Walsh G M, Annunziato L, Frossard N, Knol K, Levander S, Nicolas J M, Taglialatela M, Tharp M D, Tillement J P, Timmerman H
Department of Medicine and Therapeutics, University of Aberdeen Medical School, Scotland.
Drugs. 2001;61(2):207-36. doi: 10.2165/00003495-200161020-00006.
Second generation antihistamines are recognised as being highly effective treatments for allergy-based disease and are among the most frequently prescribed and safest drugs in the world. However, consideration of the therapeutic index or the benefit/risk ratio of the H1 receptor antagonists is of paramount importance when prescribing this class of compounds as they are used to treat non-life threatening conditions. There are many second generation antihistamines available and at first examination these appear to be comparable in terms of safety and efficacy. However, the newer antihistamines in fact represent a heterogeneous group of compounds, having markedly differing chemical structures, adverse effects, half-life, tissue distribution and metabolism, spectrum of antihistaminic properties, and varying degrees of anti-inflammatory effects. With regard to the latter, there is growing awareness that some of these compounds might represent useful adjunct medications in asthma therapy. In terms of safety issues, the current second generation grouping includes compounds with proven cardiotoxic effects and others with the potential for adverse drug interactions. Moreover, some of the second generation H1 antagonists have given cause for concern regarding their potential to cause a degree of somnolence in some individuals. It can be argued, therefore, that the present second generation grouping is too large and indistinct since this was based primarily on the concept of separating the first generation sedating compounds from nonsedating H1 antagonists. Although it is too early to talk about a third generation grouping of antihistamines, future membership of such a classification could be based on a low volume of distribution coupled with a lack of sedating effects, drug interactions and cardiotoxicity.
第二代抗组胺药被认为是治疗过敏性疾病的高效药物，也是世界上最常用且最安全的药物之一。然而，在处方这类化合物时，考虑H1受体拮抗剂的治疗指数或获益/风险比至关重要，因为它们用于治疗非危及生命的病症。市面上有许多第二代抗组胺药，初看时它们在安全性和疗效方面似乎相当。然而，事实上新型抗组胺药是一类异质性化合物，其化学结构、不良反应、半衰期、组织分布和代谢、抗组胺特性谱以及抗炎作用程度都有显著差异。关于后者，人们越来越意识到其中一些化合物可能是哮喘治疗中有用的辅助药物。在安全问题方面，当前的第二代分类包括已证实有心脏毒性作用的化合物以及有药物不良相互作用潜在风险的其他化合物。此外，一些第二代H1拮抗剂因其可能导致某些个体出现一定程度的嗜睡而引发关注。因此，可以说目前的第二代分类过于宽泛且不明确，因为这主要基于将第一代有镇静作用的化合物与无镇静作用的H1拮抗剂区分开来的概念。虽然现在谈论抗组胺药的第三代分类还为时过早，但此类分类未来的成员可能基于低分布容积以及无镇静作用、药物相互作用和心脏毒性。
