Purchase this article with an account.
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.
Download citation file:
© ARVO (1962-2015); The Authors (2016-present)
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 Aqueous humor samples (∼0.1 ml) were withdrawn and analyzed for 17–phenyl trinor PGF2α by an independent lab using HPLC–tandem mass spectrometry.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.
This PDF is available to Subscribers Only