Multiple action agents and the eye: do they really stabilize mast cells?

Curr Opin Allergy Clin Immunol. 2009 Oct;9(5):454-65. doi: 10.1097/ACI.0b013e3283303ebb.

Abstract

Purpose of review: Multiple action drugs, such as azelastine, epinastine, ketotifen and olopatadine, have recently been suggested to combine antihistaminic effect, mast cell stabilization and anti-inflammatory action. This pharmaceutical class is, therefore, rapidly becoming the first choice for prevention and treatment for allergic conjunctivitis.

Recent findings: Increasing in-vitro studies have been performed to investigate the mast-cell-stabilizing effect of multiple action drugs. Most of the study results agree that these drugs are able to inhibit histamine and several neoformed mediators, including cytokines and arachidonic acid-derived products, from mast cells. However, the mechanisms of action have not yet fully been elucidated. Most of the results from clinical trials as well as the in-vivo experimental studies, including the conjunctival provocation model, support the evidence of a stabilizing effect of these drugs.

Summary: Evidence of a different inhibitory effect of multiple action compounds on the pro-inflammatory mediators released from the mast cells suggests the possibility to target different phases of the allergic reaction, leading to a potential improvement in the management of allergic patients.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Arachidonic Acid / immunology
  • Conjunctivitis, Allergic / drug therapy*
  • Conjunctivitis, Allergic / immunology
  • Conjunctivitis, Allergic / pathology*
  • Cytokines / immunology
  • Dibenzazepines / pharmacology
  • Dibenzazepines / therapeutic use
  • Dibenzoxepins / pharmacology
  • Dibenzoxepins / therapeutic use
  • Histamine / immunology
  • Histamine Antagonists / pharmacology
  • Histamine Antagonists / therapeutic use
  • Humans
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Immunity, Innate / drug effects
  • Ketotifen / pharmacology
  • Ketotifen / therapeutic use
  • Mast Cells / drug effects*
  • Mast Cells / immunology
  • Mast Cells / metabolism
  • Mast Cells / pathology
  • Olopatadine Hydrochloride
  • Phthalazines / pharmacology
  • Phthalazines / therapeutic use

Substances

  • Anti-Inflammatory Agents
  • Cytokines
  • Dibenzazepines
  • Dibenzoxepins
  • Histamine Antagonists
  • Imidazoles
  • Phthalazines
  • Arachidonic Acid
  • Olopatadine Hydrochloride
  • Histamine
  • epinastine
  • Ketotifen
  • azelastine