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Polskie Archiwum Medycyny Wewnetrznej Jun 2016INTRODUCTION Numerous studies described the effectiveness and safety of antazoline in pharmacological cardioversion of short‑duration atrial fibrillation (AF).... (Comparative Study)
Comparative Study
Comparative effectiveness and safety of antazoline‑based and propafenone‑based strategies for pharmacological cardioversion of short‑duration atrial fibrillation in the emergency department.
INTRODUCTION Numerous studies described the effectiveness and safety of antazoline in pharmacological cardioversion of short‑duration atrial fibrillation (AF). However, there are no data on the comparison of antazoline and antiarrhythmic drugs listed in clinical guidelines. OBJECTIVES The aim of the study was to assess the comparative effectiveness and safety of antazoline‑based and propafenone‑based strategies in pharmacological cardioversion of short‑duration AF performed in our emergency department. PATIENTS AND METHODS We conducted a retrospective case‑control study based on the analysis of medical records of patients undergoing pharmacological cardioversion of short‑duration AF with intravenous antazoline or propafenone at our department in the years 2008-2012. The primary endpoint was the successful cardioversion of AF. The primary safety endpoint was hospitalization due to the adverse effects of the treatment. RESULTS We analyzed 432 cases of cardioversion. The mean age of patients was 68.9 ±9.8 years; 65% of the patients were male; 90% of the patients had a history of AF. Antazoline was administered 334 times and propafenone-98 times. The mean dose of antazoline was 172 ±65 mg, while all patients in the propafenone group received the drug at a fixed dose of 70 mg (1 vial). Cardioversion with antazoline was successful in 239 cases (71.6%) and with propafenone-in 54 patients (55.1%) (relative risk [RR], 1.30; 95% confidence interval [CI], 1.07-1.57). The rate of hospitalization due to the adverse effects of the treatment were low and similar between the study groups: 10 (3.0%) for antazoline and 4 (4.1%) for propafenone (RR, 0.73; 95% CI, 0.23-2.27). CONCLUSIONS The antazoline‑based strategy was more effective and safer in comparison with propafenone‑based strategy in the pharmacological cardioversion of short‑duration AF in our emergency department.
Topics: Aged; Aged, 80 and over; Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Emergency Service, Hospital; Female; Humans; Male; Middle Aged; Patient Safety; Propafenone; Retrospective Studies; Treatment Outcome
PubMed: 27362390
DOI: 10.20452/pamw.3452 -
Journal of Pharmaceutical and... Sep 2016Cloud-point extraction (CPE) is attracting increasing interest in a number of analytical fields, including bioanalysis, as it provides a simple, safe and... (Comparative Study)
Comparative Study
Cloud-point extraction (CPE) is attracting increasing interest in a number of analytical fields, including bioanalysis, as it provides a simple, safe and environmentally-friendly sample preparation technique. However, there are only few reports on the application of this extraction technique in liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) analysis. In this study, CPE was used for the isolation of antazoline from human plasma. To date, only one method of antazoline isolation from plasma exists-liquid-liquid extraction (LLE). The aim of this study was to prove the compatibility of CPE and LC-ESI-MS/MS and the applicability of CPE to the determination of antazoline in spiked human plasma and clinical samples. Antazoline was isolated from human plasma using Triton X-114 as a surfactant. Xylometazoline was used as an internal standard. NaOH concentration, temperature and Triton X-114 concentration were optimized. The absolute matrix effect was carefully investigated. All validation experiments met international acceptance criteria and no significant relative matrix effect was observed. The compatibility of CPE and LC-ESI-MS/MS was confirmed using clinical plasma samples. The determination of antazoline concentration in human plasma in the range 10-2500ngmL(-1) by the CPE method led to results which are equivalent to those obtained by the widely used liquid-liquid extraction method.
Topics: Antazoline; Calibration; Chromatography, High Pressure Liquid; Histamine H1 Antagonists; Humans; Liquid-Liquid Extraction; Octoxynol; Polyethylene Glycols; Quality Control; Reference Standards; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; Surface-Active Agents
PubMed: 27289300
DOI: 10.1016/j.jpba.2016.05.042 -
Journal of Pharmaceutical and... May 2016Capillary electrophoretic (CE) and high performance liquid chromatographic (HPLC) methods were developed and optimized for the determination of antazoline (ANT) and...
Capillary electrophoretic (CE) and high performance liquid chromatographic (HPLC) methods were developed and optimized for the determination of antazoline (ANT) and tetrahydrozoline (TET) in ophthalmic formulations. Optimum electrophoretic conditions were achieved using a background electrolyte of 20mM phosphate buffer at pH 7.0, a capillary temperature of 25°C, a separation voltage of 22 kV and a pressure injection of the sample at 50 mbar for 17s. HPLC analysis was performed with Kinetex (150 × 4.6mm ID × 5 μm) (Phenomenex, USA) analytical column with 1 mL min(-1) flow rate of mobile phase which consisted of 0.05% TFA in bidistilled water (pH adjusted to 3.0 with 5M NaOH) and acetonitrile/buffer in the ratio of 63:37 (v/v) at room temperature. Injection volume of the samples was 10 μL and the wavelength of the detector was set at 215 nm for monitoring both analytes. Calibration graphs showed a good linearity with a coefficient of determination (R(2)) of at least 0.998 for both methods. Intraday and interday precision (expressed as RSD%) were lower than 2.8% for CE and 0.92% for HPLC. The developed methods were demonstrated to be simple and rapid for the determination of ANT and TET in ophthalmic solutions providing recoveries in the range between 97.9 and 102.70% for CE and HPLC.
Topics: Antazoline; Chromatography, High Pressure Liquid; Electrophoresis, Capillary; Imidazoles; Ophthalmic Solutions
PubMed: 26952922
DOI: 10.1016/j.jpba.2016.02.032 -
Journal of Pharmaceutical and... May 2016Antazoline is a first-generation antihistaminic agent with antiarrhythmic quinidine-like properties. In some countries, it is widely used for termination of cardiac...
Application of a novel liquid chromatography/tandem mass spectrometry method for the determination of antazoline in human plasma: Result of ELEPHANT-I [ELEctrophysiological, pharmacokinetic and hemodynamic effects of PHenazolinum (ANTazoline mesylate)] human pharmacokinetic study.
Antazoline is a first-generation antihistaminic agent with antiarrhythmic quinidine-like properties. In some countries, it is widely used for termination of cardiac arrhythmias, especially atrial fibrillation (AF). However, no human pharmacokinetic studies have been conducted with intravenous antazoline. The aim of our study was to develop and validate a novel liquid chromatography/tandem mass spectrometry (LC-MS/MS) method for the determination of antazoline in human plasma: the ELEPHANT-I [ELEctrophysiological, pharmacokinetic and hemodynamic effects of PHenazolinum (ANTazoline mesylate)] human pharmacokinetic study. Antazoline was extracted from plasma using liquid-liquid extraction. The concentration of the analyte was measured by LC-MS/MS with xylometazoline as an internal standard. The method was validated for linearity, precision, accuracy, stability (freeze/thaw stability, stability in autosampler, short and long term stability), dilution integrity and matrix effect. The analyzed validation criteria were fulfilled. The method was applied to a pharmacokinetic study involving 10 healthy volunteers. Following a single intravenous dose of antazoline mesylate (100 mg), the plasma concentration profile showed a relative fast elimination with a terminal elimination half-life of 2.29 h. A relatively high volume of distribution was observed (Vss=315 L). The values of mean residence time (MRT∞), area under the curve (AUC∞) and clearance were 3.45 h, 0.91 mg h L(-1) and 80.5 L h(-1), respectively. One volunteer showed significant differences in pharmacokinetic parameters. In conclusion, the proposed new LC-MS/MS method was successfully used for the first time for the determination of antazoline in human plasma.
Topics: Adult; Antazoline; Chromatography, Liquid; Drug Stability; Female; Half-Life; Hemodynamics; Humans; Liquid-Liquid Extraction; Male; Mesylates; Plasma; Reproducibility of Results; Tandem Mass Spectrometry
PubMed: 26895496
DOI: 10.1016/j.jpba.2016.01.060 -
Spectrochimica Acta. Part A, Molecular... Apr 2016A comparative study was developed between two classical spectrophotometric methods (dual wavelength method and Vierordt's method) and two recent methods manipulating... (Comparative Study)
Comparative Study
Comparative study between recent methods manipulating ratio spectra and classical methods based on two-wavelength selection for the determination of binary mixture of antazoline hydrochloride and tetryzoline hydrochloride.
A comparative study was developed between two classical spectrophotometric methods (dual wavelength method and Vierordt's method) and two recent methods manipulating ratio spectra (ratio difference method and first derivative of ratio spectra method) for simultaneous determination of Antazoline hydrochloride (AN) and Tetryzoline hydrochloride (TZ) in their combined pharmaceutical formulation and in the presence of benzalkonium chloride as a preservative without preliminary separation. The dual wavelength method depends on choosing two wavelengths for each drug in a way so that the difference in absorbance at those two wavelengths is zero for the other drug. While Vierordt's method, is based upon measuring the absorbance and the absorptivity values of the two drugs at their λ(max) (248.0 and 219.0 nm for AN and TZ, respectively), followed by substitution in the corresponding Vierordt's equation. Recent methods manipulating ratio spectra depend on either measuring the difference in amplitudes of ratio spectra between 255.5 and 269.5 nm for AN and 220.0 and 273.0 nm for TZ in case of ratio difference method or computing first derivative of the ratio spectra for each drug then measuring the peak amplitude at 250.0 nm for AN and at 224.0 nm for TZ in case of first derivative of ratio spectrophotometry. The specificity of the developed methods was investigated by analyzing different laboratory prepared mixtures of the two drugs. All methods were applied successfully for the determination of the selected drugs in their combined dosage form proving that the classical spectrophotometric methods can still be used successfully in analysis of binary mixture using minimal data manipulation rather than recent methods which require relatively more steps. Furthermore, validation of the proposed methods was performed according to ICH guidelines; accuracy, precision and repeatability are found to be within the acceptable limits. Statistical studies showed that the methods can be competitively applied in quality control laboratories.
Topics: Antazoline; Anti-Allergic Agents; Drug Combinations; Imidazoles; Nasal Decongestants; Quality Control; Spectrophotometry
PubMed: 26836449
DOI: 10.1016/j.saa.2016.01.014 -
Europace : European Pacing,... Oct 2017The aim of the study was to assess the clinical efficacy of antazoline, a first-generation anti-histaminic agent, in the rapid conversion of paroxysmal non-valvular... (Randomized Controlled Trial)
Randomized Controlled Trial
AIMS
The aim of the study was to assess the clinical efficacy of antazoline, a first-generation anti-histaminic agent, in the rapid conversion of paroxysmal non-valvular atrial fibrillation (AF) to sinus rhythm in patients without heart failure.
METHODS AND RESULTS
This study was a single center, randomized, double blind, placebo-controlled, superiority clinical trial. We enrolled patients with an AF episode lasting less than 43 h, in stable cardiopulmonary condition. Subjects who fulfilled the selection criteria were randomly assigned to receive intravenously either a placebo or up to 250 mg of antazoline. The primary end point was the conversion of AF to sinus rhythm confirmed in electrocardiogram (ECG). We enrolled 74 patients: 36 (48.6%) in the antazoline group and 38 (51.4%) in the control group. The mean age was 68 ± 12 years (range 31-90 years), 39 (53.3%) patients were male. The successful conversion of AF to sinus rhythm during the observation period was achieved in 26 (72.2%) patients treated with antazoline and 4 (10.5%) in the control group: RR 6.86 (95% CI: 2.66-17.72, P < 0.0001). Median time to conversion was 16.0 min in antazoline and 72.5 min in the control group (P = 0.0246). There were no cases of atrial tachycardia/flutter in the antazoline group.
CONCLUSION
Intravenous antazoline was effective and safe in the rapid conversion of non-valvular paroxysmal atrial fibrillation to sinus rhythm in patients without heart failure. Clinical Trial Registration number: NCT01527279.
Topics: Action Potentials; Administration, Intravenous; Adult; Aged; Aged, 80 and over; Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Double-Blind Method; Electrocardiography; Female; Heart Conduction System; Heart Rate; Histamine H1 Antagonists; Humans; Male; Middle Aged; Poland; Time Factors; Treatment Outcome
PubMed: 28339554
DOI: 10.1093/europace/euw384 -
The Cochrane Database of Systematic... Jun 2015Seasonal/perennial allergic conjunctivitis is the most common allergic conjunctivitis, usually with acute manifestations when a person is exposed to allergens and with... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Seasonal/perennial allergic conjunctivitis is the most common allergic conjunctivitis, usually with acute manifestations when a person is exposed to allergens and with typical signs and symptoms including itching, redness, and tearing. The clinical signs and symptoms of allergic conjunctivitis are mediated by the release of histamine by mast cells. Histamine antagonists (also called antihistamines) inhibit the action of histamine by blocking histamine H1 receptors, antagonising the vasoconstrictor, and to a lesser extent, the vasodilator effects of histamine. Mast cell stabilisers inhibit degranulation and consequently the release of histamine by interrupting the normal chain of intracellular signals. Topical treatments include eye drops with antihistamines, mast cell stabilisers, non-steroidal anti-inflammatory drugs, combinations of the previous treatments, and corticosteroids. Standard treatment is based on topical antihistamines alone or topical mast cell stabilisers alone or a combination of treatments. There is clinical uncertainty about the relative efficacy and safety of topical treatment.
OBJECTIVES
The objective of this review was to assess the effects of topical antihistamines and mast cell stabilisers, alone or in combination, for use in treating seasonal and perennial allergic conjunctivitis.
SEARCH METHODS
We searched CENTRAL (which contains the Cochrane Eyes and Vision Trials Register) (2014, Issue 7), Ovid MEDLINE, Ovid MEDLINE In-Process and Other Non-Indexed Citations, Ovid MEDLINE Daily, Ovid OLDMEDLINE (January 1946 to July 2014), EMBASE (January 1980 to July 2014), the metaRegister of Controlled Trials (mRCT) (www.controlled-trials.com), ClinicalTrials.gov (www.clinicaltrials.gov) and the World Health Organization (WHO) International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en). We did not use any date or language restrictions in the electronic searches for trials. We last searched the electronic databases on 17 July 2014. We also searched the reference lists of review articles and relevant trial reports for details of further relevant publications.
SELECTION CRITERIA
We included randomised controlled trials (RCTs) comparing topical antihistamine and mast cell stabilisers, alone or in combination, with placebo, no treatment or to any other antihistamine or mast cell stabiliser, or both, that examined people with seasonal or perennial allergic conjunctivitis, or both. The primary outcome was any participant-reported evaluation (by questionnaire) of severity of four main ocular symptoms: itching, irritation, watering eye (tearing), and photophobia (dislike of light), both separately and, if possible, by an overall symptom score. We considered any follow-up time between one week and one year.
DATA COLLECTION AND ANALYSIS
Two review authors independently extracted data and assessed risk of bias. Disagreements were resolved by discussion among review authors and the involvement of a third review author. We followed standard methodological approaches used by Cochrane.
MAIN RESULTS
We identified 30 trials with a total of 4344 participants randomised, with 17 different drugs or treatment comparisons. The following antihistamines and mast cell stabilisers were evaluated in at least one RCT: nedocromil sodium or sodium cromoglycate, olopatadine, ketotifen, azelastine, emedastine, levocabastine (or levocabastine), mequitazine, bepotastine besilate, combination of antazoline and tetryzoline, combination of levocabastine and pemirolast potassium. The most common comparison was azelastine versus placebo (nine studies).We observed a large variability in reporting outcomes. The quality of the studies and reporting was variable, but overall the risk of bias was low. Trials evaluated only short-term effects, with a range of treatment of one to eight weeks. Meta-analysis was only possible in one comparison (olopatadine versus ketotifen). There was some evidence to support that topical antihistamines and mast cell stabilisers reduce symptoms and signs of seasonal allergic conjunctivitis when compared with placebo. There were no reported serious adverse events related to the use of topical antihistamine and mast cell stabilisers treatment.
AUTHORS' CONCLUSIONS
It seems that all reported topical antihistamines and mast cell stabilisers reduce symptoms and signs of seasonal allergic conjunctivitis when compared with placebo in the short term. However, there is no long-term data on their efficacy. Direct comparisons of different antihistamines and mast cell stabilisers need to be interpreted with caution. Overall, topical antihistamines and mast cell stabilisers appear to be safe and well tolerated. We observed a large variability in outcomes reported. Poor quality of reporting challenged the synthesis of evidence.
Topics: Anti-Allergic Agents; Conjunctivitis, Allergic; Histamine; Histamine Antagonists; Humans; Mast Cells; Randomized Controlled Trials as Topic; Seasons
PubMed: 26028608
DOI: 10.1002/14651858.CD009566.pub2 -
Antazoline for termination of atrial fibrillation during the procedure of pulmonary veins isolation.Advances in Medical Sciences Sep 2015Pulmonary vein isolation is a well established method of definite treatment of atrial fibrillation (AF). Periprocedural onset of AF usually terminates spontaneously...
PURPOSE
Pulmonary vein isolation is a well established method of definite treatment of atrial fibrillation (AF). Periprocedural onset of AF usually terminates spontaneously within minutes, but not in all cases. Antazoline is an antihistaminic agent with antiarrhythmic properties. The aim of our retrospective study was to evaluate the efficacy of antazoline in termination of AF in patients undergoing pulmonary vein isolation.
MATERIALS AND METHODS
Consecutive 141 patients who received antazoline to terminate AF during pulmonary vein isolation were analyzed. The antazoline was administered at the rate of 30-50mg/min (max. 500mg) after the circumferential ablation in the ostia of pulmonary veins and before confirmation of isolation. Success was defined as restoration of sinus rhythm within 20min after antazoline infusion.
RESULTS
The efficacy of antazoline was 83.6% in paroxysmal and 31.1% in persistent AF patients. Clinical variables that were independently predictive of antazoline ineffectiveness were female (odds ratio [OR]: 4.35; 95% confidence interval [CI]: 1.26-14.3; p=0.018) and AF at the beginning of procedure (OR 28.4; 95% CI 3.89-208.0; p=0.001). Due to antazoline related side effects infusion was discontinued in 7 patients (5%).
CONCLUSIONS
Antazoline seems to be safe agent in termination of AF in patients undergoing pulmonary vein isolation. We also observed satisfying efficacy, which needs to be proved in a randomized clinical trial.
Topics: Aged; Antazoline; Atrial Fibrillation; Catheter Ablation; Female; Humans; Male; Middle Aged; Pulmonary Veins; Retrospective Studies; Treatment Outcome
PubMed: 25919055
DOI: 10.1016/j.advms.2015.03.002