Original ArticlesThe long-term safety and efficacy of brinzolamide 1.0% (Azopt) in patients with primary open-angle glaucoma or ocular hypertension☆
Section snippets
Methods
The study was a multicenter, double-masked, primary therapy trial designed to evaluate the safety and efficacy of brinzolamide 1.0% ophthalmic suspension two and three times daily. Timolol 0.5% (Timoptic, Merck and Company, Inc) ophthalmic solution twice daily was included as a therapeutic reference standard. The primary efficacy parameter was intraocular pressure reduction from baseline. Safety was assessed through the evaluation of adverse events, visual acuity, biomicroscopic examinations,
Results
at 18 investigational sites, 378 patients were randomized to treatment and were included in the safety and intent-to-treat analysis. There were no significant differences between treatment groups with respect to demographics (P > .595; Table 1). The primary efficacy group included 369 patients whose visits were determined to be invaluable for efficacy. One hundred forty-four patients were discontinued from the study after randomization with the most common reasons being the occurrence of an
Discussion
Topical ocular dosing two or three times daily with brinzolamide 1.0% ophthalmic suspension produced clinically relevant and statistically significant intraocular pressure changes from baseline in patients with primary open-angle glaucoma or ocular hypertension. The intraocular pressure reductions were maintained for the 18-month treatment period. The clinical and statistical equivalence of two and three times daily dosing with brinzolamide was demonstrated at all study visits. These findings
Acknowledgements
Statistical consultation was provided by Mark VonTress, PhD, and Russell Andrew, MS, Alcon Laboratories, Inc, Ft Worth, Texas.
THE BRINZOLAMIDE LONG-TERM THERAPY STUDY GROUP INVESTIGATORS
Delmar R. Caldwell, MD, Tulane University, New Orleans, Louisiana; John S. Cohen, MD, Cincinnati Eye Institute, Cincinnati, Ohio; George A. Cioffi, MD, Devers Eye Institute, Portland, Oregon; Miles A. Galin, MD, East Side Ophthalmology, New York, New York; Stephen C. Foster, MD, Boston, Massachusetts; Michael S.
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2017, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Primary sulfonamides constitute the main class of CA inhibitors as zinc binders in which the zinc-binding group is a SO2NH− moiety [7]. Dorzolamide with two chiral centers (4S,6S) marketed by Merck as Trusopt®, and the pure enantiomer brinzolamide (4R) marketed by Alcon as Azopt® have been use clinically as carbonic anhydrase inhibitors for many years more specifically as topically acting antiglaucoma sulfonamides [8–10]. Both of these compounds display a pronounced stereoselectivity with regard to enzyme inhibition and subsequent in vivo efficacy.
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2016, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Brinzolamide is a sulfonamide carbonic anhydrase II inhibitor indicated for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma [1]. Brinzolamide is formulated as an aqueous ophthalmic suspension 1% (w/v), which is well tolerated and does not produce many of the side effects associated with carbonic anhydrase inhibitors when administered systemically [2]. Following topical ocular administration, usually twice daily, brinzolamide is absorbed into the systematic circulation exhibiting an 111-day half- life.
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This research was supported by an unrestricted grant from Research to Prevent Blindness, New York, New York. The study was funded by Alcon Laboratories, Inc, Ft Worth, Texas.