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Johann Bartko, Christian Schoergenhofer, Michael Schwameis, Patricia Wadowski, Jacek Kubica, Bernd Jilma, Eva-Luise Hobl
Aspirin is a cornerstone in the anti-platelet therapy of acute coronary syndromes. Co-administration of morphine may potentially influence the intestinal absorption, pharmacokinetics and pharmacodynamics as seen with P2Y12-inhibitors. In this trial, healthy volunteers were randomized to receive morphine (5 mg, iv bolus injection) at one of 7 different time points before, after or with aspirin (162 mg, po) in a double-blind, placebo controlled fashion. After a 14-day washout, subjects received placebo instead of morphine...
March 14, 2018: Journal of Pharmacology and Experimental Therapeutics
Simone Grotti, Leonardo Bolognese
No abstract text is available yet for this article.
February 2018: Journal of Cardiovascular Medicine
GianMarco Podda, Mariangela Scavone, Eti Alessandra Femia, Marco Cattaneo
A variety of laboratory tests have been developed, which can diagnose a number of both congenital and acquired disorders of platelet function. Many tests of platelet function measure the ability of platelets to adhere to each other, forming platelet aggregates, which represent the major constituents of hemostatic plugs and of arterial thrombi. Light transmission aggregometry (LTA) is still considered the gold standard of platelet aggregation tests, but other platelet aggregation-based tests are also available...
March 14, 2018: Platelets
Gretchen Stern, Jessica Rimsans, Arman Qamar, Muthiah Vaduganathan, Deepak L Bhatt
AIMS: Oral antiplatelet therapy may require interruption soon after percutaneous coronary intervention (PCI) or acute coronary syndrome. The optimal parenteral antiplatelet bridge strategy with glycoprotein IIb/IIIa inhibitors or cangrelor, a P2Y12 inhibitor, is unclear. We explore real-world use of cangrelor or eptifibatide for antiplatelet bridging at a large tertiary-care center. METHODS AND RESULTS: Thirty-one patients (9 eptifibatide, 20 cangrelor, and 2 both) received bridge therapy from October 2015 to June 2017...
March 13, 2018: EuroIntervention
Jeehoon Kang, Jung-Kyu Han, Youngkeun Ahn, Shung Chull Chae, Young Jo Kim, In-Ho Chae, Seung-Ho Hur, In-Whan Seong, Jei-Keon Chae, Myeong Chan Cho, Ki-Bae Seung, Myung Ho Jeong, Han-Mo Yang, Kyung Woo Park, Hyun-Jae Kang, Bon-Kwon Koo, Hyo-Soo Kim
Third-generation P2Y12 inhibitors (prasugrel, ticagrelor) are recommended in acute myocardial infarction (AMI). We aimed to evaluate the efficacy and safety of third-generation P2Y12 inhibitors in East Asian AMI patients. From the Korean AMI Registry, 9,355 patients who received dual antiplatelet agent (aspirin with clopidogrel [AC], 6,444 [70.5%] patients; aspirin with prasugrel [AP], 1,100 [11.8%] patients; or aspirin with ticagrelor [AT], 1,811 [19.4%] patients) were analysed. In-hospital endpoints were all-cause mortality or bleeding events during admission and 1-year endpoints were major adverse cardiac and cerebrovascular events (MACCE) and major bleeding events...
March 2018: Thrombosis and Haemostasis
Leonardo De Luca, Mauro Pennacchi, Giuseppe Musumeci, Fabrizio D'Ascenzo, Pamela Gallo, Stefano Rigattieri, Antonino Granatelli, Sergio Berti, Michele Massimo Gulizia, Stefano De Servi, Leonardo Bolognese
BACKGROUND: Few data exist on temporal evolution of antithrombotic agent use in patients with acute coronary syndromes (ACS) undergoing percutaneous coronary intervention (PCI) in Italy. We sought to compare data from the most recent prospective, multicenter, nationwide registries conducted in Italy, namely EYESHOT and SCOPE. METHODS: EYESHOT enrolled 2585 consecutive ACS patients, both ST-segment elevation myocardial infarction (STEMI) and non-ST elevation ACS (NSTE-ACS), admitted to 203 Italian coronary care units over a 3-week period (2-22 Dec 2013 and 27 Jan-16 Feb 2014)...
February 2018: Giornale Italiano di Cardiologia
Olivier Gach, Astrid Nyssen, Charles Pirlet, Julien Magne, Cécile Oury, Patrizio Lancellotti
AIMS: Preload with clopidogrel, ticagrelor, or prasugrel in the setting of ST-segment elevation myocardial infarction (STEMI) treated by primary percutaneous coronary intervention (PCI) is frequently applied. Limited data are available regarding the outcome impact of pretreatment with these drugs in the real world. METHODS AND RESULTS: The outcome of 760 STEMI patients treated by primary PCI receiving clopidogrel, prasugrel, or ticagrelor (n = 269, 327, 164, respectively) was evaluated...
March 9, 2018: Journal of Cardiovascular Medicine
Francesco Franchi, Fabiana Rollini, Jose Rivas Rios, Andrea Rivas, Malhar Agarwal, Megha Kureti, Deepa Nagaraju, Mustafa Wali, Zubair Shaikh, Maryuri Briceno, Ahmed Nawaz, Jae Youn Moon, Latonya Been, Siva Suryadevara, Daniel Soffer, Martin M Zenni, Theodore A Bass, Dominick J Angiolillo
BACKGROUND : Switching between different classes of P2Y12 inhibitors, including de-escalation from ticagrelor to clopidogrel, commonly occurs in clinical practice. However, the pharmacodynamic profiles of this strategy have been poorly explored. METHODS : This was a prospective, randomized, open-label study conducted in patients on maintenance dosing (MD) of aspirin (81 mg/d) and clopidogrel (75 mg/d). After a 7-day run-in with ticagrelor (180 mg loading dose [LD] followed by 90 mg twice daily MD), patients (n=80) were randomized into 1 of 4 groups: group A, clopidogrel 600 mg LD 24 hours after the last MD of ticagrelor (C-600 mg-24h); group B, clopidogrel 600 mg LD 12 hours after the last MD of ticagrelor (C-600 mg-12h); group C, clopidogrel 75 mg/d MD 24 hours after the last MD of ticagrelor (C-75 mg-24h); and group D, ticagrelor 90 mg twice daily MD (T-90 mg twice daily)...
March 11, 2018: Circulation
Arwa M Amin, Lim Sheau Chin, Chin-Hoe The, Hamza Mostafa, Dzul Azri Mohamed Noor, Muhamad Ali S K Abdul Kader, Yuen Kah Hay, Baharudin Ibrahim
Dual antiplatelet therapy (DAPT) of clopidogrel and aspirin is crucial for coronary artery disease (CAD) patients undergoing percutaneous coronary intervention (PCI). However, some patients may endure clopidogrel high on treatment platelets reactivity (HTPR) which may cause thromboembolic events. Clopidogrel HTPR is multifactorial with some genetic and non-genetic factors contributing to it. We aimed to use nuclear magnetic resonance (1 H NMR) pharmacometabolomics analysis of plasma to investigate this multifactorial and identify metabolic phenotypes and pathways associated with clopidogrel HTPR...
March 8, 2018: European Journal of Pharmaceutical Sciences
Min Soo Kim, Eun Suk Park, Jun Bum Park, In Uk Lyo, Hong Bo Sim, Soon Chan Kwon
OBJECTIVE: The purpose of this study was to analyze the variability of clopidogrel responses according to duration of a clopidogrel drug regimen after stent-assisted coil embolization (SAC), and to determine the correlation between the variability of clopidogrel responses and thromboembolic or hemorrhagic complications. METHODS: A total of 47 patients who underwent SAC procedures to treat unruptured intracranial aneurysms were enrolled in the study. Preoperatively, patients received more than seven days of aspirin (100 mg) and clopidogrel (75 mg), daily...
March 2018: Journal of Korean Neurosurgical Society
Gerhard Selhorst, Fabian Schmidtler, Armin Ott, Evelyn Hitzke, June Tomelden, Diethmar Antoni, Ellen Hoffmann, Johannes Rieber
Dual antiplatelet therapy (DAPT) with aspirin and a P2Y12 inhibitor is a mainstay of the prevention of stent thrombosis following percutaneous coronary intervention (PCI). In the 2015 European guidelines for the management of acute coronary syndrome (ACS), prasugrel (PRA) and ticagrelor (TICA) combined with aspirin are recommended as first-line therapy. Clopidogrel (CLO) is recommended as an alternative medication for patients with contradictions to these new drugs. This single-center study analyzed the platelet function of 809 ACS patients undergoing PCI and treatment with DAPT...
March 9, 2018: Platelets
Shumaila Afrin, Yusra Rahman, Mohammad Tabish
Ticlopidine is an anti-platelet drug that functions as a P2Y12 receptor antagonist. The present study provides a detailed characterization of interaction of ticlopidine with a model transport protein, bovine serum albumin (BSA) as well as an assessment of its bilirubin displacing ability using a multi-spectroscopic approach in combination with isothermal titration calorimetry. The value of binding constant determined using ITC studies was found to be 3.03 x 103 M-1 with a binding stoichiometry of approximately 1:1...
March 7, 2018: Journal of Biomolecular Structure & Dynamics
Marilena Crescente, Laura Menke, Melissa V Chan, Paul C Armstrong, Timothy D Warner
Platelets are important players in thrombosis and haemostasis with their function being modulated by mediators in the blood and the vascular wall. Among these, eicosanoids can both stimulate or inhibit platelet reactivity. Platelet cyclooxygenase (COX)-1 generated thromboxane (TX) A2 is the primary prostanoid that stimulates platelet aggregation; its action is counter-balanced by prostaglandin (PG)I2 (prostacyclin), a product of vascular COX. PGD2 , PGE2 , 12- hydroxyeicosatraenoic acid (HETE) or 15-HETE, are other prostanoid modulators of platelet activity, but some also play a role in carcinogenesis...
March 7, 2018: British Journal of Pharmacology
Jun-Lei Li, Yu Fu, Si-Bei Qin, Guang-Kai Liang, Jian Liu, Xiao-Yan Nie, Jing Chen, Lu-Wen Shi, Hong Shao, Yun Lu
OBJECTIVE: Investigate the association between P2Y12 Purinoceptor (P2RY12) polymorphisms and adverse clinical events in coronary artery disease (CAD) patients treated with clopidogrel. METHODS: We performed a comprehensive database search, with a particular focus on P2RY12 polymorphisms and their effects in clopidogrel-treated CAD patients, in the PubMed, EMBASE, Cochrane Library,, Web of Science, and Chinese databases from their inceptions to April 8, 2017...
March 3, 2018: Gene
Runlin Gao, Yongjian Wu, Hengliang Liu, Guohai Su, Zuyi Yuan, Aidong Zhang, Yong Wang, Zhirong Wang, Yan Wang, Huanyi Zhang, Yang Zheng, Lei Liu, Lijun Shen, Maria Leonsson-Zachrisson, Yaling Han
PURPOSE: Ticagrelor is an orally administered, reversibly binding, direct-acting P2Y12 receptor antagonist previously evaluated in several phase III trials. This phase IV, multicenter, single-arm trial assessed the safety and incidence of cardiovascular (CV) events with ticagrelor in Chinese patients experiencing an acute coronary syndrome (ACS). METHODS: Patients hospitalized with an ACS received ticagrelor (180 mg loading dose, 90 mg twice daily thereafter) plus low-dose aspirin (75-100 mg/day) for up to 12 months...
February 28, 2018: Cardiovascular Drugs and Therapy
Daniel R Mangels, Ashwin Nathan, Sony Tuteja, Jay Giri, Taisei Kobayashi
PURPOSE OF REVIEW: Antiplatelet therapies are pivotal treatments in the management of acute coronary syndrome (ACS) with or without revascularization. In recent years, the use of P2Y12 antagonists prior to catheterization, so-called pretreatment, has been questioned, particularly in patients who may be at higher bleeding risks. The purpose of this review was to evaluate the current literature on contemporary and novel antiplatelet therapy in the pretreatment and treatment of ACS. RECENT FINDINGS: The P2Y12 receptor antagonists are associated with substantial reductions in morbidity and mortality for all types of ACS but only clopidogrel and ticagrelor have sufficient evidence for use in the pretreatment setting...
February 27, 2018: Current Treatment Options in Cardiovascular Medicine
Lei Zhang, Yi Li, Bai-Song Yang, Lu Li, Xiao-Zeng Wang, Mei-Ling Ge, Quan-Min Jing, Ying-Yan Ma, Geng Wang, Hai-Wei Liu, Xin Zhao, Bin Wang, Kai Xu, Ya-Ling Han
Background: High platelet reactivity (HPR) during clopidogrel treatment predicts postpercutaneous coronary intervention (PCI) ischemic events strongly and independently. Tongxinluo capsules (TCs) are a traditional Chinese medicine formulation used as antiplatelet treatment. However, its efficacy against HPR is not known. The aim of the present study was to evaluate the effects of TCs in acute coronary syndrome (ACS) patients with HPR. Methods: This multicenter, randomized, double-blind, placebo-controlled study prospectively analyzed 136 ACS patients with HPR who underwent PCI...
March 5, 2018: Chinese Medical Journal
Patricia P Wadowski, Silvia Lee, Christoph W Kopp, Renate Koppensteiner, Simon Panzer, Thomas Gremmel
Low high-density lipoprotein cholesterol (HDL-C) levels are an independent predictor of ischemic events in patients with atherosclerotic cardiovascular disease. This may in part be due to decreased clopidogrel-mediated platelet inhibition in patients with low HDL-C. We investigated the association of HDL-C with on-treatment platelet reactivity to adenosine diphosphate (ADP) in 314 patients on dual antiplatelet therapy with clopidogrel and aspirin undergoing angioplasty and stenting. Platelet P-selectin expression was assessed by flow cytometry, and platelet aggregation was determined by the VerifyNow P2Y12 assay and the Impact-R...
January 1, 2018: Angiology
Jaya Chandrasekhar, Usman Baber, Samantha Sartori, Melissa Aquino, Annapoorna S Kini, Sunil Rao, William Weintraub, Timothy D Henry, Serdar Farhan, Birgit Vogel, Sabato Sorrentino, Zhen Ge, Samir Kapadia, Joseph B Muhlestein, Sandra Weiss, Craig Strauss, Catalin Toma, Anthony DeFranco, Mark B Effron, Stuart Keller, Brian A Baker, Stuart Pocock, George Dangas, Roxana Mehran
BACKGROUND: Potent P2Y12 inhibitors might offer enhanced benefit against thrombotic events in complex percutaneous coronary intervention (PCI). We examined prasugrel use and outcomes according to PCI complexity, as well as analyzing treatment effects according to thienopyridine type. METHODS: PROMETHEUS was a multicentre observational study that compared clopidogrel vs prasugrel in acute coronary syndrome patients who underwent PCI (n = 19,914). Complex PCI was defined as PCI of the left main, bifurcation lesion, moderate-severely calcified lesion, or total stent length ≥ 30 mm...
March 2018: Canadian Journal of Cardiology
Vasiliki Tsigkou, Gerasimos Siasos, Kleanthis Rovos, Niki Tripyla, Dimitris Tousoulis
Peripheral artery disease (PAD) is one of the most important causes of cardiovascular morbidity and mortality and its prevalence is alarmingly increasing in modern societies. PAD shares common characteristics with the other atherosclerotic diseases but involves specifically the arteries of the lower extremities. Apart from the changes in lifestyle, antiplatelet agents are the hallmark of the treatment and improve the symptoms as well as the progression of the disease. Aspirin is the cornerstone of treatment and is administrated in doses ranging from 75 to 325mg daily...
February 19, 2018: Current Opinion in Pharmacology
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