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Abstract #8084 Published in IGR 4-3
Pharmacokinetic and pharmacodynamic differences between ocular and nasal instillation of carteolol on intraocular pressure and heart rate in Japanese men with high CYP2D6 activity
Ishii Y; Nakamura K; Matsuki S; Uemura N; Muraguchi R; Nakagawa M; Nakano S; Nakatsuka KJournal of Clinical Pharmacology 2002; 42: 1020-1026
The sublingual administration of carteolol or THE instillation into one eye reduces intraocular pressure (IOP) in both eyes. This suggests that carteolol absorbed systemically can reduce IOP, and that the extra-ophthalmic route (e.g., the nasal route) can be an alternative method of drug administration. The authors compared the differences between ocular and nasal instillation relating to the pharmacokinetic and pharmacodynamic effects of a carteolol-ophthalmic solution on IOP and heart rate (HR) in a randomized, double-blind, crossover, placebo-controlled design in 11 healthy young extensive metabolizers for CYP2D6. The tmax, Cmax, and AUCo-t of carteolol (0.8 mg) instilled into the nostril were significantly higher than those into the eye (p < 0.05): tmax (h) = 0.25 (0.17-5.0), 1.0 (0.17-5.0) (median value with range in the parenthesis, ocular versus nasal); Cmax (ng/ml) = 1.33 ± 1.57, 2.29 ± 2.09; and AUCo-t (ng·h/ml) = 9.36 ± 2.04, 21.13 ± 1.58 (geometric mean ± SD, ocular versus nasal). The reduction of IOP after ocular instillation persisted significantly longer than that of nasal instillation (p < 0.05). HR was significantly reduced after both ocular and nasal instillation (p < 0.05), although there were no significant differences between them. In conclusion, ocular instillation of a carteolol-ophthalmic solution has advantages over nasal instillation in controlling IOP and the potential to decrease adverse reactions due to lower plasma concentrations.
Y. Ishii, MD, Department of Ophthalmology, Oita Medical University, Hasama-machi, Oita 879-5593, Japan
Classification:
11.3.4 Betablocker (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)
