Eptifibatide

Registered South African indications:

• Unstable angina
• Non-Q wave myocardial infarction
• Adjunct to percutaneous transluminal coronary artery intervention

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe renal impairment
• Severe hepatic impairment
• Evidence of gastrointestinal bleeding, gross genitourinary bleeding or other active abnormal bleeding within the previous 30 days of treatment
• History of stroke within 30 days or any history of haemorrhagic stroke
• Known history of intracranial disease
• Major surgery or severe trauma within past 6 weeks
• History of bleeding diathesis
• Thrombocytopenia (< 100,000 cells/mm³)
• Prothrombin time > 1.2 times control, or International Normalized Ratio (INR) ≥ 2.0
• Severe hypertension
• Coadministration with another parenteral glycoprotein IIb/IIIa inhibitor

Cautions

• Pregnancy
• Breastfeeding
• Moderate renal impairment
• Mild-to-moderate hepatic impairment
• Elderly
• Women
• Patients with low body weight 
• Potential bleeding sites
• Femoral arterial access

Forms avail. in SA and covered in this monograph: inj

Unstable angina
Non-Q-wave myocardial infarction
-To reduce the risk of death or myocardial infarction
-Managed with standard medical therapies and/or with percutaneous coronary intervention

• IV: 180μg/kg, bolus; Then: 2μg/kg/min, as a continuous infusion for up to 72hrs until initiation of coronary artery bypass graft (CABG) surgery or until discharge

If a percutaneous transluminal coronary artery (PTCA) intervention is performed, the infusion should be continued for 20-24hrs for an overall maximum duration of therapy of 96hrs

Adjunct to a percutaneous transluminal coronary artery intervention (PCI)
-For the prevention of abrupt closure of the treated coronary vessel and related acute ischaemic cardiac complications

• IV: 180μg/kg, bolus immediately prior to procedure together with a continuous infusion of 2μg/kg/min; Then: 180μg/kg, 10min after 1st bolus; Continue infusion until discharged or Max: 18-24hrs post PCI

Minimum of 12hrs infusion recommended

Use concomitantly with aspirin and unfractionated heparin

If the patient requires emergency or urgent cardiac surgery during the course of eptifibatide therapy, terminate the infusion immediately. If the patient requires semi-elective surgery, stop the eptifibatide infusion at an appropriate time to allow time for platelet function to return towards normal

Not established for use in children below 18 years

Pregnancy

• Caution
• There are no adequate data from the use of eptifibatide in pregnant women.
• Animal studies are insufficient with respect to effects on pregnancy, embryonal/foetal development, parturition or postnatal development. The potential risk for humans is unknown.
• Eptifibatide should not be used during pregnancy unless clearly necessary

Breastfeeding

• Caution: not recommended
• It is not known whether eptifibatide is excreted in human milk. Interruption of breast-feeding during the treatment period is recommended

Renal Impairment

• Moderate renal impairment: Caution; dose adjustment recommended.
  Patients with renal function (eGFR ≥30-49 mL/min/1.73 m²): 180μg/kg, bolus; Then: 1μg/kg/min for the duration of therapy 
• Severe renal impairment: Contraindicated
  Use in patients with renal function (eGFR ≤29 mL/min/1.73 m²) is contraindicated

Hepatic Impairment

• Mild-to-Moderate: Caution; no dose adjustment recommended
  Use not recommended. Use with high caution.
• Severe hepatic impairment: Contraindicated

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Not porphyrinogenic (NP)

Central Nervous System Disorders

• Cerebral ischaemia

Cardiovascular Disorders

• Cardiac arrest
• Ventricular fibrillation
• Ventricular tachycardia
• Congestive heart failure
• Atrioventricular block
• Atrial fibrillation
• Shock
• Hypotension
• Phlebitis

Immune, Blood and Lymphatic System Disorders

• Bleeding 
• Thrombocytopenia

• Thrombolytic agents
• Streptokinase
• Parenteral glycoprotein IIb/IIIa inhibitor
• Agents affecting haemostasis
• Low molecular weight heparins

• Prothrombin time
• Activated partial prothrombin time
• Full blood count
• Renal function

Eptifibatide reversibly inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor and other adhesive ligands to the glycoprotein IIb/IIIa receptors. Eptifibatide inhibits platelet aggregation in a dose- and concentration-dependent manner as demonstrated by ex vivo platelet aggregation using adenosine diphosphate and other agonists to induce platelet aggregation.

Injection (per ml) 0.75mg

• Integrilin (MSD) originator

Injection (per ml) 2mg

• Integrilin (MSD) originator