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Abstract #8509 Published in IGR 5-1
Preclinical and clinical studies on brinzolamide, the newest topical carbonic anhydrase inhibitor
Yan X; Guangren PChinese Ophthalmic Research 2002; 20: 560-564
Brinzolamide, the newest topical carbonic anhydrase inhibitor, exhibits selectivity, high affinity, and potent inhibitory activity for the carbonic anhydrase type isozyme II and efficacy for lowering intraocular pressure (IOP). It is readily absorbed into the eye and has a relatively long half-life (days) in the iris-ciliary body, choroid, retina, lens, and blood. Whereas whole-blood concentrations of brinzolamide are present after topical ocular administration, plasma level of parent drug and metabolites are very low, and complete saturation of carbonic anhydrase in erythrocytes is not achieved at steady state. Thus, systemic acidosis or the other side-effects associated with oral carbonic anhydrase inhibitors are not expected to occur. Brinzolamide significantly increase optic nerve head blood flow in rabbits with minimal disturbance to systemic acid/base balance. If a possible enhancement of optic nerve head flow is proved in human, it will be a valuable benefit for the patients with glaucomatous optic neuropathy. The optimal IOP-lowering concentration of brinzolamide is 1%. When administered bid, brinzolamide 1% produce a clinically significant reduction in IOP. 1% ophthalmic suspension is well tolerated, and its ocular tolerability represents a clinically significant improvement over the topical carbonic anhydrase inhibitor dorzolamide. The most frequently reported adverse events were blurred vision (6%) and bitter, sour, or unusual taste perception (6%). In conclusion, brinzolamide 1% ophthalmic suspension can safely and effectively lower IOP in patients with open-angle glaucoma or ocular hypertension and is more comfortable when instilled in the eye. It is a valuable new anti-glaucoma medication.LA: Chinese
Dr. X. Yan, Henan Institute of Ophthalmology, Zhengzhou 450003, China
Classification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
