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Abstract #15512 Published in IGR 1-3
Alpha-1-adrenoceptor blocking activity of KT-210 Inipradilol ophthalmic solution) on intraocular pressure in the rabbit eye
Nishio K; Kimura T; Orihashi M; Yui MFolia Ophthalmologica Japonica / Nihon Ganka Kiyo 1999; 50: 655-660
The effectiveness of KT-210 (nipradilol ophthalmic solution) compared to bunazosin, timolol and betaxolol in blocking α1-adrenergic receptors was studied in an albino rabbit model of increased intraocular pressure (IOP). IOP measurements were performed at three-minute intervals, dose-dependent increase of IOP found by cumulative instillations of phenylephrine (PHE) (0.001-0.03%) at three-minute intervals, and plotting a dose-response curve; from this curve, the optimal concentration of PHE to evaluate α1-adrenergic blocking activity was determined to be 0.01%. The α1-adrenergic blocking effects of the drug were examined by administering the drug one hour before PHE, and measuring IOP for one hour after application of PHE 0.01%. KT-210 (0.125%, 0.25% and 0.5%) inhibited the increase in IOP in a concentration-dependent manner. Bunazosin (0.001%, 0.003% and 0.01%) also inhibited increased IOP in a concentration-dependent manner, but no effect were found for timolol 0.5% or betaxolol 0.5%. In this model of PHE-induced increased IOP, KT-210 potency was about 1/80 that of bunazosin. These results suggest that instillation of nipradilol produces α1-adrenergic receptor blocking activity.LA: Japanese
Dr. K. Nishio, Teika Pharmaceutical Col Ltd., 3-27, Arakawa 1-chome, Toyama 930-0982; Japan
Classification:
11.3.4 Betablocker (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)
