Document Detail

Detection of the free acid of bimatoprost in aqueous humor samples from human eyes treated with bimatoprost before cataract surgery.
MedLine Citation:
PMID:  15582073     Owner:  NLM     Status:  MEDLINE    
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.
Carl B Camras; Carol B Toris; Birgitta Sjoquist; Monica Milleson; John-Olof Thorngren; Thomas W Hejkal; Nehal Patel; Edward M Barnett; Regina Smolyak; S Fareed Hasan; Courtney Hellman; Jane L Meza; Martin B Wax; Johan Stjernschantz
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Publication Detail:
Type:  Clinical Trial; Journal Article; Multicenter Study; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Ophthalmology     Volume:  111     ISSN:  1549-4713     ISO Abbreviation:  Ophthalmology     Publication Date:  2004 Dec 
Date Detail:
Created Date:  2004-12-07     Completed Date:  2004-12-20     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  7802443     Medline TA:  Ophthalmology     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2193-8     Citation Subset:  IM    
Department of Ophthalmology, University of Nebraska Medical Center, Omaha, Nebraska 68198-5540, USA.
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MeSH Terms
Administration, Topical
Antihypertensive Agents / administration & dosage*
Aqueous Humor / chemistry*
Cataract Extraction*
Chromatography, High Pressure Liquid
Cloprostenol / analogs & derivatives
Dinoprost / analogs & derivatives*,  analysis*
Lipids / administration & dosage*
Prodrugs / administration & dosage*
Prospective Studies
Spectrometry, Mass, Electrospray Ionization
Reg. No./Substance:
0/Amides; 0/Antihypertensive Agents; 0/Lipids; 0/Prodrugs; 0/bimatoprost; 38344-08-0/17-phenyl-18,19,20-trinorprostaglandin F2 alpha; 40665-92-7/Cloprostenol; 551-11-1/Dinoprost

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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