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https://www.readbyqxmd.com/read/27366081/impact-of-selective-platelet-inhibition-in-reducing-cardiovascular-risk-role-of-vorapaxar
#1
REVIEW
Judy Wm Cheng
This article reviews the pharmacology, clinical efficacy, and safety of vorapaxar in reducing cardiovascular risk. Vorapaxar is a tricyclic himbacine-derived reversible inhibitor of platelet surface protease activator receptor-1, which prevents thrombin from activating platelets. Two Phase III clinical trials and multiple subanalyses from the two trials with vorapaxar have been published. In patients with recent acute coronary syndrome, vorapaxar, when added to standard therapy, did not reduce the composite cardiovascular end point...
2016: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/27290917/p2y12-receptor-antagonists-which-one-to-choose-a-systematic-review-and-meta-analysis
#2
Alexandros Briasoulis, Tesfaye Telila, Mohan Palla, Gerasimos Siasos, Dimitris Tousoulis
BACKGROUND: Pharmacological properties of the currently available P2Y12 receptor antagonists differ significantly and lead to different degrees of platelets inhibition and cardiovascular outcomes. METHODS: We performed a systematic review and meta-analysis of the comparative effects of newer antiplatelet agents versus clopidogrel on major adverse cardiovascular events (MACE), all-cause mortality, myocardial infarction (MI), stroke, major bleeding and stent thrombosis, in patients with acute coronary syndromes (ACS) and/or undergoing percutaneous coronary intervention (PCI)...
June 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/26402735/efficacy-and-safety-analysis-of-new-p2y12-inhibitors-versus-clopidogrel-in-patients-with-percutaneous-coronary-intervention-a-meta-analysis
#3
REVIEW
Xue-Dong Gan, Bao-Zhu Wei, Dong Fang, Qi Fang, Kai-Yong Li, Shi-Lan-Ying Ding, Song Peng, Jing Wan
OBJECTIVE: New P2Y12 inhibitors, classified as oral (prasugrel and ticagrelor) and intravenous (cangrelor and elinogrel) drugs, have shown improved antithrombotic effects compared with clopidogrel in patients with acute coronary syndrome (ACS) or patients undergoing percutaneous coronary intervention (PCI) in landmark trials. The purpose of this study was to perform a meta-analysis of randomized trials that compared new P2Y12 inhibitors with clopidogrel to determine their efficacy and safety in patients undergoing PCI...
December 2015: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/26245659/current-status-of-antiplatelet-therapy-in-acute-coronary-syndrome
#4
REVIEW
Debabrata Dash
Antiplatelet therapy is a first-line medical treatment for patients with acute coronary syndrome (ACS). As percutaneous coronary interventions (PCI) increase in number and complexity, more patients must be treated with antiplatelet therapy for cardiovascular diseases in which arterial thrombosis plays a major role. Current anti-platelet therapy is highly effective in preventing atherothrombotic complications. Nevertheless, a significant number of patients continue to experience recurrent complications despite being properly treated, due to pharmacokinetics and interactions of drugs, genetic background and increased thrombus formation...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/25954988/reappraisal-of-thienopyridine-pretreatment-in-patients-with-non-st-elevation-acute-coronary-syndrome-a-systematic-review-and-meta-analysis
#5
REVIEW
Anne Bellemain-Appaix, Mathieu Kerneis, Stephen A O'Connor, Johanne Silvain, Michel Cucherat, Farzin Beygui, Olivier Barthélémy, Jean-Philippe Collet, Laurent Jacq, François Bernasconi, Gilles Montalescot
OBJECTIVE: To investigate the effect of pretreatment with P2Y12 receptor inhibitors compared with no pretreatment on efficacy and safety of treatment of non-ST elevation acute coronary syndrome (ACS). DATA SOURCES: Two reviewers independently searched Medline, Embase, Cochrane Controlled Trials, and BioMed Central databases for randomized placebo controlled trials and observational studies from August 2001 to March 2014. STUDY ELIGIBILITY: Studies must have reported both all-cause mortality (primary efficacy endpoint) and major bleeding (safety endpoint) outcomes...
2014: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/25897998/efficacy-and-safety-of-p2y12-inhibitors-according-to-diabetes-age-gender-body-mass-index-and-body-weight-systematic-review-and-meta-analyses-of-randomized-clinical-trials
#6
REVIEW
Francesco Zaccardi, Dario Pitocco, Peter Willeit, Jari A Laukkanen
OBJECTIVE: The efficacy of antiplatelet drugs may differ in specific patient subgroups. We aimed to assess the efficacy and safety of the P2Y12 inhibitors clopidogrel, ticlopidine, prasugrel, ticagrelor, and cangrelor according to diabetes status, age, gender, body mass index, and body weight. METHODS: Randomized clinical trials (RCTs) of P2Y12 inhibitors reporting information on cardiovascular disease (defined as myocardial infarction, stroke, or cardiovascular death) and bleeding (defined as any bleeding) events among the subgroups diabetes and non-diabetes, age ≥65 and <65 year-old, men and women, body mass index ≥30 and <30 kg/m(2), and body weight ≥60 and <60 kg, were identified in Medline, Embase, Web of Science, and Cochrane Library on August 31st, 2014...
June 2015: Atherosclerosis
https://www.readbyqxmd.com/read/25700561/current-antiplatelet-agents-place-in-therapy-and-role-of-genetic-testing
#7
REVIEW
Eugene Yang
Antiplatelet therapies play a central role in reducing the risk of cardiovascular events such as myocardial infarction and stroke. While aspirin, a cyclo-oxygenase-1 inhibitor has been the cornerstone of antithrombotic treatment for several decades, P2Y12 receptor inhibitors cangrelor, clopidogrel, prasugrel, and ticagrelor and protease-activated receptor-1 antagonist vorapaxar, have emerged as additional therapies to reduce the risk of recurrent cardiovascular events in high-risk patients. Recent clinical trials evaluating the role of these agents and major society guideline updates for use of antiplatelet therapies for secondary prevention of cardiovascular events will be examined...
April 2015: Journal of Thrombosis and Thrombolysis
https://www.readbyqxmd.com/read/24534451/impact-of-new-oral-or-intravenous-p2y12-inhibitors-and-clopidogrel-on-major-ischemic-and-bleeding-events-in-patients-with-coronary-artery-disease-a-meta-analysis-of-randomized-trials
#8
REVIEW
Xiao-Fang Tang, Jing-Yao Fan, Jing Meng, Chen Jin, Jin-Qing Yuan, Yue-Jin Yang
OBJECTIVE: New P2Y12 inhibitors can be classified as oral (prasugrel and ticagrelor) and intravenous drugs (cangrelor and elinogrel). These P2Y12 inhibitors might be superior to clopidogrel for reducing ischemic events in patients with coronary artery disease (CAD). We performed a meta-analysis of randomized trials that compared new oral or intravenous P2Y12 inhibitors with clopidogrel to determine their efficacy and safety in patients. METHODS AND RESULTS: Twelve randomized, placebo-controlled studies and two subgroup analyses of included studies on ST-segment elevation myocardial infarction (STEMI) were included...
April 2014: Atherosclerosis
https://www.readbyqxmd.com/read/23863121/use-of-antiplatelet-drugs-in-the-treatment-of-acute-coronary-syndromes
#9
REVIEW
Wilbert S Aronow
Patients with unstable angina pectoris/non-ST-elevation myocardial infarction (NSTEMI) should be treated with dual antiplatelet therapy with the use of aspirin plus either clopidogrel, prasugrel, or ticagrelor depending on the clinical circumstances as discussed in this article. If ticagrelor is used, the dose of aspirin must not exceed 100 mg daily. Prasugrel must not be used in patients with a history of stroke or transient ischemic attack. Platelet glycoprotein IIb/IIIa inhibitors should not be used as part of triple antiplatelet drug therapy if there is an increased risk for bleeding or in non-high-risk patients such as those with a normal baseline cardiac troponin level, nondiabetics, and those aged 75 years and older in whom potential benefit may be significantly offset by the potential risk of bleeding...
August 2013: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/23848430/emerging-antithrombotic-drugs-for-acute-coronary-syndrome
#10
REVIEW
Yuichi J Shimada, Robert P Giugliano
INTRODUCTION: Acute coronary syndrome (ACS) encompasses acute myocardial infarction (MI) and unstable angina. Activation of platelets and coagulation cascade plays a central role in the development of ACS. Over the past decade, there have been substantial improvements in the strategies for secondary prevention of ACS, including the development of more potent oral antiplatelet agents such as prasugrel and ticagrelor. However, therapies with even better efficacy and safety profiles and more rapid onset and offset of action would be desirable...
September 2013: Expert Opinion on Emerging Drugs
https://www.readbyqxmd.com/read/23640798/udp-glucose-enhances-outward-k-currents-necessary-for-cell-differentiation-and-stimulates-cell-migration-by-activating-the-gpr17-receptor-in-oligodendrocyte-precursors
#11
Elisabetta Coppi, Giovanna Maraula, Marta Fumagalli, Paola Failli, Lucrezia Cellai, Elisabetta Bonfanti, Luca Mazzoni, Raffaele Coppini, Maria P Abbracchio, Felicita Pedata, Anna Maria Pugliese
In the developing and mature central nervous system, NG2 expressing cells comprise a population of cycling oligodendrocyte progenitor cells (OPCs) that differentiate into mature, myelinating oligodendrocytes (OLGs). OPCs are also characterized by high motility and respond to injury by migrating into the lesioned area to support remyelination. K(+) currents in OPCs are developmentally regulated during differentiation. However, the mechanisms regulating these currents at different stages of oligodendrocyte lineage are poorly understood...
July 2013: Glia
https://www.readbyqxmd.com/read/23391671/antiplatelet-drug-use-in-patients-with-non-st-segment-elevation-acute-coronary-syndromes
#12
REVIEW
Wilbert S Aronow
Patients with unstable angina pectoris/non-ST-segment elevation myocardial infarction have an acute coronary syndrome. These patients should be treated with dual antiplatelet therapy with the use of aspirin plus either clopidogrel, prasugrel, or ticagrelor, depending on the clinical circumstances. Prasugrel must not be used in patients with a history of stroke or transient ischemic attack. If ticagrelor is used, the dose of aspirin must not be > 100 mg daily. Platelet glycoprotein IIb/IIIa inhibitors should not be used as part of triple antiplatelet therapy if there is an increased risk for bleeding or in non-high-risk patients, such as those with a normal baseline cardiac troponin level, those without diabetes, and those aged ≥ 75 years for whom potential benefit may be significantly offset by the potential risk for bleeding...
January 2013: Postgraduate Medicine
https://www.readbyqxmd.com/read/22574644/improving-long-term-acs-management-is-there-a-role-for-the-new-antiplatelets
#13
REVIEW
Marc Cohen
Acute coronary syndrome (ACS) is a major health burden, resulting in increased hospital admissions and significant morbidity and mortality. Platelet activation, which leads to thrombin generation, is highly implicated in ACS, and antiplatelet agents represent the current standard of care. Established antiplatelet agents include acetylsalicylic acid (ASA), thienopyridines (clopidogrel, ticlopidine), and glycoprotein IIb/IIIa inhibitors. Recently, antiplatelet therapy for ACS has evolved to include more potent inhibitors (e...
October 2012: Journal of Interventional Cardiology
https://www.readbyqxmd.com/read/21895760/clinical-effects-and-outcomes-with-new-p2y12-inhibitors-in-acs
#14
REVIEW
Jean-Philippe Collet, Stephen O'Connor
Thienopyridines have become the cornerstone of treatment for percutaneous coronary intervention although no survival benefit has ever been shown with clopidogrel despite increasing loading doses. Newly developed P2Y12 inhibitors are more potent, more predictable, and have a faster onset of action than clopidogrel, characteristics that make them particularly attractive for high-risk percutaneous coronary intervention (PCI). Four new P2Y12 inhibitors have been tested each of them having particular individual properties...
February 2012: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/21511430/-myocardial-infarction-role-of-new-antiplatelet-agents
#15
REVIEW
Johanne Silvain, Anne Bellemain, Patrick Ecollan, Gilles Montalescot, Jean-Philippe Collet
Thienopyridines have become the cornerstone of treatment of percutaneous coronary intervention although no survival benefit has ever been shown with clopidogrel despite increasing loading doses. Newly developed P2Y(12) inhibitors are more potent, more predictable and have a faster onset of action than clopidogrel, characteristics that make them particularly attractive for high-risk PCI. Four new P2Y(12) inhibitors have been tested each of them having particular individual properties. Prasugrel is an oral prodrug leading to irreversible blockade of the P2Y(12) receptor and is approved worldwide for ACS PCI...
June 2011: La Presse Médicale
https://www.readbyqxmd.com/read/20426498/antiplatelet-drugs-do-we-need-new-options-with-a-reappraisal-of-direct-thromboxane-inhibitors
#16
REVIEW
Sergio Coccheri
This review describes the current status of antiplatelet therapy in prevention of cardiovascular events of an atherothrombotic nature. The efficacy of aspirin clearly outweighs bleeding risk in secondary prevention, with the relevant exception of patients with peripheral arterial disease (PAD). In trials of primary prevention, aspirin has a limited advantage, which is challenged by the risk of major bleeding. A typical example is primary prevention in type 2 diabetes mellitus, in which a number of trials and a recent meta-analysis have confirmed these limitations...
May 7, 2010: Drugs
https://www.readbyqxmd.com/read/20210760/advances-in-antiplatelet-therapy-for-stroke-prevention-the-new-p2y12-antagonists
#17
REVIEW
A Giossi, A Pezzini, E Del Zotto, I Volonghi, P Costa, D Ferrari, A Padovani
Thrombus formation at a site of arterial injury (eg, rupture of an atherosclerotic plaque in a carotid artery), a crucial step in the pathogenesis of cerebral ischemia, is initiated by the adhesion of platelets to the arterial wall. In vivo, activated platelets release adenosine diphosphate (ADP), whose binding to the platelet P2Y12 receptor elicits progressive and sustained platelet aggregation. As a result, this receptor has been a target for the development of clinically effective antiplatelet agents, such as the thienopyridines ticlopidine and, more recently, clopidogrel, the only two currently FDA-approved P2Y12 antagonists...
March 2010: Current Drug Targets
https://www.readbyqxmd.com/read/20094648/limitations-of-current-therapies-to-prevent-thrombosis-a-need-for-novel-strategies
#18
REVIEW
Jean-Etienne Fabre, Mark E Gurney
Bleeding limits the benefit of current anti-platelet drugs for preventing heart attacks and stroke. Aspirin and clopidogrel, the two most widely prescribed anti-platelet drugs, are metabolized to active compounds that covalently and irreversibly modify their respective therapeutic targets (COX1 and P2Y12). The enduring effects of aspirin and clopidogrel are of concern in patients receiving anti-platelet therapy who require emergency surgery as this places them at greater risk of haemorrhage. As clopidogrel must be activated by cytochrome P450 metabolism, recent pharmacogenomic studies have revealed that patients lacking a functional allele of CYP2C19 derive no therapeutic benefit from the drug...
February 2010: Molecular BioSystems
https://www.readbyqxmd.com/read/19262362/novel-antiplatelet-agents-in-development-prasugrel-ticagrelor-and-cangrelor-and-beyond
#19
REVIEW
Inna Shalito, Olga Kopyleva, Victor Serebruany
Coronary artery disease, stroke, and peripheral vascular disease are known as "atherothrombotic" manifestations of atherosclerosis. These devastating conditions remain the major contributor of mortality and disability in a modern Western world, with estimated direct and indirect cost for 403.1 billion dollars in the United States alone. The application of current evidence-based therapy including the administration of low-dose aspirin and standard of care with clopidogrel proved to exhibit absolute mortality reduction in the randomized clinical trials International Study for Infarct Survival and Clopidogrel and Metoprolol in Myocardial Infarction Trial among patients after acute vascular events...
September 2009: American Journal of Therapeutics
https://www.readbyqxmd.com/read/18991794/future-prospects-in-anti-platelet-therapy-a-review-of-potential-p2y12-and-thrombin-receptor-antagonists
#20
REVIEW
Nicholas B Norgard, Mazen Abu-Fadel
Atherothrombosis is an acute complication that develops on the surface of a ruptured atheromatous plaque or as a consequence of endothelial erosion that may cause myocardial infarction or ischemic stroke. Anti-platelet therapy has been highly effective at reducing atherothrombotic risk. However, patients continue to experience thrombotic events despite the use of agents such as aspirin and clopidogrel. Many of these events occur, in part, because of the inadequate response to these drugs. This has prompted the pursuit of novel agents with aspirations of optimizing anti-platelet therapy...
November 2008: Recent Patents on Cardiovascular Drug Discovery
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