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Ticagrelor

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https://www.readbyqxmd.com/read/27922911/meta-analysis-of-comparison-of-the-newer-p2y12-inhibitors-oral-preparation-or-intravenous-to-clopidogrel-in-patients-with-acute-coronary-syndrome
#1
Lu Zhang, Jun Lu, Weihua Dong, Huiping Tian, Weiyi Feng, Haisheng You, Hairong He, Jing Ma, Yalin Dong
AIMS: New P2Y12 adenosine diphosphate receptor antagonist that has been used in the treatment of acute coronary syndrome (ACS) with mixed results. This systematic review analyzed and compared the evidence from large, clinical trials regarding the efficacy of clopidogrel relative to that of cangrelor, prasugrel, and ticagrelor in reducing the incidence of cardiovascular events in patients with ACS. METHODS AND RESULTS: This analysis of the findings for comparing newer P2Y12 inhibitors with clopidogrel of 13 clinical trials involving a total of 87,985 patients with ACS ...
November 29, 2016: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/27920235/successful-reversal-of-bradycardia-and-dyspnea-with-aminophylline-after-ticagrelor-load
#2
Sarah A Minner, Pamela Simone, Benjamin B Chung, Atman P Shah
A 69-year-old male underwent elective percutaneous coronary intervention requiring placement of a drug-eluting stent to the first obtuse marginal artery. Four hours following the administration of a ticagrelor loading dose, he developed dyspnea and sinus pauses. Aminophylline was administered and resulted in immediate and sustained symptom resolution. Ticagrelor has been associated with dyspnea and bradyarrhythmias, both attributed to increased adenosine exposure. Ticagrelor inhibits reuptake of intracellular adenosine...
December 5, 2016: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/27914492/ticagrelor-with-aspirin-or-alone-in-high-risk-patients-after-coronary-intervention-rationale-and-design-of-the-twilight-study
#3
Usman Baber, George Dangas, David J Cohen, C Michael Gibson, Shamir R Mehta, Dominick J Angiolillo, Stuart J Pocock, Mitchell W Krucoff, Adnan Kastrati, E Magnus Ohman, Philippe Gabriel Steg, Juan Badimon, M Urooj Zafar, Jaya Chandrasekhar, Samantha Sartori, Melissa Aquino, Roxana Mehran
BACKGROUND: Dual antiplatelet therapy (DAPT) is necessary to prevent thrombosis yet increases bleeding after percutaneous coronary intervention (PCI) with drug-eluting stents (DES). Antiplatelet monotherapy with a potent P2Y12 receptor antagonist may reduce bleeding while maintaining anti thrombotic efficacy compared with conventional DAPT. METHODS: TWILIGHT is a randomized, double-blind placebo-controlled trial evaluating the comparative efficacy and safety of antiplatelet monotherapy versus DAPT in up to 9000 high-risk patients undergoing PCI with DES...
December 2016: American Heart Journal
https://www.readbyqxmd.com/read/27905478/vascular-disease-ticagrelor-not-superior-to-clopidogrel-for-pad
#4
Irene Fernández-Ruiz
No abstract text is available yet for this article.
December 1, 2016: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/27904901/effect-of-ticagrelor-on-endothelial-calcium-signalling-and-barrier-function
#5
Dursun Gündüz, Christian Tanislav, Klaus-Dieter Schlüter, Rainer Schulz, Christian Hamm, Muhammad Aslam
The P2Y12 receptor is a Gi-coupled receptor whose activation inhibits adenylyl cyclase and thereby reduces the concentration of intracellular cAMP. Here the hypothesis was tested whether AR-C 66096 or ticagrelor, two direct-acting and reversibly binding P2Y12 receptor antagonists, protect endothelial cell (EC) barrier function by raising intracellular cAMP in ECs. The study was carried out on primary human umbilical vein ECs (HUVECs) and human pulmonary microvascular ECs (hPMECs). AR-C66096 (10 µM) induced a 50 % increase in cAMP in ECs whereas ticagrelor (2-10 µM) had no effect...
December 1, 2016: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/27899747/ticagrelor-in-acute-stroke-or-transient-ischemic-attack-in-asian-patients-from-the-socrates-trial-acute-stroke-or-transient-ischemic-attack-treated-with-aspirin-or-ticagrelor-and-patient-outcomes
#6
Yongjun Wang, Kazuo Minematsu, Ka Sing Lawrence Wong, Pierre Amarenco, Gregory W Albers, Hans Denison, J Donald Easton, Scott R Evans, Peter Held, Jenny Jonasson, Carlos A Molina, S Claiborne Johnston
BACKGROUND AND PURPOSE: In the SOCRATES trial (Acute Stroke or Transient Ischemic Attack Treated With Aspirin or Ticagrelor and Patient Outcomes), ticagrelor was not superior to aspirin. Because of differences in patient demographics and stroke disease pattern in Asia, outcomes of ticagrelor versus aspirin were assessed among Asian patients in a prespecified exploratory analysis. METHODS: Baseline demographics, treatment effects, and safety of ticagrelor and aspirin were assessed among Asian patients...
November 29, 2016: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/27886822/ticagrelor-effects-beyond-the-p2y12-receptor
#7
REVIEW
Wael Sumaya, Robert F Storey
Platelet P2Y12 receptor inhibitors are crucial in the treatment of patients with acute coronary syndrome or undergoing percutaneous coronary intervention. Ticagrelor is a reversibly binding, potent oral P2Y12 inhibitor that also is a weak inhibitor of the equilibrative nucleoside transporter-1 pathway for cellular adenosine uptake. It is hypothesized that ticagrelor has clinically relevant "off-target" effects, independent of its effect on platelet aggregation and thrombosis. This review considers the pleiotropic effects of ticagrelor and some of the possible mechanisms related to these effects...
January 2017: Interventional cardiology clinics
https://www.readbyqxmd.com/read/27886818/genetic-determinants-of-p2y12-inhibitors-and-clinical-implications
#8
REVIEW
Larisa H Cavallari, Aniwaa Owusu Obeng
There is significant interpatient variability in clopidogrel effectiveness, which is due in part to cytochrome P450 (CYP) 2C19 genotype. Approximately 30% of individuals carry CYP2C19 loss-of-function alleles, which have been consistently shown to reduce clopidogrel effectiveness after an acute coronary syndrome and percutaneous coronary intervention. Guidelines recommend consideration of prasugrel or ticagrelor in these patients. A clinical trial examining outcomes with CYP2C19 genotype-guided antiplatelet therapy is ongoing...
January 2017: Interventional cardiology clinics
https://www.readbyqxmd.com/read/27885888/cangrelor-in-combination-with-ticagrelor-provides-consistent-and-potent-p2y12-inhibition-during-and-after-primary-percutaneous-coronary-intervention-in-real-world-patients-with-st-segment-elevation-myocardial-infarction
#9
Moman A Mohammad, Pontus Andell, Sasha Koul, Stefan James, Fredrik Scherstén, Matthias Götberg, David Erlinge
Patients pretreated with ticagrelor with less than 1 hour from percutaneous coronary intervention (PCI) or receiving ticagrelor in cath lab were prospectively included and received cangrelor. Cangrelor was infused for 2 hours and platelet function was assessed as P2Y12 reactivity units (PRU) with the VerifyNow P2Y12 function assay before start of infusion, 15 min after the start of infusion, and 30 min after the end of infusion. A total of n = 32 patients with an average age of 68 (±13) years with n = 22 (69%) males were included...
November 25, 2016: Platelets
https://www.readbyqxmd.com/read/27885768/gram-scale-synthesis-of-chiral-cyclopropane-containing-drugs-and-drug-precursors-with-engineered-myoglobin-catalysts-featuring-complementary-stereoselectivity
#10
Priyanka Bajaj, Gopeekrishnan Sreenilayam, Vikas Tyagi, Rudi Fasan
Engineered hemoproteins have recently emerged as promising systems for promoting asymmetric cyclopropanations, but variants featuring predictable, complementary stereoselectivity in these reactions have remained elusive. In this study, a rationally driven strategy was implemented and applied to engineer myoglobin variants capable of providing access to 1-carboxy-2-aryl-cyclopropanes with high trans-(1R,2R) selectivity and catalytic activity. The stereoselectivity of these cyclopropanation biocatalysts complements that of trans-(1S,2S)-selective variants developed here and previously...
November 25, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27881505/prasugrel-versus-ticagrelor-uncertainty-remains
#11
EDITORIAL
Marc P Bonaca, Stephen D Wiviott
No abstract text is available yet for this article.
November 22, 2016: Circulation
https://www.readbyqxmd.com/read/27881255/cost-effectiveness-analysis-of-ticagrelor-and-prasugrel-for-the-treatment-of-acute-coronary-syndrome
#12
Ying Jiao Zhao, Ai Leng Khoo, Liang Lin, Monica Teng, Tuck Seng Wu, Mark Y Chan, Boon Peng Lim
BACKGROUND: In the management of Asian patients with acute coronary syndrome (ACS), the comparative cost-effectiveness of ticagrelor and prasugrel, referenced to generic clopidogrel, is unknown. OBJECTIVE: To assess the cost-effectiveness of ticagrelor and prasugrel as compared with generic clopidogrel in patients with ACS in Singapore. METHODS: A Markov model simulating a typical cohort of 62-year-old patients with ACS was constructed from a patient's perspective over a lifetime horizon...
May 2016: Value in Health Regional Issues
https://www.readbyqxmd.com/read/27870977/longitudinal-treatment-patterns-with-adp-receptor-inhibitors-after-myocardial-infarction-insights-from-the-canadian-observational-antiplatelet-study
#13
Akshay Bagai, Tracy Y Wang, Shaun G Goodman, Harold N Fisher, Robert C Welsh, Jean-Pierre Dery, Xiang Zhang, Yajun E Zhu, Asim N Cheema, Payam Dehghani, Saleem A Kassam, John Ducas, Neil Brass, Hahn Hoe Kim, Anthony Fung, Erick Schampaert, Ata Ur Rehman Quraishi, Shamir R Mehta
BACKGROUND: After myocardial infarction (MI) treated with percutaneous coronary intervention (PCI), guidelines recommend dual antiplatelet therapy (DAPT) with aspirin and an ADP receptor inhibitor (ADPri) for at least 1year. However, whether real-world Canadian practice patterns reflect this recommendation is unknown. METHODS: We studied 2175 MI patients treated with PCI and discharged from 26 Canadian hospitals between 12/2011 and 05/2013 in the Canadian Observational Antiplatelet sTudy (COAPT)...
November 14, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/27869899/-patients-with-non-st-elevation-acute-coronary-syndrome-managed-without-coronary-revascularization-an-undertreated-population
#14
Alberto Menozzi, Leonardo De Luca, Zoran Olivari, Roberta Rossini, Marco Ferlini, Daniela Lina, Maurizio Giuseppe Abrignani, Piera Capranzano, Nazario Carrabba, Marcello Galvani, Alfredo Marchese, Gianfranco Mazzotta, Luciano Moretti, Nicola Signore, Massimo Uguccioni, Stefano De Servi
Non-ST-elevation acute coronary syndromes (NSTE-ACS) represent one of the most common clinical presentations of ischemic heart disease. Patients with NSTE-ACS are a heterogeneous population, with different clinical features and prognosis. A significant proportion of this population is medically managed, without any revascularization. In the Italian EYESHOT and French FAST-MI registries, patients managed with a conservative strategy were 40% and 35%, respectively. NSTE-ACS patients not undergoing coronary revascularization are at higher risk of adverse cardiovascular events and have a worse prognosis, including short- and long-term mortality, compared with those receiving revascularization...
October 2016: Giornale Italiano di Cardiologia
https://www.readbyqxmd.com/read/27865197/efficacy-and-safety-of-ticagrelor-versus-clopidogrel-with-different-dosage-in-high-risk-patients-with-acute-coronary-syndrome
#15
Yan-Guo Xin, Hai-Shan Zhang, Yu-Ze Li, Qi-Gang Guan, Liang Guo, Yuan Gao, Hai-Jie Yu, Xin-Gang Zhang, Feng Xu, Yue-Lan Zhang, Da-Lin Jia, Ying-Xian Sun, Guo-Xian Qi, Wen Tian
BACKGROUND: Dual antiplatelet therapy is recommended as a standard antiplatelet strategy in acute coronary syndrome. For those with reduced pharmacologic response to clopidogrel, strengthening antiplatelet therapy (clopidogrel 150mg daily) may reduce adverse clinical events. Ticagrelor is a direct-acting inhibitor of the adenosine diphosphate receptor P2Y12 that has a more rapid onset and offset than clopidogrel. METHODS: In this retrospective study, we compared ticagrelor (180mg loading dose 90mg twice daily thereafter), clopidogrel (300mg loading dose, 75mg or 150mg daily thereafter) for the prevention of cardiovascular events in 273 high-risk patients admitted to coronary care unit with acute coronary syndrome...
November 9, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/27863938/corrigendum-to-one-quarter-standard-dose-ticagrelor-better-than-standard-dose-clopidogrel-in-chinese-patients-with-stable-coronary-artery-disease-a-randomized-single-blind-crossover-clinical-study-int-j-cardiol-215-2016-209-213
#16
Meijiao He, Bin Liu, Danghui Sun, Yujiao Pan, Wanbin Zheng, Jing Shi, Shiqi Zhao, Xinwen Dong, Shuang Lu, Minghui Li, Yu Han, Yue Li
No abstract text is available yet for this article.
November 15, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/27859337/exposure-response-analyses-supporting-ticagrelor-dosing-recommendation-in-patients-with-prior-myocardial-infarction
#17
Daniel Röshammar, Joakim Nyberg, Tomas Andersson, Donald Stanski, Robert F Storey, Bengt Hamrén
The relationships between drug exposure and the composite risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke as well as the risk of TIMI major bleeding were estimated following long-term treatment with ticagrelor 60 or 90 mg twice daily in 20,942 patients with prior MI. These analyses support the primary reported efficacy and safety evaluations by showing that there were clear separations from placebo early in treatment with both doses, regardless of ticagrelor exposure, for both endpoints...
November 18, 2016: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27846735/perioperative-management-of-dual-anti-platelet-therapy
#18
Tyler D Webster, Prashant Vaishnava, Kim A Eagle
Dual anti-platelet therapy denotes a regimen of aspirin plus a P2Y12 receptor inhibitor, clopidogrel, prasugrel, or ticagrelor. Such therapy is a cornerstone of medical management following acute coronary syndromes and is imperative following percutaneous coronary interventions. While there is uncertainty about the optimal duration of dual antiplatelet therapy following percutaneous coronary intervention, the new 2016 American College of Cardiology/American Heart Association Guidelines suggest that for patients with stable ischemic heart disease at least six months of such therapy following a drug eluting stent and one month following a bare metal stent should be implemented...
November 16, 2016: Hospital Practice (Minneapolis)
https://www.readbyqxmd.com/read/27830382/ticagrelor-and-rosuvastatin-have-additive-cardioprotective-effects-via-adenosine
#19
Yochai Birnbaum, Gilad D Birnbaum, Itamar Birnbaum, Sven Nylander, Yumei Ye
BACKGROUND: Ticagrelor inhibits the equilibrative-nucleoside-transporter-1 and thereby, adenosine cell re-uptake. Ticagrelor limits infarct size (IS) in non-diabetic rats and the effect is adenosine-dependent. Statins, via ecto-5'-nucleotidase activation, also increase adenosine levels and limit IS. HYPOTHESIS: Ticagrelor and rosuvastatin have additive effects on myocardial adenosine levels, and therefore, on IS and post-reperfusion activation of the NLRP3-inflammasome...
November 10, 2016: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/27830294/single-mutations-of-ketoreductase-chkred20-enhance-the-bioreductive-production-of-1s-2-chloro-1-3-4-difluorophenyl-ethanol
#20
Feng-Jiao Zhao, Yan Liu, Xiao-Qiong Pei, Chao Guo, Zhong-Liu Wu
(1S)-2-chloro-1-(3, 4-difluorophenyl) ethanol ((S)-CFPL) is an intermediate for the drug ticagrelor, and is manufactured via chemical approaches. To develop a biocatalytic solution to (S)-CFPL, an inventory of ketoreductases from Chryseobacterium sp. CA49 were rescreened, and ChKRED20 was found to catalyze the reduction of the ketone precursor with excellent stereoselectivity (>99 % ee). After screening an error-prone PCR library of the wild-type ChKRED20, two mutants, each bearing a single amino acid substitution of H145L or L205M, were identified with significantly increased activity...
November 9, 2016: Applied Microbiology and Biotechnology
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