University of Hertfordshire

From the same journal

By the same authors

Metabolism of ticagrelor in patients with acute coronary syndromes.

Research output: Contribution to journalArticle

Documents

  • Piotr Adamski
  • Katarzyna Buszko
  • Joanna Sikora
  • Piotr Niezgoda
  • Malwina Barańska
  • Małgorzata Ostrowska
  • Przemysław Paciorek
  • Eliano P Navarese
  • Diana Gorog
  • Jacek Kubica
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Original languageEnglish
Article number11746
Number of pages8
Pages (from-to)1-8
JournalScientific Reports
Journal publication date6 Sep 2018
Volume8
Early online date6 Sep 2018
DOIs
Publication statusE-pub ahead of print - 6 Sep 2018

Abstract

Ticagrelor is a state-of-the-art antiplatelet agent used for the treatment of patients with acute coronary syndromes (ACS). Unlike remaining oral P2Y12 receptor inhibitors ticagrelor does not require metabolic activation to exert its antiplatelet action. Still, ticagrelor is extensively metabolized by hepatic CYP3A enzymes, and AR-C124910XX is its only active metabolite. A post hoc analysis of patient-level (n = 117) pharmacokinetic data pooled from two prospective studies was performed to identify clinical characteristics affecting the degree of AR-C124910XX formation during the first six hours after 180 mg ticagrelor loading dose in the setting of ACS. Both linear and multiple regression analyses indicated that ACS patients presenting with ST-elevation myocardial infarction or suffering from diabetes mellitus are more likely to have decreased rate of ticagrelor metabolism during the acute phase of ACS. Administration of morphine during ACS was found to negatively influence transformation of ticagrelor into AR-C124910XX when assessed with linear regression analysis, but not with multiple regression analysis. On the other hand, smoking appears to increase the degree of ticagrelor transformation in ACS patients. Mechanisms underlying our findings and their clinical significance warrant further research.

Notes

© The Author(s) 2018

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