• Parasites, Hosts and Diseases
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• v.61 no.2
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• pp.172-182
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• 2023

At the time of host attachment, ticks are very sensitive to histamine, but during rapid blood sucking they paradoxically require histamine. Using a rabbit model, we studied the effects of histamine and antihistamine during attachment and fast-feeding in different life stages of Haemaphysalis longicorns. We examined how they responded to histamine and antihistamine by analyzing the detachment rate, histology of feeding lesions, and post-feeding behavior. A significant difference (P<0.01) was found in the detachment rate between experimental and control treatments throughout the observation period. Ticks exhibited a higher detachment rate (30.1%) at 12 h after histamine application during attachment time and on antihistamine-treated skin (25.4%) at 96 h during fast-feeding. After feeding on histamine-treated rabbits, the fully engorged body weights of larvae and nymphs were 0.7±0.36 mg and 3.5±0.65 mg, respectively. An average increase in body weight of 0.6±0.05 mg and 3.2±0.30 mg was observed for larvae and nymphs compared to the respective control weights. Nymphs and adults engorged after antihistamine treatment had an average body weight of 1.3±0.54 mg and 54±0.81 mg, respectively. An average decrease in body weight was observed in antihistamine-treated H. longicornis compared with control nymphs (3.3±0.42 mg) and adults (174±1.78 mg). Skin biopsies were collected after treatment, and differential histopathological characteristics were found between the treatment and control groups. Tick-infested skin collected from rabbits in the antihistamine-treated group lacked erythrocytes in the feeding pool, indicating that antihistamine impaired tick fast-feeding stage.

• Biomolecules & Therapeutics
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• v.16 no.4
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• pp.416-424
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• 2008

A series of N,N'-substituted iminodiacetamide derivatives was synthesized and evaluated their inhibitory effects on the histamine-induced smooth muscle contraction in guinea-pig ileum and on the histamine release from IgE-sensitized RBL-2H3 cells (rat basophilic leukemia cell line). Compounds A3, A4 and A5 which have 1-(4-chlorobenzhydryl) piperazine moiety, showed both moderate antihistamine activity and histamine release inhibitory activity.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.3
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• pp.215-220
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• 2009

Chlorpheniramine is a potent first-generation histamine $H_1$ receptor antagonist that can increase action potential duration and induce QT prolongation in several animal models. Since block of cardiac human ether-a-go-go-related gene (hERG) channels is one of leading causes of acquired long QT syndrome, we investigated the acute effects of chlorpheniramine on hERG channels to determine the electrophysiological basis for its proarrhythmic potential. We examined the effects of chlorpheniramine on the hERG channels expressed in Xenopus oocytes using two-microelectrode voltage-clamp techniques. Chlorpheniramine induced a concentration-dependent decrease of the current amplitude at the end of the voltage steps and hERG tail currents. The $IC_{50}$ of chlorpheniramine-dependent hERG block in Xenopus oocytes decreased progressively relative to the degree of depolarization. Chlorpheniramine affected the channels in the activated and inactivated states but not in the closed states. The S6 domain mutations Y652A and F656A partially attenuated (Y652A) or abolished (F656A) the hERG current block. These results suggest that the $H_1$ antihistamine, chlorpheniramine is a blocker of the hERG channels, providing a molecular mechanism for the drug-induced arrhythmogenic side effects.

• Tuberculosis and Respiratory Diseases
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• v.52 no.3
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• pp.219-229
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• 2002

Background : Sepsis-induced acute lung injury (ALI) is caused by many cellular and humoral mediators induced by an endotoxin. Histamine, which is widely distributed in the lungs and has been considered as an important mediator of sepsis. It increases P-selectin expression on the endothelial cell surfaces and induces IL-8 secretion. Therefore, an endotoxin-induced histamine may be related to neutrophil-mediated ALI by inducing the migration and activation of neutrophils in the lung tissue. However, the role of endogenous histamine in endotoxin ALI has not been clarified. The purpose of this study was to investigate how endotoxin-induced ALI is influenced by endogenous histamine and to identify the possible mechanism of action. Materials and Methods : The study consisted of 4 groups using Sprague-Dawley rats : 1) control group, where the rats were infused intratracheally by normal saline, 2) an endotoxin group, where lipopolysaccharide (LPS) was administered intratracheally 3) the $H_2$ receptor antagonist-treated group ($H_2$ group) and 4) the $H_1$ receptor antagonist-treated group ($H_1$ group), where $H_2$-receptor blocker (ranitidine) and $H_1$-receptor blocker(pyrilamine) were co-treated intravenously with the intratracheal administration of an endotoxin. The lung leak index using $I^{125}$-BSA, the total protein and LDH concentration in the lung lavage fluid, myeloperoxidase(MPO) activity in the lung tissue, the pathologic score and the total number of neutrophils, TNF-$\alpha$, IL-$1{\beta}$ and IL-10 in lung lavage (BAL) fluid were measured in each group as the indices of lung injury. Results : Compared to the control group, the endotoxin group exhibited significant increases in all lung injury indices. Significant reductions in the endotoxin-mediated increases in lung leak index (p<0.05) were observed in both the $H_1$ and $H_2$ groups. In addition the total protein (p<0.05) and LDH concentration (p<0.05) in the BAL fluid were also lower in the $H_2$ group compared to the endotoxin group. However, there was no change in the MPO activity in the lung tissue, the pathologic score and the total number of neutrophils in the BAL fluid in both the $H_2$ and $H_1$ groups compared to the endotoxin group. The increases in TNF-$\alpha$ IL-$1{\beta}$ and IL-10 concentrations in the BAL fluid observed in the endotoxin group were not reduced in the $H_2$ and $H_1$ groups. Conclusion : Antihistamine attenuated the enhanced alveolar-capillary permeability induced by the endotoxin via the $H_2$ receptor. However the attenuating mechanism may not be related to the pathogenesis of neutrophil dependent lung injury.

• Journal of The Korean Society of Clinical Toxicology
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• v.8 no.1
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• pp.37-42
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• 2010

Purpose: The purpose of this study was to determine the optimal length of time to observe patients with contrast media anaphylaxis in the Emergency Department. Methods: This study included the patients of all age groups who presented with anaphylaxis due to contrast media to the ED of Pusan National University Hospital from January 2006 to August 2009. The medical records were retrospectively reviewed. We analyzed the 100 patients who met the inclusion criteria. Their median age was 55 (46-62), and 38 out of the 100 patients (38%) were male. Results: The most common symptom of patients was urticaria. Corticosteroid and H1 antihistamine were given to most of the patients in the ED. All were discharged after observation in the ED and none were admitted to the ward. The average time from injection of the contrast media to the onset of symptom was 31 minutes (24-39) and the average time to symptom recovery was 127 minutes (89-188). The mean observation time in the ED was 93 minutes (59-153). Biphasic reactions were reported in only one case (1/100, 1%). Conclusion: These results suggest that patients who present with an anaphylactic reaction after radiologic studies that use intravenous contrast media can be safely discharged early from the ED because the symptom recovery time is not long and a biphasic reaction is rare.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.192-198
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• 1995

The affinity of mequitazine, a non-sedating antihistamine, for muscarinic receptors was evaluated in the guinea-pig ventricle and ileum by in vitro binding techniques and functional studies. In binding studies, [$^3$H]quinuclidinyl benzilate (QNB) identified a single class of muscarinic receptors with similar apparent $K_{D}$ value of about 100 pM in two tissues. Mequitazine inhibited [$^3$H]QNB binding to muscarinic receptors competitively. Analysis of the mequitazine inhibition curve of [$^3$H]QNB binding to ventricular microsome and ileal homogenate indicated the presence of a single homogeneous binding site with Ki value of 25 nM and 18 nM, respectively. In functional studies, mequitazine caused parallel rightward shifts of concentration-response curves for carbachol and histamine in the isolated guinea-pig ileum. The slope values obtained from Schild plot analysis for the antagonistic action of mequitazine on muscarinic and histamine $H_1$-receptors were not significantly different from unity. The p $A_2$values of mequitazine for muscarinic and histamine $H_1$-receptors were about 7.6 ( $K_{M}$= 25.1 nM) and 8.88 ( $K_{H}$= 1.32 nM), respectively. These results indicate that the muscarinic receptor blocking action of mequitazine is 15 times less potent than the $H_1$receptor blocking action, but high concentration of this drug may cause the peripheral muscarinic receptor blocking effect.t.t.t.

• Journal of The Korean Society of Clinical Toxicology
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• v.8 no.2
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• pp.79-87
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• 2010

Purpose: The previous studies on $H_1$ antihistamine overdose have generally been limited to cases of acute doxylamine succinate (DS) poisoning, yet there have been some studies on diphenhydramine (DPH) overdosing. But many clinicians consider the two drugs to be very similar and to have similar ingredients. The purpose of this study was to clarify the toxicologic characteristics and clinical outcomes between DS and DPH poisoning/overdose. Methods: We reviewed the medical and intensive care records of the patients with acute DS or DPH poisoning and who admitted to our emergency department from January 2008 and April 2010. We collected patient information regarding the features of the poisoning and the clinical and demographic characteristics. The patients were assessed for the clinical outcomes, the GCS, the PSS (Poisoning Severity Score) and the SOFA (Sequential Organ Failure Assessment). Results: Fifty seven patients (45 cases of DS poisoning and 12 cases of DPH poisoning) were enrolled. Compared with the DS group, the DPH group had higher incidences of intubation, serious mental change, QTc prolongation and ECG conduction abnormality (p=0.041, <0.001, 0.014 and 0.044, respectively). The DPH group had a higher PSS and a longer ICU stay. The peak CPK time and the CPK normalization time were longer for the patients with rhabdomyolysis due to DS poisoning. Conclusion: Two common $H_1$ antihistamines, doxylamine and diphenhydramine, are in the same ethanolamine-structural class, but the toxico-clinical outcomes are different according to many aspects. Therefore, clinicians could take a careful approach for the differential diagnosis and management between DS and DPH poisoning.

• Korean Journal of Pharmacognosy
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• v.13 no.4
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• pp.157-162
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• 1982

This study was undertaken to investigate effects of 'Oyo-Tang' on the respiratory system. The results of this study were summarized as follows; 1. Antihistamine and relaxed dialating actions were recognized on the extracted ileum and serial broncheal samples in guinea-pigs. 2. Mild hypertensive action was recognized on the carotid artery in rabbits. 3. Antitussive action was noted on mechanically irritated coughs in dogs and cats. In connection with the results of these studies, effects based on the Oriental medical references were consistent with the actual experimental results. It was considered that effective application of 'Oyo-Tang' for the treatment of cough and asthma could be justified.

• Natural Product Sciences
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• v.12 no.1
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• pp.55-61
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• 2006

A description of simple, isocratic and precise reversed phase HPLC methods is given for simultaneous quantification of pholcodine and ephedrine hydrochloride together with either carbinoxamine maleate or terfenadine in antitussive-antihistaminic oral pharmaceutical formulations. Separations were carried out on X-Terra and symmetry shield C18 column $(250\;{\times}\;4.6\;mm,\;5\;{\mu}m)$. The used isocratic elution systems were either $0.02\;M\;KH_2PO_4-acetonitrile$ in the ratio of 75 : 25 and pH adjusted to 7.70 with orthophosphoric acid or sodium hydroxide, for syrup (method A), or 0.02 octanesulphonic acid sodium salt solution-acetonitrile-acetic acid in the ratio of 75 : 25 : 0.5 for suspension (method B). The elution of both mixtures was achieved with a flow rate of 1 ml/min. Detection was carried out by UV absorbance at wavelengths of 220 and 250 nm for syrup and suspension, respectively. The quantification of the components in synthetic mixtures and actual syrup and suspension were calculated using the internal standard technique with metoclopramide HCl and codeine phosphate as internal standards (IS), respectively. The methods, for both mixtures, were validated and met all the requirements for the quality control analysis recommended by FDA and ICH.

• Journal of Korean society of Dental Hygiene
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• v.15 no.2
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• pp.319-324
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• 2015

Objectives: The purpose of this study was to verify the oral environmental change in using the natural oral cleaner containing propolis and prevention effect of oral disease. Methods: The subjects were 60 university students in Gangwon province. The groups consisted of 30 students of experimental group and 30 students of control group. The subjects were those who did not take the antipsychotic, diuretic, antihistamine, and anesthetic. The students rinsed their mouth with propolis mixture of oral cleanser for 4 weeks after receiving informed consent from October 1 to November 2, 2012. Collected saliva was measured for amount, salivary consistency, pH, plague index, gingival index, and halitosis. Results: The amount of salivary in propolis mixture of oral cleansing group remarkably increased (t=2.16, p<0.05). pH was alkaline in the group with oral cleaner containing the propolis (t=2.80, p<0.01). The bad breath remarkably decreased in the group with oral cleaner containing the propolis (t=-5.77, p<0.001). Conclusions: The use of the oral cleaner containing the propolis increased the amount of salivary and pH. The use of oral cleaner containing the propolis reduces halitosis and maintains good quality of oral hygiene.