• Title/Summary/Keyword: 항히스타민제

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Effects of Loratadine, Cetirizine, and Terfenadine on Histamine-Induced Wheal and Erythema Responses in Normal Canine Skin (개 피부에서 Histamine에 의한 팽진과 발적에 대한 loratadine, cetirizine과 terfenadine의 억제효과)

  • Jeong, A-Young;Jeong, Hyo-Hoon;Heo, Woo-Phil;Eom, Ki-Dong;Jang, Kawng-Ho;Oh, Tae-Ho
    • Journal of Veterinary Clinics
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    • v.19 no.2
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    • pp.186-190
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    • 2002
  • This crossover study was performed in order to compare the effects of cetirizine, loratadine, and terfenadine in canine skin. Five healthy dogs were used. Cetirizine 0.5 mg/kg, loratadine 5 mg/kg and terfenadine 5 mg/kg were administered orally 4 hours before the experiment. Erythema indices and wheal size were assessed by Hexameter ($MX^{\circledR}$ 18, CK, Germany) and skin reaction guide, respectively. Cetirizine-induced erythema inhibition was generally higher than other drugs and was significantly different from placebo. Cetirizine was superior to placebo at 3, 4, 5, 6, 7, and 8 minutes (p< 0.01). Cetirizine also was superior to placebo at 9 minutes (p< 0.05). Loratadine and terfenadine erythema inhibition were better than after placebo treatment from 4 to 9 minutes, but erythema index of terfenadine at 7 minutes was not observed probability of 95% and 99%. At 10 minutes, intradermal injection of the histamine caused a mean wheal dimension for placebo, cetirizine, loratadine and terfenadine, which were 13.25$\pm$0.75 mm,7.5$\pm$ 1.02 mm (53% reduction, p<0.007),6.2$\pm$0.58 mm(43% reduction, p <0.01), and 8.4 $\pm$0.67 mm(37% reduction, p< 0.05), respectively, comparing with placebo. Loratadine and cetirizine were good antihistamines for clinical therapy for atopic dermatitis in dog.

Improvement of the Synthetic Route for Epinastine Antihistamine (에피나스틴 항히스타민제의 합성법 개선)

  • Baek, Du-Jong;Kim, Moon-Sik
    • 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.

Modification of Physical Properties of Certain Antitussive and Antihistaminic Agents by Formation of N-Cyclohexylsulfamate Salts. (N-Cyclohexylsulfamate 염형성에 의한 진해제와 항히스타민제의 물리적성질의 개량)

  • 고현기
    • YAKHAK HOEJI
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    • v.9 no.1_2
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    • pp.23-26
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    • 1965
  • The N-Cyclohexylsulfamic acid salts of four well known therapeutic agents were prepared. Salts of two of the compounds, ephedrine and diphenhydramine, were found to have great improved taste and increased solubility.

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Bradykinin Antagonistic Activities of Antihistamine Agents Containing Piperazine Moiety (피페라진계 항히스타민제들의 브라디키닌 길항작용)

  • 정성현;이소영;윤혜숙
    • 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.

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Extraction Spectrophotometric Determination of Antihistamines with Picric Acid (피크린 산에 의한 항히스타민제의 추출분광광도 정량)

  • 신태용;엄동옥
    • YAKHAK HOEJI
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    • v.37 no.2
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    • pp.119-123
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    • 1993
  • A spectrophotomertic method is proposed for the determination of antihistamines. The method is based on solvent extraction of the ion pair formed between antihistamines and colored picric acid into chloroform. The binding state of antihistamines-picric acid complexes were presumed by IR and $^{1}$H-NMR spectra as intermolecular hydrogen bonding. This method was applicable to the determination of antihistamines in the pharamaceutical preparations.

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Synthesis of Azelastine.HCl from 4-Chlorophenyl Acetic Acid (4-염화페닐 아세트산을 이용한 염산 아젤라스틴의 합성)

  • Ji, Hyun;Jeong, Noh-Hee
    • Journal of the Korean Applied Science and Technology
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    • v.29 no.3
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    • pp.429-434
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    • 2012
  • A kind of Antihistamines, Azelastine HCl which known as modern H1-blockers, was synthesized by four step process using phthalic anhydride, 4-chlorophenylacetic acid, hydrazine 2HCl. The first step was the reaction of removing carboxyl group and hydroxyl group and the second step was saponification of 3-(4-chlorobenzylidene)phthalide. The third step was the nucleophilic addition reactions of primary amines and the fourth step was addition reaction of N-methyl-1-aza-bicyclo[3,2,0]heptane to 4-(4-chlorobenzyl)-1-(2H)phthalazinone. As a result, product was analyzed by FT-IR and $^1H$-NMR and could be obtained with a yield of 80%.

Hypersensitivity to Local Anesthetics: A Case Report (국소마취제로 인한 과민반응 : 증례 보고)

  • Rah, Yujin;Lee, Jewoo;Ra, Jiyoung
    • Journal of the korean academy of Pediatric Dentistry
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    • v.44 no.3
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    • pp.365-369
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    • 2017
  • Local anesthetics are widely used in clinical dentistry. However, while rare, there have been some reports of true hypersensitivity to local anesthetics. A case of hypersensitivity in a 26-month-old boy is reported. After administering local anesthesia with lidocaine, treatment was performed while the patient was under oral sedation. After treatment, the patient presented with lower lip edema. Treatment with anti-histamines and a steroid successfully reversed his symptoms.