Faculty Collaboration Database

Detection of the free acid of bimatoprost in aqueous humor samples from human eyes treated with bimatoprost before cataract surgery. Ophthalmology 2004 Dec;111(12):2193-8

Date

12/08/2004

Pubmed ID

15582073

DOI

10.1016/j.ophtha.2004.06.028

Scopus ID

2-s2.0-9644276868 (requires institutional sign-in at Scopus site)   52 Citations

Abstract

PURPOSE: To determine whether bimatoprost is hydrolyzed to its free acid after topical application in humans in vivo.

DESIGN: Prospective, masked, and vehicle controlled.

PARTICIPANTS: Thirty-one eyes of 31 patients with cataracts.

METHODS: 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.

MAIN OUTCOME MEASURE: Detection of the free acid of bimatoprost in aqueous humor.

RESULTS: 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.

CONCLUSION: 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.

Author List

Camras CB, Toris CB, Sjoquist B, Milleson M, Thorngren JO, Hejkal TW, Patel N, Barnett EM, Smolyak R, Hasan SF, Hellman C, Meza JL, Wax MB, Stjernschantz J

Author

Edward M. Barnett MD, PhD Professor in the Ophthalmology and Visual Sciences department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Administration, Topical
Amides
Antihypertensive Agents
Aqueous Humor
Bimatoprost
Cataract Extraction
Chromatography, High Pressure Liquid
Cloprostenol
Dinoprost
Humans
Hydrolysis
Lipids
Prodrugs
Prospective Studies
Spectrometry, Mass, Electrospray Ionization