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左西替利嗪:过敏症专科医生的武器库日益壮大。

Levocetirizine: the allergist's arsenal grows larger.

作者信息

Bloebaum R Matthew, Grant J Andrew

机构信息

The University of Texas Medical Branch, Department of Internal Medicine, Allergy and Immunology Division, Medical Research Bldg. 8.104, 301 University Boulevard, Galveston, Texas 77555-1083, USA.

出版信息

Expert Opin Pharmacother. 2004 Jul;5(7):1581-8. doi: 10.1517/14656566.5.7.1581.

Abstract

Antihistamines are the cornerstone of treatment for many allergic diseases, such as allergic rhinitis and chronic urticaria. Since the discovery of their beneficial effects in the 1940s, scientists have found molecules with greater selectivity to block specific histamine receptors without some of the detrimental side effects that are seen if antihistamines cross the blood-brain barrier. Levocetirizine is the active enantiomer of cetirizine and a selective H(1)-histamine blocker. It exhibits many favourable characteristics of an ideal antihistamine, both pharmacodynamically and pharmacokinetically, including high bioavailability, rapid onset of action, limited distribution and low degree of metabolism. Furthermore, clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal amount of untoward effects.

摘要

抗组胺药是许多过敏性疾病(如过敏性鼻炎和慢性荨麻疹)治疗的基石。自20世纪40年代发现其有益作用以来,科学家们已找到对特定组胺受体具有更高选择性的分子,这些分子不会产生抗组胺药穿过血脑屏障时出现的一些有害副作用。左西替利嗪是西替利嗪的活性对映体,是一种选择性H(1)组胺阻滞剂。它在药效学和药代动力学方面均表现出理想抗组胺药的许多有利特性,包括高生物利用度、起效迅速、分布有限和低代谢程度。此外,临床试验表明,它治疗过敏性鼻炎和慢性荨麻疹安全有效,不良反应极少。

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