Azopt (brinzolamide)

For the treatment of open-angle glaucoma or ocular hypertension in adults, the usual dosage of brinzolamide is 1 drop of a 1% ophthalmic suspension in the affected eye(s) 3 times daily.

If the target intraocular pressure (IOP) is not achieved, alternative or additional ocular hypotensive agents may be required. (See Uses: Ocular Hypertension and Glaucoma.) When brinzolamide is used in fixed combination with brimonidine tartrate, the usual adult dosage is 1 drop of an ophthalmic suspension containing brinzolamide 1% and brimonidine tartrate 0.2% in the affected eye(s) 3 times daily. Because of the potential for additive systemic effects, combined use of topical brinzolamide and an oral carbonic anhydrase inhibitor (e.g., acetazolamide, dichlorphenamide, methazolamide) is not recommended by the manufacturer.

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There is no enhanced messaging for this drug.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

Moderate Interaction: Assess the risk to the patient and take action as needed.

Brinzolamide/Carbonic Anhydrase Inhibitors

SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.

MECHANISM OF ACTION: Brinzolamide and other carbonic anhydrase inhibitors cause a decrease in aqueous humor secretion by slowing the formation of bicarbonate ions with a subsequent reduction of sodium and fluid transport which results in a reduction of intraocular pressure.(1)

CLINICAL EFFECTS: If brinzolamide is given with other carbonic anhydrase inhibitors it may cause electrolyte disturbances, because brinzolamide can be absorbed systemically.(1)

PREDISPOSING FACTORS: Patients with conditions that predispose to acidosis (such as renal disease, severe respiratory disorders, status epilepticus, diarrhea, and being on a ketogenic diet) may be at increased risk of experiencing adverse effects from concurrent carbonic anhydrase inhibitors.

PATIENT MANAGEMENT: It is not recommended to use brinzolamide with systemic carbonic anhydrase inhibitors.

DISCUSSION: Although no human data is available, electrolyte imbalance, development of an acidotic state, and possible nervous system effects may occur following oral administration of brinzolamide and another carbonic anhydrase inhibitor.(1)

Brinzolamide is contraindicated in patient with known hypersensitivity to the drug or any ingredient in the formulation.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

• No disease contraindications

Adverse effects reported in approximately 1-10% of patients receiving brinzolamide include blurred vision, taste abnormality (bitter, sour, or unusual taste), blepharitis, dermatitis, dry eye, foreign body sensation, headache, hyperemia, ocular discharge, ocular discomfort, ocular keratitis, ocular pain, ocular pruritus, and rhinitis.

Less Frequent

• Allergic dermatitis
• Blepharitis
• Erythema
• Headache disorder
• Keratitis
• Ocular discharge
• Ocular pain

Rare or Very Rare

• Alopecia
• Chest pain
• Conjunctivitis
• Diplopia
• Disorder of cornea
• Dizziness
• Dyspnea
• Eyelid edema
• Hypertonia
• Hypotension
• Keratoconjunctivitis
• Ocular inflammation
• Ocular itching
• Pharyngitis
• Renal colic
• Stevens-johnson syndrome
• Toxic epidermal necrolysis
• Urticaria

More Frequent

• Blurred vision
• Dysgeusia

Less Frequent

• Dry eye
• Ocular discomfort
• Rhinitis

Rare or Very Rare

• Arthralgia
• Bronchitis
• Cough
• Depression
• Epistaxis
• Hypoesthesia
• Nausea
• Sinusitis
• Skin inflammation
• Skin rash
• Tinnitus

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Safety and efficacy of topical ophthalmic brinzolamide have not been established in children. A 3-month controlled clinical trial in 32 pediatric patients 4 weeks to 5 years of age failed to demonstrate intraocular pressure (IOP)-lowering efficacy of twice-daily topical administration of brinzolamide 1%. Patients were not required to discontinue their current IOP-lowering therapy until initiation of monotherapy with brinzolamide. The mean decrease in elevated IOP with brinzolamide therapy was 0-2 mm Hg. An increase in corneal diameter of 1 mm was observed in 5 patients.

Following oral administration of radiolabeled brinzolamide in rats, radioactivity crossed the placenta and was detected in fetal circulation and tissues. In studies in rats, no drug-related malformations or effects on organ or tissue development were observed, and reductions in fetal body weight were proportional to reductions in maternal weight gain. In developmental toxicity studies in rabbits, a slight increase in the number of fetal variations (e.g., accessory skull bones) was observed.

There are no adequate and well-controlled studies of brinzolamide to date in pregnant women. Brinzolamide should be used during pregnancy only if potential benefits to the woman justify the potential risk to the fetus.

Brinzolamide is distributed into milk in rats following oral administration. It is not known whether brinzolamide is distributed into human milk following topical application to the eye. A decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

No overall differences in safety and efficacy of topical ophthalmic brinzolamide have been observed between geriatric patients and younger adults.