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Trade Names:
Integrilin
- Solution for Injection 0.75 mg/mL
- Solution for Injection 2 mg/mL

Mechanism of Action

Pharmacology

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

Pharmacokinetics

Distribution

Approximately 25% is protein bound.

Elimination

The t _½ is approximately 2.5 h. Majority 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

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

Higher plasma levels and lower total body Cl.

Indications and Usage

Treatment of acute coronary syndrome, 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 previous 30 days; severe hypertension (systolic BP greater than 200 mm Hg or diastolic BP greater than 110 mm Hg); major surgery within 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

Ccr 50 mL/min or greater: 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 96 h of therapy.

Ccr less than 50 mL/min: IV bolus 180 mcg/kg as soon as possible after diagnosis followed by continuous infusion of 1 mcg/kg/min.

Ccr 50 mL/min or greater: 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.

Ccr less than 50 mL/min: IV bolus 180 mcg/kg as IV bolus 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 first bolus.

General Advice

• For IV administration only. Not for intradermal, subcutaneous, IM, or intra-arterial administration.
• Do not administer if particulate matter or discoloration 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 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 same IV line with alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil.
• Do not administer through same IV line as furosemide.
• Administer appropriate doses of aspirin and heparin if indicated.
• Discontinue eptifibatide infusion in patients requiring thrombolytic therapy.

Storage/Stability

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

Drug Interactions

Use with caution because eptifibatide inhibits platelet aggregation.

Avoid because of additive pharmacologic effects with eptifibatide.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (at least 1%).

Hematologic-Lymphatic

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

Local

Overall incidence of major bleeding (11%); major bleeding at femoral access site (3%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

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

aPTT/ACT

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 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.

CABG surgery

Discontinue infusion prior to CABG surgery.

Platelet count

Discontinue eptifibatide and heparin in patient 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.

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, jugular veins) when obtaining necessary IV access.

Overdosage

Symptoms

None reported because of limited data.

Patient Information

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