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]
Pharmacology
Mechanism of Action
Brinzolamide inhibits carbonic anhydrase, leading to decreased aqueous humor secretion. This results in a reduction of intraocular pressure.
Pharmacokinetics/Pharmacodynamics
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
Dosage and Administration
Dosing: Adult
Elevated intraocular pressure: Ophthalmic: Instill 1 drop in affected eye(s) 3 times daily
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
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Brinzolamide. Monitor therapy
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).
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed.
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
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.
Frequently reported side effects of this drug
- Blurred vision
- Bad taste
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- 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 a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of 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 brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
