Dosing & Uses
Dosage Forms & Strengths
premixed IV infusion solution
- 5mg/100mL (50mcg/mL)
- 12.5mg/250mL (50mcg/mL)
IV solution vials
- 5mg/100mL vial (50mcg/mL)
- 3.75mg/15mL bolus vial (250mcg/mL)
Non-ST Elevation Acute Coronary Syndrome (NSTE-ACS)
Indicated to reduce rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in NSTE-ACS
Loading dose: 25 mcg/kg IV infused within 5 min, THEN
Post loading dose infusion: 0.15 mcg/kg/min IV for up to 18 hr
Refer to prescribing information for dosing chart by weight and CrCl
Renal Impairment
CrCl ≤60 mL/min: Decrease post loading dose infusion by 50% to 0.075 mcg/kg/min IV
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Bleeding, minor (11%)
1-10%
Pelvic pain (6%)
Coronary artery dissection (5%)
Bradycardia (4%)
Dizziness (3%)
Lower extremity pain (3%)
Edema (2%)
Sweating (2%)
Bleeding, major (1-2%)
Thrombocytopenia (1.5%)
Warnings
Contraindications
Severe hypersensitivity reaction to drug (i.e., anaphylactic reactions) or excipients
History of thrombocytopenia following prior exposure to therapy
Active internal bleeding or history of bleeding diathesis, major surgical procedure or severe physical trauma within previous month
Cautions
Bleeding is most common complication encountered during therapy; most bleeding associated with therapy occurs at arterial access site for cardiac catheterization; minimize use of traumatic or potentially traumatic procedures such as arterial and venous punctures, intramuscular injections, nasotracheal intubation, etc.
Concomitant use of fibrinolytics, anticoagulants and antiplatelet drugs increases risk of bleeding
Profound thrombocytopenia reported; monitor platelet counts beginning about 6 hr after treatment initiation and daily thereafter; If platelet count decreases to < 90,000/mm3, monitor platelet counts to exclude pseudothrombocytopenia; if thrombocytopenia confirmed, discontinue therapy and heparin; previous exposure to a glycoprotein (GP) IIb/IIIa receptor antagonist may increase risk of developing thrombocytopenia
Pregnancy & Lactation
Pregnancy
While published data cannot definitively establish the absence of risk, available published case reports have not established an association with therapy during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes
Untreated myocardial infarction can be fatal to the pregnant woman and fetus; myocardial infarction is a medical emergency in pregnancy which can be fatal to pregnant woman and fetus if left untreated
Animal data
- Studies with intravenous doses up to 5 mg/kg/day (about 5 and 13 times maximum recommended daily human dose for rat and rabbit, respectively, compared on a body surface area basis) have revealed no harm to fetus
Lactation
There is no data on presence of drug in human milk, effects on breastfed infant, or on human milk production; however, the drug is present in rat milk; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition
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
Mechanism of Action
Blocks binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptor on platelet surface; inhibits platelet aggregation
Pharmacokinetics
Half-life: 2 hr
Duration: 4 hr
Protein bound: 65%
Vd: 22-42 L
Clearance: 213-314 mL/min
Excretion: Urine (65%); feces (25%)
Dialyzable: Yes
Administration
IV Incompatibilities
Y-site: diazepam
IV Compatibilities
Solution: D5W, D5/½NS, NS
Y-site: amiodarone, atropine, bivalirudin, dobutamine, dopamine, epinephrine, famotidine, furosemide, heparin, lidocaine, midazolam, morphine, nitroglycerin, KCl, propranolol
IV Preparation
Available only as premixed 50 mcg/mL solution for injection (100 mL or 250 mL bags)
IV Administration
See adult dosing for infusion rate
Storage
Store at 25°C (77°F) with excursions permitted between 15-30°C (59-86°F)
Do not freeze
Protect from light during storageIV IncompatibilitiesY-site: diazepamIV CompatibilitiesSolution: D5W, D5/½NS, NSY-site: amiodarone, atropine, bivalirudin, dobutamine, dopamine, epinephrine, famotidine, furosemide, heparin, lidocaine, midazolam, morphine, nitroglycerin, KCl, propranololIV PreparationAvailable only as premixed 50 mcg/mL solution for injection (100 mL or 250 mL bags)IV AdministrationSee adult dosing for infusion rateStorageStore at 25°C (77°F) with excursions permitted between 15-30°C (59-86°F)Do not freezeProtect from light during storage
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Formulary
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