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Polish Archives of Internal Medicine Jun 2022
Topics: Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Humans
PubMed: 35766936
DOI: 10.20452/pamw.16264 -
Polish Archives of Internal Medicine Sep 2023The choice between rhythm and rate control strategy represents one of the most intriguing dilemmas in the management of atrial fibrillation (AF). Although the advantage... (Review)
Review
The choice between rhythm and rate control strategy represents one of the most intriguing dilemmas in the management of atrial fibrillation (AF). Although the advantage of rhythm over rate control in terms of outcome has not been unequivocally proven, the initial management of patients with symptomatic episodes of AF frequently involves early cardioversion. As electrical cardioversion (EC) is challenging in terms of fasting status and involvement of an anesthesiologic team, pharmacological cardioversion (PC) is usually selected as the first step toward rhythm conversion. Qualification criteria for PC or EC are similar and should comprise assessment of hemodynamic status, estimation of arrhythmic episode duration, evaluation of anticoagulation regimen, exclusion of other supraventricular arrhythmias, and assessment of the chance of rhythm conversion and persistence of sinus rhythm. Finally, the choice of adequate antiarrhythmic drug (AAD) depends on the presence of structural heart disease (SHD) and local experience. In patients without any SHD, complications occur rarely, hence traditional (propafenone, flecainide) or nonclassical Vaughan-Williams class I (antazoline) or class III (vernakalant, ibutilide, or dofetilide) drugs are preferred. The presence of SHD consistent with any left ventricular hypertrophy, heart failure, myocardial ischemia, or valvular heart disease limits the choice of AAD to amiodarone. Given the risk of ventricular proarrhythmia of AAD, safety should always prevail over the enticing possibility of rhythm conversion. The present review aims to provide a comprehensible summary of proper qualification for PC, selection of suitable AAD, and state‑of‑the‑art periprocedural management of patients with recent‑onset AF.
Topics: Humans; Atrial Fibrillation; Electric Countershock; Anti-Arrhythmia Agents; Propafenone; Heart Failure; Heart Diseases; Treatment Outcome
PubMed: 37622443
DOI: 10.20452/pamw.16547 -
Pharmaceuticals (Basel, Switzerland) Mar 2022Antazoline is an antihistaminic drug that is effective in the termination of paroxysmal atrial fibrillation. Despite its long presence in the market, antazoline's ADME...
Antazoline is an antihistaminic drug that is effective in the termination of paroxysmal atrial fibrillation. Despite its long presence in the market, antazoline's ADME parameters and pharmacokinetic effects in humans are poorly characterized. The objective of this study was to fill this gap by generation of in vitro and in vivo data and the development of a physiologically based pharmacokinetic model describing antazoline and its main metabolite disposition. A set of ADME parameters for the antazoline and its hydroxy metabolite is provided based on literature data, QSAR predictions, in vitro binding and metabolic stability assays. These can be used to feed PBPK models. In our current work, the developed PBPK model simulating simultaneously the pharmacokinetic profile of antazoline and its metabolite was successfully verified against the available clinical data and the presented capability to account for the clinically observed variability. When used to feed the PD model (e.g., simulating ECG), concentration-time profiles predicted by the model enable the assessment of antazoline's effect in various clinical scenarios with the possibility to account for population differences or CP mediated drug-drug interactions.
PubMed: 35337175
DOI: 10.3390/ph15030379 -
Polish Archives of Internal Medicine Jan 2022There is insufficient evidence on the efficacy and safety of pharmacological cardioversion of recent‑onset atrial fibrillation (AF) in elderly patients. Antazoline has...
INTRODUCTION
There is insufficient evidence on the efficacy and safety of pharmacological cardioversion of recent‑onset atrial fibrillation (AF) in elderly patients. Antazoline has been shown to be effective and safe in various patient populations.
OBJECTIVES
We aimed to compare the clinical efficacy and safety of intravenous antazoline for pharmacological cardioversion of recent‑onset AF between patients aged 75 years or older and those younger than 75 years.
PATIENTS AND METHODS
This retrospective analysis was conducted using data derived from emergency room medical records of patients referred for pharmacological cardioversion due to symptomatic AF lasting less than 48 hours. The threshold for old age was set at 75 years. Conversion to sinus rhythm was considered the primary efficacy outcome. The primary safety outcome was defined as any adverse event requiring hospitalization.
RESULTS
The study included 334 participants, of whom 110 patients were aged 75 years or older (study group) and 224 patients were younger than 75 years (controls). Successful cardioversion was achieved using lower mean (SD) antazoline doses in the study group than in controls: 151 (59) mg vs 168 (58) mg (P = 0.039). Study and control groups showed a similar efficacy and safety of antazoline (78.2% and 68.3%, respectively; odds ratio [OR], 1.66; 95% CI, 0.98-1.31; P = 0.06) as well as hospitalization rates (0.9% and 4.0%, respectively; OR, 0.22; 95% CI, 0.03-1.75; P = 0.17).
CONCLUSIONS
Intravenous antazoline seems to be effective and safe for pharmacological cardioversion of recent‑onset AF in elderly patients in the emergency setting.
Topics: Aged; Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Electric Countershock; Humans; Retrospective Studies; Treatment Outcome
PubMed: 34643078
DOI: 10.20452/pamw.16120 -
Polish Archives of Internal Medicine Jun 2022Due to safety concerns about available antiarrhythmic drugs (AADs), reliable agents for termination of atrial fibrillation (AF) are requisite.
INTRODUCTION
Due to safety concerns about available antiarrhythmic drugs (AADs), reliable agents for termination of atrial fibrillation (AF) are requisite.
OBJECTIVES
The aim of the study was to evaluate the efficacy and safety of antazoline, a first‑generation antihistamine, for cardioversion of recent‑onset AF in the setting of an emergency department.
PATIENTS AND METHODS
This multicenter, retrospective registry covered 1365 patients (median [interquartile range] age, 69.0 [61.0-76.0] years, 53.1% men) with new‑onset AF submitted to urgent pharmacological cardioversion. AAD allocation was performed by the attending physician: antazoline alone was utilized in 600 patients (44%), amiodarone in 287 (21%), propafenone in 150 (11%), and ≥2 AADs in 328 patients (24%). Antazoline in monotherapy or combination was administered to 897 patients (65.7%). Matched antazoline and nonantazoline groups were identified using propensity score matching (PSM, n = 330). The primary end point was return to sinus rhythm within 12 hours after initiation of the treatment.
RESULTS
Before PSM, antazoline alone was superior to amiodarone (78.3% vs 66.9%; relative risk [RR], 1.17; 95% CI, 1.07-1.28; P <0.001) and comparable to propafenone (78.3% vs 72.7%; RR, 1.08; 95% CI, 0.97-1.20; P = 0.14) in terms of rhythm conversion rate. In the post‑PSM population, the rhythm conversion rate was higher among patients receiving antazoline alone than in the nonantazoline group (84.2% vs 66.7%; RR, 1.26; 95% CI, 1.11-1.43; P <0.001), and the risk of adverse events was comparable (P = 0.2).
CONCLUSIONS
Antazoline appears to be an efficacious agent for termination of AF in real‑world setting. Randomized controlled trials are required to evaluate its safety in specific patient populations.
Topics: Aged; Amiodarone; Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Electric Countershock; Female; Humans; Male; Propafenone; Propensity Score; Registries; Retrospective Studies; Treatment Outcome
PubMed: 35293200
DOI: 10.20452/pamw.16234 -
Journal of Fluorescence Feb 2024A green developed spectrofluorimetric method has been applied for Antazoline (ANT) and Xylometazoline (XLO) determination in both pharmaceutical formulation and pure...
A green developed spectrofluorimetric method has been applied for Antazoline (ANT) and Xylometazoline (XLO) determination in both pharmaceutical formulation and pure form. The developed method is synchronous spectrofluorimetry coupled with the second derivative mathematical tool for the determination of antazoline and xylometazoline in their dosage form. The developed method depends on reacting the cited drugs with dansyl chloride, a suitable derivatizing agent, to generate highly fluorescent derivatives. The products formed were measured at emission wavelengths; 703.0 and 712.0 nm after being excited at wavelengths; 350.0 and 355.0 nm for antazoline and xylometazoline, respectively. Synchronous spectrofluorimetry coupled with second derivative mathematical tool was developed and optimized using fluorescence data manager software generating second derivative peak amplitudes at 556.5 nm for antazoline and 598.0 nm for xylometazoline. Linear responses have been represented over a wide range of concentration 0.5-12.0 µg/mL for antazoline and 0.1-10.0 µg/mL for xylometazoline, correspondingly. Method validation was successfully applied. Additionally, statistical comparison of developed method with official ones has been carried out where no significant difference was found. Evaluation of the method's greenness was proven using several assessment tools. Indeed, the method developed is found to be precise, sensitive, and discriminating to assess the cited drugs for regular analysis.
PubMed: 38319520
DOI: 10.1007/s10895-024-03585-0 -
Virologica Sinica Jun 2021Hepatitis B virus (HBV) belongs to Hepadnaviridae family and mainly infects hepatocytes, which can cause acute or chronic hepatitis. Currently, two types of antiviral...
Hepatitis B virus (HBV) belongs to Hepadnaviridae family and mainly infects hepatocytes, which can cause acute or chronic hepatitis. Currently, two types of antiviral drugs are approved for chronic infection clinically: interferons and nucleos(t)ide analogues. However, the clinical cure for chronic infection is still rare, and it is a huge challenge for all researchers to develop high-efficiency, safe, non-tolerant, and low-toxicity anti-HBV drugs. Antazoline hydrochloride is a first-generation antihistamine with anticholinergic properties, and it is commonly used to relieve nasal congestion and in eye drops. Recently, an in vitro high-throughput evaluation system was constructed to screen nearly 800 compounds from the Food and Drug Administration (FDA)-approved Drug Library. We found that arbidol hydrochloride and antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC of 4.321 μmol/L and 2.910 μmol/L in HepAD38 cells, respectively. Moreover, the antiviral effects and potential mechanism of action of antazoline hydrochloride were studied in different HBV replication systems. The results indicate that antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells, with an EC of 2.349 μmol/L. These findings provide new ideas for screening and research related to HBV agents.
Topics: Antazoline; Antiviral Agents; DNA; DNA, Viral; Drug Repositioning; Hepatitis B; Hepatitis B virus; Hepatitis B, Chronic; Humans; Virus Replication
PubMed: 33165771
DOI: 10.1007/s12250-020-00306-2 -
Advances in Medical Sciences Apr 2024Little is known about the effectiveness of pharmacological cardioversion (PCV) with antazoline in comparison to flecainide. The aim of this study was to compare the...
PURPOSE
Little is known about the effectiveness of pharmacological cardioversion (PCV) with antazoline in comparison to flecainide. The aim of this study was to compare the effectiveness of antazoline in restoring sinus rhythm (SR) versus amiodarone, flecainide and propafenone in a group of emergency department (ED) patients.
MATERIALS/METHODS
This was a single-centre retrospective analysis of patient records from an ED in a large hospital in Poland. We analysed a total of 1878 patient records, divided based on the anti-arrhythmic drug (AAD) administered during PCV: antazoline (n = 1080), antazoline + β-blocker (n = 479), amiodarone (n = 129), flecainide (n = 102), propafenone (n = 88). Of the patients, 63.5 % were female (median 65 years, [19-100]).
RESULTS
The percentage of successful PCV was significantly higher in the antazoline group (84.3 %) than in the antazoline + β-blocker (75.8 %, p = 0.0001), propafenone (75.6 %, p = 0.0364) and amiodarone (68.8 %, p < 0.0001) groups. Post-hoc analysis revealed that patients who received PCV with antazoline, antazoline + β-blocker, flecainide and propafenone had significantly shorter time to SR than those who received amiodarone (p < 0.0001). Univariate regression analysis revealed that patients who underwent PCV with antazoline were almost twice as likely to return to SR compared to the other groups (p < 0.0001, OR 1.81, 95 % CI 1.44-2.27).
CONCLUSIONS
This is the first study comparing the effectiveness of antazoline in PCV versus flecainide in addition to the previously studied amiodarone and propafenone. Our results indicate that antazoline is more effective in restoring SR than amiodarone, flecainide and propafenone. In addition, antazoline restored SR significantly faster than amiodarone or propafenone.
PubMed: 38649031
DOI: 10.1016/j.advms.2024.04.003 -
American Journal of Cardiovascular... Jul 2023Since atrial fibrillation (AF) is one of the major arrhythmias managed in hospitals worldwide, it has a major impact on public health. The guidelines agree on the... (Meta-Analysis)
Meta-Analysis
PURPOSE
Since atrial fibrillation (AF) is one of the major arrhythmias managed in hospitals worldwide, it has a major impact on public health. The guidelines agree on the desirability of cardioverting paroxysmal AF episodes. This meta-analysis aims to answer the question of which antiarrhythmic agent is most effective in cardioverting a paroxysmal AF.
MATERIALS AND METHODS
A systematic review and Bayesian network meta-analysis, searching MEDLINE, Embase, and CINAHL, were performed, including randomized controlled trials (RCTs) enrolling a population of unselected adult patients with a paroxysmal AF that compared at least two pharmacological regimes to restore the sinus rhythm or a cardioversion agent against a placebo. The main outcome was efficacy in restoring sinus rhythm.
RESULTS
Sixty-one RCTs (7988 patients) were included in the quantitative analysis [deviance information criterion (DIC) 272.57; I = 3%]. Compared with the placebo, the association verapamil-quinidine shows the highest SUCRA rank score (87%), followed by antazoline (86%), vernakalant (85%), tedisamil at high dose (i.e., 0.6 mg/kg; 80%), amiodarone-ranolazine (80%), lidocaine (78%), dofetilide (77%), and intravenous flecainide (71%). Taking into account the degree of evidence of each individual comparison between pharmacological agents, we have drawn up a ranking of pharmacological agents from the most effective to the least effective.
CONCLUSIONS
In comparing the antiarrhythmic agents used to restore sinus rhythm in the case of paroxysmal AF, vernakalant, amiodarone-ranolazine, flecainide, and ibutilide are the most effective medications. The verapamil-quinidine combination seems promising, though few RCTs have studied it. The incidence of side effects must be taken into account in the choice of antiarrhythmic in clinical practice.
CLINICAL TRIAL REGISTRATION
PROSPERO: International prospective register of systematic reviews, 2022, CRD42022369433 (Available from: https://www.crd.york.ac.uk/prospero/display_record.php?ID=CRD42022369433 ).
Topics: Adult; Humans; Atrial Fibrillation; Quinidine; Flecainide; Electric Countershock; Ranolazine; Network Meta-Analysis; Randomized Controlled Trials as Topic; Systematic Reviews as Topic; Anti-Arrhythmia Agents; Amiodarone; Verapamil
PubMed: 37233967
DOI: 10.1007/s40256-023-00586-5 -
Journal of Pharmaceutical and... Oct 2023This work implements a stability indicating HPLC method developed to simultaneously determine xylometazoline (XYLO) and antazoline (ANT) in their binary mixture, rabbit...
Exquisite integration of quality-by-design and green analytical approaches for simultaneous determination of xylometazoline and antazoline in eye drops and rabbit aqueous humor, application to stability study.
This work implements a stability indicating HPLC method developed to simultaneously determine xylometazoline (XYLO) and antazoline (ANT) in their binary mixture, rabbit aqueous humor and cited drug's degradates by applying analytical quality-by-design (AQbD) combined with green analytical chemistry (GAC) experiment for the first time. This integration was designed to maximize efficiency and minimize environmental impacts, as well as energy and solvent consumption. Analytical quality-by-design was applied to achieve our aim starting with evaluation of quality risk and scouting analysis, tracked via five parameters chromatographic screening using Placket-Burman design namely: pH, temperature, organic solvent percentage, flow rate, and wavelength detection. Recognizing the critical method parameters was done followed by optimization employing central composite design and Derringer's desirability toward assess optimum conditions that attained best resolution with satisfactory peak symmetry with short run time. Optimal chromatographic separation was attained by means of an XBridge® C18 (4.6 × 250 mm, 5 µm) column through isocratic elution using a mobile phase consists of phosphate buffer (pH 3.0): ethanol (60:40, by volume) at a 1.6 mL/min flow rate and 230.0 nm UV detection. Linearity acquired over a concentration range of 1.0-100.0 µg/mL and 0.5-100.0 µg/mL for XYLO and ANT, respectively. Furthermore, imperiling cited drugs' stock solutions to stress various conditions and satisfactory peaks of degradation products were obtained indicating that cited drugs are vulnerable to oxidative degradation and basic hydrolysis. Degradates' structures were elucidated using mass spectrometry. Applying various assessment tools; namely: analytical greenness (AGREE), green analytical procedure index (GAPI), analytical eco-scale, and national environmental method index (NEMI), Greenness method's evaluation was applied and proved to be green. In fact, the developed method is established to be perceptive, accurate, and selective to assess cited drugs for routine analysis.
Topics: Animals; Rabbits; Antazoline; Ophthalmic Solutions; Aqueous Humor; Limit of Detection; Solvents; Chromatography, High Pressure Liquid
PubMed: 37516064
DOI: 10.1016/j.jpba.2023.115598