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儿童新型口服H1抗组胺药:现状与未满足的需求

New oral H1 antihistamines in children: facts and unmeet needs.

作者信息

de Benedictis F M, de Benedictis D, Canonica G W

机构信息

Pediatric Department, Salesi Children's Hospital, Ancona, Italy.

出版信息

Allergy. 2008 Oct;63(10):1395-404. doi: 10.1111/j.1398-9995.2008.01771.x.

Abstract

BACKGROUND

Second-generation antihistamines differ from first-generation ones because of their elevated specificity and affinity for peripheral H1-receptors and because of their lower penetration to the central nervous system, having fewer sedative effects as a result. Over the last few years, new compounds with different pharmacokinetic properties have been synthesized. More recent improvements of the molecules, generally in the form of active metabolites, led to the synthesis of new-generation antihistamines.

METHODS

Recommendations on the minimum criteria that would have to be met for compounds to be classified as new-generation antihistamines have been recently established by a consensus statement. In the past, the pharmacokinetics and pharmacodynamics of H1 antihistamines have not been optimally investigated in the pediatric population, especially in infants and young children.

RESULTS

The pharmacology of second-generation H1 antihistamines has been investigated relatively deeper than old antihistamines in children. In the pediatric population, clinical studies with new-generation antihistamines are still limited in number and, with rare exceptions, of brief duration. Comparative trials on the efficacy and safety between different compounds are also lacking.

CONCLUSIONS

Properly designed, long-term trials with new-generation H1 antihistamines need to be performed in single age groups, in order to better define the effects of these drugs in all pediatric population.

摘要

背景

第二代抗组胺药与第一代不同,因为它们对外周H1受体具有更高的特异性和亲和力,并且对中枢神经系统的穿透性较低,因此镇静作用较少。在过去几年中,已经合成了具有不同药代动力学特性的新化合物。分子的最新改进,通常以活性代谢物的形式,导致了新一代抗组胺药的合成。

方法

最近通过共识声明确定了将化合物归类为新一代抗组胺药必须满足的最低标准建议。过去,H1抗组胺药的药代动力学和药效学在儿科人群中,特别是在婴儿和幼儿中,尚未得到最佳研究。

结果

第二代H1抗组胺药在儿童中的药理学研究比旧的抗组胺药相对更深入。在儿科人群中,新一代抗组胺药的临床研究数量仍然有限,并且除了极少数例外,持续时间较短。不同化合物之间的疗效和安全性的比较试验也缺乏。

结论

需要在单一年龄组中进行设计合理的新一代H1抗组胺药长期试验,以便更好地确定这些药物在所有儿科人群中的作用。

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