Eptifibatide information from DrugsUpdate
P - Caution when used during pregnancy
L - Contraindicated in lactation
Eptifibatide (Integrilin, Millennium Pharmaceuticals, also co-promoted by Schering-Plough/Essex), is an antiplatelet drug that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide has a short half-life. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody abciximab and the non-peptide tirofiban entered the global market.
Integrilin is sold in two strengths, globally: vials containing 2 mg/ml (20 mg totally) and 0.75 mg/ml (75 mg totally). A third size is sold in the US: 100 ml vials containing 2 mg/ml (200 mg totally).
Pharmacodynamics
Pharmacokinetics
Eptifibatide is a cyclic heptapeptide which blocks the platelet glycoprotein IIb/IIIa receptor thus preventing platelet aggregation and thrombosis.
Onset
Within 1 hour.
Eptifibatide Indications / Eptifibatide Uses
Information Not Available
Eptifibatide Adverse Reactions / Eptifibatide Side Effects
Bleeding, hypotension; localised Inj site reaction; thrombocytopaenia; back pain; anaphylaxis; GI, intracranial or pulmonary haemorrhage.
Precautions
Monitor
Obtain Hct or Hgb, platelet count, serum creatinine, and PT/aPTT before starting therapy and periodically during treatment. Also obtain activated clotting time (ACT) in patients undergoing PCI. Closely monitor patient for unusual bleeding or unusual bruising, especially at vascular access sites.
Renal Function
Reduce dose in patients with moderate to severe renal function impairment (Ccr less than 50 mL/min).
aPTT/ACT
Maintain aPTT between 50 and 70 sec in patients being treated concurrently with heparin unless a PCI is to be performed. Maintain ACT between 200 and 300 sec during PCI.
Bleeding
Bleeding is most common complication of therapy. Take special care to minimize risk of bleeding; if bleeding occurs and cannot be controlled with pressure or other means, immediately discontinue eptifibatide infusion and concomitant heparin.
CABG surgery
Discontinue infusion prior to CABG surgery.
Platelet count
Discontinue eptifibatide and heparin in patient whose platelet count decreases to less than 100,000/mm 3 .
Sheath removal
Do not remove arterial sheath unless aPTT is less than 45 sec or the ACT is less than 150 sec.
Trauma
Minimize use of arterial or venous punctures, IM injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes. Avoid noncompressible sites (eg, subclavian, jugular veins) when obtaining necessary IV access.
Overdosage
Symptoms
None reported because of limited data.
Special Precautions
Discontinue in case of serious uncontrolled bleeding, or if emergency surgery or thrombolytic therapy is required. Hepatic impairment, platelet counts <100,000 mm3; hemorrhagic retinopathy, drugs affecting haemostasis. Check aPTT or ACT prior to sheath removal. Severe renal impairment, vasculitis, haemorrhagic retinopathy, acute pericarditis or aortic dissection. Pregnancy.
Other Drug Interactions
Increased risk of bleeding with heparin, other anticoagulants, antiplatelet and thrombolytic agents.
Other Interactions
Information Not Available
Dosage
Intravenous
Unstable Angina
Adult: 180 mcg/kg via IV inj followed by 2 mcg/kg/minute by IV infusion for up to 72 hr. If percutaneous coronary intervention is performed during therapy, infusion should be continued for 18-24 hr after procedure, up to a max total duration of 96 hr of therapy.
Renal impairment: Dose reduction may be needed.
CrCl (ml/min) Dosage Recommendation
<30 Contraindicated.
Intravenous
Angioplasty
Adult: Initially, 180 mcg/kg via IV inj, to be given immediately before procedure, followed by 2 mcg/kg/minute via IV infusion. A 2nd dose of 180 mcg/kg via IV inj should be given 10 minutes after the 1st dose. Continue infusion until hospital discharge or for up to 18-24 hr (min treatment duration: 12 hr).
Renal impairment: Dose reduction may be needed.
CrCl (ml/min) Dosage Recommendation
<30 Contraindicated.
Food(before/after)
Information Not Available
List of Contraindications
Eptifibatide and Pregnancy
Caution when used during pregnancy.
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Eptifibatide and Lactation
Contraindicated in lactation
Eptifibatide and Children
Information Not Available
Eptifibatide and Geriatic
Information Not Available
Eptifibatide and Other Contraindications
Active bleeding, increased risk of haemorrhage including hemorrhagic disorders, cerebrovascular disorders, history of stroke, uncontrolled hypertension, severe trauma, severe renal impairment, recent major surgery. Lactation.
Storage
Information Not Available
Lab interference
Information Not Available
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