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https://www.readbyqxmd.com/read/29754923/enhanced-late-sodium-current-underlies-pro-arrhythmic-intracellular-sodium-and-calcium-dysregulation-in-murine-sodium-channelopathy
#1
Mathilde R Rivaud, Antonius Baartscheer, Arie O Verkerk, Leander Beekman, Sridharan Rajamani, Luiz Belardinelli, Connie R Bezzina, Carol Ann Remme
BACKGROUND: Long QT syndrome mutations in the SCN5A gene are associated with an enhanced late sodium current (INa,L ) which may lead to pro-arrhythmic action potential prolongation and intracellular calcium dysregulation. We here investigated the dynamic relation between INa,L , intracellular sodium ([Na+ ]i ) and calcium ([Ca2+ ]i ) homeostasis and pro-arrhythmic events in the setting of a SCN5A mutation. METHODS AND RESULTS: Wild-type (WT) and Scn5a1798insD/+ (MUT) mice (age 3-5 months) carrying the murine homolog of the SCN5A-1795insD mutation on two distinct genetic backgrounds (FVB/N and 129P2) were studied...
July 15, 2018: International Journal of Cardiology
https://www.readbyqxmd.com/read/29749631/persistence-of-a-posaconazole-mediated-drug-drug-interaction-with-ranolazine-after-cessation-of-posaconazole-administration-impact-of-obesity-and-implications-for-patient-safety
#2
Christina R Chow, Jerold S Harmatz, Michael J Ryan, David J Greenblatt
The antianginal agent ranolazine (Ranexa®) is metabolized primarily by cytochrome P450-3A (CYP3A) enzymes. Coadministration with strong CYP3A inhibitors, such as ketoconazole and posaconazole, is contraindicated due to risk of QT prolongation from high levels of ranolazine. This study evaluated the time course of recovery from the posaconazole drug interaction in normal-weight and otherwise healthy obese subjects. Subjects received single doses of ranolazine in the baseline control condition, again during coadministration of posaconazole, and at 4 additional time points during the 2 weeks after posaconazole discontinuation...
May 11, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29746286/ranolazine-for-symptomatic-management-of-microvascular-angina
#3
Erin Rayner-Hartley, Mahraz Parvand, Karin H Humphries, Andrew Starovoytov, Julie E Park, Tara Sedlak
BACKGROUND: Ranolazine is approved in the United States and Europe for chronic stable angina. Microvascular angina (MVA) is defined as angina with no obstructive coronary artery disease. STUDY QUESTION: Our objective was to assess the effectiveness of ranolazine at improving angina scores and quality of life in a Canadian cohort with severe refractory angina due to MVA. STUDY DESIGN: We administered questionnaires to 31 patients at baseline and after at least 6 weeks of ranolazine treatment...
May 9, 2018: American Journal of Therapeutics
https://www.readbyqxmd.com/read/29741611/crispr-cas9-editing-in-human-pluripotent-stem-cell-cardiomyocytes-highlights-arrhythmias-hypocontractility-and-energy-depletion-as-potential-therapeutic-targets-for-hypertrophic-cardiomyopathy
#4
Diogo Mosqueira, Ingra Mannhardt, Jamie R Bhagwan, Katarzyna Lis-Slimak, Puspita Katili, Elizabeth Scott, Mustafa Hassan, Maksymilian Prondzynski, Stephen C Harmer, Andrew Tinker, James G W Smith, Lucie Carrier, Philip M Williams, Daniel Gaffney, Thomas Eschenhagen, Arne Hansen, Chris Denning
Aims: Sarcomeric gene mutations frequently underlie hypertrophic cardiomyopathy (HCM), a prevalent and complex condition leading to left ventricle thickening and heart dysfunction. We evaluated isogenic genome-edited human pluripotent stem cell-cardiomyocytes (hPSC-CM) for their validity to model, and add clarity to, HCM. Methods and results: CRISPR/Cas9 editing produced 11 variants of the HCM-causing mutation c.C9123T-MYH7 [(p.R453C-β-myosin heavy chain (MHC)] in 3 independent hPSC lines...
May 8, 2018: European Heart Journal
https://www.readbyqxmd.com/read/29720563/pharmacology-of-cardio-oncology-chronotropic-and-lusitropic-effects-of-b-type-natriuretic-peptide-in-cancer-patients-with-early-diastolic-dysfunction-induced-by-anthracycline-or-nonanthracycline-chemotherapy
#5
Pierantonio Menna, Vito Calabrese, Grazia Armento, Ombretta Annibali, Carlo Greco, Emanuela Salvatorelli, Francesco Marchesi, Giorgio Reggiardo, Giorgio Minotti
B-type natriuretic peptide (BNP) is widely used as a diagnostic marker of systolic dysfunction. We previously conducted a clinical study in which anthracycline or nonanthracycline chemotherapy did not cause systolic dysfunction in cancer patients; however, some patients showed asymptomatic alterations of diastolic relaxation while others showed persistent elevations of BNP, measured as prohormone BNP aminoterminal fragment. Here we describe post hoc pharmacological analyses showing that i) impaired relaxation and persistent elevations of BNP were mutually exclusive manifestations of diastolic dysfunction ii), in some patients BNP elevations were induced by an early compromisation of myocardial relaxation iii), BNP elevations then halted further deterioration of relaxation in a concentration-dependent manner iv), high BNP increased heart rate (HR)...
May 2, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29719406/cardiotoxic-effects-of-the-novel-approved-anti-erbb2-agents-and-reverse-cardioprotective-effects-of-ranolazine
#6
Claudia De Lorenzo, Rolando Paciello, Gennaro Riccio, Domenica Rea, Antonio Barbieri, Carmela Coppola, Nicola Maurea
Purpose: Pertuzumab, a novel anti-epidermal growth factor receptor 2 humanized monoclonal antibody, and trastuzumab-emtansine (TDM1), a novel antibody-drug conjugate made up of trastuzumab covalently linked to the highly potent microtubule inhibitory agent DM1, have been recently approved by the US Food and Drug Administration for increasing the efficiency and safety of breast cancer therapy with trastuzumab. We investigated for the first time the potential cardiotoxic effects of pertuzumab and TDM1, which are not yet fully elucidated, and we tested whether ranolazine could blunt their cardiotoxicity...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29718449/cross-site-reliability-of-human-induced-pluripotent-stem-cell-derived-cardiomyocyte-based-safety-assays-using-microelectrode-arrays-results-from-a-blinded-cipa-pilot-study
#7
Daniel Millard, Qianyu Dang, Hong Shi, Xiaou Zhang, Chris Strock, Udo Kraushaar, Haoyu Zeng, Paul Levesque, Hua-Rong Lu, Jean-Michel Guillon, Joseph C Wu, Yingxin Li, Greg Luerman, Blake Anson, Liang Guo, Mike Clements, Yama A Abassi, James Ross, Jennifer Pierson, Gary Gintant
Recent in vitro cardiac safety studies demonstrate the ability of human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) to detect electrophysiologic effects of drugs. However, variability contributed by unique approaches, procedures, cell lines and reagents across laboratories makes comparisons of results difficult, leading to uncertainty about the role of hiPSC-CMs in defining proarrhythmic risk in drug discovery and regulatory submissions. A blinded pilot study was conducted to evaluate the electrophysiologic effects of eight well-characterized drugs on four cardiomyocyte lines using a standardized protocol across three microelectrode array (MEA) platforms (18 individual studies)...
April 27, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29671538/stable-coronary-artery-disease-treatment
#8
Michael M Braun, William A Stevens, Craig H Barstow
Stable coronary artery disease refers to a reversible supply/demand mismatch related to ischemia, a history of myocardial infarction, or the presence of plaque documented by catheterization or computed tomography angiography. Patients are considered stable if they are asymptomatic or their symptoms are controlled by medications or revascularization. Treatment involves risk factor management, antiplatelet therapy, and antianginal medications. Tobacco cessation, exercise, and weight loss are the most important lifestyle modifications...
March 15, 2018: American Family Physician
https://www.readbyqxmd.com/read/29666676/ranolazine-a-true-pluripotent-cardiovascular-drug-or-jack-of-all-trades-master-of-none
#9
REVIEW
Alice Mezincescu, V J Karthikeyan, Sunil K Nadar
Cardiovascular disease (CVD) is a leading cause of morbidity and mortality worldwide. Although the majority of patients with CVD are treated with interventional procedures, a substantial number require medical therapy in terms of both prognosis and symptomatic relief. However, commonly used agents such as β-blockers and calcium channel blockers reduce blood pressure in patients whose resting pressures are often already low. Ranolazine is a promising agent that does not have significant effects on blood pressure or heart rate...
February 2018: Sultan Qaboos University Medical Journal
https://www.readbyqxmd.com/read/29657587/impact-of-ranolazine-on-ventricular-arrhythmias-a-systematic-review
#10
REVIEW
George Bazoukis, Gary Tse, Konstantinos P Letsas, Costas Thomopoulos, Katerina K Naka, Panagiotis Korantzopoulos, Xenophon Bazoukis, Paschalia Michelongona, Stamatis S Papadatos, Konstantinos Vlachos, Tong Liu, Michael Efremidis, Adrian Baranchuk, Stavros Stavrakis, Costas Tsioufis
Ranolazine is a new medication for the treatment of refractory angina. However, except its anti-anginal properties, it has been found to act as an anti-arrhythmic. The aim of our systematic review is to present the existing data about the impact of ranolazine in ventricular arrhythmias. We searched MEDLINE and Cochrane databases as well clinicaltrials.gov until September 1, 2017 to find all studies (clinical trials, observational studies, case reports/series) reported data about the impact of ranolazine in ventricular arrhythmias...
April 2018: Journal of Arrhythmia
https://www.readbyqxmd.com/read/29617054/activation-of-voltage-gated-sodium-current-and-inhibition-of-erg-mediated-potassium-current-caused-by-telmisartan-an-antagonist-of-angiotensin-ii-type-1-receptor-in-hl-1-atrial-cardiomyocytes
#11
Wei-Ting Chang, Sheng-Nan Wu
Telmisartan (TEL) is a non-peptide blocker of angiotensin II type-1 (AT1 ) receptor. However, the mechanisms through which this drug interacts directly with ion currents in hearts remain largely unclear. Herein, we aim to investigate the effects of TEL the on ionic currents and membrane potential of murine HL-1 cardiomyocytes. In whole-cell recordings, addition of TEL stimulated the peak and late components of voltage-gated Na+ currents (IN a ) with different potencies. The EC50 values required to achieve the stimulatory effect of this drug on peak and late IN a were 0...
April 4, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29593564/dynamic-action-potential-restitution-contributes-to-mechanical-restitution-in-right-ventricular-myocytes-from-pulmonary-hypertensive-rats
#12
Matthew E L Hardy, Eleftheria Pervolaraki, Olivier Bernus, Ed White
We investigated the steepened dynamic action potential duration (APD) restitution of rats with pulmonary artery hypertension (PAH) and right ventricular (RV) failure and tested whether the observed APD restitution properties were responsible for negative mechanical restitution in these myocytes. PAH and RV failure were provoked in male Wistar rats by a single injection of monocrotaline (MCT) and compared with saline-injected animals (CON). Action potentials were recorded from isolated RV myocytes at stimulation frequencies between 1 and 9 Hz...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29579779/late-sodium-current-inhibitors-to-treat-exercise-induced-obstruction-in-hypertrophic-cardiomyopathy-an-in-vitro-study-in-human-myocardium
#13
Cecilia Ferrantini, Josè Manuel Pioner, Luca Mazzoni, Francesca Gentile, Benedetta Tosi, Alessandra Rossi, Luiz Belardinelli, Chiara Tesi, Chiara Palandri, Rosanna Matucci, Elisabetta Cerbai, Iacopo Olivotto, Corrado Poggesi, Alessandro Mugelli, Raffaele Coppini
BACKGROUND AND PURPOSE: In 30-40% of hypertrophic cardiomyopathy (HCM) patients, symptomatic left-ventricular (LV) outflow gradients develop only during exercise due to catecholamine-induced LV-hypercontractility (inducible obstruction). Negative-inotropic pharmacological options are limited to β-blockers or disopyramide, with scarce efficacy and tolerability. We assessed the potential use of late Na+ -current (INaL )-inhibitors to treat inducible obstruction in HCM. EXPERIMENTAL APPROACH: The electrophysiological and mechanical responses to β-adrenergic stimulation were studied in human myocardium from HCM versus control patients...
March 26, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29531764/rationale-and-design-of-the-ranolazine-ph-rv-study-a-multicentred-randomised-and-placebo-controlled-study-of-ranolazine-to-improve-rv-function-in-patients-with-non-group-2-pulmonary-hypertension
#14
Yuchi Han, Paul R Forfia, Anjali Vaidya, Jeremy A Mazurek, Myung H Park, Gautam Ramani, Stephen Y Chan, Aaron B Waxman
Introduction: A major determining factor on outcomes in patients with pulmonary arterial hypertension (PAH) is right ventricular (RV) function. Ranolazine, which is currently approved for chronic stable angina, has been shown to improve RV function in an animal model and has been shown to be safe in small human studies with PAH. We aim to study the effect of ranolazine on RV function using cardiovascular magnetic resonance (CMR) in patients with pulmonary hypertension (non-group 2 patients) and monitor the effect of ranolazine on metabolism using metabolic profiling and changes of microRNA...
2018: Open Heart
https://www.readbyqxmd.com/read/29508636/emerging-pharmacotherapies-for-the-treatment-of-atrial-fibrillation
#15
Alessandro Capucci, Laura Cipolletta, Federico Guerra, Irene Giannini
The main aim of current research on the field of atrial fibrillation (AF) treatment is to find new antiarrhythmic drugs with less side effects. Areas covered: Dronedarone and vernakalant showed promising result in term of efficacy and safety in selected patients. Ranolazine and colchicine are obtaining a role as a potential antiarrhythmic drug. Ivabradine is used in experimental studies for the rate control of AF. Moreover, new compounds (vanoxerine, moxonidine, budiodarone) are still under investigation. Monoclonal antibodies or selective antagonist of potassium channel are under investigation for long term maintenance of sinus rhythm...
March 2018: Expert Opinion on Emerging Drugs
https://www.readbyqxmd.com/read/29490168/antioxidant-defense-and-protection-against-cardiac-arrhythmias-lessons-from-a-mammalian-hibernator-the-woodchuck
#16
Zhenghang Zhao, Raymond K Kudej, Hairuo Wen, Nadezhda Fefelova, Lin Yan, Dorothy E Vatner, Stephen F Vatner, Lai-Hua Xie
Hibernating animals show resistance to hypothermia-induced cardiac arrhythmias. However, it is not clear whether and how mammalian hibernators are resistant to ischemia-induced arrhythmias. The goal of this investigation was to determine the susceptibility of woodchucks ( Marmota monax) to arrhythmias and their mechanisms after coronary artery occlusion at the same room temperature in both winter, the time for hibernation, and summer, when they do not hibernate. By monitoring telemetric electrocardiograms, we found significantly higher arrhythmia scores, calculated as the severity of arrhythmias, with incidence of ventricular tachycardia, ventricular fibrillation, and thus sudden cardiac death (SCD) in woodchucks in summer than they had in winter...
February 28, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29483621/the-efficacy-of-ranolazine-on-e1784k-is-altered-by-temperature-and-calcium
#17
Mena Abdelsayed, Manpreet Ruprai, Peter C Ruben
E1784K is the most common mixed syndrome SCN5a mutation underpinning both Brugada syndrome type 1 (BrS1) and Long-QT syndrome type 3 (LQT3). The charge reversal mutant enhances the late sodium current (INa ) passed by the cardiac voltage-gated sodium channel (NaV 1.5), delaying cardiac repolarization. Exercise-induced triggers, like elevated temperature and cytosolic calcium, exacerbate E1784K late INa . In this study, we tested the effects of Ranolazine, the late INa blocker, on voltage-dependent and kinetic properties of E1784K at elevated temperature and cytosolic calcium...
February 26, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29467663/ranolazine-attenuates-trastuzumab-induced-heart-dysfunction-by-modulating-ros-production
#18
Gennaro Riccio, Salvatore Antonucci, Carmela Coppola, Chiara D'Avino, Giovanna Piscopo, Danilo Fiore, Carlo Maurea, Michele Russo, Domenica Rea, Claudio Arra, Gerolama Condorelli, Fabio Di Lisa, Carlo G Tocchetti, Claudia De Lorenzo, Nicola Maurea
The ErbB2 blocker trastuzumab improves survival in oncologic patients, but can cause cardiotoxicity. The late Na+ current inhibitor ranolazine has been shown to counter experimental HF, including doxorubicin cardiotoxicity (a condition characterized by derangements in redox balance), by lowering the levels of reactive oxygen species (ROS). Since ErbB2 can modulate ROS signaling, we tested whether trastuzumab cardiotoxicity could be blunted by ranolazine via redox-mediated mechanisms. Trastuzumab decreased fractional shortening and ejection fraction in mice, but ranolazine prevented heart dysfunction when co-administered with trastuzumab...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29432398/ranolazine-treatment-in-the-heterogeneous-symptomatic-stable-coronary-artery-disease-population
#19
Mauro Borzi, Alfredo Intorcia, Marco A Perrone, Giulia Grilli, Domenico Sergi, Martina Borzi, Francesco Romeo
No abstract text is available yet for this article.
April 2018: Journal of Cardiovascular Medicine
https://www.readbyqxmd.com/read/29424967/predicting-drug-induced-arrhythmias-by-multiscale-modeling
#20
Francisco Sahli Costabal, Jiang Yao, Ellen Kuhl
Drugs often have undesired side effects. In the heart, they can induce lethal arrhythmias such as torsades de pointes. The risk evaluation of a new compound is costly and can take a long time, which often hinders the development of new drugs. Here, we establish a high-resolution, multiscale computational model to quickly assess the cardiac toxicity of new and existing drugs. The input of the model is the drug-specific current block from single cell electrophysiology; the output is the spatio-temporal activation profile and the associated electrocardiogram...
February 9, 2018: International Journal for Numerical Methods in Biomedical Engineering
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