eptifibatide (ep-ti-fib-a-tide) Integrilin

 Indications

Acute coronary syndrome (unstable angina/non-Qwave

MI), including patients who will be managed

medically and those who will undergo percutaneous

coronary intervention (PCI) that may consist of percutaneous

transluminal angioplasty (PCTA) or atherectomy.

Treatment of patients undergoing PCI. Usually

used concurrently with aspirin and heparin.

Action

Decreases platelet aggregation by reversibly antagonizing

the binding of fibrinogen to the glycoprotein IIb/

IIIa binding site on platelet surfaces. Therapeutic

Effects: Inhibition of platelet aggregation resulting in

decreased incidence of new MI, death, or refractory ischemia,

reducing the need for repeat urgent cardiac intervention.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unknown.

Metabolism and Excretion: 50% excreted by the

kidneys.

Half-life: 2.5 hr.

TIME/ACTION PROFILE (effects on platelet

function)

ROUTE ONSET PEAK DURATION

IV immediate following bolus

brief†

†Inhibition is reversible following cessation of infusion.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Active internal

bleeding or history of bleeding within previous 30 days; Severe uncontrolled hypertension (systolic BP

200 mm Hg and/or diastolic BP 110 mm Hg); Major

surgical procedure within 6 wk; History of hemorrhagic

stroke or other stroke within 30 days; Concurrent

use of other glycoprotein IIb/IIIa receptor

antagonists; Platelet count 100,000/mm3; Severe renal

insufficiency (serum creatinine 4 mg/dL) or dependency

on renal dialysis.

Use Cautiously in: Geri:qrisk of bleeding ; Renal

insufficiency (pinfusion rate if CCr 50 mL/min); OB,

Pedi: Pregnancy, lactation, or children (safety not established;

use in pregnancy only if clearly needed).

Adverse Reactions/Side Effects

Noted for patients receiving heparin and aspirin in addition

to eptifibatide.

CV: hypotension. Hemat: BLEEDING (including GI and

intracranial bleeding, hematuria, and hematomas),

thrombocytopenia.

Interactions

Drug-Drug:qrisk of bleeding with other drugs that

affect hemostasis (heparins, warfarin, NSAIDs,

thrombolytic agents, abciximab, dipyridamole,

clopidogrel, some cephalosporins, valproates).

Drug-Natural Products:qbleeding risk with arnica,

chamomile, clove, dong quai, feverfew, garlic,

ginger, ginkgo, and Panax ginseng.

Route/Dosage

Acute Coronary Syndrome

IV (Adults 121 kg): 180 mcg/kg as a bolus dose,

followed by 2 mcg/kg/min until hospital discharge or

surgical intervention (up to 72 hr).

Percutaneous Coronary Intervention

IV (Adults): 180 mcg/kg as a bolus dose, immediately

before PCI, followed by 2 mcg/kg/min infusion; a second

bolus of 180 mcg/kg is given 10 min after first bolus;

infusion should continue for 18–24 or hospital

discharge (minimum of 12 hr).

Renal Impairment

(Adults CCr 50 mL/min): 180 mcg/kg bolus followed

by 1 mcg/kg/min infusion; second bolus of 180 mcg/kg

is given 10 min after first bolus for patients undergoing

PCI.

Availability (generic available)

Solution for injection: 20 mg/10 mL, 75 mg/100 mL,

200 mg/100 mL.