Metabolism of ticagrelor in patients with acute coronary syndromes.
Article Details
- CitationCopy to clipboard
Adamski P, Buszko K, Sikora J, Niezgoda P, Baranska M, Ostrowska M, Paciorek P, Navarese EP, Gorog DA, Kubica J
Metabolism of ticagrelor in patients with acute coronary syndromes.
Sci Rep. 2018 Aug 6;8(1):11746. doi: 10.1038/s41598-018-29619-9.
- PubMed ID
- 30082687 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Ticagrelor Cytochrome P450 3A5 Protein Humans UnknownSubstrateActivatorDetails - Drug Reactions
Reaction Details - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareTicagrelorLumacaftor The metabolism of Ticagrelor can be increased when combined with Lumacaftor. TicagrelorApalutamide The metabolism of Ticagrelor can be increased when combined with Apalutamide. TicagrelorFosphenytoin The metabolism of Ticagrelor can be increased when combined with Fosphenytoin. TicagrelorCarbamazepine The metabolism of Ticagrelor can be increased when combined with Carbamazepine. TicagrelorRifamycin The metabolism of Ticagrelor can be increased when combined with Rifamycin.
