作者:Garry M. Walsh、Lucio Annunziato、Nelly Frossard、Klaas Knol、Sten Levander、Jean-Marie Nicolas、Maurizo Taglialatela、Michael D. Tharp、Jean P. Tillement、Henk Timmerman
DOI:10.2165/00003495-200161020-00006
日期:——
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 ahererogeneous 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有效药物,并且是全球最常用和最安全的药物之一。然而,在开处方时考虑H1受体拮抗剂的治疗指数或收益/风险比至关重要,因为它们用于治疗非危及生命的疾病。目前有许多第二代抗组胺药可供选择,初步查看其安全性和疗效似乎是相当可比的。然而,较新一代的抗组胺药实际上代表了一组异质化的化合物,具有显著不同的化学结构、不良反应、半衰期、组织分布和代谢、抗组胺特征的谱系,以及不同程度的抗炎效果。关于抗炎效果,越来越多的人意识到这些化合物可能在哮喘治疗中作为有用的辅助药物。在安全性问题方面,目前的第二代抗组胺药中包括一些具有已知心脏毒性影响的药物,以及一些具有潜在不良药物相互作用的药物。此外,一些第二代H1拮抗剂引起了人们对其在某些个体中引起嗜睡的潜在风险的担忧。因此,可以认为目前的第二代药物分组过于庞大且不明确,因为这一分类主要是基于将第一代镇静药物与非镇静H1拮抗剂分开的概念。虽然谈论第三代抗组胺药的分组还为时尚早,但未来这类分类的成员资格可能基于较低的分布量,以及缺乏镇静作用、药物相互作用和心脏毒性。