Antihistaminic Agent

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Piotr Wroczynski - One of the best experts on this subject based on the ideXlab platform.

  • 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 hum
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebultowicz, Roman Piotrowski, Jakub Baran, Piotr Kulakowski, Piotr Wroczynski
    Abstract:

    Abstract 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 ( V ss  = 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.

Joanna Giebultowicz - One of the best experts on this subject based on the ideXlab platform.

  • 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 hum
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebultowicz, Roman Piotrowski, Jakub Baran, Piotr Kulakowski, Piotr Wroczynski
    Abstract:

    Abstract 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 ( V ss  = 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.

Roman Piotrowski - One of the best experts on this subject based on the ideXlab platform.

  • 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 hum
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebultowicz, Roman Piotrowski, Jakub Baran, Piotr Kulakowski, Piotr Wroczynski
    Abstract:

    Abstract 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 ( V ss  = 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.

  • 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
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebułtowicz, Roman Piotrowski, Piotr Kułakowski, Jakub Baran, Piotr Wroczyński
    Abstract:

    Abstract 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 ( V ss  = 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.

Jakub Baran - One of the best experts on this subject based on the ideXlab platform.

  • 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 hum
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebultowicz, Roman Piotrowski, Jakub Baran, Piotr Kulakowski, Piotr Wroczynski
    Abstract:

    Abstract 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 ( V ss  = 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.

  • 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
    Journal of Pharmaceutical and Biomedical Analysis, 2016
    Co-Authors: Joanna Giebułtowicz, Roman Piotrowski, Piotr Kułakowski, Jakub Baran, Piotr Wroczyński
    Abstract:

    Abstract 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 ( V ss  = 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.

Hanna Szwed - One of the best experts on this subject based on the ideXlab platform.

  • clinical efficacy of antazoline in rapid cardioversion of paroxysmal atrial fibrillation a protocol of a single center randomized double blind placebo controlled study the anpaf study
    Trials, 2012
    Co-Authors: Michal M Farkowski, Aleksander Maciag, Ilona Kowalik, Mariusz Pytkowski, Rafal Dabrowski, Hanna Szwed
    Abstract:

    Background Rapid conversion of atrial fibrillation (AF) to sinus rhythm may be achieved by the administration of class IA, IC and III antiarrhythmic drugs or vernakalant hydrochloride. However, that treatment may be related to potential pro-arrhythmia, lack of efficacy or the exceptionally high cost of a compound used. Antazoline is a first generation Antihistaminic Agent with chinidin-like properties. When administered intravenously, antazoline exerts a strong antiarrhythmic effect on supraventricular arrhythmia, especially on AF, facilitating rapid conversion to sinus rhythm. Despite a relative lack of published data antazoline has been marketed in Poland and widely used in cardiology wards and emergency rooms for many years due to its efficacy, safety and rapid onset of action within minutes of administration.

  • Clinical efficacy of antazoline in rapid cardioversion of paroxysmal atrial fibrillation -- a protocol of a single center, randomized, double-blind, placebo-controlled study (the AnPAF Study)
    Trials, 2012
    Co-Authors: Michal M Farkowski, Aleksander Maciag, Ilona Kowalik, Mariusz Pytkowski, Rafal Dabrowski, Hanna Szwed
    Abstract:

    Background Rapid conversion of atrial fibrillation (AF) to sinus rhythm may be achieved by the administration of class IA, IC and III antiarrhythmic drugs or vernakalant hydrochloride. However, that treatment may be related to potential pro-arrhythmia, lack of efficacy or the exceptionally high cost of a compound used. Antazoline is a first generation Antihistaminic Agent with chinidin-like properties. When administered intravenously, antazoline exerts a strong antiarrhythmic effect on supraventricular arrhythmia, especially on AF, facilitating rapid conversion to sinus rhythm. Despite a relative lack of published data antazoline has been marketed in Poland and widely used in cardiology wards and emergency rooms for many years due to its efficacy, safety and rapid onset of action within minutes of administration. Methods/design A randomized, double blind, placebo-controlled, superiority clinical trial was designed to assess clinical efficacy of antazoline in rapid conversion of AF to sinus rhythm. Eligible patients will present AF lasting less than 43 hours, will be in stable cardio-pulmonary condition and will have no prior history of advanced heart failure or significant valvular disease. Long-term antiarrhythmic therapy is not considered an exclusion criterion. Subjects who fulfill selection criteria will be randomly assigned to receive intravenously either antazoline or placebo in divided doses and observed for 1.5 hours after conversion to sinus rhythm or after the last i.v. bolus. Primary end point will be the conversion of AF to sinus rhythm confirmed in an electrocardiogram (ECG) during the observation period. Secondary end points will be comprised of time to conversion and return of AF during the observation period. Special consideration will be given to the observation of any adverse events. A sample size of 80 patients was calculated based on the following assumptions: two-tailed test, a type I error of 0.01, a power of 90%, efficacy of placebo 5%, efficacy of antazoline 50% and 20% drop-out rate to fulfill the criteria of intention-to-treat analysis. Due to the presumed lack of statistical power, the secondary end points and safety endpoints will be considered exploratory. Clinical trials registry ClinicalTrials.gov, NCT01527279