eptifibatide (Integrilin)

Dosing and uses of Integrilin (eptifibatide)

• Adult
• Pediatric
• Geriatric

 

Adult dosage forms and strengths

injection solution

• 2mg/mL
• 0.75mg

 

Acute Coronary Syndromes

180 mcg/kg IV bolus over 1-2 min, THEn

2 mcg/kg/min IV for up to 72 hr

 

Percutaneous Coronary Intervention

180 mcg/kg IV, THEn

Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one

Continue infusion for at least 12 hours

 

Renal Impairment

(CrCl <50 mL/min)

ACS: 180 mcg/kg IV, THEN continuous infusion 1 mcg/kg/min

PCI: 180 mcg/kg IV, THEN continuous infusion 1 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one

Hemodialysis: Safety and using during hemodialysis not established

 

Pediatric dosage forms and strengths

Safety & efficacy not established

 

Geriatric dosage forms and strengths

In clinical trials, incidence of bleeding complications was higher in the elderly in both placebo and eptifibatide groups, and the incremental risk of eptifibatide-associated bleeding was greater in the older patients. Adjust dose to renal function

 

Acute Coronary Syndromes

180 mcg/kg IV bolus over 1-2 min, THEn

2 mcg/kg/min IV for up to 72 hr

 

Percutaneous Coronary Intervention

180 mcg/kg IV, THEn

Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st one

Continue infusion for at least 12 hours

 

Integrilin (eptifibatide) adverse (side) effects

1-10%

Bleeding (8%)

Hypotension (7%)

Thrombocytopenia (2.3%)

Injection site reaction

 

<1%

Hypersensitivity

Intracranial hemorrhage

Pulmonary hemorrhage

Thrombocytopenia

GI hemorrhage

 

Postmarketing Reports

Immune-mediated thrombocytopenia (thought to be caused by antibodies that react with GP IIb/IIIa complex)

 

Warnings

Contraindications

Hypersensitivity

History of internal bleeding, intracranial hemorrhage or neoplasm, CVA, thrombocytopenia

AV malformation or aneurysm, aortic dissection, severe HTN, acute pericarditis

Other parenteral glycoprotein IIb/IIIa inhibitors

 

Cautions

Bleeding at the site of arterial sheath placement is the most common complication

Early sheath removal is encouraged while eptifibatide is being infused; prior to removing the sheath, it is recommended that heparin be discontinued for 3-4 hr and an aPTT of <45 seconds or ACT <150 seconds be achieved

Thrombocytopenia: Discontinue if platelet levels <100,000 mm/cu.mm

 

Pregnancy and lactation

Pregnancy category: B

Lactation: excretion in milk unknown; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Integrilin (eptifibatide)

Mechanism of action

Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface

 

Pharmacokinetics

Half-life, elimination: 2.5 hr

Onset: 1 hr

Duration: 4 hr

Protein bound: 25%

Vd: 185-260 mL/kg

Metabolites: Deaminated eptifibatide, other more polar metabolites detected in urine, no metabolites detected in plasma

Clearance: 55-58 mL/kg/hr

Excretion: Urine

 

Administration

IV Incompatibilities

Y-site, additive, syringe: furosemide

 

IV Compatibilities

Y-site: alteplase, amiodarone, atropine, bivalirudin, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine sulfate, nitroglycerin, verapamiL

 

IV Preparation

Bolus injection: withdraw from 10 mL vial (2 mg/mL; 10, 100 mL)

Infusion: no prep needed; spike 100 ml vial with vented infusion set (0.75 mg/mL; 100 mL)

 

IV Administration

Bolus: administer undiluted over 1-2 min