Brinzolamide
FDA Drug Information • Also known as: Azopt, Brinzolamide
- Brand Names
- Azopt, Brinzolamide
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
Description
11 DESCRIPTION Brinzolamide ophthalmic suspension USP, 1% contains a carbonic anhydrase inhibitor formulated for multidose topical ophthalmic use. Brinzolamide is described chemically as: (R)-(+)-4-Ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno [3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide. Its empirical formula is C 12 H 21 N 3 O 5 S 3 , and its structural formula is: Brinzolamide has a molecular weight of 383.5 g/mol and a melting point of about 131°C. It is a white powder, which is insoluble in water, very soluble in methanol and soluble in ethanol. Brinzolamide ophthalmic suspension USP, 1% is supplied as a sterile, aqueous suspension of brinzolamide which has been formulated to be readily suspended and slow settling, following shaking. It has a pH of approximately 7.5 and an osmolality of 300 mOsm/kg. Each mL of brinzolamide ophthalmic suspension USP, 1% contains: Active ingredient: brinzolamide 10 mg; Preservative: benzalkonium chloride 0.1 mg; Inactives: carbomer 974P, edetate disodium, mannitol, sodium chloride, tyloxapol, water for injection, with hydrochloric acid and/or sodium hydroxide to adjust pH. ChemStructure
What Is Brinzolamide Used For?
1 INDICATIONS AND USAGE Brinzolamide ophthalmic suspension is a carbonic anhydrase inhibitor indicated in the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma. Brinzolamide ophthalmic suspension is a carbonic anhydrase inhibitor indicated for the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION The recommended dose is one drop of brinzolamide ophthalmic suspension in the affected eye(s) 3 times daily. Shake well before use. Brinzolamide ophthalmic suspension 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 )
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS 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 Bausch & Lomb Incorporated at 1-800-553-5340 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 brinzolamide ophthalmic suspension, 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. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Serious skin and subcutaneous tissue reactions such as Stevens-Johnson syndrome (SJS) and Toxic epidermal necrolysis (TEN) may occur with the use of brinzolamide due to its sulfonamide component [see Warnings and Precautions (5.1) ] .
Drug Interactions
7 DRUG INTERACTIONS There is a potential additive effect of the known systemic effects of carbonic anhydrase inhibition in patients receiving both oral and topical carbonic anhydrase inhibitors. ( 7.1 ) Rare instances of acid-base alterations have occurred with high-dose salicylate therapy. ( 7.2 ) 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. The concomitant administration of brinzolamide ophthalmic suspension 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.
Contraindications
4 CONTRAINDICATIONS Brinzolamide ophthalmic suspension is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product. ( 4 )
Pregnancy and Breastfeeding
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). Embryo-fetal studies were conducted in pregnant rabbits administered 0, 1, 3, or 6 mg/kg/day of brinzolamide by oral gavage on gestation days 6 to 18, to target the period of organogenesis. No treatment-related fetal effects were observed at any dose. The NOAEL for fetal toxicity was 6 mg/kg/day (125 times the RHOD based on mg/kg). Maternal weight loss during pregnancy was observed at 3 mg/kg/day (63 times the RHOD) and above. The NOAEL for maternal toxicity was 1 mg/kg/day (21 times the RHOD). A peri-/postnatal study was conducted in rats administered brinzolamide by oral gavage from gestation day 16 through lactation day 20. Decreased pup body weight was observed at 15 mg/kg/day (313 times the RHOD based on mg/kg). The NOAEL for developmental toxicity was 5...
Overdosage
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.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Brinzolamide ophthalmic suspension USP, 1% is supplied in a round LDPE bottle with an extended LLDPE controlled dropper tip and orange cap as follows: 10 mL NDC 24208-464-10 15 mL NDC 24208-464-15 Storage and Handling Store brinzolamide ophthalmic suspension USP, 1% at 4°C to 30°C (39°F to 86°F). Shake well before use. After opening, brinzolamide ophthalmic suspension USP, 1% can be used until the expiration date on the bottle.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.