May 2004
Volume 45, Issue 13
Free
ARVO Annual Meeting Abstract  |   May 2004
Determination of Bimatoprost Hydrolysis in the Aqueous Humor of Cataract Patients
Author Affiliations & Notes
  • L.B. Cantor
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • J. Hoop
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • D. WuDunn
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • C.–W. Yung
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • Y. Catoira
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • S. Valluri
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • A. Cortes
    Department of Ophthalmology, Indiana University Medical Ctr, Indianapolis, IN
  • A. Acheampong
    Research & Development, Allergan, Inc., Irvine, CA
  • A.H. Krauss
    Research & Development, Allergan, Inc., Irvine, CA
  • D.F. Woodward
    Research & Development, Allergan, Inc., Irvine, CA
  • Footnotes
    Commercial Relationships  L.B. Cantor, Pharmacia/Pfizer F; Alcon F; Allergan, Inc. F, R; J. Hoop, None; D. WuDunn, Allergan, Inc. C, R; Pfizer/Pharmacia C, R; C. Yung, None; Y. Catoira, None; S. Valluri, None; A. Cortes, None; A. Acheampong, Allergan, Inc. E; A.H. Krauss, Allergan, Inc. E; D.F. Woodward, Allergan, Inc. E.
  • Footnotes
    Support  none
Investigative Ophthalmology & Visual Science May 2004, Vol.45, 3956. doi:
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      L.B. Cantor, J. Hoop, D. WuDunn, C.–W. Yung, Y. Catoira, S. Valluri, A. Cortes, A. Acheampong, A.H. Krauss, D.F. Woodward; Determination of Bimatoprost Hydrolysis in the Aqueous Humor of Cataract Patients . Invest. Ophthalmol. Vis. Sci. 2004;45(13):3956.

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

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Abstract

Abstract: : Purpose: Hydrolysis of bimatoprost appears to be very slow in human ocular tissues in vitro. In the living primate eye, levels of an acid hydrolysis product of bimatoprost have been found to be negligible or absent after topical treatment. This study was designed to determine the aqueous humor concentrations of 17–phenyl trinor PGF2α (bimatoprost acid) in humans. Methods: 40 patients scheduled for routine cataract surgery were topically treated with a single 30 microliter drop of bimatoprost (LUMIGAN®) or placebo (in a 4:1 ratio) 1, 3, 6, or 12 hours prior to their scheduled surgical procedure in this randomized, controlled, double masked, prospective study. Aqueous humor samples (∼0.1 ml) were withdrawn and analyzed for 17–phenyl trinor PGF2α by an independent lab using HPLC–tandem mass spectrometry. Results: 17–phenyl trinor PGF2α was detected at concentrations of 5.1, 6.7 and 1.9 nM in 1, 3 and 6–hour samples, respectively. No acid metabolite was quantifiable in any of the 12–hour samples. Conclusions: Levels of the acid hydrolysis product 17–phenyl trinor PGF2α were low or absent in aqueous humor samples of cataract patients. Similarly, levels of 17–phenyl trinor PGF2α had previously been reported as low or absent in the aqueous humor of the living primate eye (Woodward et al, J Pharmacol Exp Ther 2003;305:772). In contrast, latanoprost acid concentrations are substantially higher in the aqueous humor of cataract patients after a single topical dose of latanoprost (Xalatan®) averaging approximately 100 nM at peak (Sjöquist and Stjernschantz, Surv Ophthalmol 2002;47(Suppl 1):S6). The results from this study further support that bimatoprost hydrolysis does not account for the ocular hypotensive efficacy of bimatoprost.

Keywords: aqueous • pharmacology • metabolism 
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