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Brinzolamide

Medically reviewed by Drugs.com. Last updated on May 24, 2020.

Pronunciation

(brin ZOH la mide)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension, Ophthalmic:

Azopt: 1% (10 mL, 15 mL) [contains benzalkonium chloride, edetate disodium]

Brand Names: U.S.

  • Azopt

Pharmacologic Category

  • Carbonic Anhydrase Inhibitor (Ophthalmic)
  • Ophthalmic Agent, Antiglaucoma

Pharmacology

Brinzolamide inhibits carbonic anhydrase, leading to decreased aqueous humor secretion. This results in a reduction of intraocular pressure.

Absorption

Topical: Into systemic circulation

Distribution

Accumulates in red blood cells, binding to carbonic anhydrase (brinzolamide and metabolite)

Metabolism

To N-desethyl brinzolamide

Excretion

Urine (as unchanged drug and metabolites)

Protein Binding

~60%

Use: Labeled Indications

Elevated intraocular pressure: Treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma

Contraindications

Hypersensitivity to brinzolamide or any component of the formulation

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to sulfonamide; severe renal impairment (CrCl <30 mL/minute); hyperchloremic acidosis

Dosing: Adult

Elevated intraocular pressure: Ophthalmic: Instill 1 drop in affected eye(s) 3 times daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

Ophthalmic: Shake well before use. 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. Avoid allowing the tip of the dispensing container to contact the eye or surrounding structures.

Storage

Store at 4°C to 30°C (39°F to 86°F). Shake well before use.

Drug Interactions

Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Monitor therapy

Amantadine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Amantadine. Monitor therapy

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. Avoid combination

Adverse Reactions

1% to 10%:

Cardiovascular: Hyperemia (1% to 5%)

Central nervous system: Foreign body sensation of eye (1% to 5%), headache (1% to 5%)

Dermatologic: Dermatitis (1% to 5%)

Gastrointestinal: Dysgeusia (5% to 10%)

Ophthalmic: Blurred vision (5% to 10%), blepharitis (1% to 5%), eye discharge (1% to 5%), eye discomfort (1% to 5%), eye pain (1% to 5%), eye pruritus (1% to 5%), keratitis (1% to 5%), xerophthalmia (1% to 5%)

Respiratory: Rhinitis (1% to 5%)

<1%, postmarketing, and/or case reports: Alopecia, asthenopia, chest pain, conjunctivitis, corneal disease, crusting of eyelid, diarrhea, diplopia, dizziness, dyspepsia, dyspnea, hypersensitivity reaction, hypertonia, keratoconjunctivitis, lacrimation, nausea, pharyngitis, renal pain, urticaria, xerostomia

Warnings/Precautions

Concerns related to adverse effects:

• Ophthalmic effects: Vision may be temporarily blurred, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

• Sulfonamide (“sulfa”) allergy: The FDA-approved product labeling for many medications containing a sulfonamide chemical group includes a broad contraindication in patients with a prior allergic reaction to sulfonamides. There is a potential for cross-reactivity between members of a specific class (eg, two antibiotic sulfonamides). However, concerns for cross-reactivity have previously extended to all compounds containing the sulfonamide structure (SO2NH2). An expanded understanding of allergic mechanisms indicates cross-reactivity between antibiotic sulfonamides and nonantibiotic sulfonamides may not occur or at the very least this potential is extremely low (Brackett 2004; Johnson 2005; Slatore 2004; Tornero 2004). In particular, mechanisms of cross-reaction due to antibody production (anaphylaxis) are unlikely to occur with nonantibiotic sulfonamides. T-cell-mediated (type IV) reactions (eg, maculopapular rash) are less well understood and it is not possible to completely exclude this potential based on current insights. In cases where prior reactions were severe (Stevens-Johnson syndrome/TEN), some clinicians choose to avoid exposure to these classes.

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 may contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.

Monitoring Parameters

Ophthalmic exams and intraocular pressure

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to lower high eye pressure.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Blurred vision

• Bad taste

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Vision changes

• Eye pain

• Severe eye irritation

• Severe sulfonamide reaction like rash; red, swollen, blistered, or peeling skin; red or irritated eyes; mouth, throat, nose, or eye sores; fever, chills, or sore throat; cough that is new or worse; loss of strength and energy; any bruising or bleeding; or signs of liver problems like dark urine, fatigue, lack of appetite, nausea or abdominal pain, light-colored stools, vomiting, or yellow skin.

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.