Glycoprotein IIb/IIIa Inhibitors

Glycoprotein IIb/IIIa inhibitors are potent antiplatelet agents that block fibrinogen binding at platelet receptors, preventing aggregation and thrombus formation—commonly used in acute coronary syndromes and percutaneous coronary interventions to reduce ischemic complications.

Name of the Glycoprotein IIb/IIIa Inhibitors drugs:

  1. Tirofiban
  2. Eptifibatide

Mechanism of Action:

A non-peptide antagonist that prevents fibrinogen from binding to the glycoprotein IIb/IIIa receptor, thus blocking platelet aggregation.

Indications:

  • Unstable angina/ non-ST elevation MI (given with aspirin and heparin)
  • Acute coronary syndrome
  • Reduce the immediate risk of vascular occlusion in patients undergoing percutaneous coronary intervention

Cautions and Contraindications:

  • Major bleeding diathesis and active major internal bleeding
  • Major surgery or trauma in the past 6 weeks.
  • Ischemic stroke within 30 days or any history of haemorrhagic stroke.
  • Intracranial pathology (e.g., aneurysm, neoplasm or AV malformation).
  • Severe hypertension.
  • Deranged clotting or thrombocytopenia.
                                                           Tirofiban
Availability: premixed IV infusion solution : 5mg/100mL (50mcg/mL)  and 12.5mg/250mL (50mcg/mL) IV solution vials  :   5mg/100mL vial (50mcg/mL)  and  3.75mg/15mL bolus vial (250mcg/mL).
Administration and Handling: IV Preparation- Available only as premixed 50 mcg/mL solution for injection (100 mL or 250 mL bags) Storage: Store at 25°C (77°F) with excursions permitted between 15-30°C (59-86°F). Do not freeze. Protect from light during storage.
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 hours. 
Renal Impairment CrCl ≤60 mL/min: Decrease post loading dose infusion by 50% to 0.075 mcg/kg/min IV 
                                                        Eptifibatide
Availability: injection solution : 2mg/mL  and 0.75mg/mL
Administration and Handling: IV Preparation Bolus injection: withdraw from 10 mL vial (2 mg/mL; 10, 100 mL) Infusion: no prep needed; spike 100 ml vial with vented infusion set (0.75 mg/mL; 100 mL) IV Administration: Inspect for particulate matter and discoloration prior to administration, whenever solution and container permit. Do not administer through the same intravenous line as furosemide Withdraw bolus dose(s) from the 10-mL vial into a syringe; administer bolus dose(s) by IV push.
Immediately following bolus dose administration, initiate a continuous infusion. When using an intravenous infusion pump, administer undiluted directly from 100-mL vial. Spike the 100-mL vial with a vented infusion set; center the spike within the circle on the stopper top. Discard any unused portion left in the vial.
Acute Coronary Syndromes: 180 mcg/kg IV bolus over 1-2 min, THEN 2 mcg/kg/min IV continuous infusion; continue infusion until hospital discharge or initiation of coronary artery bypass graft surgery (CABG), up to 72 hours Patient to undergo PCI: infusion should be continued until hospital discharge or for up to 18- 24 hr after procedure, whichever comes first, allowing for up to 96 hrs of therapy. Administer aspirin (160-325 mg) daily.
Percutaneous Coronary Intervention: 180 mcg/kg IV bolus immediately, THEN Continuous infusion 2 mcg/kg/min with another 180 mcg/kg IV bolus 10 minutes after 1st bolus. Continue infusion until hospital discharge, or for up to 18 to 24 hours, whichever comes first; minimum 12 hrs infusion recommended. In patients who undergo CABG surgery, drug infusion should be discontinued prior to surgery. Administer aspirin, 160 to 325 mg, 1 to 24 hours prior to PCI and daily thereafter.

Side – Effects:

  • Bleeding
  • Nausea
  • Headache
  • Fever
  • Reversible thrombocytopenia
  • Hypotension
  • Bradycardia

Metabolism And Half- Life:

Tirofiban: Half-life: 2 hr; Excretion: Urine (65%); feces (25%)

Eptifibatide : Half-life, elimination: 2.5 hr; Excretion: Urine

Drug Interactions:

Risk of hemorrhage is increased with heparin and antiplatelet drug.

Important Points:

Treatment should be for a minimum of 48 h a maximum of 108h if the patient remains unstable with a view to in-patient angiography and potential revascularization as soon as possible.

Nursing Considerations:

  • Check coagulation labs such as the international normalized ratio (INR), prothrombin time (PT), and activated partial thromboplastin time (aPTT).
  • •Make sure the patient is not allergic to the agent before its administration.
  • Confirm the dosage of the antiplatelets and anticoagulants that the patient is receiving.
  • Check for any absolute and relative contraindications. 
  • Perform post-administration labs. 
  • Patients should be monitored for thrombocytopenia which may occur as soon as 24 hours after treatment with glycoprotein IIb/IIIa inhibitors. The platelet count should be checked within four hours of the start of the infusion and again at 24 hours. Watch for signs of bleeding and hemorrhage, including bleeding gums, nosebleeds, unusual bruising, black/tarry stools, hematuria, or a fall in hematocrit or blood pressure (BP).
  • The infusion of glycoprotein IIb/IIIa inhibitors should be stopped if the platelet count drops below 100,000/mm. Patients at high risk for thrombus should remain in intensive care if the glycoprotein IIb/IIIa inhibitors need to be continued. Typically, it takes up to two weeks for the platelet count to return to normal. 
  • Be especially alert for signs of intracranial bleeds, including sudden severe headache, confusion, nausea, vomiting, paralysis, numbness, speech problems, and visual disturbances.
  • Assess BP periodically and compare to normal values. Report low BP (hypotension), especially if patient experiences dizziness or syncope.
  • Because eptifibatide is cleared by the kidneys, patients with decreased renal function (i.e, estimated creatinine clearance less than 50 ml/min) should receive the following adjusted dosage of eptifibatide: 180 mcg/kg IV bolus just before PCI followed by continuous infusion of 1 mcg/kg/min and a second bolus of 180 mcg/kg.

Interventions

  • Use caution with any physical interventions that could increase bleeding, including wound debridement, chest percussion, joint mobilization, and application of local heat.
  • Use caution during aerobic exercise and endurance conditioning in patients being treated for unstable angina and coronary artery disease. Assess exercise tolerance frequently (BP, heart rate, fatigue levels), and terminate exercise immediately if any untoward responses occur.

Patient Teaching:

  • Instruct patient to report immediately signs of GI bleeding, including abdominal pain, vomiting blood, blood in stools, or black, tarry stools.
  • Remind patients to take medication as directed to reduce the risk of coronary infarction even if they are asymptomatic.
  • Counsel patients about additional interventions to help reduce the risk of heart disease, including regular exercise, weight loss, sodium restriction, stress reduction, moderation of alcohol consumption, and smoking cessation.

REFERENCES

  1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
  2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
  3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
  4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
  5. Nursebro.com, Search – Nursebro

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