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Introduction Antazoline (ANT) is an old antihistaminic medication with antiarrhythmic properties. After intravenous administration ANT exerts rapid antiarrhythmic effect often resulting in conversion of atrial fibrillation (AF) to sinus rhythm (SR) and is widely used in Poland for this purpose in the last years. However, published data on its effectiveness, safety and clinical utility for rapid AF termination are limited and ANT is not recognized as a cardioversion drug. Aim To assess the real-world efficacy of ANT for pharmacological cardioversion of paroxysmal and persistent non-valvular AF. Methods Our single center, retrospective, observational study included patients (pts) with history paroxysmal or persistent AF episode lasting less than 6 months, in stable cardiopulmonary condition who were qualified for elective pharmacological cardioversion with intravenous ANT. The primary end-point was the conversion of AF to SR confirmed in electrocardiography (ECG) during the 6-hours observation. Results A total of 176 pts (mean age 68.4±12.0 years, 49% male) were enrolled into the study. In 93 patients (52%) AF duration was shorter than 48 hours and median AF duration time was 24 (7–432) hours. The overall success rate of pharmacological cardioversion of AF with intravenous ANT was 45.5% (80/176 pts). The mean used dose of ANT was 250.9±65.4mg. The subgroup analysis, regarding the AF duration, suggested the effectiveness of ANT mainly in in short-lasting AF (effectiveness of antazoline based cardioversion for AF lasting Conclusions Antazoline is effective and safe in rapid pharmacological cardioversion of paroxysmal AF, especially in the short-lasting AF ( Funding Acknowledgement Type of funding sources: None. Figure 1. ROC curve analysis

Funding Acknowledgements Type of funding sources: None. Introduction Antazoline (ANT) is an old antihistaminic medication with antiarrhythmic properties. After intravenous administration ANT exerts rapid antiarrhythmic effect often resulting in conversion of persistent atrial fibrillation (AF) to sinus rhythm (SR). However, published data on its effectiveness, safety and clinical utility for rapid AF termination are limited and ANT is not recognized as a cardioversion drug. Aim To assess the real-world efficacy of ANT for pharmacological cardioversion of paroxysmal and persistent non-valvular AF. Methods We conducted a single center, retrospective, observational study including patients (pts) with history paroxysmal or persistent AF episode lasting less than 6 months, in stable cardiopulmonary condition who were qualified for elective pharmacological cardioversion with intravenous ANT. The primary end-point was the conversion of AF to SR confirmed in electrocardiography (ECG) during the 6-hours observation. Results A total of 176 pts (mean age 68.4 ± 12.0 years, 49% male) were enrolled into the study. In 93 patients (52%) AF duration was shorter than 48 hours and median AF duration time was 24 (7 – 432) hours. The overall success rate of pharmacological cardioversion of AF with intravenous ANT was 45.5% (80/176 pts). The mean used dose of ANT was 250.9 ± 65.4mg. The subgroup analysis, regarding the AF duration, suggested the effectiveness of ANT mainly in in short-lasting AF (effectiveness of antazoline based cardioversion for AF lasting Conclusions Intravenous antazoline administration is effective and safe in rapid pharmacological cardioversion of paroxysmal AF, especially in the short-lasting AF (

Background Antazoline mesylate represents a first generation antihistamine with quinidine-like antiarrhythmic properties, which allows for rapid and effective termination of atrial fibrillation (AF). Despite its widespread use in Polish emergency departments, paucity of data exists concerning safety and efficacy of antazoline in comparison to other antiarrhythmic agents. Purpose This study aimed to evaluate the pooled hitherto data on effectiveness and safety of pharmacological Cardioversion with intravenous ANTazoline (CANT Study) in short-duration atrial fibrillation. Methods This retrospective observational study was performed in 5 medical centers and comprised 1300 patients with paroxysmal or persistent AF who underwent emergent pharmacological cardioversion in the real-world setting of emergency or cardiology department. The choice of antiarrhythmic drug was left to the discretion of attending physician. The exclusion criteria involved permanent AF, other supraventricular arrhythmias, including atrial flutter, chronic antiarrhythmic therapy or preemptive electrical cardioversion. The primary endpoint was restoration of sinus rhythm up to 12 hours after antiarrhythmic drug infusion. The combined safety endpoint was bradycardia Results The mean age of study population was 67.7±11.6 years and the majority of patients were men (52.9%). The median AF episode duration was 10 (4; 24) hours, while median CHA2DS2-VASc score was 3 (2; 4) pts. Antazoline alone was administered in 45.6% of patients (n=593); amiodarone in 22.1% (n=287); propafenone in 11.5% (n=150); sotalol in 0.5% (n=6), while 20.3% (n=264) received overlapping antiarrhythmic therapy. Antazoline had the highest rhythm conversion rate (Figure), which was comparable to propafenone (78.2% vs 72.7%; RR 1.08; 95% CI:0.97–1.20; P=0.175) and superior to amiodarone (vs 66.9%; RR 1.17, 95% CI:1.07–1.28; P=0.0008) and collective amiodarone/propafenone/sotalol treatment (vs 68.6%; RR 1.14; 95% CI:1.06–1.23; P=0.0006). The rate of combined safety endpoint was comparable in patients treated with antazoline and other antiarrhythmic drugs (5.2% vs 3.9%; P=0.297). Among patients treated with antazoline, 29 exhibited bradycardia Conclusion Antazoline appears to be an effective antiarrhythmic drug for cardioversion of atrial fibrillation, which is associated with low rate of relatively benign adverse events. Figure 1 Funding Acknowledgement Type of funding source: None

Background Former studies corroborated promising quinidine-like properties of antazoline mesylate facilitating rapid cardioversion atrial fibrillation (AF). Still, paucity of data exists concerning direct comparison of antazoline to other antiarrhythmic agents. Purpose The study aimed to verify the hypothesis that intravenous antazoline is non-inferior to amiodarone and/or propafenone in terms of rhythm conversion rate and safety among patients with AF. Methods After reviewing 2344 consecutive medical records with I48 code of international classification of diseases (ICD), 505 eligible patients (21.5%) with paroxysmal or persistent AF who underwent emergent pharmacological cardioversion in the real-world setting of emergency department were enrolled in retrospective observational analysis. The choice of antiarrhythmic drug was left to the discretion of attending physician. Antazoline group was separately matched with corresponding amiodarone (n=218) and propafenone (n=90) cohort using propensity score matching (PSM) with nearest neighbor algorithm (ratio 1:1), adjusting for age, sex, arterial hypertension, diabetes, depressed left ventricular ejection fraction, coronary artery disease, history of stroke, AF ablation, CHA2DS2-VASc score, chronic kidney disease and duration of AF episode. The primary endpoint was restoration of sinus rhythm in the emergency department. Results The study population (mean age of 67 (59; 74) years; 53.7% females) was characterized by median AF episode duration of 10.5 (5; 24) hours. Antazoline alone was administered in 23.4% of patients (n=118); amiodarone in 47.5% (n=240); propafenone in 9.9% (n=50); while 19.2% (n=97) received ≥2 antiarrhythmic drugs. Before PSM adjustment, antazoline had comparable rhythm conversion rate to propafenone (85.6% vs. 80.0%; P=0.367) and higher than amiodarone treatment (vs. 66.7%, P=0.0002), and greater than combined amiodarone/propafenone group (68.6%; RR 1.25; 95% CI: 1.12–1.39, P=0.0001). After PSM, the use of antazoline was associated with the efficacy similar to propafenone (82.2% vs. 80.0%, RR 1.03; 95% CI: 0.84–1.25, P=0.788) and superior to amiodarone (85.3% vs. 67.0%, RR 1.27, 95% CI: 1.09–1.48, P=0.0019, number needed to treat 5.5; Figure). No major adverse actions were reported in the antazoline group. Conclusion Antazoline appears to be an efficacious and safe drug for pharmacological cardioversion of AF in real-life setting, which is at least non-inferior to existing antiarrhythmic drugs. Acknowledgement/Funding None

Different HPLC chromatographic systems were investigated on a C18ACE 5 μm, 150 × 4.6 mm id column for the determination of tymazoline, tramazoline, and antazoline, with either naphazoline or xylometazoline, in commercial preparations. For the development and optimization of the systems, a Response Surface Method (r = 0.925–0.980) was used to illustrate the changes in k as a function of pH values and different salt concentrations. The simultaneous separation of 2-imidazolines was accomplished at 40°C with 0.01 M ammonium acetate–methanol (50 + 50, v/v, pH 6.0) mobile phase at a flow rate of 1.2 mL/min. In order to deal with the usual coexistence of 2-imidazolines with benzethonium and benzalkonium chloride preservatives, it was necessary to use another chromatographic system, 0.01 M ammonium acetate–methanol (50 + 50, v/v) mobile phase on a cyano ACE 5 μm, 150 × 4.6 mm id column. As part of a more thorough theoretical investigation, a partial least-squares (PLS) technique was used for modeling the RP-HPLC retention data. The model was based on molecular structure descriptors of the analytes' X variables and on their retention time (Log K) Y. The goodness of fit was estimated by the PLS correlation coefficient (r2) and root mean square error of estimation values, which were 0.994 and 0.0479, respectively.

A liquid chromatographic (LC) analysis has been developed for determining naphazoline and antazoline in ophthalmic preparations. The LC system is designed so that a variety of ophthalmic solutions containing naphazoline and antazoline can be analyzed with precision.

A method has been developed using a diffusion cell in an attempt to determine the drug release from viscous solutions under conditions simulating the blinking movements in the rabbit and human eye. Diffusion coefficients were determined at rest and at different velocities. For the solutions at rest, corresponding with the conditions at the surface of the rabbit cornea, the diffusion velocity decreases with increasing viscosity. When the solution is moved at a velocity corresponding to that of lachrymal fluid at the surface of the human eye, the influence of viscosity may be neglected.

Summary Tripelennamine hydrochloride and antazoline hydrochloride were administered orally and subcutaneously, in amounts of from 1 mg./kg. body weight up to lethal doses, to albino rats assembled in Wahmann vertically-revolving drums for the recording of locomotor activity. Tripelennamine hydrochloride had a statistically insignificant effect upon locomotor activity, while antazoline hydrochloride depressed locomotor activity.

An analysis was made of the effect of effluents from both outside and inside of the isolated guinea pig ileum segments. The action of the outside effluents was directed towards nervous elements of the test segment of the isolated ileum. According to the effect of atropine, morphine and hexamethonium, the action of theeffluent resembled that of 5-HT. Atropine and antazoline did not inhibit the effect of the effluent obtained from the inside of the donor gut upon the isolated rat fundus, but BOL and LSD did so in most experiments. The effect of this effluent upon the test segment of the guinea pig ileum was inhibited by morphine, or by a previous desensitation of the preparation by large doses of 5-HT. The smooth muscle stimulating effect of the effluent probably was due to its content in 5-HT and at least partly to some other as yet unidentified substance(s).

A rapid method for the determination of naphazoline in antazoline- naphazoline drops is discussed. The method depends upon precipitating antazoline by a solution of sodium carbonate. Naphazoline is determined in the filtrate using (i) the modified Vierordt method and (ii) Glenn's method of orthogonal functions to correct for the unprecipitated fraction of antazoline.