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Thienopyridines and other ADP-receptor antagonists.

Authors
  • Bernlochner, Isabell1
  • Sibbing, Dirk
  • 1 Deutsches Herzzentrum and 1. Medizinische Klinik rechts der Isar, Lazarettstrasse 36, 80636, München, Germany. , (Germany)
Type
Published Article
Journal
Handbook of experimental pharmacology
Publication Date
Jan 01, 2012
Issue
210
Pages
165–198
Identifiers
DOI: 10.1007/978-3-642-29423-5_7
PMID: 22918731
Source
Medline
License
Unknown

Abstract

Platelet P2Y12 receptor inhibition plays a pivotal role in preventing thrombotic vascular events in patients with ACS and in patients undergoing percutaneous coronary intervention (PCI). Among the P2Y12 receptor inhibitors, the group of thienopyridines include ticlopidine, clopidogrel and prasugrel, all of which are orally administered prodrugs leading to irreversible P2Y12 receptor inhibition. Non-thienopyridine derivatives including ticagrelor, cangrelor and elinogrel do not require metabolic activation and lead to a reversible P2Y12 receptor inhibition in contrast to thienopyridines. The extend of platelet inhibition is subject to the administered antiplatelet agent and influenced by individual genetic and clinical factors. Insufficient platelet inhibition, termed high platelet reactivity (HPR) is associated with an increased risk for ischemic events after PCI whereas exceeding platelet inhibition results in an increased bleeding risk. Pharmacologic properties and clinical outcome data differ substantially between the existing P2Y12 receptor inhibitors. Whether individualized antiplatelet treatment incorporating different P2Y12 receptor inhibitors improves patients' clinical outcomes warrants further investigation.

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