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Elínborg Guđmundsdóttir, Einar Stefánsson, Gyđa Bjarnadóttir, Jóhanna F. Sigurjónsdóttir, Guđrún Guđmundsdóttir, Mar Masson, Thorsteinn Loftsson; Methazolamide 1% in Cyclodextrin Solution Lowers IOP in Human Ocular Hypertension. Invest. Ophthalmol. Vis. Sci. 2000;41(11):3552-3554.
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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 are compared with those of dorzolamide (Trusopt).
methods. Methazolamide 1% was formulated in a 2-hydroxypropyl-β-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 dosages of three times a day for 1 week. IOP
was measured before treatment was begun and on days 1, 3, and 8 at 9 AM
(peak) and 3 PM (trough).
results. After 1 week of treatment, the peak IOP in the methazolamide group had
decreased from 24.4 ± 2.1 mm Hg (mean ± SD) to 21.0 ±
2.0 mm Hg, which is a 14% pressure decrease (P =
0.006). In the dorzolamide group, the peak IOP decreased from 23.3 ± 2.1 mm Hg to 17.2 ± 3.1 mm Hg, which is a 26% pressure
decrease (P < 0.001). On average, the IOP declined
3.4 ± 1.8 mm Hg after methazolamide administration and 6.1 ± 3.6 mm Hg 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.
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