Multiple-dose, dose-response relationship for the topical carbonic anhydrase inhibitor MK-927
E. A. Lippa, H. Aasved, P. J. Airaksinen, A. Alm, T. Bertelsen, B. Calissendorff, O. Dithmer, L. O. Eriksson, L. Gustad, G. Hovding and al. et
Department of Ophthalmology, University of Bergen, Norway.
The multiple-dose, dose-response curve of MK-927 was studied in a
five-center, double-masked, randomized, placebo-controlled, parallel study
of 2%, 1%, and 0.5% MK-927 in 76 patients with bilateral primary open angle
glaucoma or ocular hypertension and intraocular pressure greater than 24 mm
Hg following washout of ocular hypotensive medications. Patients received
doses at 8 AM and 8 PM for 14 days, and parallel 12-hour intraocular
pressure curves were performed prestudy and on day 14, with 4-hour curves
on days 1 and 4. There was a significant dose-response relationship, with
0.5% MK-927 twice daily being a minimal-effect dose. Both 1% and 2% MK-927
were active through 12 hours postdose, and peak mean percent decrease in
pressure at 2 hours postdose was 18.6% and 20.6%, respectively.