EPTIFIBATIDE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

EPTIFIBATIDE (UNII: NA8320J834) (EPTIFIBATIDE - UNII:NA8320J834)

Available from:

Athenex Pharmaceutical Division, LLC.

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death or new myocardial infarction (MI) in patients with ACS (unstable angina [UA]/non-ST-elevation myocardial infarction [NSTEMI]), including patients who are to be managed medically and those undergoing percutaneous coronary intervention (PCI). Eptifibatide injection is indicated to decrease the rate of a combined endpoint of death, new MI, or need for urgent intervention in patients undergoing PCI, including those undergoing intracoronary stenting [see Clinical Studies ( 14.1, 14.2)] . Treatment with eptifibatide is 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 - Major surgery within the preceding 6 weeks - History of stroke within 30 days or any history of hemorrhagic stroke - Current or planned administration of another parenteral GP IIb/IIIa inhibitor - Dependency on renal dialysis - Hypersensitivity to eptifibatide or any component of the product (hypersensitivity reactions that occurred included anaphylaxis and urticaria) Risk Summary Available data on eptifibatide use in pregnant women from published literature and the pharmacovigilance database are insufficient to establish a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Untreated myocardial infarction can be fatal to the pregnant woman and fetus (see Clinical Considerations) . In animal reproduction studies, there was no evidence of adverse developmental effects when eptifibatide was administered intravenously to pregnant rats and rabbits at approximately 4 times the recommended maximum daily human dose. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Myocardial infarction is a medical emergency in pregnancy which can be fatal to the pregnant woman and fetus if left untreated. Therapy for the pregnant woman should not be withheld because of potential concerns regarding the effects of eptifibatide on the fetus. Data Animal Data Embryo-fetal development studies have been performed by continuous intravenous infusion of eptifibatide in pregnant rats during the period of organogenesis at total daily doses of up to 72 mg/kg/day (about 4 times the recommended maximum daily human dose on a body surface area basis) and in pregnant rabbits during the period of organogenesis at total daily doses of up to 36 mg/kg/day (also about 4 times the recommended maximum daily human dose on a body surface area basis). These studies revealed no evidence of harm to the fetus due to eptifibatide. Risk Summary There are no available data on the presence of eptifibatide in human milk, the effects on the breastfed infant, or the effects on milk production. As eptifibatide is a peptide, it is likely to be destroyed in the infant's gastrointestinal tract and not absorbed orally by the breastfed infant. Safety and effectiveness of eptifibatide in pediatric patients have not been studied. The PURSUIT and IMPACT II clinical studies enrolled patients up to the age of 94 years (45% were age 65 and over; 12% were age 75 and older). There was no apparent difference in efficacy between older and younger patients treated with eptifibatide. The 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. No dose adjustment was made for elderly patients, but patients over 75 years of age had to weigh at least 50 kg to be enrolled in the PURSUIT study; no such limitation was stipulated in the ESPRIT study [see Adverse Reactions ( 6.1)] . Approximately 50% of eptifibatide is cleared by the kidney in patients with normal renal function. Total drug clearance is decreased by approximately 50% and steady-state plasma eptifibatide concentrations are doubled in patients with an estimated CrCl <50 mL/min (using the Cockcroft-Gault equation). Therefore, the infusion dose should be reduced to 1 mcg/kg/min in such patients [see Dosage and Administration ( 2)] . The safety and efficacy of eptifibatide in patients dependent on dialysis has not been established.

Product summary:

Eptifibatide Injection is supplied as follows: Vials should be stored refrigerated between 2° and 8°C (36° and 46°F). Vials may be transferred to room temperature storage * for a period not to exceed 2 months. Upon transfer, vial 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 between 15° and 30°C (59° and 86°F). [See USP Controlled Room Temperature.] Sterile, Nonpyrogenic, Preservative-free. The container closure is not made with natural rubber latex.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

EPTIFIBATIDE- EPTIFIBATIDE INJECTION, SOLUTION
ATHENEX PHARMACEUTICAL DIVISION, LLC.
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HIGHLIGHTS OF PRESCRIBING INFORMATION
THESE HIGHLIGHTS DO NOT INCLUDE ALL THE INFORMATION NEEDED TO USE
EPTIFIBATIDE INJECTION
SAFELY AND EFFECTIVELY. SEE FULL PRESCRIBING INFORMATION FOR
EPTIFIBATIDE INJECTION.
EPTIFIBATIDE INJECTION, FOR INTRAVENOUS USE
INITIAL U.S. APPROVAL: 1998
INDICATIONS AND USAGE
Eptifibatide injection is a platelet aggregation inhibitor indicated
for:
Treatment of acute coronary syndrome (ACS) managed medically or with
percutaneous coronary
intervention (PCI). ( 1.1)
Treatment of patients undergoing PCI (including intracoronary
stenting). ( 1.2)
DOSAGE AND ADMINISTRATION
ACS or PCI: 180 mcg/kg IV bolus as soon as possible after diagnosis
followed by infusion at 2 mcg/kg/min. (
2.1, 2.2)
PCI: Add a second 180 mcg/kg bolus at 10 minutes. ( 2.2)
In patients with creatinine clearance less than 50 mL/min, reduce the
infusion to 1 mcg/kg/min. ( 2.1, 2.2,
2.3)
DOSAGE FORMS AND STRENGTHS
20 mg per 10 mL (2 mg per mL) in a single-dose vial for bolus
injection ( 3)
75 mg per 100 mL (0.75 mg per mL) in a single-dose vial for infusion (
3)
CONTRAINDICATIONS
Bleeding diathesis or bleeding within the previous 30 days ( 4)
Severe uncontrolled hypertension ( 4)
Major surgery within the preceding 6 weeks ( 4)
Stroke within 30 days or any history of hemorrhagic stroke ( 4)
Coadministration of another parenteral GP IIb/IIIa inhibitor ( 4)
Dependency on renal dialysis ( 4)
Known hypersensitivity to any component of the product ( 4)
WARNINGS AND PRECAUTIONS
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. ( 5.1)
Thrombocytopenia: Discontinue eptifibatide and heparin. Monitor and
treat condition appropriately. (
5.2)
ADVERSE REACTIONS
Bleeding and hypotension are the most commonly reported adverse
reactions. ( 6.1)
TO REPORT SUSPECTED ADVERSE REACTIONS, CONTACT