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Munchener Medizinische Wochenschrift... Oct 1970
Topics: Adolescent; Electrocardiography; Epinephrine; Female; Heart Arrest; Heart Block; Heart Diseases; Heart Massage; Humans; Hypokalemia; Imidazoles; Infusions, Parenteral; Potassium; Quinolizines; Respiration, Artificial; Sparteine; Suicide
PubMed: 5536215
DOI: No ID Found -
Talanta Feb 2004The mixed dissociation constants of five drug acids-ambroxol, antazoline, naphazoline, oxymetazoline and ranitidine-at various ionic strengths I of range 0.01 and 1.0...
The mixed dissociation constants of five drug acids-ambroxol, antazoline, naphazoline, oxymetazoline and ranitidine-at various ionic strengths I of range 0.01 and 1.0 and at temperatures of 25 and 37 degrees C were determined using SQUAD(84) regression analysis of the pH-spectrophotometric titration data. A proposed strategy of efficient experimentation in a protonation constants determination, followed by a computational strategy for the chemical model with a protonation constants determination, is presented on the protonation equilibria of ambroxol. The thermodynamic dissociation constant pK(a)(T) was estimated by non-linear regression of {pK(a), I} data at 25 and 37 degrees C: for ambroxol p K (a ,1)(T )=8.05 (6) and 8.25 (4), logbeta (21)(T )=11.67 (6) and 11.83 (8), for antazoline p K (a ,1)(T )=7.79 (2) and 7.83 (6), p K (a ,2)(T )=9.74 (3) and 9.55 (2), for naphazoline pK (a ,1)(T )=10.81 (1) and 10.63 (1), for oxymethazoline pK (a ,1)(T )=10.62 (2) and 10.77 (7), pK(a,2)(T)=12.03(3) and 11.82 (4) and for ranitidine p K (a ,1)(T )=1.89 (1) and 1.77 (1). Goodness-of-fit tests for various regression diagnostics enabled the reliability of the parameter estimates to be found.
PubMed: 18969326
DOI: 10.1016/j.talanta.2003.08.027 -
Journal of Pharmaceutical Sciences Apr 1995HPLC analysis of an anti-infective ophthalmic solution (Albalon-A), containing the active drugs naphazoline and antazoline, revealed a degradation peak of unknown...
Synthesis and identification of the primary degradation product in a commercial ophthalmic formulation using NMR, MS, and a stability-indicating HPLC method for antazoline and naphazoline.
HPLC analysis of an anti-infective ophthalmic solution (Albalon-A), containing the active drugs naphazoline and antazoline, revealed a degradation peak of unknown identity. To elucidate the identity of the degradant, the active drugs were each hydrolyzed by refluxing at high pH, and their respective hydrolysis products were isolated and spectrally characterized by NMR, FT-IR, and MS for conclusive structure elucidation. The degradant's identity was confirmed by HPLC-MS analysis of Albalon-A ophthalmic solution to be the antazoline hydrolysis product N-[(N-benzylanilino)acetyl]ethylenediamine (IV). A stability-indicating HPLC method was then developed which was able to resolve IV from the active drugs. This HPLC method was then validated for quantitating the active drugs and IV. Validation studies demonstrated linear UV response at 280 nm, recovery > 98%, good reproducibility, and a detection limit of 2 micrograms/mL IV. Overall, the data demonstrated that the HPLC method was quantitative and specific for antazoline, naphazoline, and IV. Analysis of an expired stabilitry lot of the ophthalmic solution indicated the concentration of IV was 0.002% (w/v).
Topics: Antazoline; Chromatography, High Pressure Liquid; Drug Stability; Hydrolysis; Magnetic Resonance Spectroscopy; Mass Spectrometry; Naphazoline; Ophthalmic Solutions; Spectroscopy, Fourier Transform Infrared
PubMed: 7629745
DOI: 10.1002/jps.2600840422 -
Journal of the South Carolina Medical... Feb 1964
Topics: Antazoline; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Atrial Fibrillation; Atrial Flutter; Cardiac Complexes, Premature; Electrocardiography; Geriatrics; Heart Block; Histamine H1 Antagonists; Humans; Injections, Intravenous; Tachycardia; Toxicology
PubMed: 14125202
DOI: No ID Found -
Journal of the American Medical... Nov 1952
Topics: Antazoline; Anti-Allergic Agents; Histamine H1 Antagonists
PubMed: 12990396
DOI: No ID Found -
Revista Espanola de Cardiologia 1976
Topics: Adult; Antazoline; Drug Evaluation; Electrocardiography; False Negative Reactions; False Positive Reactions; Female; Heart Conduction System; Humans; Imidazoles; Injections, Intravenous; Male; Middle Aged; Wolff-Parkinson-White Syndrome
PubMed: 1257543
DOI: No ID Found -
Zeitschrift Fur Rechtsmedizin. Journal... 1974
Topics: Autopsy; Chromatography, Thin Layer; Histamine H1 Antagonists; Humans; Imidazoles; Kidney; Lethal Dose 50; Liver; Male; Mass Spectrometry; Middle Aged; Poisoning; Spectrophotometry, Ultraviolet
PubMed: 4155194
DOI: 10.1007/BF02114845 -
Acta Anaesthesiologica 1968
Topics: Adult; Aged; Anesthesia; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Electrocardiography; Female; Humans; Imidazoles; Male; Middle Aged
PubMed: 5757184
DOI: No ID Found -
Acta Ophthalmologica Scandinavica.... 1999Two important realizations about pathophysiological mechanisms involved in allergic conjunctivitis have led to novel drug discovery efforts and new topical ocular... (Review)
Review
Two important realizations about pathophysiological mechanisms involved in allergic conjunctivitis have led to novel drug discovery efforts and new topical ocular medications for prevention and treatment of this prevent allergic disease. The first of these, interspecies and intraspecies mast cell heterogeneity, was established in the mid-1980's by investigators working in the field of asthma. It is now appreciated that secretory responses as well as effects of pharmacological agents differ depending upon the mast cell population studied. Two types of human mast cells, the tryptase containing (T) and the tryptase/chymase containing (TC) mast cells, have been characterized in a variety of tissues. Significantly, Irani et al. (1) demonstrated by immunohistochemical staining that the mast cells present in conjunctival tissues from patients with allergic conjunctivitis were 100% TC. Functional responses of human conjunctival mast cells to a variety of secretagogues (2) were consistent with their classification as TC or connective tissue type mast cells. Importantly, the studies by Miller et al. mentioned above allowed the harvesting and preparation of human conjunctival mast cells for use in drug screening studies. Utilization of these cells has led to the identification of Patanol, the most effective human conjunctival mast cell stabilizer available for topical use in allergic conjunctivitis (3). These same studies demonstrated the lack of mast cell stabilizing activity for cromolyn and nedocromil in these connective tissue type, TC containing, human conjunctival mast cells. Similar lack of effect was noted with these drugs on human skin mast cell degranulation (4). The second important discovery in the area of allergic conjunctivitis has been the demonstration that conjunctival epithelial cells may contribute to the perpetuation of the allergic response. A report from Gamache et al. (5) identified cytokines produced by human conjunctival epithelial cells following treatment with a number of stimuli. Significantly, Sharif et al. (6) subsequently identified functional histamine H1 receptors on these same cell types. Recently, Weimer et al. (7) have shown that exposure of human conjunctival epithelial cells to histamine leads to the production of pro-inflammatory cytokines IL-6 and IL-8. Importantly, treatment of the epithelial cells with drugs that possess histamine H1 antagonist properties prevents cytokine production. It is noteworthy that first generation anti-histamines antazoline and pheniramine are not potent inhibitors of histamine-stimulated cytokine synthesis in intact epithelial cells, while newer anti-histamines Emadine and levocabastine are more potent. Surprisingly, Patanol was more potent as an inhibitor of histamine-stimulated cytokine production by the epithelial cells than would be predicted from its histamine H1 antagonist affinity. These inhibitory effects on conjunctival epithelial cell production of pro-inflammatory cytokines may contribute to enhanced clinical activity noted with these recently approved drugs.
Topics: Anti-Allergic Agents; Conjunctivitis, Allergic; Cytokines; Drug Therapy, Combination; Epithelial Cells; Histamine H1 Antagonists; Histamine Release; Humans; Mast Cells; Ophthalmic Solutions; Vasoconstrictor Agents
PubMed: 10337430
DOI: 10.1111/j.1600-0420.1999.tb01171.x -
International Journal of Environmental... Apr 2022Pharmacological cardioversion (PCV) is commonly a primary option for termination of recent-onset atrial fibrillation (AF) in emergency departments (ED). This is a...
Pharmacological cardioversion (PCV) is commonly a primary option for termination of recent-onset atrial fibrillation (AF) in emergency departments (ED). This is a subanalysis of the CANT II study, evaluating the effectiveness and safety of antazoline in patients (n = 777) at three stages of chronic kidney disease (CKD): Group I > 60 mL/min (n = 531), Group II 45−59 mL/min (n = 149), and Group III < 45 mL/min (n = 97). Patients in Group III were older and with a higher prevalence of co-morbidities; however, we did not find statistically significant differences in the overall effectiveness of PCV in comparison with the other groups. In patients receiving amiodarone, the PCV success rate was similar in all the studied groups, but along with a renal function decline, it decreased in patients receiving antazoline (79.1 vs. 35%; p < 0.001), and it increased almost significantly in patients receiving propafenone (69.9 vs. 100%; p = 0.067). In patients in Group I, antazoline restored a sinus rhythm as effectively as propafenone and amiodarone; however, in patients in Group III, both antazoline and amiodarone became less effective in restoring a sinus rhythm than propafenone (p = 0.002 and p = 0.034, respectively). The rate of safety endpoint was the highest in patients in Group III (eGFR < 45 mL/min), and it was significantly higher than in patients in Groups I and II (p = 0.008 and p = 0.036, respectively). We did not observe antazoline-related adverse events in any of the studied groups of patients. This real-world registry analysis revealed a different influence of CKD on the effectiveness of individual drugs, and while propafenone and amiodarone maintained their AF termination efficacy, antazoline became significantly less effective in restoring sinus rhythm.
Topics: Amiodarone; Antazoline; Anti-Arrhythmia Agents; Atrial Fibrillation; Electric Countershock; Female; Humans; Male; Propafenone; Renal Insufficiency, Chronic; Treatment Outcome
PubMed: 35457747
DOI: 10.3390/ijerph19084880