Simons F E
Department of Pediatrics and Child Health, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
Drug Saf. 1994 May;10(5):350-80. doi: 10.2165/00002018-199410050-00002.
First-generation histamine H1-receptor antagonists, such as diphenhydramine, triprolidine, hydroxyzine or chlorpheniramine (chlorphenamine), frequently cause somnolence or other CNS adverse effects. Second-generation H1-antagonists, such as terfenadine, astemizole, loratadine and cetirizine, represent a true advance in therapeutics. In manufacturers' recommended doses, they have a more favourable benefit/risk ratio than their predecessors with regard to lack of CNS effects, and do not exacerbate the adverse CNS effects of alcohol or other CNS-active chemicals. Rarely, some of the newer H1-antagonists may cause cardiac dysrhythmias after overdose or under other specific conditions. The concept of a risk-free H1-antagonist is proving to be an oversimplification. An H1-antagonist absolutely free from adverse effects under all circumstances is not yet available for use. The magnitude of the beneficial effects of each H1-antagonist should be related to the magnitude of the unwanted effects, especially in the CNS and cardiovascular system, and a benefit-risk ratio or therapeutic index should be developed for each medication in this class.
第一代组胺H1受体拮抗剂，如苯海拉明、曲普利啶、羟嗪或氯苯那敏（扑尔敏），常引起嗜睡或其他中枢神经系统不良反应。第二代H1拮抗剂，如特非那定、阿司咪唑、氯雷他定和西替利嗪，代表了治疗学上的真正进步。在制造商推荐的剂量下，它们在缺乏中枢神经系统作用方面比其前身具有更有利的效益/风险比，并且不会加重酒精或其他中枢神经系统活性化学物质的中枢神经系统不良反应。很少有情况是，一些较新的H1拮抗剂在过量用药或其他特定条件下可能会引起心律失常。无风险H1拮抗剂的概念被证明过于简单化。目前还没有一种在所有情况下都完全没有不良反应的H1拮抗剂可供使用。每种H1拮抗剂的有益作用程度应与不良作用程度相关，尤其是在中枢神经系统和心血管系统方面，并且应该为这类药物中的每种药物制定效益-风险比或治疗指数。
