How to optimise clopidogrel therapy? Reducing the low-response incidence by aggregometry-guided therapy modification

Thromb Haemost. 2008 Feb;99(2):357-62. doi: 10.1160/TH07-10-0624.

Abstract

The inhibitory platelet effect of clopidogrel is insufficient in approximately 5 to 30% of patients. These low responders (LR) face a significantly higher risk of cardiovascular complications. The therapeutic management of LR is still undefined. In the present study, we evaluate a novel therapeutic algorithm to reduce the incidence of clopidogrel resistance. One hundred sixty-one patients on 100 mg of aspirin co-medication underwent elective coronary stenting and were given an initial dosage of 600 mg clopidogrel, followed by 75 mg clopidogrel daily. 48 h later, the platelet responsiveness was tested with ADP (5-20 microM) stimulation by impedance aggregometry (Chronolog 590). A significant rise in impedance (>5 Omega after 6 minutes, aggregation index >65%) was defined as LR. In this subgroup, platelets were stimulated with the selective P2Y(12)-ADP receptor antagonist 2-MeS-AMP. One hundred twenty-three patients were clopidogrel-responders (76.4%) and 38 patients were LR (23.6%). A defect of the ADP-receptor P2Y(12) was found in three out of 38 LR (7.9%). Inhibition of platelet aggregation indicating clopidogrel-responsiveness was achieved with either a clopidogrel high-dose regimen (22/38, 57.9%); a repeat loading dose, doubling the maintenance dose) or with an alternative therapy with ticlopidine (8/38 (21.1%); 250 mg twice daily). Thus the incidence of LR was reduced from 23.6% to 5.0%. Our aggregometer-guided therapeutic algorithm reduced the relative percentage of clopidogrel LR by 78.9%. This approach could prove to be helpful in achieving a further decrease in the incidence of clopidogrel resistance.

MeSH terms

  • Adenosine Diphosphate / analogs & derivatives
  • Aged
  • Algorithms
  • Angioplasty, Balloon, Coronary / adverse effects*
  • Angioplasty, Balloon, Coronary / instrumentation
  • Aspirin / administration & dosage
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Cardiovascular Diseases / blood
  • Cardiovascular Diseases / etiology
  • Cardiovascular Diseases / prevention & control*
  • Clinical Protocols
  • Clopidogrel
  • Coronary Artery Disease / blood
  • Coronary Artery Disease / drug therapy
  • Coronary Artery Disease / therapy*
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Drug Monitoring / methods*
  • Drug Resistance*
  • Feasibility Studies
  • Female
  • Humans
  • Male
  • Middle Aged
  • Pilot Projects
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / administration & dosage*
  • Platelet Function Tests
  • Prospective Studies
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2 / blood
  • Receptors, Purinergic P2Y12
  • Stents
  • Ticlopidine / administration & dosage
  • Ticlopidine / analogs & derivatives*

Substances

  • P2RY12 protein, human
  • Platelet Aggregation Inhibitors
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2Y12
  • Adenosine Diphosphate
  • Clopidogrel
  • Ticlopidine
  • Aspirin