Vitreous concentration of topically applied brimonidine tartrate 0.2%

Ophthalmology. 2001 Apr;108(4):784-7. doi: 10.1016/s0161-6420(00)00654-0.

Abstract

Objective: To determine the vitreous concentration of brimonidine after topical administration of Alphagan.

Design: Prospective observational case series.

Participants: Eighteen patients scheduled for elective pars plana vitrectomy.

Methods: Brimonidine tartrate, 0.2%, was topically administered twice or three times daily for 4 to 14 days preoperatively in 13 patients. Four patients served as controls, without application of brimonidine. A dry, undiluted vitrectomy specimen obtained intraoperatively was collected, frozen, and sent to an independent bioanalytical facility for quantitative determination of vitreous concentration of brimonidine using gas chromatography/mass spectrometry.

Main outcome measures: The concentration of brimonidine in human vitreous.

Results: All patients treated with brimonidine measured above the lower limit of quantitation with a mean vitreous concentration of 185 +/- 500 nM. All patients not treated with brimonidine measured at or below the lower limit of quantitation of 0.05 nM. There was a trend toward higher concentration in patients who were either aphakic or pseudophakic compared with those that were phakic.

Conclusions: Topically applied brimonidine results in vitreous levels at or above 2 nM, the concentration shown to activate alpha(2)-receptors.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Adrenergic alpha-Agonists / administration & dosage
  • Adrenergic alpha-Agonists / pharmacokinetics*
  • Aged
  • Biological Availability
  • Brimonidine Tartrate
  • Female
  • Gas Chromatography-Mass Spectrometry
  • Humans
  • Male
  • Prospective Studies
  • Quinoxalines / administration & dosage
  • Quinoxalines / pharmacokinetics*
  • Tissue Distribution
  • Vitrectomy
  • Vitreous Body / metabolism*

Substances

  • Adrenergic alpha-Agonists
  • Quinoxalines
  • Brimonidine Tartrate