Azopt (brinzolamide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Brinzolamide is a carbonic anhydrase inhibitor.
Brinzolamide is a carbonic anhydrase inhibitor. Similar to other carbonic anhydrase inhibitors (e.g., acetazolamide, dichlorphenamide, dorzolamide, methazolamide), brinzolamide is a nonbacteriostatic sulfonamide derivative. All these agents contain an unsubstituted sulfamyl group.
Brinzolamide is pharmacologically related to other carbonic anhydrase inhibitors. Although the exact mechanism of action by which carbonic anhydrase inhibitors lower intraocular pressure (IOP) has not been fully elucidated, fluorophotometric studies suggest that reduced aqueous humor formation is the principal effect. Topical brinzolamide can produce mean IOP reductions of about 16-19%.
Brinzolamide is a highly specific inhibitor of carbonic anhydrase II (CA-II), the main carbonic anhydrase isoenzyme involved in aqueous humor secretion. Inhibition of carbonic anhydrase in the ciliary process of the eye decreases the rate of aqueous humor secretion and IOP by slowing bicarbonate formation and reducing sodium and fluid transport.
Some systemic absorption occurs following topical administration of brinzolamide to the eye. Following long-term administration of topical brinzolamide, the drug accumulates in erythrocytes as a result of CA-II binding and exhibits a half-life in whole blood of approximately 111 days. In addition, the N-desethyl metabolite accumulates in erythrocytes as a result of binding to carbonic anhydrase.
However, sufficient CA-II activity remains so that adverse effects resulting from systemic carbonic anhydrase inhibition are not observed. Following topical application to the eye, plasma concentrations of both the parent drug and N-desethyl metabolite generally are below the quantitation limits of the assay. Brinzolamide is eliminated mainly in urine as unchanged drug; the N-desethyl metabolite also is recovered in urine along with lower concentrations of N-desmethoxypropyl and O-desmethyl metabolites.
USES: Brinzolamide is used to treat high pressure inside the eye due to glaucoma (open angle-type) or other eye diseases (such as ocular hypertension). Lowering high pressure inside the eye helps to prevent blindness. This medication works by decreasing the amount of fluid within the eye.
It belongs to a class of drugs known as carbonic anhydrase inhibitors.
Generic name: brinzolamide
Pronunciation: (brin-ZOE-la-mide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Azopt
Indications
The following indications are listed for Azopt:
- Ocular Hypertension
- Open Angle Glaucoma
Also known as: Chronic Glaucoma, Compensated Glaucoma, Glaucoma Simplex, Increased Intraocular Pressure, Increased Iop, Open-Angle Glaucoma, Raised Intraocular Pressure, Simple Glaucoma.
Dosing
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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No dosing information is available for this tab.
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Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
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.
There are no moderate contraindications for this drug.
Adverse reactions
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.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
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.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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