Histamine and H1-antihistamines: Celebrating a century of progress
Histamine and H1-antihistamines: Celebrating a century of progress
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DOI：
10.1016/j.jaci.2011.09.005
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发表时间：
2011-12-01
影响因子：
14.2
通讯作者：
Simons, Keith J.
中科院分区：
文献类型：
--
作者：
Simons, F. Estelle R.;Simons, Keith J.
在这篇综述中，我们庆祝自首次描述组胺的生理和病理作用以来一个世纪的进步，以及自 H-1-抗组胺药引入临床使用以来 70 年的进步。我们讨论组胺以及有关 H-1-抗组胺药作为具有免疫调节作用的反向激动剂（不是拮抗剂或阻滞剂）的分子作用机制的临床相关信息。与1942年至80年代中期推出的第一代（老）H-1-抗组胺药不同，随后推出的第二（新）代H-1-抗组胺药大多在临床药理学、功效和安全性方面进行了广泛的研究；此外，它们相对来说不会产生不良影响，并且与服药过量后的死亡没有因果关系。重要的进展包括改进的鼻用和眼用 H-1-抗组胺药，分别在过敏性鼻炎和过敏性结膜炎治疗中快速起效（几分钟），以及有效且安全地使用高剂量（高达 4 倍）口服第二代 H-1-抗组胺药治疗慢性荨麻疹。用于临床的新型 H-1-抗组胺药包括口服制剂（比拉斯汀和卢帕他定）和眼用制剂（阿卡他定和贝托斯汀）。已在过敏性鼻炎患者中进行了具有增强减充血作用的 H-3-抗组胺药的临床研究。正在研究的其他新化合物包括对过敏性鼻炎、特应性皮炎和其他疾病具有抗炎作用的 H-4-抗组胺药。抗组胺药有着悠久的历史和光明的未来。 （过敏临床免疫杂志 2011 年；128：1139-50。）
In this review we celebrate a century of progress since the initial description of the physiologic and pathologic roles of histamine and 70 years of progress since the introduction of H-1-antihistamines for clinical use. We discuss histamine and clinically relevant information about the molecular mechanisms of action of H-1-antihistamines as inverse agonists (not antagonists or blockers) with immunoregulatory effects. Unlike first (old)-generation H-1-antihistamines introduced from 1942 to the mid-1980s, most of the second (new)-generation H-1-antihistamines introduced subsequently have been investigated extensively with regard to clinical pharmacology, efficacy, and safety; moreover, they are relatively free from adverse effects and not causally linked with fatalities after overdose. Important advances include improved nasal and ophthalmic H-1-antihistamines with rapid onset of action (in minutes) for allergic rhinitis and allergic conjunctivitis treatment, respectively, and effective and safe use of high (up to 4-fold) doses of oral second-generation H-1-antihistamines for chronic urticaria treatment. New H-1-antihistamines introduced for clinical use include oral formulations (bilastine and rupatadine), and ophthalmic formulations (alcaftadine and bepotastine). Clinical studies of H-3-antihistamines with enhanced decongestant effects have been conducted in patients with allergic rhinitis. Additional novel compounds being studied include H-4-antihistamines with anti-inflammatory effects in allergic rhinitis, atopic dermatitis, and other diseases.Antihistamines have a storied past and a promising future. (J Allergy Clin Immunol 2011;128:1139-50.)