Effective suppression of atrial fibrillation by the antihistaminic agent antazoline: First experimental insights into a novel antiarrhythmic agent

Frommeyer, Gerrit; Sterneberg, Magdalena; Dechering, Dirk G.; Kaese, Sven; Bögeholz, Nils; Pott, Christian; Fehr, Michael; Bogossian, Harilaos; Milberg, Peter; Eckardt, Lars

doi:10.1111/1755-5922.12244

Cited by 20 publications

(22 citation statements)

References 22 publications

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“…Therefore, noncardiovascular drugs with potential antiarrhythmic properties move into focus. The antihistaminic drug antazoline presented antiarrhythmic effects in an experimental model of AF 8 that reproduced the results of clinical pilot experiences. 9 Recurrent discussion on the 'French Paradox' directed interest to some compounds of red wine.…”

Section: Introductionsupporting

confidence: 59%

Acute electrophysiologic effects of the polyphenols resveratrol and piceatannol in rabbit atria

Frommeyer

Wolfes

Ellermann

et al. 2018

Clin Exp Pharma Physio

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The natural polyphenol resveratrol and its analogue piceatannol have various beneficial effects including antiarrhythmic properties. The aim of the present study was to examine potential electrophysiologic effects in an experimental whole-heart model of atrial fibrillation (AF). Simultaneous infusion of resveratrol (50μM) or piceatannol (10μM) in rabbit hearts resulted in an increase of atrial refractory period. Both agents induced a significant slowing of atrial conduction and of intrinsic heart rate. In both groups, a trend towards a reduction of AF and a regularization of AF was observed. This article is protected by copyright. All rights reserved.

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Section: Introductionsupporting

confidence: 59%

Acute electrophysiologic effects of the polyphenols resveratrol and piceatannol in rabbit atria

Frommeyer

Wolfes

Ellermann

et al. 2018

Clin Exp Pharma Physio

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“…1,4 Antazoline is a I generation antihistaminic drug with antifibrillatory properties. 5 Basic studies have suggested a multichannel mode of action resulting in, among others, changes in inter-and intraatrial conduction and prolongation of QRS and QT intervals without significant influence on atrio-ventricular node or accessory pathway effective refractory periods. [6][7][8][9] In human healthy volunteers, the terminal elimination half-life of antazoline was 2.29 hours with a mean residence time 3.45 hours.…”

Section: Introductionmentioning

confidence: 99%

Clinical effectiveness and safety of antazoline‐based therapy in patients with stable coronary artery disease undergoing pharmacological cardioversion of short‐duration atrial fibrillation in the emergency department

Farkowski

Maciąg

Zurawska

et al. 2018

Cardiovascular Therapeutics

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Summary Introduction Options for a pharmacological cardioversion (CV) of short‐duration atrial fibrillation (AF) in patients with a stable coronary artery disease (CAD) are limited to amiodarone or vernakalant. Antazoline has been reported to achieve high rates of AF conversion to sinus rhythm, but data on its effectiveness and, more importantly, safety in stable CAD patients, have been sparse. Aims To assess the effectiveness and safety of antazoline‐based therapy in patients with a stable CAD undergoing pharmacological CV of short‐duration AF in the emergency department (ED). Results A retrospective case‐control study. We conducted an analysis of medical records of patients with a stable CAD undergoing CV of short duration (≤48 hours) AF in the ED using intravenous antazoline. The main endpoints of the study were successful cardioversion of AF and hospitalization due to the adverse effects (AE) of the treatment. Between 2008 and 2012, out of 548 CVs, antazoline was administered 334 times: 138 in CAD and 196 in the control group. Patients in the CAD group were older and had more comorbidities than controls; 65 patients had had a history of myocardial infarction (MI). In CAD group, the effectiveness was higher (82.6% vs 63.8%, RB: 1.30 [95% CI: 1.14‐1.48], P = 0.0002) and the hospitalization rate due to AE was similar (1.4% vs 4.1%, RR: 0.36 [95% CI: 0.08‐1.65], P = 0.2054) to the control group. Among patients with CAD, a history of MI did not influence the effectiveness or safety of the CV (P = 0.2252 and P = 1.0000, respectively). Conclusions In selected patients with a stable CAD, even with a history of MI, antazoline‐based CV of short‐duration AF may be an effective and safe therapeutic option.

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“…An AF induction during the procedure may affect PVI assessment and generally requires electrical or pharmacological cardioversion. Antazoline is a I generation antihistaminic drug displaying antiarrhythmic properties . Antazoline is administered intravenously in 50–100 mg boluses until conversion of AF to sinus occurs or up to a cumulative dose of 250–300 mg .…”

Section: Introductionmentioning

confidence: 99%

Intravenous antazoline, a first‐generation antihistaminic drug with antiarrhythmic properties, is a suitable agent for pharmacological cardioversion of atrial fibrillation induced during pulmonary vein isolation due to the lack of influence on atrio‐venous conduction and high clinical effectiveness (AntaEP Study)

Farkowski

Maciąg

Kowalik

et al. 2019

Brit J Clinical Pharma

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Aims: Antazoline is a first-generation antihistaminic drug used primarily in eye drop formulations. When administered intravenously, antazoline displays antiarrhythmic properties resulting in a rapid conversion of recent-onset atrial fibrillation (AF) to sinus rhythm (SR).The aim of the study was to assess the influence of antazoline on atrio-venous conduction and other electrophysiological parameters in patients undergoing AF ablation.Methods: An experimental prospective study. Patients scheduled for the first-time AF ablation, in SR and not on amiodarone were enrolled. Atrio-venous conduction assessment and invasive electrophysiological study (EPS) were performed before and after intravenous administration of 250 mg of antazoline. In case of AF induction during EPS, antazoline was administered until conversion to SR or a cumulative dose of 300 mg. Results:We enrolled 14 patients: 13 (93%) men, mean age 63.4 (59.9-66.8) years, mean CHA 2 DS 2 -VASc score 1.6 (1.0-2.2). Antazoline was administered in a mean dose 257.1 (246.7-267.6) mg. Pulmonary vein potentials and atrial capture during pulmonary vein stimulation were present before and after the administration of antazoline. Wenckebach point and atrial conduction times did not change significantly, but atrio-ventricular node effective refractory period improved-324.7 (275.9-373.5) ms vs 284.3 (256.2-312.4) ms, P = 0.02. Antazoline was effective in all 5 (100%) cases of AF induction during EPS. There were no serious adverse events.Conclusion: Due to the lack of influence on atrio-venous conduction and high clinical effectiveness, antazoline may be suitable for pharmacological cardioversion of AF occurring during AF ablation.The authors confirm that the Principal Investigator for this paper is Michal M. Farkowski and that he had direct clinical responsibility for patients.

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Effective suppression of atrial fibrillation by the antihistaminic agent antazoline: First experimental insights into a novel antiarrhythmic agent

Abstract: Administration of ANT was highly effective in suppressing AF. The antiarrhythmic effect could be explained by a significant increase in postrepolarization refractoriness as a result of a more marked increase in aERP as compared with aAPD.

Cited by 20 publications

References 22 publications

Acute electrophysiologic effects of the polyphenols resveratrol and piceatannol in rabbit atria

Acute electrophysiologic effects of the polyphenols resveratrol and piceatannol in rabbit atria

Clinical effectiveness and safety of antazoline‐based therapy in patients with stable coronary artery disease undergoing pharmacological cardioversion of short‐duration atrial fibrillation in the emergency department

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