Brinzolamide

Carbonic anhydrase is an enzyme found in many tissues of the body, including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid.

• AZOPT is a carbonic anhydrase inhibitor indicated in the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma. AZOPT is a carbonic anhydrase inhibitor indicated for the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma.ICD-10: H40.059, H40.9

• AZOPT is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product.contraindicated

The recommended dose is one drop of AZOPT in the affected eye(s) 3 times daily. Shake well before use. AZOPT may be used concomitantly with other topical ophthalmic drug products to lower IOP. If more than one topical ophthalmic drug is being used, the drugs should be administered at least 10 minutes apart. • Instill one drop in the affected eye(s) 3 times daily. ( 2 ) • If more than one topical ophthalmic drug is being used, the drugs should be administered at least 10 minutes apart. ( 2 )

• Sulfonamide hypersensitivity reactions. ( 5.1 ) • Corneal edema may occur in patients with low endothelial cell counts. ( 5.2 ) 5.1 Sulfonamide Hypersensitivity Reactions AZOPT 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 AZOPT. Fatalities have occurred, although rarely, due to severe reactions to sulfonamides, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitization may recur when a sulfonamide is readministered irrespective of the route of administration. If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation immediately. 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 AZOPT to this group of patients. 5.3 Severe Renal Impairment AZOPT has not been studied in patients with severe renal impairment [creatinine clearance (CrCl) less than 30 mL/min]. Because AZOPT and its metabolite are excreted predominantly by the kidney, AZOPT is not recommended in such patients.

Most common adverse reactions (incidence 5% to 10%) are blurred vision and bitter, sour, or unusual taste. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sandoz Inc. at 1-800-525-8747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the rates in the clinical trials of another drug and may not reflect the rates observed in practice. In clinical studies of AZOPT, 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. 6.2 Postmarketing Experience The following adverse reactions have been identified during postapproval use of brinzolamide containing products.

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies in pregnant women to inform drug-associated risk. In reproductive toxicity studies, brinzolamide administered orally to rats induced fetal toxicity at 375 times the recommended human ophthalmic dose (RHOD) based on mg/kg. In rabbits, no fetal toxicity was observed following oral administration (see Data) . The background risk of major birth defects and miscarriage for the indicated population is unknown; however, in the U.S. general population, the estimated background risk of major birth defects is 2% to 4%, and of miscarriage is 15% to 20%, of clinically recognized pregnancies. Data Animal Data Embryo-fetal studies were conducted in pregnant rats administered 0, 2, 6, or 18 mg/kg/day brinzolamide by oral gavage on gestation days 6 to 17, to target the period of organogenesis. Decreased fetal body weight with reduced skeletal ossification were observed at 18 mg/kg/day (375 times the RHOD based on mg/kg). The no-observed-adverse-effect-level (NOAEL) for fetal toxicity was 6 mg/kg/day (125 times the RHOD). Decreased maternal weight gain was observed at 18 mg/kg/day. The NOAEL for maternal toxicity was 6 mg/kg/day (125 times the RHOD).

Metabolism

Following topical ocular administration, brinzolamide is absorbed into the systemic circulation. Due to its affinity for carbonic anhydrase II, brinzolamide distributes extensively into the RBCs and exhibits a long half-life in whole blood (approximately 111 days).

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.

• Apr 1, 1998NDANDA020816Sandoz
• Apr 19, 2013NDANDA204251Alcon Labs Inc
• Aug 18, 2021ANDAANDA204884Bausch And Lomb
• Jul 28, 2023ANDAANDA211914Padagis Us

1. 1Treatment Failure1,74414%
2. 2Drug Ineffective8396.8%
3. 3Eye Pain6995.6%
4. 4Dizziness6645.3%
5. 5Dyspnoea6635.3%
6. 6Vision Blurred6625.3%
7. 7Eye Irritation6445.2%
8. 8Fatigue6265.0%
9. 9Ocular Hyperaemia5684.6%
10. 10Headache5444.4%
11. 11Diarrhoea5304.3%
12. 12Fall5104.1%
13. 13Intraocular Pressure Increased4984.0%
14. 14Asthenia4743.8%
15. 15Blindness4513.6%

The 10 most recently updated of 74 ClinicalTrials.gov registrations naming Brinzolamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Retinal Ganglion Cell Neuroprotection Under Prostaglandin Analogues
  Not yet recruiting · Observational · 1,500 enrolled · Association for Innovation and Biomedical Research on Light and Image
  NCT07074782updated 2026-05-06
• Stop Retinal Ganglion Cell Dysfunction Study
  Terminated · Phase 3 · Interventional · 28 enrolled · University of Miami
  NCT02390284updated 2025-08-26
• Efficacy of Simbrinza and Rocklatan vs Cosopt and Latanoprost
  Recruiting · Phase 4 · Interventional · 70 enrolled · Prairie Eye Center
  NCT06883123updated 2025-05-15
• To Compare the Efficacy and Safety of Perrigo's Product to an FDA Approved Product for the Treatment of Glaucoma or Ocular Hypertension in Both Eyes
  Completed · Phase 3 · Interventional · 447 enrolled · Padagis LLC
  NCT04944290updated 2025-04-02
• A Therapeutic Equivalence Study in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension
  Completed · Phase 3 · Interventional · 599 enrolled · Sun Pharmaceutical Industries Limited
  NCT05022004updated 2024-01-18
• Azopt (Brinzolamide 1.0%) Plus Travatan (Travoprost 0.004%) in Treating Patients With Chronic Angle-Closure Glaucoma (CACG)
  Terminated · Phase 4 · Interventional · 37 enrolled · Alcon Research
  NCT00758342updated 2023-12-05
• Therapeutic Equivalence Study of Generic Brinzolamide vs Azopt
  Completed · Phase 1 · Phase 2 · Interventional · 637 enrolled · Bausch & Lomb Incorporated
  NCT03896633updated 2023-05-09
• Therapeutic Equivalence Study of Generic Brinzolamide vs Azopt
  Completed · Phase 3 · Interventional · 258 enrolled · Bausch & Lomb Incorporated
  NCT01722604updated 2023-05-09
• To Compare the Safety and Efficacy of Perrigo's Product to an FDA Approved Product for the Treatment of Glaucoma or Ocular Hypertension in Both Eyes
  Completed · Phase 3 · Interventional · 495 enrolled · Padagis LLC
  NCT04024072updated 2023-03-06
• Augmented Macular Pigment-containing Nutraceutical and Central Visual Function
  Withdrawn · Phase 4 · Interventional · 0 enrolled · University of the Incarnate Word
  NCT04676126updated 2022-10-04

Frequently asked questions

How does Brinzolamide work?

Carbonic anhydrase is an enzyme found in many tissues of the body, including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid.

What is Brinzolamide used for?

According to FDA labeling, Brinzolamide carries indications including: AZOPT is a carbonic anhydrase inhibitor indicated in the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma. AZOPT is a carbonic anhydrase inhibitor indicated for the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Brinzolamide?

Brinzolamide is classified as Carbonic anhydrase inhibitors, Carbonic Anhydrase Inhibitor, Carbonic Anhydrase Inhibitors, Decreased Intraocular Fluid Pressure.

What are the brand names for Brinzolamide?

Brinzolamide is marketed under brand names including Azopt, Simbrinza.

What are the contraindications for Brinzolamide?

Brinzolamide labeling lists contraindications including: AZOPT is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product.. Always consult the full prescribing information and a clinician.