• Archives of Pharmacal Research
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• v.28 no.1
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• pp.111-114
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• 2005

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

• 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.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.324-328
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• 2000

Three dimensional QSAR studies for antihistamine and antibradykinin effects of new piperazine derivatives were conducted using the comparative molecular field analysis. Electrostatic and steric factors, but not hydrophobic factor, of the synthesized compounds were correlated with the antagonistic effect.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.625-630
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• 1993

Among the six antihistamine agents tested in this study, homochlorcyclizine showed the highest bradykinin antagonistic activity in the receptor binding assay as well as the isolated rat ileum assay. Schild plot analysis of bradykinin-induced ileal contraction in the presence of three different concentrations of homochlorcyclizine revealed a pA$_{2}$=6.26, and a correlation coefficient of 0.984. Homochlorcyclizine of (100 $\mu{M}$ final concentration) also showed 25% antagonistic activity in the receptor binding assay.

• 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.

• Korean Journal of Clinical Pharmacy
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• v.23 no.4
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• pp.327-333
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• 2013

Background: Antihistamine and anti-allergy medications are widely used during pregnancy. Reading label information is one of the easiest ways to get safety information. But there are content gaps among countries. Objective: To compare the risk level and the recommendation level of antihistamine/anti-allergy drug's label information in pregnant women among Korea, the USA, the UK, and Japan. Method: Study drugs of antihistamine/anti-allergy medications were selected according to Korea drug classification codes. Based on the label information of selected product, risk level was classified into 5 categories as follows: 'Definite', 'Probable', 'Possible', and 'Unlikely', 'Unclassified' according to the level of evidence. Recommendation level was classified into 4 categories as follows: 'Contraindicated', 'Cautious', 'Compatible', and 'Unclassified'. Frequency and proportion were presented according to the each category. To estimate agreement of each category among 4 countries, percent agreement and kappa (k) coefficient were calculated. Results: Total 13 drug ingredients were selected for antihistamine/anti-allergy medications. In risk level, Korea (46%) and Japan (69%) were mostly classified in the category of 'Unclassified', but 'Unlikely' category was more frequent in the UK (62%) and the USA (46%). In recommendation level, the proportion of 'Contraindicated' was highest in Korea (46%) compared to other countries. In contrast, the category of 'Cautious' was 77%-85% in the USA, the UK, and Japan. The percent agreement for risk level was highest in the USA-UK (54%). The recommendation level of Korea-USA showed lowest agreement for percent agreement (46%) and kappa coefficient (k=0.02). Conclusion: We confirmed the differences among safety information provided by four different countries. 'Contraindicated' was more likely in Korea compared with other countries.

• Journal of the Korean Chemical Society
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• v.54 no.4
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• pp.447-450
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• 2010

In this study, the improved large-scale synthetic route for epinastine hydrochloride, the second-generation antihistamine, was developed. The original synthetic route involves the synthesis of an aminomethyl derivative, the main intermediate, and in this process hazardous materials such as very toxic phosgene and sodium cyanide along with the explosive and expensive aluminum chloride and lithium aluminum hydride were used. In order to improve the synthetic route, we developed industrially very useful process to prepare the aminomethyl intermediate by the synthesis of the phthalimidomethyl derivative first and easy removal of the phthalyl group using hydrochloric acid or methyl hydrazine, and hazardous materials and expensive reagents were excluded in this process.

• Journal of Sasang Constitutional Medicine
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• v.34 no.2
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• pp.84-96
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• 2022

Introduction Chronic idiopathic urticaria in patients diagnosed with an unfavorable pattern in Soyangin and Taeumin based on Sasang medicine showed a significant improvement after herbal medicine treatment. Methods The patients had treatment with both herbal medication and antihistamine. We checked the patients' cutaneous manifestation, original symptoms, and the number of antihistamine doses in each visit. We evaluated the medical records retrospectively. Results After one month of treatment, the patients showed cutaneous manifestation relief. Each patient reduced and withdrew antihistamine at four moths and eight months respectively, and the cutaneous manifestation did not recur. We maintained the herbal medicine prescription until the origin symptoms improved. Throughout the subsequent follow-up, the patients showed both urticaria and the original symptoms in good condition without treatment. Discussion Sasang medicine treatment can be an effective treatment for chronic idiopathic urticaria and long-term management is necessary for an unfavorable pattern which can take more than 6 months.

• Korean Journal of Pharmacognosy
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• v.15 no.4
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• pp.188-193
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• 1984

It was previously indicated that 'Samulanshintang' had been examined for effects of the anticonvulsive, antipyretic, analgesic, sedative and antispasmodic actions. In order to investigate the effect on the cardiovascular system and anemic rabbits induced by phenlhydrazine HCl, pharmacological studies have been carried out with extract. The results of this investigation were summarized as follows: The relaxation of bronchial smooth muscle and antihistamine action were recognized. Antihypertensive and vasodilating actions due to vascular smooth muscle relaxation were noted in frogs and rabbits. 'Samulanshintang' lowered the rate of anemia induced by phenylhydrazine and rapidly recovered from the anemia state.

• 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.