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Molecules 2016, 21(3), 284; doi:10.3390/molecules21030284

New Approaches to the Role of Thrombin in Acute Coronary Syndromes: Quo Vadis Bivalirudin, a Direct Thrombin Inhibitor?

Department of Cardiology, Hospital Universitario Virgen de la Arrixaca, Instituto Murciano de Investigación Biosanitaria, IMIB-Arrixaca, Murcia 30120, Spain
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Author to whom correspondence should be addressed.
Academic Editor: Pedro J. B. Pereira
Received: 21 December 2015 / Revised: 20 February 2016 / Accepted: 23 February 2016 / Published: 27 February 2016
(This article belongs to the Special Issue Thrombin Inhibitors: Discovery and Design)
View Full-Text   |   Download PDF [730 KB, uploaded 27 February 2016]   |  

Abstract

The pathophysiology of acute coronary syndrome (ACS) involves platelet activation and thrombus formation after the rupture of atherosclerotic plaques. Thrombin is generated at the blood-plaque interface in association with cellular membranes on cells and platelets. Thrombin also amplifies the response to the tissue injury, coagulation and platelet response, so the treatment of ACS is based on the combined use of both antiplatelet (such as aspirin, clopidogrel, prasugrel and ticagrelor) and antithrombotic drugs (unfractionated heparin, enoxaparin, fondaparinux and bivalirudin). Bivalirudin competitively inhibits thrombin with high affinity, a predictable response from its linear pharmacokinetics and short action. However, a present remarkable controversy exists between the latest main Guidelines in Clinical Practice and the key trials evaluating the use of bivalirudin in ACS. The aim of this review is to update the development of bivalirudin, including pharmacological properties, obtained information from clinical trials evaluating efficacy and safety of bivalirudin in ACS; as well as the recommendations of clinical Guidelines. View Full-Text
Keywords: bivalirudin; STEMI; non-STEMI; ACS; thrombin bivalirudin; STEMI; non-STEMI; ACS; thrombin
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Esteve-Pastor, M.A.; Hernández-Romero, D.; Valdés, M.; Marín, F. New Approaches to the Role of Thrombin in Acute Coronary Syndromes: Quo Vadis Bivalirudin, a Direct Thrombin Inhibitor? Molecules 2016, 21, 284.

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