Ticagrelor in modern cardiology - an up-to-date review of most important aspects of ticagrelor pharmacotherapy

Expert Opin Pharmacother. 2018 Feb;19(2):103-112. doi: 10.1080/14656566.2017.1421634. Epub 2017 Dec 27.

Abstract

Introduction: Ticagrelor is a first drug of a new chemical class cyclopentyltriazolopyrimidines. It is an antiplatelet agent with a unique mechanism of action, allowing a direct and reversible competitive inhibition of P2Y12 receptor. According to newest guidelines, it is recommended for prevention of thrombotic events in patients with acute coronary syndromes. Moreover, it is preferred over clopidogrel, an older generation antiplatelet drug, and therefore gains more interest in modern cardiology and vascular medicine.

Areas covered: This review is a comprehensive and thorough summary of the most important findings on ticagrelor. Pharmacokinetics, pharmacogenetics, drug-drug interactions, adverse effects, efficacy in specific patient populations and off-label properties of ticagrelor are discussed in this paper. Moreover, the results from pivotal clinical trials are presented.

Expert opinion: Introduction of ticagrelor, a first directly-acting and reversible P2Y12 inhibitor, gave some new possibilities as the efficacy of older drugs was often insufficient. Despite some drawbacks, such as a risk of bleeding events or dyspnea, a rapid onset of action, consistency in the antiplatelet effect and reports on pleiotropic properties make this drug a promising candidate for a first-choice antiplatelet agent in patients with acute coronary events.

Keywords: Antiplatelet; P2Y12 inhibitors; adverse effects; diabetes mellitus; interactions; pharmacogenetics; pharmacokinetics.

Publication types

  • Review

MeSH terms

  • Acute Coronary Syndrome / drug therapy*
  • Adenosine / adverse effects
  • Adenosine / analogs & derivatives*
  • Adenosine / pharmacokinetics
  • Adenosine / therapeutic use
  • Cytochrome P-450 CYP2C19 / genetics
  • Drug Interactions
  • Dyspnea / etiology
  • Half-Life
  • Hemorrhage / etiology
  • Humans
  • Pharmacogenetics
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / pharmacokinetics
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Purinergic P2Y Receptor Antagonists / adverse effects
  • Purinergic P2Y Receptor Antagonists / pharmacokinetics
  • Purinergic P2Y Receptor Antagonists / therapeutic use
  • Ticagrelor

Substances

  • Platelet Aggregation Inhibitors
  • Purinergic P2Y Receptor Antagonists
  • Cytochrome P-450 CYP2C19
  • Ticagrelor
  • Adenosine