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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

Treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma

Contraindications

Hypersensitivity to brinzolamide or any component of the formulation

Dosing: Adult

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 (CrCl <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.

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.

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:

• 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:

• Oral carbonic anhydrase inhibitors: Concurrent use with oral carbonic anhydrase inhibitors may result in additive systemic effects and is not recommended.

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.

Monitoring Parameters

Intraocular pressure

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse effects have been observed in animal reproduction studies.

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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