title: Pharmacokinetics and pharmacodynamics of ticagrelor when treating non-ST elevation acute coronary syndromes.
abstract: BACKGROUND
  ADP-induced platelet activation via P2Y12 receptor plays a pivotal role in the pathophysiology of arterial thrombosis and acute coronary syndrome. The value of dual antiplatelet therapy with the addition of the thienopyridine clopidogrel to aspirin has been widely established. Prasugrel, another thienopyridine, has demonstrated more potent platelet inhibition and efficacy than clopidogrel, although this drug requires metabolic activation and is associated with increased risk of bleedings.
  
  
  METHODS
  In this article, we discuss the role of ticagrelor in the management of non-ST elevation acute coronary syndromes treatment. We describe the unique pharmacokinetic and pharmacodynamic properties of this drug and the extensive data obtained by preclinical and Phase II and III clinical studies.
  
  
  CONCLUSIONS
  Current guidelines recommend ticagrelor, in addition to aspirin, for patients with non-ST-segment elevation acute coronary syndromes at moderate to high-risk regardless of initial therapeutic strategy. Benefit of ticagrelor, as regard mortality, may be related to off-target effects of the drug, especially those involving the metabolism of adenosine. Ticagrelor represents a cost-effective alternative in the spectrum of P2Y12 inhibitors; however, further studies are required to enable the physician to choose the most appropriate antiplatelet agent for each patient.
authors.affiliation: University Hospital, Cardiology Unit and Cardiothoracic Department, Policlinico Consorziale , Bari , Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Monitillo
authors.forename: Massimo
authors.initials: M
authors.lastname: Iacoviello
authors.forename: Pasquale
authors.initials: P
authors.lastname: Caldarola
authors.forename: Roberto
authors.initials: R
authors.lastname: Valle
authors.forename: Mario
authors.initials: M
authors.lastname: Chiatto
authors.forename: Nadia
authors.initials: N
authors.lastname: Aspromonte
mesh_terms: D054058:Acute Coronary Syndrome / Q000188:drug therapy* / Q000503:physiopathology; D000241:Adenosine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001241:Aspirin / Q000008:administration & dosage / Q000627:therapeutic use; D004359:Drug Therapy, Combination; D006470:Hemorrhage / Q000139:chemically induced; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D017410:Practice Guidelines as Topic; D058921:Purinergic P2Y Receptor Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D000077486:Ticagrelor
chemical_list: D010975:Platelet Aggregation Inhibitors; D058921:Purinergic P2Y Receptor Antagonists; D000077486:Ticagrelor; D000241:Adenosine; D001241:Aspirin
keywords: acute coronary syndromes; non-ST elevation myocardial infarction; pharmacodynamic; pharmacokinetic; platelet; ticagrelor; unstable angina