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GPIIb/IIIa Receptor Antagonist (Cyclic Peptide) Pregnancy: US label section 8.1: '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.' '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.' Clinical considerations: '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.' This summary may be incomplete — check the full SPC.

Eptifibatide (GPIIb/IIIa Inhibitor — ACS/PCI)

Brand names: Integrilin

Eptifibatide is an intravenous glycoprotein IIb/IIIa receptor antagonist used as an antiplatelet agent in acute coronary syndromes and during percutaneous coronary intervention.

Adult dose

Dose: ACS: 180 mcg/kg intravenous (I.V.) bolus as soon as possible after diagnosis, followed by continuous infusion of 2 mcg/kg/min. PCI: 180 mcg/kg I.V. bolus immediately before PCI followed by continuous infusion of 2 mcg/kg/min and a second bolus of 180 mcg/kg (given 10 minutes after the first bolus).
Route: Intravenous - bolus dose(s) withdrawn from the 10 mL (2 mg/mL) vial and given by I.V. push, immediately followed by the continuous infusion; when using an infusion pump the label directs administration undiluted directly from the 100 mL vial.
Frequency: Single bolus (two boluses in PCI, 10 minutes apart) then continuous infusion. ACS: '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.' PCI: '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.'
SCOPE: this is the page's primary indication and route - ACS (medical management) and PCI, IV bolus then infusion - and both regimens above are quoted verbatim from sections 2.1 and 2.2 of the fetched US label. NO ABSOLUTE MAXIMUM DOSE has been entered: the retrieved label states no 'maximum' single or daily dose for eptifibatide (the only occurrence of the word is in the animal-reproduction paragraph of section 8.1), and the label's Table 1 weight-band chart is expressed as volumes and infusion rates, not as a dose ceiling - so nothing in this bundle qualifies as an absolute cap. ADMINISTRATION (section 2.3): may be given in the same IV line as alteplase, atropine, dobutamine, heparin, lidocaine, meperidine, metoprolol, midazolam, morphine, nitroglycerin or verapamil; 'Do not administer eptifibatide injection through the same intravenous line as furosemide'; may be given in the same line with 0.9% NaCl or 0.9% NaCl/5% dextrose, which may also contain up to 60 mEq/L of potassium chloride. WEIGHT-BASED VOLUME CHART (Table 1) gives bolus volumes from 3.4 mL at 37-41 kg to 11.3 mL above 121 kg (2 mg/mL vial) and the corresponding 2 mcg/kg/min and 1 mcg/kg/min infusion rates - use the chart in the label rather than reproducing it here. CO-THERAPY quoted from the label: aspirin 160 to 325 mg daily in ACS, and 'given 1 to 24 hours prior to PCI and daily thereafter' for PCI; heparin to a target aPTT of 50 to 70 seconds during medical management (weight 70 kg or more: 5,000 units bolus then 1,000 units/h; under 70 kg: 60 units/kg bolus then 12 units/kg/h) and to a target ACT of 200 to 300 seconds during PCI, with heparin infusion after PCI 'strongly discouraged'. 'In patients who undergo CABG surgery, eptifibatide infusion should be discontinued prior to surgery' and 'Patients requiring thrombolytic therapy should discontinue eptifibatide injection.' STRENGTHS (section 3): 20 mg/10 mL (2 mg/mL) single-dose vial for bolus; 75 mg/100 mL (0.75 mg/mL) and 200 mg/100 mL (2 mg/mL) single-dose vials for infusion. Some sections of the product information we used were incomplete — check the full SPC.

Dose adjustments

Renal

US label sections 2.1/2.2, verbatim: 'In patients with creatinine clearance less than 50 mL/min, reduce the infusion to 1 mcg/kg/min.' The 180 mcg/kg bolus (and, in PCI, the second 180 mcg/kg bolus at 10 minutes) is unchanged in renal impairment. 'Dependency on renal dialysis' is an absolute contraindication (section 4). Serum creatinine is one of the tests the label requires before starting the infusion.

Hepatic

Not addressed in the retrieved sections of this label - no hepatic dose adjustment or hepatic-impairment statement was fetched. Confirm against the full label or UK SPC.

Dose independently re-sourced from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — clinician-reviewed. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • A history of bleeding diathesis, or evidence of active abnormal bleeding within the previous 30 days (US label section 4)
  • Severe hypertension (systolic blood pressure >200 mm Hg or diastolic blood pressure >110 mm Hg) not adequately controlled on antihypertensive therapy (section 4)
  • Major surgery within the preceding 6 weeks (section 4)
  • History of stroke within 30 days or any history of hemorrhagic stroke (section 4)
  • Current or planned administration of another parenteral GP IIb/IIIa inhibitor (section 4)
  • Dependency on renal dialysis (section 4)
  • Hypersensitivity to eptifibatide injection or any component of the product - reported hypersensitivity reactions included anaphylaxis and urticaria (section 4)

Side effects

  • Bleeding and hypotension were the most commonly reported adverse reactions (incidence 5% or more and greater than placebo) in the controlled clinical trial database (section 6)
  • Bleeding is the most common complication of therapy - an increase in major and minor bleeding by TIMI criteria; most major bleeding has been at the arterial access site for cardiac catheterization or from the gastrointestinal or genitourinary tract (section 5.1)
  • Thrombocytopenia - 'Discontinue eptifibatide and heparin. Monitor and treat condition appropriately.' (section 5.2)
  • Hypersensitivity reactions including anaphylaxis and urticaria (section 4)
  • Bleeding risk is higher in older patients: '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' (section 8.5)

Monitoring

  • Before the infusion, to identify pre-existing haemostatic abnormalities: haematocrit or haemoglobin, platelet count, serum creatinine, and PT/aPTT (section 2)
  • In patients undergoing PCI, the activated clotting time (ACT) should also be measured - target ACT 200 to 300 seconds during PCI (sections 2, 2.1, 2.2)
  • aPTT should be maintained between 50 and 70 seconds unless PCI is to be performed; in patients treated with heparin 'bleeding can be minimized by close monitoring of the aPTT and ACT' (sections 2, 5.1)
  • Platelet count for thrombocytopenia - discontinue eptifibatide and heparin if it occurs (section 5.2)
  • Bleeding surveillance: 'If bleeding cannot be controlled, discontinue eptifibatide immediately'; minimize vascular and other traumas, arterial and venous punctures, intramuscular injections, urinary catheters, nasotracheal intubation and nasogastric tubes, and avoid non-compressible venous access sites such as subclavian or jugular veins (sections 5, 5.1)
  • Renal function (serum creatinine) - determines the 1 vs 2 mcg/kg/min infusion rate (sections 2.1, 2.3)

Clinical monograph

How it works

It reversibly blocks the platelet glycoprotein IIb/IIIa receptor, preventing fibrinogen binding and the final common pathway of platelet aggregation.

Prescribing in practice

  • Major bleeding and thrombocytopenia are the principal risks, so it is contraindicated with active bleeding and recent haemorrhagic stroke.
  • Dosing requires adjustment in renal impairment because clearance is partly renal.
  • It is used with aspirin and an anticoagulant, increasing overall bleeding risk that must be balanced against ischaemic benefit.

Monitoring

Monitor platelet count and for bleeding during and after the infusion, and assess renal function.

Counselling the patient

  • This is an intravenous antiplatelet medicine used during treatment of a heart attack or stent procedure.
  • Report any bleeding, bruising or blood in the urine or stool.
  • The team will check your blood counts during treatment.

Evidence & guidelines

The PURSUIT and ESPRIT trials supported eptifibatide use in acute coronary syndromes and percutaneous coronary intervention.

Reference: PURSUIT Trial (NEJM 1998); ESPRIT Trial (NEJM 2001); ESC PCI Guidelines 2023; MHRA SPC Integrilin; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.

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