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阿斯咪唑(息斯敏)——一种非镇静性H1抗组胺药的药理学

[Pharmacology of astemizole (Hismanal) a non-sedating H1 antihistaminic].

作者信息

Niemegeers C J

出版信息

Z Hautkr. 1985;60 Suppl 1:14-22.

PMID:2581383
Abstract

In the compound 48/80 lethality test in rats, which is based on the specific activation of mast cells, astemizole was found to be a potent, long-acting and orally very effective inhibitor of anaphylactoid shock. In comparison to other histamine-H1 antagonists, astemizole was remarkably free of interactions with muscarine, serotonin, dopamine, noradrenaline and opiate receptors, and devoid of effects on normal body functions. No evidence of central effects was found, and astemizole did not change the intensity of action of several centrally acting drugs. Toxicity studies have shown astemizole to be a very safe drug. Astemizole is a very effective inhibitor of allergic reactions in rats and dogs. The low oral therapeutic doses of astemizole are expected to provide a pronounced and long-lasting inhibition of allergic reactions in the absence of side effects.

摘要

在基于肥大细胞特异性激活的大鼠复合48/80致死性试验中,发现阿司咪唑是类过敏性休克的一种强效、长效且口服非常有效的抑制剂。与其他组胺H1拮抗剂相比,阿司咪唑与毒蕈碱、血清素、多巴胺、去甲肾上腺素和阿片受体的相互作用非常少,并且对正常身体功能没有影响。未发现有中枢作用的证据,阿司咪唑也不会改变几种中枢作用药物的作用强度。毒性研究表明阿司咪唑是一种非常安全的药物。阿司咪唑是大鼠和狗过敏反应的非常有效的抑制剂。预计阿司咪唑的低口服治疗剂量能在无副作用的情况下对过敏反应产生显著且持久的抑制作用。

相似文献

1
[Pharmacology of astemizole (Hismanal) a non-sedating H1 antihistaminic].阿斯咪唑(息斯敏)——一种非镇静性H1抗组胺药的药理学
Z Hautkr. 1985;60 Suppl 1:14-22.
2
Antiallergic effects of astemizole on immediate type hypersensitivity reactions.阿司咪唑对速发型超敏反应的抗过敏作用。
Methods Find Exp Clin Pharmacol. 1990 Oct;12(8):531-9.
3
In vivo pharmacology of astemizole, a new type of H1-antihistaminic compound.新型H1抗组胺化合物阿司咪唑的体内药理学
Arch Int Pharmacodyn Ther. 1981 May;251(1):39-51.
4
The pharmacological profile of a specific, safe, effective and non-sedative anti-allergic, astemizole.一种特定的、安全、有效且无镇静作用的抗过敏药物——阿司咪唑的药理学特性。
Agents Actions. 1986 Apr;18(1-2):141-4. doi: 10.1007/BF01988005.
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[General review of a non-sedative antihistaminic, astemizole (Hismanal), a H1 receptor antagonist].[非镇静性抗组胺药阿司咪唑(息斯敏)——一种H1受体拮抗剂的综述]
Allerg Immunol (Paris). 1988 May;20(5):197-201.
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In vitro and in vivo studies of the non-sedating antihistamine epinastine.非镇静性抗组胺药依巴斯汀的体外和体内研究。
Arzneimittelforschung. 1988 Oct;38(10):1446-53.
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Effects of E-4716, a new antihistaminic with antiallergic properties, on chemical mediators induction of immunologic reactions.新型具有抗过敏特性的抗组胺药E - 4716对免疫反应化学介质诱导的影响。
Methods Find Exp Clin Pharmacol. 1996 Jul-Aug;18(6):397-406.
8
Pharmacology of the specific histamine H1-antagonist astemizole.
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In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.新型长效组胺H1拮抗剂阿司咪唑的体外和体内结合特性
Mol Pharmacol. 1982 Mar;21(2):294-300.
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Potential of interaction between the H1-antagonist astemizole and other drugs.H1拮抗剂阿司咪唑与其他药物之间相互作用的可能性。
Ann Allergy. 1986 Nov;57(5):321-4.