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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。

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