Brinzolamide

BRINZOLAMIDE- brinzolamide suspension/ drops
Actavis Pharma, Inc.

1 INDICATIONS AND USAGE

Brinzolamide ophthalmic suspension 1% is a carbonic anhydrase inhibitor indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

2 DOSAGE AND ADMINISTRATION

The recommended dose is one drop of brinzolamide ophthalmic suspension 1% in the affected eye(s) three times daily. Brinzolamide ophthalmic suspension 1% may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic drug is used, the drugs should be administered at least ten (10) minutes apart.

3 DOSAGE FORMS AND STRENGTHS

Solution containing 10 mg/mL brinzolamide, USP.

4 CONTRAINDICATIONS

Brinzolamide ophthalmic suspension 1% is contraindicated in patients who are hypersensitive to any component of this product.

5 WARNINGS AND PRECAUTIONS

5.1 Sulfonamide Hypersensitivity Reactions

Brinzolamide ophthalmic suspension 1% is a sulfonamide and although administered topically it is absorbed systemically. Therefore, the same types of adverse reactions that are attributable to sulfonamides may occur with topical administration of brinzolamide ophthalmic suspension 1%. Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitization may recur when a sulfonamide is re-administered irrespective of the route of administration. If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation.

5.2 Corneal Endothelium

Carbonic anhydrase activity has been observed in both the cytoplasm and around the plasma membranes of the corneal endothelium. There is an increased potential for developing corneal edema in patients with low endothelial cell counts. Caution should be used when prescribing brinzolamide ophthalmic suspension 1% to this group of patients.

5.3 Severe Renal Impairment

Brinzolamide ophthalmic suspension 1% has not been studied in patients with severe renal impairment (CrCl less than 30 mL/min). Because brinzolamide ophthalmic suspension 1% and its metabolite are excreted predominantly by the kidney, brinzolamide ophthalmic suspension 1% is not recommended in such patients.

5.4 Acute Angle-Closure Glaucoma

The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents. Brinzolamide ophthalmic suspension 1% has not been studied in patients with acute angle-closure glaucoma.

5.5 Contact Lens Wear

The preservative in brinzolamide ophthalmic suspension 1%, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of brinzolamide ophthalmic suspension 1%, but may be reinserted 15 minutes after instillation.

6 ADVERSE REACTIONS

6.1 Clinical Studies Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to the rates in the clinical studies of another drug and may not reflect the rates observed in practice.

In clinical studies of brinzolamide ophthalmic suspension 1%, the most frequently reported adverse reactions reported in 5 to 10% of patients were blurred vision and bitter, sour or unusual taste. Adverse reactions occurring in 1 to 5% of patients were blepharitis, dermatitis, dry eye, foreign body sensation, headache, hyperemia, ocular discharge, ocular discomfort, ocular keratitis, ocular pain, ocular pruritus and rhinitis.

The following adverse reactions were reported at an incidence below 1%: allergic reactions, alopecia, chest pain, conjunctivitis, diarrhea, diplopia, dizziness, dry mouth, dyspnea, dyspepsia, eye fatigue, hypertonia, keratoconjunctivitis, keratopathy, kidney pain, lid margin crusting or sticky sensation, nausea, pharyngitis, tearing and urticaria.

7 DRUG INTERACTIONS

7.1 Oral Carbonic Anhydrase Inhibitors

There is a potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and brinzolamide ophthalmic suspension 1%. The concomitant administration of brinzolamide ophthalmic suspension 1% and oral carbonic anhydrase inhibitors is not recommended.

7.2 High-Dose Salicylate Therapy

Carbonic anhydrase inhibitors may produce acid-base and electrolyte alterations. These alterations were not reported in the clinical trials with brinzolamide. However, in patients treated with oral carbonic anhydrase inhibitors, rare instances of acid-base alterations have occurred with high-dose salicylate therapy. Therefore, the potential for such drug interactions should be considered in patients receiving brinzolamide ophthalmic suspension 1%.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Category C: Developmental toxicity studies with brinzolamide in rabbits at oral doses of 1, 3, and 6 mg/kg/day (20, 62, and 125 times the recommended human ophthalmic dose) produced maternal toxicity at 6 mg/kg/day and a significant increase in the number of fetal variations, such as accessory skull bones, which was only slightly higher than the historic value at 1 and 6 mg/kg. In rats, statistically decreased body weights of fetuses from dams receiving oral doses of 18 mg/kg/day (375 times the recommended human ophthalmic dose) during gestation were proportional to the reduced maternal weight gain, with no statistically significant effects on organ or tissue development. Increases in unossified sternebrae, reduced ossification of the skull, and unossified hyoid that occurred at 6 and 18 mg/kg were not statistically significant. No treatment-related malformations were seen. Following oral administration of 14 C-brinzolamide to pregnant rats, radioactivity was found to cross the placenta and was present in the fetal tissues and blood.

There are no adequate and well-controlled studies in pregnant women. Brinzolamide ophthalmic suspension 1% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

8.3 Nursing Mothers

In a study of brinzolamide in lactating rats, decreases in body weight gain in offspring at an oral dose of 15 mg/kg/day (312 times the recommended human ophthalmic dose) were seen during lactation. No other effects were observed. However, following oral administration of 14 C-brinzolamide to lactating rats, radioactivity was found in milk at concentrations below those in the blood and plasma.

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from brinzolamide ophthalmic suspension 1%, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

8.4 Pediatric Use

A three-month controlled clinical study was conducted in which brinzolamide ophthalmic suspension 1% was dosed only twice a day in pediatric patients 4 weeks to 5 years of age. Patients were not required to discontinue their IOP-lowering medication(s) until initiation of monotherapy with brinzolamide ophthalmic suspension 1%. IOP-lowering efficacy was not demonstrated in this study in which the mean decrease in elevated IOP was between 0 and 2 mmHg. Five out of 32 patients demonstrated an increase in corneal diameter of one millimeter.

8.5 Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

10 OVERDOSAGE

Although no human data are available, electrolyte imbalance, development of an acidotic state, and possible nervous system effects may occur following oral administration of an overdose. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored.

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