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Y. Ishii, K. Nakamura, Y. Inoue, K. Nakatsuka, T. Maeda, A. Kozaki, T. Furuya; Comparison of the effects of 2% carteolol and 0.5% timolol on pharmacokinetics with oral quinidine, a selective inhibitor of CYP 2D6 . Invest. Ophthalmol. Vis. Sci. 2004;45(13):2095.
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Purpose and Methods: Systemic adverse reactions of timolol ophthalmic solution given at usual therapeutic doses have been well documented. To evaluate the drug interaction between 0.5% timolol or 2% carteolol ophthalmic solution and the treatment of quinidine, a specific inhibitor of CYP2D6, 6 healthy Japanese male volunteers aged 21 to 28 years received 0.5% timolol or 2% carteolol ophthalmic solution with and without oral quinidine (50mg) in a randomized, Latin–square design. Results: Quinidine significantly increased the area under the plasma concentration–time curve from zero time to infinity of timolol after single instillation, P=0.0197. On the contrary, there were no significant pharmacokinetic changes after carteolol instillation under the treatment of quinidine, P>0.05. Conclusions: Quinidine did not affect the pharmacokinetics of carteolol ophthalmic solution but that of timolol ophthalmic soilution. Drug interaction related with CYP2D6 would happen in 0.5% timolol ophthalmic solution more often than 2% carteolol ophthalmic solution.
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