MOA
PK & PD Properties
Efficacy
Efficacy Introduction
Risk Reduction Pre-PCI
Myocardial Perfusion
Long-term Risk Reduction Post-PCI
Dosing Administration
Dosing Guidelines & Cockcroft-Gault Equation
Ease of Administration
Bolus Delivery
Infusion Delivery
Dosing Compatibilities
Safety
Major Bleeding in PCI
Minor Bleeding in PCI
Bleeding Rates in PROTECT
Bleeding in Renally Impaired Patients
Clinical Studies Database
PURSUIT
ESPRIT
PROTECT
CLEAR PLATELETS
Clear Platelets Introduction
Platelet Aggregation Inhibition
Reduction of Troponin-I Release
Full Prescribing Information
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INTEGRILIN®: Pharmacokinetics & Pharmacodynamics

Pharmacokinetic and pharmacodynamic data for INTEGRILIN® were obtained in healthy subjects and in patients presenting with UA/NSTEMI and/or undergoing PCI in two pivotal studies, IMPACT II* and PURSUIT.† INTEGRILIN® was administered as a 180-mcg/kg IV bolus1:

  • INTEGRILIN® inhibits platelet aggregation, with specificity for the platelet receptor GP IIb-IIIa
  • Initial onset of inhibition of platelet aggregation was observed within 15 minutes after the IV bolus*†
  • INTEGRILIN® action is reversible: platelet function was restored toward baseline (<50% inhibition) within 4 hours of discontinuation of infusion
  • INTEGRILIN® and its metabolites are primarily renally excreted
  • Plasma elimination half-life of INTEGRILIN® is approximately 2.5 hours

Please see Full Prescribing Information for complete Pharmacokinetic and Pharmacodynamic properties.

 

* IMPACT II=INTEGRILIN® to Minimize Platelet Aggregation and Prevent Coronary Thrombosis II. In IMPACT II, INTEGRILIN® was administered as a 135-mcg/kg bolus, followed by a continuous infusion of 0.5 mcg/kg/min.
† PURSUIT=Platelet Glycoprotein IIb/IIIa in Unstable Angina: Receptor Suppression Using INTEGRILIN® Therapy. In PURSUIT, INTEGRILIN® was administered as a 180-mcg/kg bolus, followed by a continuous infusion of 2 mcg/kg/min.
 

IMPORTANT PRESCRIBING AND SAFETY CONSIDERATIONS

Indications for INTEGRILIN® (eptifibatide) Injection:
  • For the treatment of patients with acute coronary syndrome (UA/NSTEMI), including patients who are
    to be managed medically and those undergoing percutaneous coronary intervention (PCI)
  • For the treatment of patients undergoing percutaneous coronary intervention (PCI), including those
    undergoing intracoronary stenting
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 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
  • Known hypersensitivity to any component of the product
Precautions and Warnings:
  • In patients undergoing PCI, INTEGRILIN® (eptifibatide) Injection is associated with an increase in major and minor bleeding at the site of arterial sheath placement. Special care should be employed to minimize the risk of bleeding among these patients
  • If bleeding cannot be controlled with pressure, infusion of INTEGRILIN® and concomitant heparin should be stopped immediately
  • Because INTEGRILIN® inhibits platelet aggregation, caution should be employed when it is used with drugs that affect hemostasis, including thrombolytics, oral anticoagulants, NSAIDs, and dipyridamole
  • Use with other GP IIb-IIIa inhibitors should be avoided
  • INTEGRILIN® is cleared in part by the kidney and its plasma concentrations are doubled in patients with renal disease (creatinine clearance
    <50 mL/min). Therefore, the infusion dose of INTEGRILIN® needs to be reduced to 1 mcg/kg/min in these patients. INTEGRILIN® is contraindicated in patients who are dependent upon renal dialysis (please see dosing guidelines)
  • Caution should be exercised when administering eptifibatide to patients with a platelet count <100,000/mm3
  • Bleeding is the most common complication encountered during INTEGRILIN® therapy. The majority of excess major bleeding events were localized at the femoral artery access site. Oropharyngeal, genitourinary, gastrointestinal, and retroperitoneal bleeding were seen more commonly with INTEGRILIN® compared with placebo.

For full Prescribing Information, click here. (PDF)(1.04MB)

About Schering-Plough
Schering Corporation, of Kenilworth, NJ, is a research-based company engaged in the discovery, development, manufacturing, and marketing of pharmaceutical products worldwide. For more information, please visit the company's Web site at www.sch-plough.com.

Contact us at 1-800-222-7579

References:

  • INTEGRILIN® (eptifibatide) [prescribing information]. Kenilworth, NJ: Schering Corporation; 2005.

INTEGRILIN is a registered trademark of Millennium Pharmaceuticals, Inc.
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