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Rong Chen, Shin-Ho Chung
Molecular dynamics simulations are employed to determine the inhibitory mechanisms of three drugs, 5-(4- phenoxybutoxy)psoralen (PAP-1), vernakalant and flecainide, on the voltage-gated K+ channel Kv1.5, a target for the treatment of cardiac arrhythmia. At neutral pH, PAP-1 is neutral, whereas the other two molecules carry one positive charge. We show that PAP-1 forms stable dimers in water, primarily through the hydrophobic interactions between aromatic rings. All three molecules bind to the cavity between the Ile508 and Val512 residues from the four subunits of the channel...
April 13, 2018: Biochemistry
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
José Carbajosa Dalmau, Juan Cosín-Sales, María José Pérez-Durá, José Noceda, Amós Urtubia-Palacios, Néstor Hernández-Sori, Ana Peiró-Gómez, Javier Jacob, Pere Llorens, Luis Ruescas-Gómez, Alfonso Martín-Martínez
OBJECTIVES: To study the effectiveness and safety of vernakalant for restoration of sinus rhythm in patients with atrial fibrillation (AF) in routine hospital emergency department care, and to evaluate factors associated with a more effective response. MATERIAL AND METHODS: Prospective multicenter cohort study enrolling consecutive patients who were administered vernakalant for medical cardioversion of AF between September 2014 through March 2016 in 5 hospitals in the Spanish autonomous community of Valencia...
2017: Emergencias: Revista de la Sociedad Española de Medicina de Emergencias
Tamer Akel, James Lafferty
BACKGROUND: Atrial fibrillation is a common cardiac arrhythmia with increasing prevalence in the aging population. It is a major cause of emergency department visits worldwide. Vernakalant, a relatively new antiarrhythmic drug with selectively preferential effects on the atrial tissue is currently used in many European countries for the termination of recent-onset atrial fibrillation. Presently, the drug is still not approved by the United States Food and Drug Administration due to safety concerns...
November 4, 2017: Annals of Noninvasive Electrocardiology
Jonas Goldin Diness, Lasse Skibsbye, Rafel Simó-Vicens, Joana Larupa Santos, Pia Lundegaard, Carlotta Citerni, Daniel Rafael Peter Sauter, Sofia Hammami Bomholtz, Jesper Hastrup Svendsen, Søren-Peter Olesen, Ulrik S Sørensen, Thomas Jespersen, Morten Grunnet, Bo Hjorth Bentzen
BACKGROUND: Evidence has emerged that small-conductance Ca2+ -activated K+ (SK) channels constitute a new target for treatment of atrial fibrillation (AF). SK channels are predominantly expressed in the atria as compared with the ventricles. Various marketed antiarrhythmic drugs are limited by ventricular adverse effects and efficacy loss as AF progresses. METHODS AND RESULTS: A total of 43 pigs were used for the studies. AF reversion in conscious long-term tachypaced pigs: Pigs were subjected to atrial tachypacing (7 Hz) until they developed sustained AF that could not be reverted by vernakalant 4 mg/kg (18...
October 2017: Circulation. Arrhythmia and Electrophysiology
Gerrit Frommeyer, Magdalena Sterneberg, Dirk G Dechering, Simon Kochhäuser, Nils Bögeholz, Michael Fehr, Lars Eckardt
BACKGROUND: Current guidelines recommend vernakalant for pharmacologic cardioversion of recent-onset atrial fibrillation. However, this drug is not established as chronic therapy. METHODS AND RESULTS: In total, 15 rabbit hearts were Langendorff-perfused. A burst pacing protocol-induced atrial fibrillation in 7 of 15 hearts at baseline (10 episodes). Subsequently, a combination of acetylcholine and isoproterenol (ACH/ISO) has been administered to increase occurrence of atrial fibrillation resulting in a reduction of atrial action potential duration (-25 ms, P < 0...
September 2017: Journal of Cardiovascular Medicine
Arne van Hunnik, Hussein Nasrallah, Dennis H Lau, Marion Kuiper, Sander Verheule, Ulrich Schotten
Aims: Besides the inhibition of the sodium inward current, vernakalant also inhibits the ultra rapid rectifier (IKur) and transient outward current (Ito). Inhibition of these currents increases contractility in canine atrial myocytes and goat atria. We investigated the effect of vernakalant on early repolarization and contractility in normal and electrically remodelled atria. Methods and results: Goats were implanted a pressure catheter, piezoelectric crystals, and electrodes to obtain atrial contractility and effective refractory period (ERP)...
January 1, 2018: Europace: European Pacing, Arrhythmias, and Cardiac Electrophysiology
Alexander Simon, Jan Niederdoeckl, Ekaterini Skyllouriotis, Nikola Schuetz, Harald Herkner, Christoph Weiser, Anton N Laggner, Hans Domanovits, Alexander O Spiel
Aims: Ibutilide is a rapid-acting antiarrhythmic drug with worldwide use for conversion of recent-onset atrial fibrillation. Vernakalant, approved in the EU in 2010, is likewise used intravenously, with proven efficacy and safety compared with placebo and amiodarone in randomized clinical trials. The aim of our study was to compare the time to conversion and the conversion rate within 90 min in patients with recent-onset atrial fibrillation treated with vernakalant or ibutilide. Methods and Results: A randomized controlled trial registered at clinicaltrials...
February 1, 2017: Europace: European Pacing, Arrhythmias, and Cardiac Electrophysiology
P Stoneman, P Gilligan, P Mahon, R Sheahan
BACKGROUND: Vernakalant hydrochloride is a rapid-acting antiarrhythmic drug licensed in the EU since 2010 for the conversion of recent-onset atrial fibrillation with proven efficacy and safety when compared with placebo and amiodarone in randomized clinical trials. AIMS: The aim of our study was to determine the feasibility of same day discharge (following 2 h monitoring) from the emergency department after successful cardioversion using vernakalant hydrochloride...
November 2017: Irish Journal of Medical Science
Marta Varela, Michael A Colman, Jules C Hancox, Oleg V Aslanidi
Anti-arrhythmic drug therapy is a frontline treatment for atrial fibrillation (AF), but its success rates are highly variable. This is due to incomplete understanding of the mechanisms of action of specific drugs on the atrial substrate at different stages of AF progression. We aimed to elucidate the role of cellular, tissue and organ level atrial heterogeneities in the generation of a re-entrant substrate during AF progression, and their modulation by the acute action of selected anti-arrhythmic drugs. To explore the complex cell-to-organ mechanisms, a detailed biophysical models of the entire 3D canine atria was developed...
December 2016: PLoS Computational Biology
Gregory N Beatch, Kiran Bhirangi, Steen Juul-Moller, Jörg Rustige
Atrial fibrillation (AF) is a common clinically significant cardiac arrhythmia. This phase 3 randomized, double-blind, placebo-controlled trial assessed the efficacy and safety of vernakalant hydrochloride for the pharmacological conversion of AF to sinus rhythm in patients with recent-onset (>3 hours to ≤7 days) symptomatic AF from the Asia-Pacific region. Patients received an infusion of vernakalant (3 mg/kg) or placebo for 10 minutes. If AF had not been terminated 15 minutes later, a second infusion of vernakalant (2 mg/kg) or placebo for 15 minutes was administered...
February 2017: Journal of Cardiovascular Pharmacology
Maximilian D Hien, Fernando Benito Castro, Philippe Fournier, Anne Filleron, Tu-Anh Tran
OBJECTIVES: We report on a rare but severe complication of adenosine use in a child with reentry tachycardia. METHODS AND RESULTS: Treatment with adenosine, which is the standard medical therapy of atrioventricular reentry tachycardia, led to the development of an irregular wide complex tachycardia, caused by rapid ventricular response to atrial fibrillation. The girl was finally stabilized with electrical cardioversion. We analyze the pathomechanism and discuss possible treatment options...
October 8, 2016: Pediatric Emergency Care
Gerrit Frommeyer, Catharina Clauss, Christian Ellermann, Harilaos Bogossian, Dirk G Dechering, Simon Kochhäuser, Florian Reinke, Christian Pott, Lars Eckardt
Aims: The antiarrhythmic drug vernakalant exerts antiarrhythmic effects in atrial fibrillation. Recent experimental data suggest interactions with the late sodium current and antiarrhythmic effects in ventricular arrhythmias. We aimed at investigating whether treatment with vernakalant reduces polymorphic ventricular tachycardia (VT) in an experimental model of Long-QT-syndrome (LQTS). Methods and results: Twenty-nine isolated rabbit hearts were assigned to two groups and treated with erythromycin (300 µM, n = 15) or veratridine (0...
May 1, 2017: Europace: European Pacing, Arrhythmias, and Cardiac Electrophysiology
Caiyou Chen, Shicheng Jin, Zhefan Zhang, Biao Wei, Heng Wang, Kai Zhang, Hui Lv, Xiu-Qin Dong, Xumu Zhang
The first interrupted asymmetric hydroaminomethylation reaction was developed. The challenging trans-1,2-disubstituted olefins were employed as substrates, and a series of valuable chiral pyrrolidinones and pyrrolidines were obtained in high yields with high regioselectivities and excellent enantioselectivities. Several synthetic transformations were conducted, demonstrating the high synthetic utility of our method. A creative route for the synthesis of vernakalant and Enablex was also developed.
July 27, 2016: Journal of the American Chemical Society
R Kriz, M K Freynhofer, T W Weiss, F Egger, S C Gruber, P Eisenburger, J Wojta, K Huber, J Koch
BACKGROUND AND AIM: The management of patients with recent-onset atrial fibrillation (AF) presenting at emergency departments (EDs) varies widely. Our aim was to describe the management of patients with recent-onset (<48 hours) AF, to determine safety and efficacy of pharmacological cardioversion at the ED, and to evaluate the incidence of thromboembolism or death at 30 days. METHODS: In a prospective, observational, single-center study, 236 subjects with recent-onset AF were consecutively enrolled from January 2011 until January 2013...
August 2016: American Journal of Emergency Medicine
Gerrit Frommeyer, Christian Ellermann, Dirk G Dechering, Simon Kochhäuser, Nils Bögeholz, Fatih Güner, Patrick Leitz, Christian Pott, Lars Eckardt
BACKGROUND: Ranolazine has been reported to have an antiarrhythmic potential. The aim of this study was to assess the electrophysiologic effects of ranolazine and to compare its effects to vernakalant in an experimental whole-heart model of short-QT syndrome. METHODS: Rabbit hearts were isolated and Langendorff-perfused. After obtaining baseline data, pinacidil, an IKATP channel opener, was administered (1 μM). RESULTS: Endo- and epicardial monophasic action potentials and a 12-lead ECG showed a significant abbreviation of QT interval (- 34 milliseconds, P < 0...
October 2016: Journal of Cardiovascular Electrophysiology
Justo Juliá, María López-Gil, Lola Villagraz, Álvaro Lozano, Adolfo Fontenla, Fernando Arribas
No abstract text is available yet for this article.
July 2016: Revista Española de Cardiología
Gregory N Beatch, Brian Mangal
BACKGROUND: Atrial fibrillation (AF) is a common cardiac arrhythmia that is associated with significant health risks. One strategy to mitigate the risks associated with long-term AF is to convert AF to sinus rhythm (SR). This study assessed the efficacy and safety of vernakalant hydrochloride for the pharmacological conversion of AF to SR. METHODS: Patients with recent-onset (duration >3 h- ≤ 7 days) symptomatic AF and no evidence or history of congestive heart failure were randomized in a 2:1 ratio to receive vernakalant or placebo...
May 28, 2016: BMC Cardiovascular Disorders
Juan Cosin-Sales, Armando Loscos, Ana Peiró, M Rosa Sorando, Francisco Buendía, Luis Ruescas
No abstract text is available yet for this article.
June 2016: Revista Española de Cardiología
Toshiki Chiba, Naoto Kondo, Akira Takahara
Electrical remodeling plays a pivotal role in maintaining the reentry during atrial fibrillation. In this study, we assessed influence of electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. We used an atrial electrical remodeling model of the rabbit, subjected to rapid atrial pacing (RAP; 600 beats/min) for 2-4 weeks, leading to shortening of atrial effective refractory period (AERP). Intravenous administration of dl-sotalol (6 mg/kg), bepridil (1 mg/kg), amiodarone (10 mg/kg) or vernakalant (3 mg/kg) significantly prolonged the AERP both in the control and RAP rabbits...
March 2016: Journal of Pharmacological Sciences
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