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Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety
Dual antiplatelet therapy, composed of aspirin plus a P2Y(12)-receptor antagonist, is the cornerstone of treatment for patients with acute coronary syndrome (ACS). A number of U.S. Food and Drug Administration–approved P2Y(12)-receptor antagonists are available for treating patients with ACS, includ...
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BlackWell Publishing Ltd
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4282310/ https://www.ncbi.nlm.nih.gov/pubmed/25164528 http://dx.doi.org/10.1002/phar.1477 |
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author | Dobesh, Paul P Oestreich, Julie H |
author_facet | Dobesh, Paul P Oestreich, Julie H |
author_sort | Dobesh, Paul P |
collection | PubMed |
description | Dual antiplatelet therapy, composed of aspirin plus a P2Y(12)-receptor antagonist, is the cornerstone of treatment for patients with acute coronary syndrome (ACS). A number of U.S. Food and Drug Administration–approved P2Y(12)-receptor antagonists are available for treating patients with ACS, including the thienopyridine compounds clopidogrel and prasugrel. Ticagrelor, the first of a new class of antiplatelet agents, is a noncompetitive, direct-acting P2Y(12)-receptor antagonist. Unlike the thienopyridine compounds, ticagrelor does not require metabolism for activity. Also, whereas clopidogrel and prasugrel are irreversible inhibitors of the P2Y(12) receptor, ticagrelor binds reversibly to inhibit receptor signaling and subsequent platelet activation. In pharmacodynamic studies, ticagrelor demonstrated faster onset and more potent inhibition of platelet aggregation than clopidogrel. These properties of ticagrelor may contribute to reduced rates of thrombotic outcomes compared with clopidogrel, as demonstrated in a phase III clinical trial. However, in addition to bleeding, distinctive adverse effects of this new chemical entity have not been reported with the thienopyridine P2Y(12)-receptor inhibitors. Although ticagrelor represents an advancement in P2Y(12)-receptor inhibition therapy, a thorough understanding of this compound as an antiplatelet therapy remains to be elucidated. |
format | Online Article Text |
id | pubmed-4282310 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | BlackWell Publishing Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-42823102015-01-15 Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety Dobesh, Paul P Oestreich, Julie H Pharmacotherapy Reviews of Therapeutics Dual antiplatelet therapy, composed of aspirin plus a P2Y(12)-receptor antagonist, is the cornerstone of treatment for patients with acute coronary syndrome (ACS). A number of U.S. Food and Drug Administration–approved P2Y(12)-receptor antagonists are available for treating patients with ACS, including the thienopyridine compounds clopidogrel and prasugrel. Ticagrelor, the first of a new class of antiplatelet agents, is a noncompetitive, direct-acting P2Y(12)-receptor antagonist. Unlike the thienopyridine compounds, ticagrelor does not require metabolism for activity. Also, whereas clopidogrel and prasugrel are irreversible inhibitors of the P2Y(12) receptor, ticagrelor binds reversibly to inhibit receptor signaling and subsequent platelet activation. In pharmacodynamic studies, ticagrelor demonstrated faster onset and more potent inhibition of platelet aggregation than clopidogrel. These properties of ticagrelor may contribute to reduced rates of thrombotic outcomes compared with clopidogrel, as demonstrated in a phase III clinical trial. However, in addition to bleeding, distinctive adverse effects of this new chemical entity have not been reported with the thienopyridine P2Y(12)-receptor inhibitors. Although ticagrelor represents an advancement in P2Y(12)-receptor inhibition therapy, a thorough understanding of this compound as an antiplatelet therapy remains to be elucidated. BlackWell Publishing Ltd 2014-10 2014-08-28 /pmc/articles/PMC4282310/ /pubmed/25164528 http://dx.doi.org/10.1002/phar.1477 Text en © 2014 The Authors. Pharmacotherapy published by Wiley Periodicals, Inc. on behalf of Pharmacotherapy Publications, Inc. http://creativecommons.org/licenses/by-nc-nd/3.0/ This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made. |
spellingShingle | Reviews of Therapeutics Dobesh, Paul P Oestreich, Julie H Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title | Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title_full | Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title_fullStr | Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title_full_unstemmed | Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title_short | Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety |
title_sort | ticagrelor: pharmacokinetics, pharmacodynamics, clinical efficacy, and safety |
topic | Reviews of Therapeutics |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4282310/ https://www.ncbi.nlm.nih.gov/pubmed/25164528 http://dx.doi.org/10.1002/phar.1477 |
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