Brinzolamide

Pronunciation

(brin ZOH la mide)

U.S. Brand Names

Azopt®

Generic Available

Canadian Brand Names

Azopt®

Use

Lowers intraocular pressure in patients with ocular hypertension or open-angle glaucoma

Pregnancy Risk Factor

Pregnancy Implications

Developmental toxicities have been observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus.

Lactation

Excretion in breast milk unknown/not recommended

Contraindications

Hypersensitivity to brinzolamide, sulfonamides, or any component of the formulation

Warnings/Precautions

Effects of prolonged use on corneal epithelial cells have not been evaluated; has not been studied in acute angle-closure glaucoma. Use caution with renal impairment (parent and metabolite may accumulate). Systemic absorption may cause serious hypersensitivity reactions to recur. Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). In patients with allergy to one of these compounds, a risk of cross-reaction exists; avoid use when previous reaction has been severe. Safety and efficacy have not been established with hepatic impairment or in pediatric patients.

Adverse Reactions

1% to 10%:

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%), foreign body sensation (1% to 5%), eye discharge (1% to 5%), eye pain (1% to 5%), itching of eye (1% to 5%)

Respiratory: Rhinitis (1% to 5%)

<1%: Allergic reactions alopecia, chest pain, conjunctivitis, diarrhea, diplopia, dizziness, dyspnea, eye fatigue, headache, lid crusting, nausea, pharyngitis, urticaria, xerostomia

Overdosage/Toxicology

Theoretically, overdose could lead to electrolyte imbalance, acidosis and CNS effects; monitor serum electrolytes and blood pH. Treatment is supportive.

Drug Interactions

Substrate of CYP3A4 (minor)

Carbonic anhydrase inhibitors (CAIs): Concurrent use of oral CAIs may lead to additive effects and toxicity; use is not recommended.

Salicylates: High-dose salicylates may result in toxicity from CAIs.

Stability

Store at 4°C to 30°C (39°F to 86°F); shake well before use

Mechanism of Action

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

Pharmacodynamics/Kinetics

Onset of action: Peak effect: 2 hours

Duration: 8-12 hours

Absorption: Topical: Into systemic circulation

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

Metabolism: To N-desmethyl brinzolamide

Excretion: Urine (as unchanged drug and metabolites)

Dosage

Ophthalmic: Adults: Instill 1 drop in affected eye(s) 3 times/day

Administration

May be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic drug is being used, administer drugs at least 10 minutes apart.

Monitoring Parameters

Intraocular pressure

Patient Education

For use in eyes only. Tilt head back, place medication in conjunctival sac, and close eyes. Apply finger pressure at corner of eye for 1 minute following application. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). If using other ophthalmic preparations, administer 10 minutes apart. Avoid excessive use of aspirin or aspirin-containing medications (may cause toxicity). May cause taste changes; runny nose; or vision changes (blurred vision, dry eye, foreign body sensation, eye discharge, temporary sensitivity to bright light, blurring or stinging, altered distance perception, reduced night vision acuity). Report persistent dizziness or headache, skin rash, loss of hair, unresolved GI disturbance, difficulty breathing, or persistent sore throat. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Taste disturbances.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May rarely cause dizziness

Mental Health: Effects on Psychiatric Treatment

None reported

Dosage Forms

Suspension, ophthalmic: 1% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]

International Brand Names

Alcon Azopt® (IL); Azopt® (AR, AT, AU, BE, CA, CH, CL, CO, CZ, DE, DK, EC, ES, FI, FR, GB, HR, HU, IE, IT, NL, NO, PL, PT, RO, SE, SI, TH, TR, YU); Azoptic® (ZA)

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