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Comparison of the conjunctival toxicity of topical ocular antiallergic agents

Jong Soo Lee1, Ji Eun Lee, Nami Kim

  • 1Department of Ophthalmology, College of Medicine, Pusan National University, Medical Research Institute, Pusan National University Hospital, Busan, Korea. jongsool@pusan.ac.kr

Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics
|December 4, 2008
PubMed
Abstract

Insights

Topical allergic conjunctivitis treatments azelastine and ketotifen show more toxic effects on rabbit conjunctival cells than olopatadine. This suggests clinical consideration for ocular surface health when choosing antiallergic agents.

Area of Science:

  • Ophthalmology
  • Cell Biology
  • Pharmacology

Background:

  • Allergic conjunctivitis is a common ocular condition.
  • Topical antiallergic agents are widely used for treatment.
  • Understanding the ocular surface toxicity of these agents is crucial for patient safety.

Purpose of the Study:

  • To investigate the in vitro cytotoxic effects of three topical ocular antiallergic agents on cultured rabbit conjunctival cells.
  • To compare the toxicity profiles of azelastine hydrochloride, ketotifen fumarate, and olopatadine hydrochloride.

Main Methods:

  • Lactate dehydrogenase (LDH) leakage assay was used to quantify cell damage.
  • Conjunctival cells were exposed to varying concentrations and time points.
  • Osmolarity, pH, electrolyte composition, preservatives, and morphology were also assessed.

Main Results:

  • All tested antiallergic agents increased LDH titers, indicating cell damage, with peak effects around 4-12 hours.
  • Azelastine and ketotifen demonstrated significantly higher cytotoxicity, evidenced by increased LDH, edema, and cellular degeneration, compared to olopatadine.
  • Lower levels of Na(+), Cl(-), and pH were observed with azelastine and ketotifen.

Conclusions:

  • Azelastine and ketotifen exhibit a more pronounced toxic effect on conjunctival cells compared to olopatadine.
  • Clinicians should consider the potential ocular surface toxicity of azelastine and ketotifen when managing allergic conjunctivitis.

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