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Brinzolamide

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)

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:

US labeling: Instill 1 drop in affected eye(s) 3 times daily

Canadian labeling: Initial: Instill 1 drop in affected eye(s) twice daily; if clinical response is not adequate after 4 weeks, may increase dose to 1 drop in affected eye(s) 3 times daily.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

US labeling:

CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling.

CrCl <30 mL/minute: Use is not recommended (has not been studied; brinzolamide and metabolite are excreted predominately by the kidney).

Canadian labeling:

CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied); use with caution.

CrCl <30 mL/minute: Use is contraindicated.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

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

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% (Limited to important or life-threatening): 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.

• Hepatic impairment: Use with caution in patients with hepatic impairment (Canadian labeling).

• Renal impairment: Use is not recommended (US labeling) or contraindicated (Canadian labeling) in patients with severe renal impairment (has not been studied). Due to the potential risk of metabolic acidosis, use with caution in patients with mild to moderate renal impairment (Canadian labeling).

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 Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. The Canadian labeling recommends avoiding use during pregnancy.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience blurred vision or bad taste. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, or signs of a severe sulfonamide reaction (rash; red, swollen, blistered, or peeling skin; red or irritated eyes; sores in your mouth, throat, nose, or eyes; 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, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, 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. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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