Flow cytometric monitoring of glycoprotein IIb/IIIa blockade and platelet function in patients with acute myocardial infarction receiving reteplase, abciximab, and ticlopidine: continuous platelet inhibition by the combination of abciximab and ticlopidine

Circulation. 2000 Sep 26;102(13):1490-6. doi: 10.1161/01.cir.102.13.1490.

Abstract

Background: Improvement of thrombolysis may be achieved by concomitant strong platelet inhibition. To monitor platelet function in patients with myocardial infarction (n=46) who were treated with the fibrinolytic agent reteplase, the glycoprotein (GP) IIb/IIIa blocker abciximab, and the ADP receptor antagonist ticlopidine, we developed a flow cytometric assay.

Methods and results: Binding of abciximab to platelets was directly monitored as the percentage of platelets stained by a goat anti-mouse antibody. Blood drawn 10 minutes and 2 hours after the start of therapy with reteplase and abciximab and during the 12-hour infusion of abciximab demonstrated a maximal blockade of GP IIb/IIIa (10 minutes, 86.2+/-10.3%; 12 hours, 85.8+/-7.1%). Starting at 24 hours, abciximab binding gradually decreased (24 hours, 74.6+/-16.2%; 48 hours, 66.8+/-14.9%; 72 hours, 60.5+/-16.7%; 96 hours, 49.4+/-17.8%; 120 hours, 35.8+/-16. 4%; and 144 hours, 29.9+/-15.3%). Binding of a chicken anti-fibrinogen antibody to platelets, indicating the level of functional blockade of GP IIb/IIIa, was inversely correlated with the binding of abciximab (r=-0.72, P:<0.0001). In blood drawn at 10 minutes, platelet aggregation was maximally inhibited but recovered within 48 hours even if the majority of GP IIb/IIIa receptors were still blocked by abciximab. Reteplase did not influence abciximab binding and did not activate platelets, as measured by P-selectin expression, fibrinogen binding, and platelet aggregation. Platelet inhibition that was achieved during the first 24 hours by abciximab was directly maintained by additional treatment with ticlopidine.

Conclusions: Flow cytometric monitoring of platelet function allows differentiation of the effects of reteplase, abciximab, and ticlopidine. The combination of abciximab and ticlopidine is an attractive therapeutic strategy that provides a fast and continuous platelet inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abciximab
  • Aged
  • Antibodies, Monoclonal / blood
  • Antibodies, Monoclonal / therapeutic use*
  • Blood Platelets / drug effects*
  • Blood Platelets / physiology
  • Female
  • Fibrinolytic Agents / blood
  • Fibrinolytic Agents / therapeutic use*
  • Flow Cytometry
  • Humans
  • Immunoglobulin Fab Fragments / blood
  • Immunoglobulin Fab Fragments / therapeutic use*
  • Male
  • Middle Aged
  • Myocardial Infarction / blood*
  • Myocardial Infarction / drug therapy*
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / blood
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Platelet Glycoprotein GPIIb-IIIa Complex / drug effects*
  • Recombinant Proteins / blood
  • Recombinant Proteins / therapeutic use*
  • Ticlopidine / blood
  • Ticlopidine / therapeutic use*
  • Time Factors
  • Tissue Plasminogen Activator / blood
  • Tissue Plasminogen Activator / therapeutic use*

Substances

  • Antibodies, Monoclonal
  • Fibrinolytic Agents
  • Immunoglobulin Fab Fragments
  • Platelet Aggregation Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Recombinant Proteins
  • reteplase
  • Tissue Plasminogen Activator
  • Ticlopidine
  • Abciximab