Brinzolamide

Class: Carbonic Anhydrase Inhibitors
Chemical Name: (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
Molecular Formula: C₁₂H₂₁N₃O₅S₃
CAS Number: 138890-62-7
Brands: Azopt

Medically reviewed by Drugs.com on Dec 21, 2020. Written by ASHP.

Introduction

Carbonic anhydrase inhibitor; nonbacteriostatic sulfonamide derivative.

Uses for Brinzolamide

Ocular Hypertension and Glaucoma

Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.

Brinzolamide 1%: Efficacy when administered 3 times daily comparable to that of dorzolamide 2% administered 3 times daily in reducing IOP, but brinzolamide appeared to cause less ocular stinging and burning; reduction in IOP was approximately 4–5 mm Hg in clinical studies. When administered 2 or 3 times daily, less effective than timolol 0.5% administered twice daily.

Fixed-combination brinzolamide 1% and brimonidine tartrate 0.2%: IOP-lowering effect of the fixed combination administered 3 times daily was 1–3 mm Hg greater than that of either drug administered at the same dosage as monotherapy.

Safety and efficacy not established for the treatment of acute angle-closure glaucoma.

When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost). With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.

A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma. Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal. Adjust target IOP up or down as needed over course of disease.

Combination therapy with drugs from different therapeutic classes often required to control IOP.

Brinzolamide Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the affected eye(s) as an ophthalmic suspension containing brinzolamide alone or in fixed combination with brimonidine.

Shake suspension well prior to use.

Avoi...