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Abstract #11965 Published in IGR 7-1
Fadolmidine-induced ocular hypotension in normotensive rabbits
Savolainen J; Niemi R; Mantyla A; Huuskonen J; Jarvinen TJournal of Pharmacy and Pharmacology 2005; 57: 191-195
Fadolmidine, a novel selective α2 -adrenoceptor agonist, was evaluated for its efficacy to lower intraocular pressure in normotensive rabbits (n = 5-6). The dose-response profile between 0.004 μg and 12.5 μg of fadolmidine was determined. The effect of pH on the partition of fadolmidine was studied in order to select an optimal pH for topical fadolmidine administration. After topical administration, fadolmidine significantly lowered the intraocular pressure in normotensive rabbits. The onset of action was immediate, with no initial increase in intraocular pressure. A significant decrease in intraocular pressure was already observed at 1 h after dosing. The maximum decrease in intraocular pressure was observed after a 2.5 μg dose of fadolmidine in both eyes at 2 h after dosing. The mean maximum decrease in the treated and untreated eye was 6.4 mmHg and 3.9 mmHg, respectively. In conclusion, fadolmidine is a potent intraocular pressure lowering agent. In addition, fadolmidine does not cause a significant initial increase in intraocular pressure. Because of the strong dependence of the distribution coefficient on pH, the pH of the administered solution is important, with physiological pH being optimal in this respect.
Dr. J. Savolainen, Dept. of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FIN 70211, Kuopio, Finland
Classification:
5 Experimental glaucoma; animal models
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
