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Abstract #15857 Published in IGR 2-3
Methazolamide 1% in cyclodextrin solution lowers IOP in human ocular hypertension
Gudmundsdottir E; Stefansson E; Bjarnadottir G; Sigurjonsdottir JF; Gudmundsdottir G; Masson M; Loftsson TInvestigative Ophthalmology and Visual Science 2000; 41: 3552-3554
PURPOSE: To formulate aqueous eye drops containing methazolamide 1% in cyclodextrin solution and to evaluate their effect on intraocular pressure (IOP) in a double-blind randomized trial in humans. Methazolamide, a carbonic anhydrase inhibitor (CAI), has been used in oral doses in the treatment of glaucoma, but hitherto has not been successfully formulated in eye drops. In this study, the effects of methazolamide were compared with those of dorzolamide (Trusopt). METHODS: Methazolamide 1% was formulated in a 2-hydroxypropyl-beta-cyclodextrin with hydroxypropyl methylcellulose in aqueous solution. Eight persons with ocular hypertension were treated with the methazolamide-cyclodextrin eye drops and eight persons with dorzolamide (Trusopt), both groups at doses of three times a day for one week. IOP was measured before treatment was begun and on days 1, 3, and 8 at 9 a.m. (peak) and 3 p.m. (trough). RESULTS: After one week of treatment, the peak IOP in the methazolamide group had decreased from 24.4 ± 2.1 mmHg (mean ± SD) to 21.0 ± 2.0 mmHg, which is a 14% pressure decrease (p = 0.006). In the dorzolamide group, the peak IOP decreased from 23.3 ± 2.1 mmHg to 17.2 ± 3.1 mmHg, which is a 26% pressure decrease (p < 0.001). On average, the IOP declined 3.4 ± 1.8 mmHg after methazolamide administration and 6.1 ± 3.6 mmHg after dorzolamide. CONCLUSIONS: Through cyclodextrin complexation, it is possible to produce topically active methazolamide eye drops that lower IOP. This is the first double-blind clinical trial that demonstrates the efficacy of the classic CAIs in eye drop formulation.
Dr. E. Gudmundsdottir, Departments of Ophthalmology and Pharmacy, University of Iceland, Reykjavik, Iceland
Classification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
