Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research

Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547.

Abstract

Background: Histamine receptor activation and degranulation of mast cells are the mechanisms by which the ocular itching, hyperemia, chemosis, eyelid swelling, and tearing of seasonal allergic conjunctivitis are induced. Some of the topical solutions available as anti-allergy therapies are intended to interfere with these mechanisms, and the body of research regarding the capabilities of these therapeutic molecules continues to expand.

Objective: To review the currently available literature regarding one topical ophthalmic anti-allergy agent, olopatadine (Patanol), and its anti-histaminic and mast cell stabilizing actions, both in pre-clinical and clinical settings.

Design and methods: Relevant research of laboratory, animal model, and clinical trial studies performed using olopatadine was reviewed. MEDLINE literature searches were conducted and supplemented by additional reports which furthered relevant discussion or were necessary to verify the information resulting from original searches.

Results: Olopatadine demonstrates unique properties both pre-clinically and clinically which differentiate it from other therapeutic molecules in its class of dual action mast cell stabilizer/anti-histamine. Its non-perturbation of cell membranes, human conjunctival mast cell stabilization in vivo and in vitro, and superior efficacy as compared to other topical anti-allergic medications including mast cell stabilizers, anti-histamines, and dual action agents, all contribute to olopatadine's profile.

Conclusions: Peer-reviewed literature suggests that olopatadine is clinically superior to the other anti-allergic molecules because of its strong anti-histaminic qualities and its unique ocular mast cell stabilizing properties.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anti-Allergic Agents / administration & dosage
  • Anti-Allergic Agents / pharmacology
  • Anti-Allergic Agents / therapeutic use*
  • Dibenzoxepins / administration & dosage
  • Dibenzoxepins / pharmacology
  • Dibenzoxepins / therapeutic use*
  • Drug Evaluation, Preclinical
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / pharmacology
  • Histamine H1 Antagonists / therapeutic use*
  • Humans
  • Mast Cells / drug effects*
  • Mast Cells / metabolism
  • Olopatadine Hydrochloride
  • Ophthalmic Solutions
  • Placebo Effect
  • Treatment Outcome

Substances

  • Anti-Allergic Agents
  • Dibenzoxepins
  • Histamine H1 Antagonists
  • Ophthalmic Solutions
  • Olopatadine Hydrochloride