BRINZOLAMIDE

Following topical ocular administration, brinzolamide is absorbed into the systemic circulation. Due to its affinity for carbonic anhydrase II, brinzolamide distributes extensively into the RBCs and exhibits a long half-life in whole blood (approximately 111 days). In humans, the metabolite N-desethyl brinzolamide is formed, which also binds to carbonic anhydrase and accumulates in RBCs. This metabolite binds mainly to carbonic anhydrase I in the presence of brinzolamide. In plasma, both parent ...

In two, 3-month clinical studies, brinzolamide ophthalmic suspension dosed 3 times per day in patients with elevated IOP, produced significant reductions in IOPs (4 mmHg to 5 mmHg). These IOP reductions are equivalent to the reductions observed with TRUSOPT* (dorzolamide hydrochloride ophthalmic solution) 2% dosed 3 times per day in the same studies. In 2 clinical studies in patients with elevated IOP, brinzolamide ophthalmic suspension was associated with less stinging and burning upon instillation than TRUSOPT* 2%.

Most common adverse reactions (incidence 5% to 10%) are blurred vision and bitter, sour, or unusual taste. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the rates in the clinical trials of another d...

Brinzolamide ophthalmic suspension is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product. ( 4 )

Sulfonamide hypersensitivity reactions. ( 5.1 ) Corneal edema may occur in patients with low endothelial cell counts. ( 5.2 ) 5.1 Sulfonamide Hypersensitivity Reactions Brinzolamide ophthalmic suspension is a sulfonamide and although administered topically, it is absorbed systemically. Therefore, the same types of adverse reactions that are attributable to sulfonamides may occur with topical administration of brinzolamide ophthalmic suspension. Fatalities have occurred, although rarely, due to s...

7 DRUG INTERACTIONS There is a potential additive effect of the known systemic effects of carbonic anhydrase inhibition in patients receiving both oral and topical carbonic anhydrase inhibitors. ( 7.1 ) Rare instances of acid-base alterations have occurred with high-dose salicylate therapy. ( 7.2 ) 7.1 Oral Carbonic Anhydrase Inhibitors There is a potential for an additive effect on the known syst...