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April 1992

Dose Response and Duration of Action of Dorzolamide, a Topical Carbonic Anhydrase Inhibitor

Author Affiliations

From Clinical Research, Clinical Pharmacology, and Biostatistics, Merck Sharp & Dohme Research Laboratories, West Point, Pa (Drs Lippa and Eriksson, Ms Deasy, and Mr Holder); Department of Ophthalmology, University of Lund, Sweden (Drs Carlson, Ehinger and Holmin); Department of Ophthalmology, University of Linköping, Sweden (Drs Finnström and Nilsson); Department of Ophthalmology, University of Helsinki, Finland (Drs Nyman, Raitta, and Tarkkanen); and Department of Ophthalmology, Ullevaal Hospital, University of Oslo, Norway (Drs Ringvold, Vegge, and Ytteborg).

Arch Ophthalmol. 1992;110(4):495-499. doi:10.1001/archopht.1992.01080160073033

• The multiple-dose, dose-response relationship and duration of action of the novel topical carbonic anhydrase inhibitor dorzolamide (previously known as MK-507) were investigated in a doublemasked, randomized, placebo-controlled, parallel study in 73 patients with bilateral primary open angle glaucoma or ocular hypertension. Dorzolamide (0.7%, 1.4%, or 2%) or placebo was administered every 12 hours for 5 days and then every 8 hours for 7 days. Intraocular pressure was investigated with multiple 12-hour diurnal curves. All concentrations of dorzolamide demonstrated substantial lowering of intraocular pressure throughout the day when given twice daily (9% to 21%) or three times daily (14% to 24%). Although a dose-dependent response was observed immediately following the first dose, there were no significant differences between concentrations or dose response at either the twice or three times daily dosing regimen. Three times daily administration of 2% dorzolamide demonstrated a mean percent decrease in intraocular pressure of 18% to 22% throughout the day (mean decrease, 4.5 to 6.1 mm Hg). Dorzolamide appears to have substantial potential in the treatment of glaucoma and ocular hypertension.

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