Antigrilin

Uses

Antigrilin is used for-

• Patients with acute coronary syndrome (unstable angina/non-ST- segment elevation myocardial infarction), including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI).
• Patients undergoing PCI, including those undergoing intracoronary stenting.

Antigrilin is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Thrombotic events

How Antigrilin works

Antigrilin inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.

Dosage

Antigrilin dosage

Patients with ACS (Acute Coronary Syndrome):

Normal renal function: 180 μg/kg IV bolus of as soon as possible following diagnosis followed by a continuous infusion of 2 μg/kg/min.

Creatinine clearance: 180 μg/kg IV bolus of as soon as possible following diagnosis followed by a continuous infusion of 1 μg/kg/min

• Infusion should continue until hospital discharge or initiation of coronary artery bypass graft surgery (CABG), up to 72 hours.
• If a patient is to undergo PCI, the infusion should be continued until hospital discharge or for up to 18 to 24 hours after the procedure, whichever comes first, allowing for up to 96 hours of therapy.

Patients with PCI ( Percutaneous Coronary Intervention):

Normal renal function: 180 μg/kg IV bolus immediately before PCI followed by a continuous infusion of 2 μg/kg/min & a second bolus of 180 μg/kg (given 10 minutes after the first bolus)

Creatinine clearance: 180 μg/kg IV bolus immediately before PCI followed by a continuous infusion of 1 μg/kg/min & a second bolus of 180 μg/kg (given 10 minutes after the first bolus)

• Infusion should be continued until hospital discharge, or for up to 18 to 24 hours, whichever comes first. A minimum of 12 hours of infusion is recommended.
• In patients who undergo CABG surgery, INTEGRILIN infusion should be discontinued prior to surgery.

1. Integril solutions should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
2. Integril may be administered in the same IV line as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin, or verapamil. Integril should not be administered through the same IV line as furosemide.
3. Integril may be administered 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 KCl.
4. The bolus dose(s) of Integril should be withdrawn from the 10-mL vial into a syringe. The bolus dose(s) should be administered by IV push.
5. Immediately following the bolus dose administration, a continuous infusion of Integril should be initiated. When using an intravenous infusion pump, Integril should be administered undiluted directly from the 100 mL vial. The 100-mL vial should be spiked with a vented infusion set. Care should be taken to center the spike within the circle on the stopper top.

Side Effects

Bleeding is the most common adverse effect. Adverse reactions include intracranial hemorrhage & stroke, thrombocytopenia, allergic reactions and hypotension.

Toxicity

Antigrilin was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis)

Interaction

• In various clinical studies, eptifibatide was used concomitantly with unfractionated heparin and aspirin. In another study, clopidogrel or ticlopidine were used routinely starting the day of PCI. Because eptifibatide inhibits platelet aggregation, caution should be employed when it is used with other drugs that affect hemostasis, including thrombolytics, oral anticoagulants, NSAIDS and dipyridamole. To avoid potentially additive pharmacologic effects, concomitant treatment with other inhibitors of platelet receptor GP IIb/IIIa should be avoided
• Enoxaparin did not alter the pharmacokinetics of Integril

Food Interaction

• Avoid herbs and supplements with anticoagulant/antiplatelet activity. The use of anticoagulant/antiplatelet herbs with eptifibatide may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Antigrilin Hypertension interaction

[Major] The use of gp11b<111a platelet inhibitors is contraindicated in patients with active internal bleeding, recent significant gastrointestinal or genitourinary bleeding (within 6 weeks), recent trauma or major surgery (within 6 weeks), history of bleeding diathesis, recent stroke (within 4 weeks), history of hemorrhage stroke or residual neurologic deficit, intracranial defect (aneurysm, arteriovenous malformation, neoplasm), uncontrolled hypertension (SBP > 180; DBP > 110), or thrombocytopenia (

Antigrilin Drug Interaction

Major: clopidogrel, clopidogrelModerate: aspirin, aspirin, ginkgo, ginkgoUnknown: glucose, glucose, ethanol, ethanol, glycerin, glycerin, arginine, arginine, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, phytonadione, phytonadione

Antigrilin Disease Interaction

Major: renal dysfunction, bleeding risks

Half Life

Approximately 2.5 hours

Clearance

• 55 mL/kg/h [patients with coronary artery disease]

Pregnancy & Breastfeeding use

Pregnancy: Category B. Animal studies revealed no evidence of harm to the fetus due to Integril. There are, however, no adequate and well-controlled studies in pregnant women with Integril.

Lactating Mothers: It is not known whether Integril is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Integril is administered to a nursing mother.

Contraindication

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.

Special Warning

Use in Children: Safety and effectiveness of Integril in pediatric patients have not been studied.

Acute Overdose

There has been only limited experience with overdosage of Integril. Symptoms of acute toxicity were loss of righting reflex, dyspnea, ptosis, and decreased muscle tone in rabbits, and petechial hemorrhages in the femoral and abdominal areas of monkeys.

From in vitro studies, eptifibatide is not extensively bound to plasma proteins and thus may be cleared from plasma by dialysis.

Storage Condition

• Vials should be stored refrigerated at 2-8° C
• Vials may be transferred to room temperature storage for up to 2 months.
• Unused portion left in the vial should be discarded.
• Vials should be protected from light until administration.

Innovators Monograph

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