MEDICATION

Glycoprotein IIb/IIIa Inhibitors in Stroke Therapy and Prevention

David Goldemund M.D.
Updated on 07/09/2024, published on 04/09/2024
  • glycoprotein IIb/IIIa inhibitors (GP IIb/IIIa inhibitors) are a class of antiplatelet agents that target the final common pathway of platelet aggregation by blocking the GP IIb/IIIa receptors on platelets, thereby inhibiting fibrinogen binding and subsequent platelet aggregation
  • this action reduces the thrombus formation
  • these inhibitors are primarily used in the management of acute coronary syndromes (ACS) and during percutaneous coronary interventions (PCI)
  • their role in the treatment and prevention of stroke is limited and is currently under investigation

Glycoprotein IIb/IIIa receptors

  • glycoprotein receptors have two subunits, α, and β, which are responsible for platelet aggregation and adhesion
  • they are present on the platelet membrane and undergo a conformational change upon platelet activation, allowing them to adhere to each other
  • inhibitors bind to the receptor and prevent fibrinogen and von Willebrand factor (vWF) from binding to the receptors

Indications in neurology

Acute ischemic stroke

  • the use of GP IIb/IIIa inhibitors in acute ischemic stroke is the subject of ongoing research; their use is limited due to the risk of intracranial hemorrhage
  • guidelines do not recommend their routine use outside of clinical trials

Periprocedural complications (stent thrombosis, distal embolization)

  • can be used to treat thrombotic complications during endovascular procedures (such as intrastent thrombosis, distal embolization, etc.)
  • dosing is not standardized; the most commonly published doses are summarized in the tab below

Role in stroke prevention

  • GP IIb/IIIa inhibitors are currently not recommended for long-term stroke prevention

Contraindications

  • absolute: major bleeding diathesis, active major internal bleeding, and hemorrhagic stroke within 30 days
  • relative: history of stroke, thrombocytopenia, major surgery < 6 weeks, and decompensated hypertension

Adverse events

  • bleeding (especially when combined with other antithrombotic agents)
  • cardiovascular side effects such as hypotension and bradycardia
  • thrombocytopenia

Drugs and their dosing

Eptifibatid

(Integrilin) usually vial = 1mL/2mg or 1mL/0.75 mg

  • mechanism of action
    • a cyclic heptapeptide that specifically targets the glycoprotein IIb/IIIa receptor 
    • onset of action occurs in 1 hour; the effect of the drug lasts several hours (~ 4h)
  • dosing in neurology (from case series + derived from cardiology)
    • IV bolus:  0.2 mg/kg over 3-5 minutes, followed by infusion  (Sedat, 2014)
    • IV infusion:  5mL(10mg) + 45mL of NS (1mL=0.2 mg)  …… 3mL/h (0.6 mg/h)  or 0.125ug/kg/min (max 10ug/min!)
    • IA bolus:  5mL /10mg) + 45 mL of NS (1mL=0.2 mg) …… bolus 10 mL (2mg) every 5 minutes till max dose 10 mg

Abciximab

(REOPRO)   amp 5mL/10 mg

 

  • monoclonal antibody fragment (Fab) that binds to the GPIIb/IIIa receptor
  • half-life is short, but its effects on platelet function can last up to 24-48 hours
    • in cases where reversal of the antiplatelet effects is urgently needed, platelet transfusion can be considered
  • dosing:
    • IA:  1amp/5ml + 45 ml FR (1ml=0.2 mg) …… bolus 10 mL/2mg every 5 minutes to max dose of 10 mg |(50mL of the solution)
    • IV: bolus 0.25 mg/kg within 5 min followed by an infusion
      • 5mL/10mg + 45ml FR (1mL=0.2 mg)  at rate of   3mL/h (0.6 mg/h) or  0.125ug/kg/min (max 10ug/min!)
    • another dosing reported: 5 mg IA followed by  5 mg bolus IV  (Kittusamy, 2001)

Tirofiban

(Aggrastat)   

 

  • a non-peptide, small-molecule antagonist that binds to GP IIb/IIIa receptor
  • duration of action is 4 hours; it is dialyzable
  • dosing:
    • IV 0.4 µg/kg/min loading dose for 30 minutes (12 µg/kg in total)
    • followed by 0.1 µg/kg/min in a continuous infusion (12-24 hours)  (Seo, 2008)

Monitoring

  • monitor for signs and symptoms of bleeding or other AEs
  • check coagulation parameters and platelet count before and during infusion; usually 2-4 hours after the start of infusion and at 24 hours
    • if the platelet count falls below 100,000/mm during the infusion, discontinue the GP IIb/IIIa inhibitor
  • the glycoprotein IIb/IIIa inhibitors may need to be continued after the procedure in high-risk patients; such patients should be monitored closely in the ICU

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Glycoprotein IIb/IIIa inhibitors in stroke therapy and prevention
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