July 2018
Volume 59, Issue 9
Open Access
ARVO Annual Meeting Abstract  |   July 2018
Plasma Pharmacokinetics and Safety following Topical Administration of Brimonidine Tartrate Ophthalmic Solution 0.025% in Healthy Adults
Author Affiliations & Notes
  • Lester O Hosten
    Clinical and Medical Affairs, Bausch + Lomb, Bridgewater, New Jersey, United States
  • Jason L Vittitow
    Clinical Affairs, Bausch + Lomb, Bridgewater, New Jersey, United States
  • Footnotes
    Commercial Relationships   Lester Hosten, Bausch & Lomb, Inc. (E); Jason Vittitow, Bausch & Lomb, Inc. (E)
  • Footnotes
    Support  None
Investigative Ophthalmology & Visual Science July 2018, Vol.59, 140. doi:https://doi.org/
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      Lester O Hosten, Jason L Vittitow; Plasma Pharmacokinetics and Safety following Topical Administration of Brimonidine Tartrate Ophthalmic Solution 0.025% in Healthy Adults. Invest. Ophthalmol. Vis. Sci. 2018;59(9):140. doi: https://doi.org/.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose : The objective of this study was to characterize the plasma pharmacokinetics (PK) and safety profile of brimonidine following a single dose and 5-day QID dosing of brimonidine tartrate ophthalmic solution 0.025% in healthy adult subjects.

Methods : This was an open-label, single-center study. One drop of brimonidine 0.025% was administered bilaterally in eligible subjects (≥18 years), with plasma collections post-instillation at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, and 24 hours. Identically timed blood draws were performed following QID dosing for 5 days. Brimonidine plasma concentrations were determined by liquid chromatography-tandem mass spectrometry. Safety parameters included adverse events (AEs), comprehensive ophthalmic exams, physical exams, vital signs, and clinical laboratory evaluations.

Results : A total of 14 subjects (ages 19-46; mean 27.3) were enrolled; the majority of subjects were female (64.3%). Plasma concentrations of brimonidine were below the lower limit of quantitation (LLOQ=0.025 ng/mL) at all time points in 13/14 subjects. Only 1 subject had a detectable level (0.0253 ng/mL) at 1 time point (1 hour after a single dose). Seven subjects reported 8 non-serious AEs: 2 ocular AEs of transient mild hyperemia considered related to treatment in 2 subjects, and 6 non-ocular AEs of mild/moderate severity in 5 subjects, only one of which (headache) was deemed related to treatment. One subject was discontinued due to a non-ocular AE unrelated to study medication (bilateral antecubital bruising); all other safety exam findings were within normal range.

Conclusions : These data indicate that topical ophthalmic administration of brimonidine 0.025% results in negligible systemic exposure during and after 5 days of bilateral QID dosing. Consistent with previous studies, there were no safety concerns identified suggesting that brimonidine tartrate ophthalmic solution 0.025% is well-tolerated.

This is an abstract that was submitted for the 2018 ARVO Annual Meeting, held in Honolulu, Hawaii, April 29 - May 3, 2018.

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