Version May 2024
Elevated intraocular pressure: Ophthalmic: Instill 1 drop in affected eye(s) 3 times daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling.
CrCl <30 mL/minute: Use is not recommended (has not been studied; brinzolamide and metabolite are excreted predominately by the kidney).
There are no dosage adjustments provided in the manufacturer’s labeling.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Dermatologic: Dermatitis (1% to 5%)
Gastrointestinal: Bitter taste (≤10%), sour taste (≤10%), unusual taste (≤10%)
Nervous system: Headache (1% to 5%)
Ophthalmic: Blepharitis (1% to 5%), blurred vision (5% to 10%), dry eye syndrome (1% to 5%), eye discharge (1% to 5%), eye discomfort (1% to 5%), eye pain (1% to 5%), eye pruritus (1% to 5%), foreign body sensation of eye (1% to 5%), keratitis (1% to 5%), ocular hyperemia (1% to 5%)
Respiratory: Rhinitis (1% to 5%)
<1%:
Cardiovascular: Chest pain
Dermatologic: Alopecia, urticaria
Gastrointestinal: Diarrhea, dyspepsia, nausea, xerostomia
Hypersensitivity: Hypersensitivity reaction
Nervous system: Dizziness, hypertonia
Ophthalmic: Asthenopia, conjunctivitis, corneal disease, crusting of eyelid, diplopia, keratoconjunctivitis, lacrimation
Renal: Renal pain
Respiratory: Dyspnea, pharyngitis
Postmarketing:
Dermatologic: Toxic epidermal necrolysis (Chun 2008)
Ophthalmic: Corneal edema (Zhao 2005), follicular conjunctivitis (Young 2018)
Hypersensitivity to brinzolamide or any component of the formulation.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to sulfonamide; severe renal impairment (CrCl <30 mL/minute); hyperchloremic acidosis; concomitant use with oral carbonic anhydrase inhibitors.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Concerns related to adverse effects:
• Ophthalmic effects: Vision may be temporarily blurred, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).
• Sulfonamide (“sulfa”) allergy: The FDA-approved product labeling for many medications containing a sulfonamide chemical group includes a broad contraindication in patients with a prior allergic reaction to sulfonamides. There is a potential for cross-reactivity between members of a specific class (eg, two antibiotic sulfonamides). However, concerns for cross-reactivity have previously extended to all compounds containing the sulfonamide structure (SO2NH2). An expanded understanding of allergic mechanisms indicates cross-reactivity between antibiotic sulfonamides and nonantibiotic sulfonamides may not occur or at the very least this potential is extremely low (Brackett 2004; Johnson 2005; Slatore 2004; Tornero 2004). In particular, mechanisms of cross-reaction due to antibody production (anaphylaxis) are unlikely to occur with nonantibiotic sulfonamides. T-cell-mediated (type IV) reactions (eg, maculopapular rash) are less well understood and it is not possible to completely exclude this potential based on current insights. In cases where prior reactions were severe (Stevens-Johnson syndrome/TEN), some clinicians choose to avoid exposure to these classes.
Disease-related concerns:
• Acute angle-closure glaucoma: Use has not been studied in acute angle-closure glaucoma.
• Corneal endothelium: Use with caution in patients with low endothelial cell counts; may be at increased risk of corneal edema.
• Renal impairment: Use is not recommended in patients with severe renal impairment (has not been studied).
Special populations:
• Contact lens wearers: Product may contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Suspension, Ophthalmic:
Azopt: 1% (10 mL, 15 mL) [contains benzalkonium chloride, edetate (edta) disodium]
Generic: 1% (10 mL, 15 mL)
Yes
Suspension (Azopt Ophthalmic)
1% (per mL): $43.25
Suspension (Brinzolamide Ophthalmic)
1% (per mL): $36.60 - $39.13
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Suspension, Ophthalmic:
Azopt: 1% (5 mL) [contains benzalkonium chloride, edetate (edta) disodium]
Ophthalmic: Shake well before use. Remove contact lenses prior to administration; wait 15 minutes before reinserting. If more than one topical ophthalmic drug is being used, administer drugs at least 10 minutes apart. Avoid allowing the tip of the dispensing container to contact the eye or surrounding structures.
Elevated intraocular pressure: Treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma
Azopt [US, Canada, and multiple international markets] may be confused with Atropt brand name for atropine [Australia and New Zealand]
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Risk C: Monitor therapy
Amantadine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Amantadine. Risk C: Monitor therapy
Carbonic Anhydrase Inhibitors: May enhance the adverse/toxic effect of other Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Risk X: Avoid combination
Adverse events have been observed in animal reproduction studies.
Other agents may be preferred for the treatment of glaucoma in pregnant patients. Use of topical carbonic anhydrase inhibitors may be considered after the first trimester. In general, if ophthalmic agents are needed in pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease exposure to the fetus (Belkin 2020; Strelow 2020).
It is not known if brinzolamide is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. In general, topical carbonic anhydrase inhibitors are considered compatible with breastfeeding. Administering after breastfeeding may help decrease potential exposure to the infant via breast milk (Belkin 2020; Strelow 2020).
Ophthalmic exams and intraocular pressure
Brinzolamide inhibits carbonic anhydrase, leading to decreased aqueous humor secretion. This results in a reduction of intraocular pressure.
Absorption: Topical: Into systemic circulation
Distribution: Accumulates extensively in red blood cells, binding to carbonic anhydrase (brinzolamide and metabolite)
Protein binding: ~60%
Metabolism: To N-desethyl brinzolamide
Excretion: Urine (as unchanged drug and metabolites)
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