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Ocular hypertension or open-angle glaucoma: Ophthalmic: Instill 1 drop in affected eye(s) 3 times/day Dosing: Geriatric Refer to adult dosing. Dosing: Renal Impairment Severe renal impairment (Cl cr <30 mL/minute): Use is not recommended (has not been studied; brinzolamide and metabolite are excreted predominately by the kidney). Dosing: Hepatic Impairment No dosage adjustment provided in manufacturer’s labeling. Dosage Forms: U.S. Excipient information presented when available (limited, particularly for generics); consult specific product labeling. Suspension, ophthalmic [drops]: Azopt®: 1% (10 mL, 15 mL) [contains benzalkonium chloride] Generic Equivalent Available: U.S. No Administration Remove contact lenses prior to administration; wait 15 minutes before reinserting. If more than one topical ophthalmic drug is being used, administer drugs at least 10 minutes apart. Shake well before use. Use Treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma Adverse Reactions Significant 1% to 10%: Cardiovascular: Hyperemia (1% to 5%) Central nervous system: Headache (1% to 5%) Dermatologic: Dermatitis (1% to 5%) Gastrointestinal: Taste disturbances (5% to 10%) Ocular: Blurred vision (5% to 10%), blepharitis (1% to 5%), dry eye (1% to 5%), eye discharge (1% to 5%), eye discomfort (1% to 5%), eye pain (1% to 5%), foreign body sensation (1% to 5%), itching of eye (1% to 5%), keratitis (1% to 5%) Respiratory: Rhinitis (1% to 5%) <1% (Limited to important or life-threatening): Allergic reactions, alopecia, chest pain, conjunctivitis, diarrhea, diplopia, dizziness, dyspepsia, dyspnea, eye fatigue, hypertonia, keratoconjunctivitis, keratopathy, kidney pain, lid crusting, nausea, pharyngitis, tearing, urticaria, xerostomia Contraindications Hypersensitivity to brinzolamide or any component of the formulation Warnings/Precautions

Concerns related to adverse effects: • Sulfonamide allergy: Brinzolamide is a sulfonamide; although administered ocularly, systemic absorption may occur and could result in hypersensitivity. Discontinue use if signs of hypersensitivity or a serious reaction occur.

Disease-related concerns: • Acute angle-closure glaucoma: Use has not been studied in acute angle-closure glaucoma. • Corneal endothelium: Use with caution in patients with low endothelial cell counts; may be at increased risk of corneal edema. • Renal impairment: Use is not recommended in patients with severe renal impairment (has not been studied).

Special populations: • Contact lens wearers: Product contains benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting. Metabolism/Transport Effects

Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential Drug Interactions (For additional information: Launch Lexi-Interact™ Drug Interactions Program ) Carbonic Anhydrase Inhibitors: May enhance the adverse/toxic effect of other Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Risk X: Avoid combination CYP3A4 Inhibitors (Strong): May increase the serum concentration of Brinzolamide. Risk C: Monitor therapy Pregnancy Risk Factor C ( show table ) Pregnancy Implications Adverse effects have been observed in animal reproduction studies. Lactation Excretion in breast milk unknown/not recommended Breast-Feeding Considerations According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother. Pricing: U.S. (Medi-Span®)

Suspension (Azopt Ophthalmic) 1% (10 mL): $145.26 Monitoring Parameters Intraocular pressure International Brand Names Azopt (AR, AT, AU, BE, BG, BR, CH, CL, CN, CO, CR, CZ, DE, DK, EE, ES, FI, FR, GB, GR, GT, HK, HN, ID, IE, IL, IT, KP, MT, MX, MY, NI, NL, NO, NZ, PA, PE, PH, PL, PT, PY, RU, SE, SG, SK, SV, TH, TR, TW, UY, VE); Azoptic (ZA); BrinzoQuin (AU) Mechanism of Action Brinzolamide inhibits carbonic anhydrase, leading to decreased aqueous humor secretion. This results in a reduction of intraocular pressure. Pharmacodynamics/Kinetics Absorption: Topical: Into systemic circulation Distribution: Accumulates extensively in red blood cells, binding to carbonic anhydrase (brinzolamide and metabolite) Protein binding: ~60% Metabolism: To N-desethyl brinzolamide Excretion: Urine (as unchanged drug and metabolites) Use of UpToDate is subject to the Subscription and License Agreement . Topic 8658 Version 38.0 © 2013 UpToDate, Inc. All rights reserved. | Subscription and License Agreement | Release: 21.6- C21.56 Licensed to: AsanBook Dig. Med. Lib. | Support Tag: [0503-61.234.146.186-C88E1676B6-S244013.14]