigerator (36° to 46°F). May be transferred for storage at room temperature (59° to 86°F) for up to 2 mo. Protect from light until administration.

Drug Interactions

Antiplatelet agents (eg, clopidogrel, ticlopidine), aspirin, dipyridamole, heparin, NSAIDs, oral anticoagulants (eg, warfarin), thrombolytics (eg, alteplase, streptokinase, urokinase)

Use with caution because risk of bleeding may be increased.

Direct thrombin inhibitors (eg, dabigatran, desirudin), other glycoprotein IIb/IIIa inhibitors (eg, abciximab, tirofiban), selective factor Xa inhibitors (eg, rivaroxaban)

Avoid coadministration because of additive pharmacologic effects with eptifibatide. Coadministration is not recommended.

Adverse Reactions

Cardiovascular

Hypotension (7%).

Hematologic-Lymphatic

Thrombocytopenia (1%); acute profound thrombocytopenia; cerebral, GI, and pulmonary hemorrhage; fatal bleeding events; immune mediated thrombocytopenia (postmarketing).

Local

Minor bleeding (14%); bleeding requiring transfusion (13%); overall incidence of major bleeding (11%); major bleeding at femoral access site (3%).

Precautions

Monitor

Obtain Hct or Hgb, platelet count, serum creatinine, and PT/APTT before starting therapy and periodically during treatment. Also obtain activated clotting time (ACT) in patients undergoing PCI. Closely monitor patients for unusual bleeding or unusual bruising, especially at vascular access sites.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in pediatric patients.

Renal Function

Reduce dose in patients with moderate to severe renal function impairment (CrCl less than 50 mL/min).

Activated partial thromboplastin time/Activated clotting time

Maintain APTT between 50 and 70 sec in patients being treated concurrently with heparin unless a PCI is to be performed. Maintain ACT between 200 and 300 sec during PCI.

Bleeding

Bleeding is the most common complication of therapy. Take special care to minimize risk of bleeding; if bleeding occurs and cannot be controlled with pressure or other means, immediately discontinue eptifibatide infusion and concomitant heparin.

Coronary artery bypass graft surgery

Discontinue infusion prior to CABG surgery.

Platelet count

Discontinue eptifibatide and heparin in patients whose platelet count decreases to less than 100,000/mm 3 .

Sheath removal

Do not remove arterial sheath unless APTT is less than 45 sec or the ACT is less than 150 sec.

Thrombocytopenia

Discontinue eptifibatide and heparin in patients whose platelet count decreases to less than 100,000/mm 3 .

Trauma

Minimize use of arterial or venous punctures, IM injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes. Avoid noncompressible sites (eg, subclavian or jugular veins) when obtaining necessary IV access.

Overdosage

Symptoms

None reported because of limited data.

Patient Information

  • Advise patients, families, or caregivers that medication will be prepared and administered by health care providers in an intensive care setting.
  • Advise patients, families, or caregivers that medication may be used in combination with other agents, including aspirin and heparin, to achieve the maximum benefit possible.
  • Advise patients, families, or caregivers to report any bleeding or unusual bruising to their health care provider while medication is being administered.

Copyright © 2009 Wolters Kluwer Health.

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