Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases

Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. doi: 10.1517/14656560903078410.


Background: 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.

Objective: 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.

Methods: 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.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Allergic Agents / adverse effects
  • Anti-Allergic Agents / pharmacology
  • Anti-Allergic Agents / therapeutic use*
  • Benzimidazoles / adverse effects
  • Benzimidazoles / pharmacology
  • Benzimidazoles / therapeutic use*
  • Clinical Trials as Topic
  • Humans
  • Hypersensitivity / drug therapy*
  • Hypersensitivity / immunology
  • Hypersensitivity / physiopathology
  • Inflammation / drug therapy
  • Inflammation / etiology
  • Inflammation / immunology
  • Skin / drug effects
  • Skin / immunology


  • Anti-Allergic Agents
  • Benzimidazoles
  • emedastine