Ocular hypotensive effect of 8-hydroxycarteolol, a metabolite of carteolol.
8-hydroxycarteolol hydrochloride (8-OH carteolol) is a main metabolite of carteolol hydrochloride (carteolol). We conducted a randomized double-masked single-drop study in an attempt to compare the effects of the ophthalmic solution of 8-OH carteolol and carteolol on intraocular pressure (IOP) in rabbits with water-load and monkeys. Both 8-OH carteolol (0.01 and 0.1%) and carteolol (1 and 2%) suppressed the water-load induced IOP rise in rabbits. 8-OH carteolol was more effective in suppressing the water-load induced IOP rise in rabbits compared with carteolol on equimolar basis. Both 8-OH carteolol (0.1%) and carteolol (2%) caused a statistically significant decrease in IOP in monkeys. 8-OH carteolol was estimated to be more potent than carteolol in lowering IOP on equimolar basis in monkeys.
Sugiyama
K
K
Department of Ophthalmology, Gifu University School of Medicine, Japan.
Enya
T
T
Kitazawa
Y
Y
D000287:Administration, Topical; D000818:Animals; D002354:Carteolol / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D004311:Double-Blind Method; D007429:Intraocular Pressure / Q000187:drug effects*; D008252:Macaca fascicularis; D015394:Molecular Structure; D011412:Propanolamines / Q000493:pharmacokinetics*; D011817:Rabbits; D011897:Random Allocation; D013997:Time Factors; D014065:Tonometry, Ocular
D011412:Propanolamines; C060345:8-hydroxycarteolol; D002354:Carteolol