Murota Hiroyuki, Katayama Ichiro
Osaka University, Graduate School of Medicine, Course of Integrated Medicine, Dermatology Department, 2-2 Yamadaoka, Suita-city, Osaka 5650871, Japan.
Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. doi: 10.1517/14656560903078410.
Emedastine difumarate, a selective histamine-H1 receptor antagonist and effective antiallergic agent, inhibits various clinical symptoms of allergic rhinitis, allergic conjunctivitis, urticaria, allergic dermatitis, pruritus cutaneous, and prurigo. In addition to greater efficacy than other antihistamines, emedastine difumarate produces no adverse cardiovascular effects and exhibits minimal anticholinergic activity. Moreover, a recent study revealed that the effect of emedastine difumarate on inhibition of histamine-induced collagen synthesis in vitro was greater in dermal fibroblasts than in nasal mucosa fibroblasts. This result indicates that there are tissue-specific effects of emedastine difumarate and that it may be more effective for treating fibrosis in skin than in nasal mucosa. However, the mechanism and role of tissue remodeling is less well established for allergic skin diseases and allergic conjunctivitis, in comparison to respiratory allergic diseases.
This review outlines the involvement of histamine in the pathogenesis of tissue remodeling in a variety of organs, and presents the evidence for the effect of antihistamines on this process. Furthermore, this review also discusses antihistamines as an intervention strategy in tissue remodeling.
The scientific literature, published abstracts, and selected textbooks were reviewed.
RESULTS/CONCLUSION: Although additional evidence is required, emerging evidence suggests that emedastine difumarate may be of value in the prevention of excess tissue remodeling in allergic skin inflammation.
富马酸依美斯汀是一种选择性组胺-H1受体拮抗剂及有效的抗过敏药物,可抑制过敏性鼻炎、过敏性结膜炎、荨麻疹、过敏性皮炎、皮肤瘙痒症及痒疹的各种临床症状。除了比其他抗组胺药疗效更佳外,富马酸依美斯汀不会产生不良心血管影响,且抗胆碱能活性极小。此外,最近一项研究表明,富马酸依美斯汀在体外对组胺诱导的真皮成纤维细胞胶原蛋白合成的抑制作用比对鼻黏膜成纤维细胞的抑制作用更强。这一结果表明,富马酸依美斯汀存在组织特异性效应,且其在治疗皮肤纤维化方面可能比治疗鼻黏膜纤维化更有效。然而,与呼吸道过敏性疾病相比,过敏性皮肤病和过敏性结膜炎中组织重塑的机制和作用尚未完全明确。
本综述概述了组胺在多种器官组织重塑发病机制中的作用,并提供了抗组胺药对这一过程影响的证据。此外,本综述还讨论了抗组胺药作为组织重塑干预策略的情况。
对科学文献、发表的摘要及选定的教科书进行了综述。
结果/结论:尽管还需要更多证据,但新出现的证据表明,富马酸依美斯汀在预防过敏性皮肤炎症中过度的组织重塑方面可能具有一定价值。