抗过敏药H1-receptor拮抗剂的影响。

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Baroody调频,Naclerio RM

抗过敏药H1-receptor拮抗剂的影响。

过敏。2000;55增刊64:17-27。

PubMed ID
11291777 (在PubMed
]
文摘

抗组胺剂作用的主要机制治疗过敏疾病被认为是竞争性拮抗组胺与细胞受体结合(特别是H1-receptors),存在于神经末梢,平滑肌肉和腺体细胞。支持这个概念的结构无关的药物对抗H1-receptor并提供临床受益。然而,H1-receptor对抗可能不是他们唯一的作用机制在治疗过敏性鼻炎。的基础上,在体外和动物实验中,药物分为H1-receptor对手长期以来被公认有额外的药理特性。大多数第一代H1-antihistamines抗胆碱能镇静,局部麻醉,和anti-5-HT效应,这可能会积极影响过敏反应的症状也导致副作用。这些额外的属性不是均匀分布在药物分为H1-receptor拮抗剂。例如,阿扎他定能抑制体外ige组胺和白三烯(LT)从肥大细胞和嗜碱粒细胞释放。在人类挑战模型、terfenadine阿扎他定,氯雷他定减少ige组胺释放。西替利嗪减少嗜酸性渗透皮肤抗原的挑战,而不是鼻子。在鼻抗原挑战模型中,西替利嗪预处理并不影响组胺的水平和前列腺素D2恢复postchallenge灌洗,而白蛋白的水平,N-tosyl-L-arginine甲酯(温和)酯酶活动,和LTs减少。 Terfenadine, cetirizine, and loratadine blocked allergen-induced hyperresponsiveness to methacholine. In view of the complexity of the pathophysiology of allergy, a number of H1 antagonists with additional properties are currently under development for allergic diseases. Mizolastine, a new H1-receptor antagonist, has been shown to have additional actions that should help reduce the allergic response. In animal models, mizolastine inhibits antigen-induced eosinophil infiltration into mouse skin and into the nasal cavity of guinea-pigs. Mizolastine also significantly inhibits antigen-induced neutrophil infiltration into the bronchoalveolar lavage fluids of guinea-pigs. In addition, it inhibits arachidonic acid-induced paw oedema in rats without affecting carrageenin-induced rat paw oedema, suggesting an effect on LT generation. In man, mizolastine inhibits early and late antigen-induced soluble intercellular adhesion molecule 1 (ICAM-1) levels in skin blisters. It also inhibits anaphylactic release of histamine from rodent mast cells, LTC4 and LTB4 release from mouse bone-marrow-derived mast cells, LTC4 release from rat intestinal mast cells, and 5-lipoxygenase activity of polymorphonuclear neutrophils of guinea-pig intestines and rat basophilic leukaemia cells. It is clear that a number of H1-antihistamines have multiple effects on the allergic inflammatory response. It is equally clear that these antiallergic effects are not uniformly shared among all drugs of this class. The assessment of the clinical significance of these results and research regarding the parts of the molecules responsible for these activities are underway.

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