title: Detection of the free acid of bimatoprost in aqueous humor samples from human eyes treated with bimatoprost before cataract surgery.
abstract: OBJECTIVE
  To determine whether bimatoprost is hydrolyzed to its free acid after topical application in humans in vivo.
  
  
  METHODS
  Prospective, masked, and vehicle controlled.
  
  
  METHODS
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Ophthalmology, University of Nebraska Medical Center, Omaha, Nebraska 68198-5540, USA. cbcamras@unmc.edu
authors.forename: Carl B
authors.initials: CB
authors.lastname: Camras
authors.forename: Carol B
authors.initials: CB
authors.lastname: Toris
authors.forename: Birgitta
authors.initials: B
authors.lastname: Sjoquist
authors.forename: Monica
authors.initials: M
authors.lastname: Milleson
authors.forename: John-Olof
authors.initials: JO
authors.lastname: Thorngren
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Hejkal
authors.forename: Nehal
authors.initials: N
authors.lastname: Patel
authors.forename: Edward M
authors.initials: EM
authors.lastname: Barnett
authors.forename: Regina
authors.initials: R
authors.lastname: Smolyak
authors.forename: S Fareed
authors.initials: SF
authors.lastname: Hasan
authors.forename: Courtney
authors.initials: C
authors.lastname: Hellman
authors.forename: Jane L
authors.initials: JL
authors.lastname: Meza
authors.forename: Martin B
authors.initials: MB
authors.lastname: Wax
authors.forename: Johan
authors.initials: J
authors.lastname: Stjernschantz
mesh_terms: D000287:Administration, Topical; D000577:Amides; D000959:Antihypertensive Agents / Q000008:administration & dosage*; D001082:Aqueous Humor / Q000737:chemistry*; D000069580:Bimatoprost; D002387:Cataract Extraction; D002851:Chromatography, High Pressure Liquid; D003008:Cloprostenol / Q000031:analogs & derivatives; D015237:Dinoprost / Q000031:analogs & derivatives* / Q000032:analysis*; D006801:Humans; D006868:Hydrolysis; D008055:Lipids / Q000008:administration & dosage*; D011355:Prodrugs / Q000008:administration & dosage*; D011446:Prospective Studies; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000577:Amides; D000959:Antihypertensive Agents; D008055:Lipids; D011355:Prodrugs; C013646:17-phenyl-18,19,20-trinorprostaglandin F2 alpha; D003008:Cloprostenol; D015237:Dinoprost; D000069580:Bimatoprost