May 2007
Volume 48, Issue 13
Free
ARVO Annual Meeting Abstract  |   May 2007
Toxicity and Pharmacokinetics of Intravitreous Triamcinolone Hexacetonide
Author Affiliations & Notes
  • P. E. Carvounis
    Baylor College of Medicine, Houston, Texas
    Ophthalmology,
  • T. A. Albini
    Ophthalmology, Bascom Palmer Eye Institute, Miami, Florida
  • M. M. Abd-El-Barr
    Baylor College of Medicine, Houston, Texas
    School of Medicine,
  • R. P. A. Manzano
    Ophthalmology, University of Sao Paolo, Sao Paolo, Brazil
  • F. He
    Baylor College of Medicine, Houston, Texas
    Biochemistry,
  • T. G. Wensel
    Baylor College of Medicine, Houston, Texas
    Biochemistry,
  • S. M. Wu
    Baylor College of Medicine, Houston, Texas
    Ophthalmology,
  • E. R. Holz
    Baylor College of Medicine, Houston, Texas
    Ophthalmology,
  • Footnotes
    Commercial Relationships P.E. Carvounis, None; T.A. Albini, None; M.M. Abd-El-Barr, None; R.P.A. Manzano, None; F. He, None; T.G. Wensel, None; S.M. Wu, None; E.R. Holz, None.
  • Footnotes
    Support Supported by NIH EY04446, EY02520, the Retina Research Foundation (Houston), the International Retinal Research Foundation, Inc. and Research to Prevent Blindness.
Investigative Ophthalmology & Visual Science May 2007, Vol.48, 272. doi:
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      P. E. Carvounis, T. A. Albini, M. M. Abd-El-Barr, R. P. A. Manzano, F. He, T. G. Wensel, S. M. Wu, E. R. Holz; Toxicity and Pharmacokinetics of Intravitreous Triamcinolone Hexacetonide. Invest. Ophthalmol. Vis. Sci. 2007;48(13):272.

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

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Abstract

Purpose:: Intra-articular triamcinolone hexacetonide (TH) has been used as longer-acting alternative to intra-articular triamcinolone acetate (TA). We were interested in evaluating whether intravitreous triamcinolone hexacetonide would be a safe and longer-lasting alternative to intravitreous triamcinolone acetonide in the rabbit eye.

Methods:: Three groups of 15 Dutch-belted rabbits each received unilateral injections of study drug and 0.1 ml balanced salt solution in the fellow eye. Group I received TA (Kenalog) 4mg/0.1ml, group II received commercially-available TH (Aristospan) 2mg/0.1 ml and group III received 2mg/0.1 ml purified TH suspended in an especially formulated vehicle (89.18% saline, 10.02% water, 0.75% sodium carboxymethylcellulose and 0.04% polysorbate 80). Electroretinography was used to assess for retina toxicity while high performance liquid chromatography of vitreous isolated from enucleated eyes 2, 4, 8 and 12 weeks after injection was used to calculate drug concentrations and half-life estimates.

Results:: No toxicity was demonstrable on electroretinography in Groups I and III, however in Group II there was a significant reduction in both saturated a-wave amplitude and maximal scotopic b-wave amplitude in the injected eyes at both 2 and 12 weeks following injection (p<0.01). The half-life of intravitreous drug in group I was 17.7 ±1.7 days, in group II 44 ±13 days, and in group III 12.8 ±2.3 days.

Conclusions:: While intravitreous commercially-available TH has a significantly longer half-life relative to intravitreous TA, it results in retina toxicity. Intravitreous TH in the reformulated vehicle did not lead to retina toxicity but had a similar pharmacokinetic profile to TA. Further study will establish whether there are differences in efficacy or adverse effect profile between the two drugs.

Keywords: drug toxicity/drug effects • corticosteroids • injection 
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