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Brinzolamide

CAT#
10-101-134
Synonyms/Alias
AGN-190342; AL-4862; UK-14304; (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide(R)-4-Ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-thieno[3,2-e][1,2]thiazine-6-sulfonic acid amide
CAS No.
138890-62-7
M.W/Mr.
383.51
Molecular Formula
C12H21N3O5S3
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Glaucoma Ocular hypertension
Description
Brinzolamide is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Areas of Interest
Diseases

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Brinzolamide is a highly specific carbonic anhydrase (CA) inhibitor which lowers intraocular pressure (IOP) by reducing the rate of aqueous humour formation. Formulated as a 1% ophthalmic suspension (Azopt) and administered twice or three times daily, brinzolamide is indicated for the topical management of primary open-angle glaucoma (POAG) and ocular hypertension (OH) as either monotherapy or adjunctive therapy with topical beta-blockers.

Brinzolamide is a novel carbonic anhydrase inhibitor that elicits an ocular hypotensive effect when instilled topically. A multicenter, double-masked, placebo-controlled, parallel trial was conducted to evaluate the optimal intraocular pressure (IOP)-lowering concentration and ocular tolerability of topically administered brinzolamide (0.3%, 1%, 2%, and 3%) in patients with primary, open-angle glaucoma or ocular hypertension.

Silver L H, Brinzolamide Dose-Response Study Group. Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt®)[J]. Survey of ophthalmology, 2000, 44: S147-S153.

To assess the effects of brinzolamide and dorzolamide on ocular haemodynamics and retinal oxygen saturation in patients with primary open-angle glaucoma (OAG). This pilot study suggests that brinzolamide and dorzolamide may increase retinal oxygen saturation in patients with OAG.

Siesky B, Harris A, Cantor L B, et al. A comparative study of the effects of brinzolamide and dorzolamide on retinal oxygen saturation and ocular microcirculation in patients with primary open-angle glaucoma[J]. British journal of ophthalmology, 2008, 92(4): 500-504.

Brinzolamide 1.0% produced clinically relevant intraocular pressure reductions in substantial numbers of patients. Brinzolamide's effectiveness equaled that of dorzolamide 2.0% and it produced less ocular discomfort (burning and stinging) on instillation.

Silver L H, Group T B P T S. Clinical efficacy and safety of brinzolamide (AzoptTM), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension[J]. American journal of ophthalmology, 1998, 126(3): 400-408.

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