Brinzolamide

Prescription

상품명: Azopt

제형

Drops

투여 경로

OPHTHALMIC

제조사

Sandoz Inc

About This Medication

11 DESCRIPTION AZOPT 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. AZOPT 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 AZOPT contains: Active ingredient: brinzolamide 10 mg; Inactives: carbomer 974P, edetate disodium, hydrochloric acid and/or sodium hydroxide to adjust pH, mannitol, purified water, sodium chloride, and tyloxapol; Preservative: benzalkonium chloride 0.1 mg. Brinzolamide structural formula

유효 성분

성분	함량
Brinzolamide	-

적응증 및 용법

1 INDICATIONS AND USAGE 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. ( 1 )

작용 원리

12.1 Mechanism of Action 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. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II, found primarily in red blood cells (RBCs), but also in other tissues. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in IOP. AZOPT contains brinzolamide, an inhibitor of carbonic anhydrase II. Following topical ocular administration, brinzolamide inhibits aqueous humor formation and reduces elevated IOP. Elevated IOP is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss.

용량 및 투여 방법

2 DOSAGE AND ADMINISTRATION 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 )

Side Effects Overview

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 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. 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)] .

경고 및 주의 사항

5 WARNINGS AND PRECAUTIONS • 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. 5.4 Acute Angle-Closure Glaucoma The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents. AZOPT has not been studied in patients with acute angle-closure glaucoma. 5.5 Risk of Contamination Avoid allowing the tip of the dispensing container to contact the eye or surrounding structures or other surfaces, since the product can become contaminated by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions. 5.6 Contact Lens Wear The preservative in AZOPT, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of AZOPT, but may be reinserted 15 minutes after instillation.

금기

4 CONTRAINDICATIONS AZOPT is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product. ( 4 )

약동학

12.3 Pharmacokinetics 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). In humans, the metabolite N-desethyl brinzolamide is formed, which also binds to carbonic anhydrase and accumulates in RBCs. This metabolite binds mainly to carbonic anhydrase I in the presence of brinzolamide. In plasma, both parent brinzolamide and N-desethyl brinzolamide concentrations are low and generally below assay quantitation limits (less than 10 ng/mL). Binding to plasma proteins is approximately 60%. Brinzolamide is eliminated predominantly in the urine as unchanged drug. N-Desethyl brinzolamide is also found in the urine along with lower concentrations of the N-desmethoxypropyl and O-desmethyl metabolites. An oral pharmacokinetic study was conducted in which healthy volunteers received 1 mg capsules of brinzolamide twice per day for up to 32 weeks. This regimen approximates the amount of drug delivered by topical ocular administration of AZOPT dosed to both eyes 3 times per day and simulates systemic drug and metabolite concentrations similar to those achieved with long-term topical dosing. Red blood cell carbonic anhydrase activity was measured to assess the degree of systemic carbonic anhydrase inhibition. Brinzolamide saturation of RBC carbonic anhydrase II was achieved within 4 weeks (RBC concentrations of approximately 20 mcM). N-Desethyl brinzolamide accumulated in RBCs to steady-state within 20 to 28 weeks reaching concentrations ranging from 6 to 30 mcM. The inhibition of carbonic anhydrase II activity at steady-state was approximately 70% to 75%, which is below the degree of inhibition expected to have a pharmacological effect on renal function or respiration in healthy subjects.

Frequently Asked Questions

1 INDICATIONS AND USAGE 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. ( 1 )

2 DOSAGE AND ADMINISTRATION 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 …

5 WARNINGS AND PRECAUTIONS • 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), …

4 CONTRAINDICATIONS AZOPT is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product. ( 4 )

Brinzolamide is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

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References & Data Sources

• DailyMed — Brinzolamide drug label (National Library of Medicine)
• openFDA — Brinzolamide label data (U.S. Food & Drug Administration)
• RxNorm — RXCUI 213272 (NLM Normalized Drug Names)
• NDC Directory — Brinzolamide (FDA National Drug Code)

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데이터 출처: DailyMed (NLM), openFDA, MFDS