Aqueous concentration of tranexamic acid after 5% and 10% eyedrop administration

Eur J Ophthalmol. 2009 Jul-Aug;19(4):661-6. doi: 10.1177/112067210901900422.

Abstract

Purpose: To determine whether topical tranexamic acid can provide acceptable therapeutic concentration in the aqueous humor.

Methods: A total of 47 patients with cataract as the sole eye disease who have been scheduled for cataract operation received one drop of tranexamic acid 5% solution at various time intervals prior to operation (from 15 minutes to 9 hours). Two patients received 10% solution of the drug. Paracentesis of the anterior chamber was done and the aqueous humor was aspirated in the operation room. The aqueous samples were analyzed using high-performance liquid chromatography method with the limit of quantification around 0.1 microg/mL. Systemic and ocular side effects were evaluated.

Results: Aqueous concentrations of tranexamic acid was higher than 1.5 microg/mL up to 160 minutes after administration of a single drop of 5% solution of the drug and then declined to an average concentration of 1 microg/mL at 300 minutes which persisted up to 9 hours after administration.In two patients for whom a single drop of 10% tranexamic acid solution was used, aqueous concentrations of 2.72 and 2.90 microg/mL were detected 60 minutes after administration. None of the patients experienced ocular or systemic side effects.

Conclusions: Topical administration of tranexamic acid is effective in yielding therapeutic intraocular concentrations of drug without any ocular or systemic toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Adult
  • Aged
  • Aged, 80 and over
  • Antifibrinolytic Agents / administration & dosage
  • Antifibrinolytic Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Biological Availability
  • Cataract / metabolism
  • Chromatography, High Pressure Liquid
  • Female
  • Humans
  • Hyphema / drug therapy
  • Male
  • Middle Aged
  • Tranexamic Acid / administration & dosage
  • Tranexamic Acid / pharmacokinetics*

Substances

  • Antifibrinolytic Agents
  • Tranexamic Acid