Eptifibatide

What is Eptifibatide?

• Eptifibatide (Integrilin) is a platelet aggregation inhibitor, use for treatment of acute coronary syndrome (ACS) managed medically or with percutaneous coronary intervention (PCI) and treatment of patients undergoing PCI (including intracoronary stenting).

Eptifibatide structure

Eptifibatide

Eptifibatide ball-and-stick

What are the uses of this medicine?

• Eptifibatide (Integrilin) is used for:
• Treatment of acute coronary syndrome (ACS) managed medically or with percutaneous coronary intervention (PCI).
• Treatment of patients undergoing PCI (including intracoronary stenting).
• Eptifibatide is a cyclic heptapeptide derived from a disintegrin protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri).

How does this medicine work?

• Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands to GP IIb/IIIa.
• When administered intravenously, eptifibatide inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner.
• Platelet aggregation inhibition is reversible following cessation of the eptifibatide infusion; this is thought to result from dissociation of eptifibatide from the platelet.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Bleeding diathesis or bleeding within the previous 30 days
• Severe uncontrolled hypertension
• Major surgery within the preceding 6 weeks
• Stroke within 30 days or any history of hemorrhagic stroke
• Coadministration of another parenteral GP IIb/IIIa inhibitor
• Dependency on renal dialysis
• Known hypersensitivity to any component of the product

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antiplatelet agents, thrombolytics, heparin, aspirin, and chronic NSAID

• Concomitant treatment with other inhibitors of platelet receptor GP IIb/IIIa should be avoided.

Is this medicine FDA approved?

• Initial U.S. Approval: 1998

How should this medicine be used?

Recommended dosage:

Dosing in Acute Coronary Syndrome (ACS):

• 180 mcg/kg IV bolus as soon as possible after diagnosis followed by infusion at 2 mcg/kg/min.

Dosage in Percutaneous Coronary Intervention (PCI):

• Add a second 180 mcg/kg bolus at 10 minutes.

• In patients with creatinine clearance <50 mL/min, reduce the infusion to 1 mcg/kg/min.

Administration:

• Eptifibatide injection in GALAXY container is for intravenous infusion only, not for intravenous bolus use.
• Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration.
• Use only if solution is clear and container and seals are intact.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 20 mg/10 mL (2 mg/mL) in a single-dose vial for bolus injection
• 75 mg/100 mL (0.75 mg/mL) in a single-dose vial for infusion

This medicine is available in fallowing brand namesː

• Integrilin

What side effects can this medication cause?

The most common side effects of this medicine may include:

• Bleeding and hypotension

Less common, but serious side effects may include:

• Intracranial Hemorrhage and Stroke
• Immunogenicity/Thrombocytopenia
• cerebral, GI, and pulmonary hemorrhage

What special precautions should I follow?

• Eptifibatide can cause serious bleeding. If bleeding cannot be controlled, discontinue eptifibatide immediately. Minimize vascular and other traumas. If heparin is given concomitantly, monitor aPTT or ACT.
• There have been reports of acute, profound thrombocytopenia (immune-mediated and non-immune mediated) with eptifibatide. Monitor serial platelet counts, assess the presence of drug-dependent antibodies, and treat as appropriate. If a patient with low platelet counts is receiving eptifibatide, their platelet count should be monitored closely.
• It is not known whether eptifibatide is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when eptifibatide is administered to a nursing mother.
• Risk of bleeding increases with age.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• loss of righting reflex, dyspnea, ptosis, and decreased muscle tone in rabbits and petechial hemorrhages in the femoral and abdominal areas.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• eptifibatide is not extensively bound to plasma proteins and thus may be cleared from plasma by dialysis.

Can this medicine be used in pregnancy?

• There are, however, no adequate and well-controlled studies in pregnant women with eptifibatide.
• Because animal reproduction studies are not always predictive of human response, eptifibatide should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• Safety and effectiveness of eptifibatide in pediatric patients have not been studied.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• eptifibatide

Inactive ingredients:

• citric acid monohydrate
• sodium hydroxide
• water

Who manufactures and distributes this medicine?

• Baxter Healthcare Corporation, Deerfield, IL USA
• Made in USA

What should I know about storage and disposal of this medication?

• GALAXY containers should be stored refrigerated at 2-8°C (36-46°F).
• GALAXY containers may be transferred to room temperature storage1 for a period not to exceed 2 months.
• Upon transfer, Eptifibatide injection cartons must be marked by the dispensing pharmacist with a “DISCARD BY” date (2 months from the transfer date or the labeled expiration date, whichever comes first).
• Protect from light.
• Retain in carton until time of use.
• Discard unused portion.
• Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).

• Dailymed label info on Eptifibatide
• FDA Eptifibatide