Class: Carbonic Anhydrase Inhibitors
Chemical Name: (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
Molecular Formula: C12H21N3O5S3
CAS Number: 138890-62-7
Brands: Azopt
Introduction
Carbonic anhydrase inhibitor;2 4 6 nonbacteriostatic sulfonamide derivative.1
Uses for Brinzolamide
Ocular Hypertension and Glaucoma
Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.1 3 4 5 6 8
Efficacy comparable to that of dorzolamide in reducing IOP in patients with open-angle glaucoma or ocular hypertension;1 3 6 8 less effective than timolol.5
Safety and efficacy not established for the treatment of acute angle-closure glaucoma.1
Brinzolamide Dosage and Administration
Administration
For topical ophthalmic use only.1 Not for injection or oral use.1
Ophthalmic Administration
Apply topically to the affected eye(s) as an ophthalmic suspension.1
Shake suspension well prior to use.1
Avoid contamination of the suspension container.1
If more than one topical ophthalmic drug is used, administer the drugs at least 10 minutes apart.1
Dosage
Adults
Ocular Hypertension and Glaucoma
Ophthalmic
One drop of a 1% suspension in the affected eye(s) 3 times daily.1
Cautions for Brinzolamide
Contraindications
Known hypersensitivity to brinzolamide or any ingredient in the formulation.1
Warnings/Precautions
Sensitivity Reactions
Sulfonamide Sensitivity Reactions
Serious adverse events (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, other blood dyscrasias) associated with sulfonamide therapy possible.1
Usual precautions associated with systemic use of sulfonamides apply.1 Discontinue brinzolamide if serious reactions or signs or symptoms of hypersensitivity occur.1
General Precautions
Ocular Effects
Effect on corneal endothelium not fully evaluated.1
Specific Populations
Pregnancy
Category C.1
Lactation
Distributed into milk in rats following oral administration; not known whether distributed into human milk following topical application to eye.1 Discontinue nursing or the drug.1
Pediatric Use
Safety and efficacy not established.1 9
Geriatric Use
No overall differences in safety and efficacy relative to younger adults.1
Hepatic Impairment
Not studied in patients with hepatic impairment; use with caution.1
Renal Impairment
Not studied in patients with severe renal impairment (Clcr< 30 mL/minute).1 Not recommended in such patients, since brinzolamide and its metabolite are excreted mainly by the kidneys.1
Common Adverse Effects
Blurred vision, taste disturbances (bitter, sour, or unusual taste).1
Interactions for Brinzolamide
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
Carbonic anhydrase inhibitors, oral | Additive systemic effects1 | Concomitant use not recommended1 |
Ocular hypotensive agents | Additive IOP-lowering effects1 | Used to therapeutic advantage1 |
Salicylates | Rare reports of toxicity associated with acid-base disturbances in patients receiving oral carbonic anhydrase inhibitors with high-dose salicylates1 | Consider possibility of similar interaction with ophthalmic brinzolamide1 |
Brinzolamide Pharmacokinetics
Absorption
Bioavailability
Absorbed into systemic circulation following topical application to eye.1
Distribution
Extent
Brinzolamide accumulates in erythrocytes due to carbonic anhydrase-II (CA-II) binding; N-desmethyl metabolite accumulates in erythrocytes due to CA-I binding.1
Plasma Protein Binding
60%.1
Elimination
Metabolism
Not fully characterized.1
Elimination Route
Brinzolamide and N-desmethyl brinzolamide are eliminated in urine.1
Half-life
Brinzolamide: 111 days in whole blood.1
Stability
Storage
Ophthalmic
Suspension
4–30°C.1
ActionsActions
Potent ocular hypotensive agent; can produce mean IOP reductions of about 16–19% in patients with elevated IOP.1 3 8
Highly specific inhibitor of CA-II, the main carbonic anhydrase isoenzyme involved in aqueous humor secretion.1 2 3 Inhibition of carbonic anhydrase in the ciliary process of the eye decreases the rate of aqueous humor secretion and IOP by slowing bicarbonate formation and reducing sodium and fluid transport.1 2
Accumulates in erythrocytes as a result of CA-II binding; however, sufficient CA-II activity remains so that adverse effects resulting from systemic carbonic anhydrase inhibition are not observed.1 5
Advice to Patients
Risk of adverse effects, including sensitivity reactions; discontinue therapy and consult clinician if serious or unusual ocular or systemic reactions or signs of sensitivity occur.1
Risk of temporary blurring of vision; use caution when driving or operating machinery.1
Importance of learning and adhering to proper administration techniques to avoid contamination of the product.1
Importance of informing clinicians if an intercurrent ocular condition (e.g., trauma, infection) develops or ocular surgery is planned.1
Importance of administering different topical ophthalmic preparations at least 10 minutes apart.1
Importance of removing soft contact lenses prior to administering the drug and of delaying reinsertion of the lenses for at least 15 minutes after administration.1
Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing patient of other important precautionary information.1 (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Ophthalmic | Suspension | 1% | Azopt (with benzalkonium chloride) | Alcon |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Azopt 1% Suspension (ALCON VISION): 10/$119.99 or 30/$336.98
Azopt 1% Suspension (ALCON VISION): 15/$161.99 or 45/$461.98
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
1. Alcon. Azopt (brinzolamide) ophthalmic suspension 1% prescribing information. Fort Worth, TX; 2003 Dec.
2. DeSantis L. Preclinical overview of brinzolamide. Surv Ophthalmol. 2000; 44(Suppl 2):119-29.
3. Silver LH and the Brinzolamide Primary Therapy Study Group. Clinical efficacy and safety of brinzolamide (Azopt), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension. Am J Ophthalmol. 1998; 126:400-8. [IDIS 414483] [PubMed 9744373]
4. Shin D and the Brinzolamide Adjunctive Therapy Study Group. Adjunctive therapy with brinzolamide 1% ophthalmic suspension (Azopt) in patients with open-angle glaucoma or ocular hypertension maintained on timolol therapy. Surv Ophthalmol. 2000; 44(Suppl 2):163-8.
5. March WF, Ochsner KI and the Brinzolamide Long-Term Therapy Study Group. The long-term safety and efficacy of brinzolamide 1.0% (Azopt) in patients with primary open-angle glaucoma or ocular hypertension. Am J Ophthalmol. 2000; 129:136-43. [IDIS 442914] [PubMed 10682964]
6. Anon. Brinzolamide-a new topical carbonic anhydrase inhibitor for glaucoma. Med Lett Drugs Ther. 1998; 40:95-6. [PubMed 9774966]
7. Ingram CJ, Brubaker RF. Effect of brinzolamide and dorzolamide on aqueous humor flow in human eyes. Am J Ophthalmol. 1999; 128:292-6. [IDIS 435005] [PubMed 10511022]
8. Sall K and the Brinzolamide Primary Therapy Study Group. The efficacy and safety of brinzolamide 1% ophthalmic suspension (Azopt) as a primary therapy in patients with open-angle glaucoma or ocular hypertension. Surv Ophthalmol. 2000; 44(Suppl 2):155-62.
9. Alcon, Fort Worth, TX: Personal communication.
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