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[PMID]:28039911
[Au] Autor:Frommeyer G; Sterneberg M; Dechering DG; Kaese S; Bögeholz N; Pott C; Fehr M; Bogossian H; Milberg P; Eckardt L
[Ad] Endereço:Division of Clinical and Experimental Electrophysiology, Department of Cardiology and Angiology, University Hospital of Münster, Münster, Germany.
[Ti] Título:Effective suppression of atrial fibrillation by the antihistaminic agent antazoline: First experimental insights into a novel antiarrhythmic agent.
[So] Source:Cardiovasc Ther;35(2), 2017 Apr.
[Is] ISSN:1755-5922
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: The antihistaminic antazoline (ANT) was reported to be highly effective and safe for rapid conversion of atrial fibrillation (AF). We therefore analyzed underlying mechanisms in an experimental whole-heart model. METHODS AND RESULTS: Isolated and retrogradely perfused rabbit hearts underwent a standardized protocol employing atrial burst pacing-induced AF in five of 20 hearts under baseline conditions (seven episodes). Thereafter, a combination of acetylcholine and isoproterenol was employed to enhance AF occurrence. Two monophasic action potential recordings on the left- and two on the right atrial epicardium showed a decrease in atrial action potential duration (aAPD, -25 msec, P<.05) and atrial effective refractory period (aERP; -52 msec, P<.01) after infusion of acetylcholine (1 µmol/L) and isoproterenol (1 µmol/L). This led to induction of AF in 14 of 20 hearts (145 episodes). Simultaneous infusion of ANT (20 µmol/L) led to a complete suppression of AF in all inducible hearts. Treatment with ANT also led to a significant increase in aAPD (+41 msec, P<.01) and aERP (+74 msec, P<.05), leading to a marked increase in atrial postrepolarization refractoriness (aPRR, +33 msec, P<.01). Results were compared to 13 rabbits treated with flecainide. Flecainide induced a significant increase in aPRR and resulted in induction of AF in seven of 13 hearts (51 episodes) while 11 of 13 hearts were inducible with acetylcholine and isoproterenol (93 episodes). CONCLUSION: 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.
[Mh] Termos MeSH primário: Antazolina/farmacologia
Antiarrítmicos/farmacologia
Fibrilação Atrial/prevenção & controle
Frequência Cardíaca/efeitos dos fármacos
Antagonistas dos Receptores Histamínicos H1/farmacologia
[Mh] Termos MeSH secundário: Acetilcolina
Potenciais de Ação
Animais
Fibrilação Atrial/induzido quimicamente
Fibrilação Atrial/fisiopatologia
Estimulação Cardíaca Artificial
Relação Dose-Resposta a Droga
Descoberta de Drogas
Eletrocardiografia
Técnicas Eletrofisiológicas Cardíacas
Flecainida/farmacologia
Preparação de Coração Isolado
Isoproterenol
Coelhos
Período Refratário Eletrofisiológico
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 0 (Histamine H1 Antagonists); DHA8014SS1 (Antazoline); K94FTS1806 (Flecainide); L628TT009W (Isoproterenol); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170327
[Lr] Data última revisão:
170327
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170101
[St] Status:MEDLINE
[do] DOI:10.1111/1755-5922.12244


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[PMID]:27362390
[Au] Autor:Farkowski MM; Maciag A; Zurawska M; Pytkowski M; Kowalik I; Wozniak J; Sterlinski M; Szwed H
[Ti] Título:Comparative effectiveness and safety of antazoline­based and propafenone­based strategies for pharmacological cardioversion of short­duration atrial fibrillation in the emergency department.
[So] Source:Pol Arch Med Wewn;126(6):381-7, 2016 Jun 24.
[Is] ISSN:1897-9483
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION    Numerous studies described the effectiveness and safety of antazoline in pharmacological cardioversion of short­duration 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 antazoline­based and propafenone­based strategies in pharmacological cardioversion of short­duration AF performed in our emergency department. PATIENTS AND METHODS    We conducted a retrospective case­control study based on the analysis of medical records of patients undergoing pharmacological cardioversion of short­duration 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 antazoline­based strategy was more effective and safer in comparison with propafenone­based strategy in the pharmacological cardioversion of short­duration AF in our emergency department.
[Mh] Termos MeSH primário: Antazolina/uso terapêutico
Antiarrítmicos/uso terapêutico
Fibrilação Atrial/tratamento farmacológico
Propafenona/uso terapêutico
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Antazolina/efeitos adversos
Antiarrítmicos/efeitos adversos
Serviço Hospitalar de Emergência
Feminino
Seres Humanos
Masculino
Meia-Idade
Segurança do Paciente
Propafenona/efeitos adversos
Estudos Retrospectivos
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 68IQX3T69U (Propafenone); DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160701
[St] Status:MEDLINE
[do] DOI:10.20452/pamw.3452


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[PMID]:27289300
[Au] Autor:Giebultowicz J; Kojro G; Piotrowski R; Kulakowski P; Wroczynski P
[Ad] Endereço:Department of Bioanalysis and Drugs Analysis, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097 Warsaw, Poland. Electronic address: joanna.giebultowicz@wum.edu.pl.
[Ti] Título:Cloud-point extraction is compatible with liquid chromatography coupled to electrospray ionization mass spectrometry for the determination of antazoline in human plasma.
[So] Source:J Pharm Biomed Anal;128:294-301, 2016 Sep 05.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo: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.
[Mh] Termos MeSH primário: Antazolina/sangue
Antagonistas dos Receptores Histamínicos H1/sangue
[Mh] Termos MeSH secundário: Antazolina/farmacocinética
Calibragem
Cromatografia Líquida de Alta Pressão
Antagonistas dos Receptores Histamínicos H1/farmacocinética
Seres Humanos
Extração Líquido-Líquido
Polietilenoglicóis
Controle de Qualidade
Padrões de Referência
Reprodutibilidade dos Testes
Espectrometria de Massas por Ionização por Electrospray
Tensoativos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Surface-Active Agents); 30IQX730WE (Polyethylene Glycols); 9036-19-5 (Nonidet P-40); DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170812
[Lr] Data última revisão:
170812
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160613
[St] Status:MEDLINE


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[PMID]:26952922
[Au] Autor:Gumustas M; Alshana U; Ertas N; Goger NG; Ozkan SA; Uslu B
[Ad] Endereço:Department of Analytical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Ankara, Turkey.
[Ti] Título:Determination of antazoline and tetrahydrozoline in ophthalmic solutions by capillary electrophoresis and stability-indicating HPLC methods.
[So] Source:J Pharm Biomed Anal;124:390-8, 2016 May 30.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo: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.
[Mh] Termos MeSH primário: Antazolina/análise
Cromatografia Líquida de Alta Pressão/métodos
Eletroforese Capilar/métodos
Imidazóis/análise
Soluções Oftálmicas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Imidazoles); 0 (Ophthalmic Solutions); DHA8014SS1 (Antazoline); S9U025Y077 (tetrahydrozoline)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170112
[Lr] Data última revisão:
170112
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160309
[St] Status:MEDLINE


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[PMID]:26895496
[Au] Autor:Giebultowicz J; Piotrowski R; Baran J; Kulakowski P; Wroczynski P
[Ad] Endereço:Bioanalysis and Drugs Analysis Department, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha Street, 02-097 Warsaw, Poland. Electronic address: joanna.giebultowicz@wum.edu.pl.
[Ti] Título: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.
[So] Source:J Pharm Biomed Anal;123:113-9, 2016 May 10.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo: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.
[Mh] Termos MeSH primário: Antazolina/sangue
Antazolina/farmacocinética
Cromatografia Líquida/métodos
Mesilatos/sangue
Mesilatos/farmacocinética
Plasma/química
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Adulto
Antazolina/química
Estabilidade de Medicamentos
Feminino
Meia-Vida
Hemodinâmica/fisiologia
Seres Humanos
Extração Líquido-Líquido/métodos
Masculino
Mesilatos/química
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Mesylates); DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160220
[St] Status:MEDLINE


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[PMID]:26836449
[Au] Autor:Abdel-Halim LM; Abd-El Rahman MK; Ramadan NK; El Sanabary HF; Salem MY
[Ad] Endereço:National Organization for drug control and research (NODCAR), 6 Abu HazemStreet, Pyramids Ave, P.O. Box 29, Giza, Egypt. Electronic address: lamiasalam22@yahoo.com.
[Ti] Título: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.
[So] Source:Spectrochim Acta A Mol Biomol Spectrosc;159:98-105, 2016 Apr 15.
[Is] ISSN:1873-3557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo: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.
[Mh] Termos MeSH primário: Antazolina/análise
Antialérgicos/análise
Imidazóis/análise
Descongestionantes Nasais/análise
Espectrofotometria/métodos
[Mh] Termos MeSH secundário: Combinação de Medicamentos
Controle de Qualidade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Allergic Agents); 0 (Drug Combinations); 0 (Imidazoles); 0 (Nasal Decongestants); DHA8014SS1 (Antazoline); S9U025Y077 (tetrahydrozoline)
[Em] Mês de entrada:1611
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160203
[St] Status:MEDLINE


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[PMID]:25919055
[Au] Autor:Balsam P; Kozluk E; Peller M; Piatkowska A; Lodzinski P; Kiliszek M; Koltowski L; Grabowski M; Opolski G
[Ad] Endereço:1st Department of Cardiology, Medical University of Warsaw, Warsaw, Poland.
[Ti] Título:Antazoline for termination of atrial fibrillation during the procedure of pulmonary veins isolation.
[So] Source:Adv Med Sci;60(2):231-5, 2015 Sep.
[Is] ISSN:1898-4002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo: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.
[Mh] Termos MeSH primário: Antazolina/uso terapêutico
Fibrilação Atrial/tratamento farmacológico
Fibrilação Atrial/cirurgia
Ablação por Cateter/métodos
Veias Pulmonares/cirurgia
[Mh] Termos MeSH secundário: Idoso
Feminino
Seres Humanos
Masculino
Meia-Idade
Veias Pulmonares/patologia
Estudos Retrospectivos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:150928
[Lr] Data última revisão:
150928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150429
[St] Status:MEDLINE


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[PMID]:23990192
[Au] Autor:Piotrowski R; Krynski T; Baran J; Futyma P; Stec S; Kulakowski P
[Ad] Endereço:Department of Cardiology, Grochowski Hospital, Postgraduate Medical School, Warsaw, Poland. rpiotrow@op.pl.
[Ti] Título:Antazoline for rapid termination of atrial fibrillation during ablation of accessory pathways.
[So] Source:Cardiol J;21(3):299-303, 2014.
[Is] ISSN:1897-5593
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND AIM: To assess safety and efficacy of antazoline for termination of atrial fibrillation (AF) occurring during ablation of accessory pathways (AP). METHODS: We analyzed electrophysiological mechanism of antazoline (changes in A-A interval) and the percentage of pre-excited QRS complexes before and after antazoline administration. The total dose administered and the time from the start of injection to sinus rhythm restoration were also measured. RESULTS: Out of consecutive 290 patients with Wolff-Parkinson-White syndrome undergoing radiofrequency (RF) ablation, 12 (4.1%) (4 females, mean age 36 ± 20 years) developed sustained AF which did not stop spontaneously within 10 min, and antazoline in 100 mg repeated boluses was administered. In all 12 patients the drug restored sinus rhythm after a mean of 425 ± 365 s (range 43-1245 s) using a mean cumulative dose of 176 ± 114 mg (range 25-400 mg). The drug slightly prolonged R-R intervals during AF (from 383 ± 106 to 410 ± 70 ms) and reduced the percentage of fully pre-excited QRS complexes (from 35% to 26%). Intracardiac recordings showed gradual increase in A-A intervals, as well as regularization and decreasing fractionation of atrial activity following drug injection (mean A-A interval of 162 ± 30 ms at baseline vs. 226 ± 26 ms shortly before sinus rhythm restoration, p < 0.001). AP was not completely blocked in any patient which enabled continuation of ablation. CONCLUSIONS: Antazoline safely and rapidly converts AF into sinus rhythm during ablation of AP. The drug does not block AP completely, enabling continuation of ablation. The drug converting AF into more organized atrial activity (atrial flutter/tachycardia) before sinus rhythm resumption.
[Mh] Termos MeSH primário: Feixe Acessório Atrioventricular/cirurgia
Antazolina/administração & dosagem
Fibrilação Atrial/tratamento farmacológico
Ablação por Cateter
Átrios do Coração/fisiopatologia
Complicações Intraoperatórias/tratamento farmacológico
Síndrome de Wolff-Parkinson-White/cirurgia
[Mh] Termos MeSH secundário: Adulto
Fibrilação Atrial/etiologia
Fibrilação Atrial/fisiopatologia
Relação Dose-Resposta a Droga
Eletrocardiografia
Feminino
Seguimentos
Frequência Cardíaca/efeitos dos fármacos
Antagonistas dos Receptores Histamínicos H1/administração & dosagem
Seres Humanos
Injeções Intravenosas
Complicações Intraoperatórias/etiologia
Complicações Intraoperatórias/fisiopatologia
Masculino
Síndrome de Wolff-Parkinson-White/fisiopatologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:140625
[Lr] Data última revisão:
140625
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130831
[St] Status:MEDLINE
[do] DOI:10.5603/CJ.a2013.0121


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[PMID]:23847054
[Au] Autor:Wang R; Chu Y; Li X; Wan B; Yu T; Wang L; Hao L; Guo M
[Ad] Endereço:Department of Pharmacy, Zhengzhou University, Zhengzhou, 450001, China; Luohe Central Hospital Affiliated to Luohe Medical College, Luohe, 462000, China.
[Ti] Título:Determination of antazoline hydrochloride in rat plasma and excreta by reversed-phase ion-pair chromatography and its application to pharmacokinetics.
[So] Source:Biomed Chromatogr;27(12):1595-602, 2013 Dec.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A reversed-phase ion pair chromatography method with liquid-liquid extraction analytical method was developed and validated for the determination of antazoline hydrochloride in plasma and excreta of rat. The aim of our study was to characterize the preclinical pharmacokinetics and excretion profiles of antazoline hydrochloride in rats after intravenous injection at the dose of 10 mg/kg. Plasma and excreta samples were extracted with ethyl acetate, and phenacetin was used as the internal standard. The result showed that the method is suitable for the quantification of antazoline hydrochloride in plasma and excreta samples. Analysis of accuracy (90.89-112.33%), imprecision (<7.1%) and recovery (>82.5%) showed adequate values. After a single intravenous administration at 10 mg/kg to rats, plasma concentration profile showed a relative fast elimination proceeding with a terminal elimination half-life of 3.53 h. Approximately 61.8 and 14.2% of the administered dose were recovered in urine and bile after 72 and 24 h post-dosing respectively; 5.9% of the administered dose was recovered in feces after 72 h post-dosing. The above results show that the major elimination route is urinary excretion.
[Mh] Termos MeSH primário: Antazolina/análise
Cromatografia de Fase Reversa/métodos
[Mh] Termos MeSH secundário: Animais
Antazolina/química
Antazolina/farmacocinética
Bile/química
Fezes/química
Feminino
Modelos Lineares
Masculino
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1410
[Cu] Atualização por classe:140304
[Lr] Data última revisão:
140304
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130713
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.2965


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[PMID]:23669609
[Au] Autor:Li X; Chu Y; Ke Y; Wang L; Yu T; Hao L
[Ad] Endereço:Department of Pharmacy, Zhengzhou University, Zhengzhou 450001, China. lixt@zzu.edu.cn
[Ti] Título:Determination of antazoline hydrochloride in Beagle dog plasma by HPLC-UV and its application to pharmacokinetics.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;929:97-101, 2013 Jun 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In order to evaluate the pharmacokinetics characteristic of antazoline hydrochloride in Beagle dogs, a sensitive and specific HPLC method was developed and validated using phenacetin as the internal standard (IS). The analyte and the IS were extracted from dog plasma by ethyl acetate under the basic condition. The analyte was separated by a C18 column and detected with a variable wavelength UV-detector. The mobile phase consisted of methanol-5mmolL(-1) tetrabutyl ammonium bromide (45:55, v/v) containing 0.5% glacial acetic acid in a flow rate of 1.0mLmin(-1). Standard calibration graph for antazoline was linear over a curve range of 20-1600ngmL(-1) (R>0.99) and the lower limit of quantification was 20ngmL(-1) using a plasma sample of 500µL. The intra- and inter-day precision values were less than 14.3% relative standard deviation (RSD). The intra-day assay accuracy was in the range of 98.1-100.6% and the inter-day assay accuracy in the range of 99.2-101.1%. The extraction recoveries were on the average of 88.4% for antazoline and 76.8% for IS. Plasma samples were stable at least for 1 month at -20°C. This method was successfully applied to pharmacokinetics study of antazoline after intravenous administration to Beagle dogs.
[Mh] Termos MeSH primário: Antazolina/sangue
Cromatografia Líquida de Alta Pressão/métodos
Cromatografia de Fase Reversa/métodos
[Mh] Termos MeSH secundário: Animais
Antazolina/farmacocinética
Cães
Feminino
Masculino
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
DHA8014SS1 (Antazoline)
[Em] Mês de entrada:1310
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130515
[St] Status:MEDLINE



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