TY - JOUR
T1 - Detection of the free acid of bimatoprost in aqueous humor samples from human eyes treated with bimatoprost before cataract surgery
AU - Camras, Carl B.
AU - Toris, Carol B.
AU - Sjoquist, Birgitta
AU - Milleson, Monica
AU - Thorngren, John Olof
AU - Hejkal, Thomas W.
AU - Patel, Nehal
AU - Barnett, Edward M.
AU - Smolyak, Regina
AU - Hasan, S. Fareed
AU - Hellman, Courtney
AU - Meza, Jane L.
AU - Wax, Martin B.
AU - Stjernschantz, Johan
N1 - Funding Information:
Supported in part by Pfizer Ophthalmics, New York, New York, and an unrestricted grant from Research to Prevent Blindness, Inc., New York, New York. Dr Camras was a Research to Prevent Blindness Senior Scientific Investigator and a consultant to the Pharmacia Corporation. Dr Barnett was supported by a Research to Prevent Blindness Career Development Award and is a consultant/speaker for Pharmacia/Pfizer. Dr Wax was an employee of Pfizer, and now is an employee of Alcon.
PY - 2004/12
Y1 - 2004/12
N2 - To determine whether bimatoprost is hydrolyzed to its free acid after topical application in humans in vivo. Prospective, masked, and vehicle controlled. Thirty-one eyes of 31 patients with cataracts. Beginning 7 days before scheduled cataract surgery, one eye of each patient was treated with bimatoprost 0.03% or vehicle once daily, with the last drop administered 2 to 12 hours before anterior chamber paracentesis before cataract surgery. In a masked fashion, aqueous humor specimens were assayed for bimatoprost and its free acid by high-pressure liquid chromatography and mass spectrometry. Detection of the free acid of bimatoprost in aqueous humor. Aqueous humor concentrations of the free acid of bimatoprost were 22.0±7.0 nmol/l (mean ± standard error of the mean, n = 12) and 7.0±4.6 nmol/l (n = 8) at 2 and 12 hours, respectively, and below the limit of detection after vehicle (n = 10). Concentrations of bimatoprost (amide) were 5.7±1.4 and 1.1±0.4 nmol/l at 2 and 12 hours, respectively, and undetectable after vehicle. After topical application of bimatoprost in humans, a sufficient concentration of its free acid, a potent FPprostanoid receptor agonist, is found in the aqueous humor to account for its ability to reduce intraocular pressure.
AB - To determine whether bimatoprost is hydrolyzed to its free acid after topical application in humans in vivo. Prospective, masked, and vehicle controlled. Thirty-one eyes of 31 patients with cataracts. Beginning 7 days before scheduled cataract surgery, one eye of each patient was treated with bimatoprost 0.03% or vehicle once daily, with the last drop administered 2 to 12 hours before anterior chamber paracentesis before cataract surgery. In a masked fashion, aqueous humor specimens were assayed for bimatoprost and its free acid by high-pressure liquid chromatography and mass spectrometry. Detection of the free acid of bimatoprost in aqueous humor. Aqueous humor concentrations of the free acid of bimatoprost were 22.0±7.0 nmol/l (mean ± standard error of the mean, n = 12) and 7.0±4.6 nmol/l (n = 8) at 2 and 12 hours, respectively, and below the limit of detection after vehicle (n = 10). Concentrations of bimatoprost (amide) were 5.7±1.4 and 1.1±0.4 nmol/l at 2 and 12 hours, respectively, and undetectable after vehicle. After topical application of bimatoprost in humans, a sufficient concentration of its free acid, a potent FPprostanoid receptor agonist, is found in the aqueous humor to account for its ability to reduce intraocular pressure.
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U2 - 10.1016/j.ophtha.2004.06.028
DO - 10.1016/j.ophtha.2004.06.028
M3 - Article
C2 - 15582073
AN - SCOPUS:9644276868
SN - 0161-6420
VL - 111
SP - 2193
EP - 2198
JO - Ophthalmology
JF - Ophthalmology
IS - 12
ER -