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Ticagrelor

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https://www.readbyqxmd.com/read/28097533/long-term-use-of-ticagrelor-in-patients-with-coronary-artery-disease
#1
REVIEW
Sara Ariotti, Giuseppe Gargiulo, Marco Valgimigli
PURPOSE OF REVIEW: This review aims to summarize and discuss safety and effectiveness of the long-term use of ticagrelor in patients with coronary artery disease (CAD). RECENT FINDINGS: Ticagrelor is an orally administered, direct, and reversible inhibitor of the P2Y12-platelet receptor. Long-term use of ticagrelor in patients with previous myocardial infarction (MI) has been investigated in the PEGASUS-TIMI-54 trial. Overall, 21,162 patients with a spontaneous MI 1 to 3 years before randomization were randomly assigned to ticagrelor 90 mg bid, ticagrelor 60 mg bid, or placebo...
January 2017: Current Cardiology Reports
https://www.readbyqxmd.com/read/28092426/incomplete-reversibility-of-platelet-inhibition-following-prolonged-exposure-to-ticagrelor
#2
A J Gerrits, J A Jakubowski, A Sugidachi, A D Michelson, A L Frelinger
INTRODUCTION: Ticagrelor is described as a reversible P2Y12 antagonist. However, residual platelet inhibition persists after discontinuation of ticagrelor when plasma levels are undetectable. We assessed the reversibility of platelet inhibition by ticagrelor and its active metabolite (T-AM) in comparison with cangrelor and prasugrel's active metabolite (P-AM). METHODS: Whole blood was treated in vitro with ~50% inhibitory concentrations of ticagrelor, T-AM, cangrelor, P-AM and assessed for ADP-stimulated activated GPIIb-IIIa and P-selectin and vasodilator stimulated phosphoprotein (VASP) platelet reactivity index (PRI) before and after 100-fold dilution...
January 16, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28089137/a-comparison-of-cangrelor-prasugrel-ticagrelor-and-clopidogrel-in-patients-undergoing-percutaneous-coronary-intervention-a-network-meta-analysis
#3
Peter C Westman, Michael J Lipinski, Rebecca Torguson, Ron Waksman
BACKGROUND: Newer P2Y12 inhibitors have more rapid onset of platelet inhibition compared with clopidogrel, especially the intravenous P2Y12 inhibitor cangrelor. Direct comparisons between cangrelor and oral P2Y12 inhibitors ticagrelor and prasugrel do not exist. Thus, we performed a network meta-analysis to directly and indirectly compare different P2Y12 inhibitors in patients undergoing percutaneous coronary intervention (PCI). METHODS: MEDLINE/PubMed and ClinicalTrials...
October 21, 2016: Cardiovascular Revascularization Medicine: Including Molecular Interventions
https://www.readbyqxmd.com/read/28070882/effect-of-a-180-mg-ticagrelor-loading-dose-on-myocardial-necrosis-in-patients-undergoing-elective-percutaneous-coronary-intervention-a-preliminary-study
#4
QuanFu Xu, YingGang Sun, Yi Zhang, Bo Liu, Lu Fang, ChengXing Shen, YiGang Li, Shu Meng
BACKGROUND: To examine whether a loading dose of ticagrelor on top of clopidogrel reduced post-percutaneous coronary intervention (PCI) myonecrosis. METHODS: Seventy seven coronary artery disease patients received a loading dose of 300 mg clopidogrel pre-PCI and were divided into three groups: group TT (n = 36): a loading dose of 180 mg ticagrelor pre-PCI, followed by ticagrelor 90 mg twice daily commencing one day post-PCI; group CT (n = 26): a maintenance dose of ticagrelor 90 mg twice daily; group CC (n = 15): clopidogrel 75 mg daily post-PCI...
January 10, 2017: Cardiology Journal
https://www.readbyqxmd.com/read/28066572/ticagrelor-and-heart-surgery-controversy-we-may-have-better-antiplatelet-options
#5
EDITORIAL
Victor Serebruany, Naida Bulaeva, Elena Golukhova
No abstract text is available yet for this article.
November 2016: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28065908/ticagrelor-but-not-clopidogrel-active-metabolite-displays-antithrombotic-properties-in-the-left-atrial-endocardium
#6
Martin F Reiner, Alexander Breitenstein, Erik W Holy, Martina Glanzmann, Heidi Amstalden, Simon F Stämpfli, Nicole R Bonetti, Volkmar Falk, Stephan Keller, Gianluigi Savarese, Stefano Benussi, Francesco Maisano, Thomas F Lüscher, Jürg H Beer, Jan Steffel, Giovanni G Camici
AIMS: Oral anticoagulation is considered standard therapy for stroke prevention in atrial fibrillation (AF). Endocardial activation triggers expression of pro-thrombotic mediators including tissue factor (TF) and plasminogen activator inhibitor-1 (PAI-1), and contributes to thrombus formation in the left atrial appendage (LAA) of AF patients. Recently, pleiotropic effects of specific P2Y12 receptor antagonists were demonstrated; however, whether these drugs possess antithrombotic effects on LAA endocardial cells currently remains unknown...
January 8, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28065907/platelet-reactivity-in-human-immunodeficiency-virus-infected-patients-on-dual-antiplatelet-therapy-for-an-acute-coronary-syndrome-the-evere2st-hiv-study
#7
Marie Hauguel-Moreau, Franck Boccara, Anders Boyd, Joe-Elie Salem, Delphine Brugier, Angélique Curjol, Jean-Sébastien Hulot, Mathieu Kerneis, Sophie Galier, Ariel Cohen, Gilles Montalescot, Jean-Philippe Collet, Johanne Silvain
AIM: To explore platelet reactivity on dual antiplatelet therapy (DAPT) of acute coronary syndrome (ACS) patients infected with HIV. METHODS AND RESULTS: Acute coronary syndrome patients infected with HIV (n = 80) were matched to ACS patients without HIV (n = 160) on age, sex, diabetes, and DAPT (aspirin 100%, clopidogrel 68%, prasugrel 31%, ticagrelor 1%). Platelet reactivity was evaluated after ACS (>30 days) by measuring residual platelet aggregation (RPA) to aspirin and to P2Y12 inhibitors with light transmission aggregometry (LTA), VerifyNow aspirin assay (ARU), and P2Y12 assay (PRU) and with the VASP platelet reactivity index (VASP-PRI)...
January 8, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28062136/p2y12-receptor-inhibition-with-prasugrel-and-ticagrelor-in-stemi-patients-after-fibrinolytic-therapy-analysis-from-the-sampa-randomized-trial
#8
Leonardo de F C Guimarães, Philippe Généreux, Diego Silveira, Antonio Eduardo Pesaro, Felipe Falcão, Bruno Robalinho C Barbosa, Cristiano Freitas de Souza, Francisco A H Fonseca, Cláudia Maria Rodrigues Alves, Antônio Carlos de Camargo Carvalho, Gregg W Stone, Adriano Caixeta
BACKGROUND: A pharmacodynamic comparison between ticagrelor and prasugrel after fibrinolytic therapy has not yet been performed. METHODS: In the single-center SAMPA trial, 50 consecutive STEMI patients previously treated with clopidogrel and undergoing a pharmacoinvasive strategy were randomized to either a ticagrelor (n=25) 180mg loading dose followed by 90mg bid, or a prasugrel (n=25) 60mg loading dose followed by 10mg/day, initiated after fibrinolytic therapy but before angiography...
December 27, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/28058211/organ-transplantation-and-drug-eluting-stents-perioperative-challenges
#9
REVIEW
Aparna Dalal
Patients listed for organ transplant frequently have severe coronary artery disease (CAD), which may be treated with drug eluting stents (DES). Everolimus and zotarolimus eluting stents are commonly used. Newer generation biolimus and novolimus eluting biodegradable stents are becoming increasingly popular. Patients undergoing transplant surgery soon after the placement of DES are at increased risk of stent thrombosis (ST) in the perioperative period. Dual antiplatelet therapy (DAPT) with aspirin and a P2Y12 inhibitor such as clopidogrel, prasugrel and ticagrelor is instated post stenting to decrease the incident of ST...
December 24, 2016: World Journal of Transplantation
https://www.readbyqxmd.com/read/28056791/ticagrelor-induced-systemic-inflammatory-response-syndrome
#10
Philipp Krisai, Manuel Haschke, Peter T Buser, Christian Mueller
BACKGROUND: Ticagrelor is a reversible and direct-acting oral antagonist of the adenosine diphosphate receptor P2Y12. Possible adenosine-mediated effects of ticagrelor on inflammation are complex and incompletely understood. To our knowledge, ticagrelor-induced systemic inflammatory response syndrome (SIRS) has not yet been described. CASE PRESENTATION: We report the case of an 84 years old patient presenting with SIRS subsequent to initiation of ticagrelor after implantation of two drug eluting stents...
January 6, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28052578/ticagrelor-increased-adenosine-and-cyclic-adenosine-monophosphate-plasma-concentration-compared-with-clopidogrel-in-acute-coronary-syndromes-patients
#11
Xiao-Ye Li, Qi-Bing Wang, Ying Xue, Jia-Hui Chen, Qian-Zhou Lv
Ticagrelor produces a more potent antiplatelet effect than clopidogrel, and inhibits cellular uptake of adenosine, which is associated with several cardiovascular consequences. We aimed to explore the correlation between adenosine and cyclic adenosine monophosphate (cAMP) plasma concentration and antiplatelet effect by clopidogrel or ticagrelor in acute coronary syndrome (ACS) patients receiving dual antiplatelet therapy (DAPT). We conducted a prospective, observational and single-centre cohort study enrolling 68 patients with non-ST-segment elevation ACS from January 2016 to May 2016...
January 4, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28049954/no-effect-of-slco1b1-and-cyp3a4-5-polymorphisms-on-the-pharmacokinetics-and-pharmacodynamics-of-ticagrelor-in-healthy-chinese-male-subjects
#12
Mupeng Li, Yaodong Hu, Huilan Li, Zhipeng Wen, Xiaolei Hu, Daoyu Zhang, Yanjiao Zhang, Jian Xiao, Jie Tang, Xiaoping Chen
Ticagrelor is a direct-acting P2Y12 receptor antagonist. It is rapidly absorbed and partly metabolized to the active metabolite AR-C124910XX by CYP3A4 and CYP3A5. Three genetic loci (SLCO1B1, CYP3A4, and UGT2B7) were reported to affect ticagrelor pharmacokinetics. This study aimed to investigate the possible effects of SLCO1B1 and CYP3A4/5 genetic polymorphisms on the pharmacokinetics and pharmacodynamics of ticagrelor in healthy Chinese male volunteers. Eighteen healthy male volunteers who participated in pharmacogenetics study of ticagrelor were genotyped for SLCO1B1 rs113681054, SLCO1B1*5 (rs4149056), CYP3A4*1G (rs2242480), and CYP3A5*3 (rs776746)...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28045759/efficacy-and-safety-of-novel-oral-p2y12-receptor-inhibitors-in-st-segment-elevation-myocardial-infarction-patients-undergoing-pci-a-systematic-review-and-meta-analysis
#13
Jianjun Sun, Qian Xiang, Chao Li, Zining Wang, Kun Hu, Qiufen Xie, Yimin Cui
The efficacy and safety of novel oral P2Y12 receptor inhibitors (prasugrel and ticagrelor) are subjects of contention in ST-segment elevation myocardial infarction (STEMI) patients undergoing PCI, the optimal duration of therapy remains uncertain. We searched PubMed, Embase, Cochrane Library, CNKI, VIP, and WanFang Data to identify randomized controlled trials comparing novel oral P2Y12 receptor inhibitors to clopidogrel in STEMI patients undergoing PCI until February 2016. The primary efficacy and safety endpoint were all-cause mortality and major/minor bleeding...
January 3, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28041785/a-semi-quantitative-translational-pharmacology-analysis-to-understand-the-relationship-between-in-vitro-ent1-inhibition-and-the-clinical-incidence-of-dyspnoea-and-bronchospasm
#14
Lyn Rosenbrier Ribeiro, R Ian Storer
Adenosine contributes to the pathophysiology of respiratory disease, and adenosine challenge leads to bronchospasm and dyspnoea in patients. The equilibrative nucleoside transporter 1 (ENT1) terminates the action of adenosine by removal from the extracellular environment. Therefore, it is proposed that inhibition of ENT1 in respiratory disease patients leads to increased adenosine concentrations, triggering bronchospasm and dyspnoea. This study aims to assess the translation of in vitro ENT1 inhibition to the clinical incidence of bronchospasm and dyspnoea in respiratory disease, cardiovascular disease and healthy volunteer populations...
December 29, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28028070/ticagrelor-but-not-clopidogrel-reduces-arterial-thrombosis-via-endothelial-tissue-factor-suppression
#15
Martin F Reiner, Alexander Akhmedov, Simona Stivala, Stephan Keller, Daniel S Gaul, Nicole R Bonetti, Gianluigi Savarese, Martina Glanzmann, Cuicui Zhu, Wolfram Ruf, Zhihong Yang, Christian M Matter, Thomas F Lüscher, Giovanni G Camici, Juerg H Beer
AIMS: The P2Y12 antagonist ticagrelor reduces mortality in patients with acute coronary syndrome (ACS), compared with clopidogrel, and the mechanisms underlying this effect are not clearly understood. Arterial thrombosis is the key event in ACS; however, direct vascular effects of either ticagrelor or clopidogrel with focus on arterial thrombosis and its key trigger tissue factor have not been previously investigated. METHODS AND RESULTS: Human aortic endothelial cells were treated with ticagrelor or clopidogrel active metabolite (CAM) and stimulated with tumour necrosis factor-alpha (TNF-α); effects on procoagulant tissue factor (TF) expression and activity, its counter-player TF pathway inhibitor (TFPI) and the underlying mechanisms were determined...
November 15, 2016: Cardiovascular Research
https://www.readbyqxmd.com/read/28025947/genetics-in-the-clinical-decision-of-antiplatelet-treatment
#16
Gerasimos Siasos, Marina Zaromitidou, Evangelos Oikonomou, Manolis Vavuranakis, Vicky Tsigkou, Nikolaos Papageorgiou, Dimitrios Chaniotis, Dimitrios A Vrachatis, Christodoulos Stefanadis, Athanasios G Papavassiliou, Dimitrios Tousoulis
BACKGROUND: Coronary artery disease remains the leading cause of death globally. Dual antiplatelet treatment with aspirin and aP2Y12 receptor significantly reduces thrombotic events. However, antiplatelet drug response displays considerable interindividual variability. METHODS: Genetic factors account for up to 70% of impaired drug response. A number of genes encoding proteins involved in the pharmacokinetic pathway have been found to alter drug response. RESULTS: According to most studies, CYP2C19 gene is the strongest genetic determinant...
December 26, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28025925/contemporary-trends-in-oral-antiplatelet-agent-use-in-patients-treated-with-percutaneous-coronary-intervention-for-acute-coronary-syndrome
#17
Kibum Kim, Todd A Lee, Daniel R Touchette, Robert J DiDomenico, Amer K Ardati, Surrey M Walton
BACKGROUND: Recent trials demonstrated the efficacy of prasugrel and ticagrelor compared with clopidogrel in the reduction of cardiovascular complications in patients with acute coronary syndrome (ACS). However, it is unclear how use of the 3 antiplatelet medications has changed in commercially insured patients since the advent of the new agents. OBJECTIVES: To (a) describe the adoption of prasugrel and ticagrelor in patients who received percutaneous coronary intervention (PCI) for the onset of ACS and (b) explore patient factors associated with the selection of the drug to provide insight into utilization patterns of these antiplatelet agents...
January 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28017673/outcome-after-surgery-for-acute-aortic-dissection-influence-of-preoperative-antiplatelet-therapy-on-prognosis
#18
Raphaelle Avigael Chemtob, Hasse Moeller-Soerensen, Lene Holmvang, Peter Skov Olsen, Hanne Berg Ravn
OBJECTIVES: Outcome in patients with acute coronary syndrome (ACS) is improved with dual antiplatelet therapy (DAPT). Patients with acute aortic dissection type A (AAD) often present with similar symptoms and may therefore be prescribed DAPT before diagnosis. The aim of this study was to evaluate the use of antiplatelet therapy (APT) prior to AAD surgery and patient outcome, including indications according to the European Society of Cardiology's (ESC) recent guidelines. DESIGN: A retrospective, observational study...
October 11, 2016: Journal of Cardiothoracic and Vascular Anesthesia
https://www.readbyqxmd.com/read/28007881/platelet-function-recovery-after-ticagrelor-withdrawal-in-patients-awaiting-urgent-coronary-surgery
#19
Emma C Hansson, Carl Johan Malm, Camilla Hesse, Björn Hornestam, Mikael Dellborg, Helena Rexius, Anders Jeppsson
OBJECTIVE: Dual antiplatelet therapy with ticagrelor and aspirin is associated with an increased risk of perioperative bleeding complications. Current guidelines recommend therefore discontinuation of ticagrelor 5 days before surgery to allow sufficient recovery of platelet function. It is not known how the time to recovery varies between individual patients after discontinuation of ticagrelor. METHODS: Twenty-five patients accepted for urgent coronary artery bypass surgery and treated with ticagrelor and aspirin were included in a prospective observational study...
December 22, 2016: European Journal of Cardio-thoracic Surgery
https://www.readbyqxmd.com/read/28004060/switching-from-ticagrelor-to-clopidogrel-new-answers-and-further-questions
#20
Francesco Franchi, Fabiana Rollini
No abstract text is available yet for this article.
December 22, 2016: Thrombosis and Haemostasis
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