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brinzolamide (Azopt)

Tradename: Azopt Indications: - increased intraocular pressure - glaucoma (may be used concurrently with other glaucoma medications) Contraindications: - hypersensitivity to brinzolamide, sulfonamide Pregnancy category: C Dosage: 1 drop in affected eye TID Suspension, ophthalmic 1%, (5 mL, 10 mL, 15 mL) contains benzalkonium chloride Storage: - 4-30 degrees C (39-86 degrees F) Pharmacokinetics: - ophthalmic absorbed systemically - distributes to erythrocytes - 1/2life in erythrocytes 111 days - metabolite N-desmethylbrinzolamide accumulates in erythrocytes Adverse effects: 1) not common (1-10%) - dermatitis, taste disturbance, blurred vision, blepharitis, foreign body senstation eye, eye pain, eye itching dysgeusia, xerophthalmia, headache, hyperemia, ocular discharge, ocular keratitis, rhinitis 2) uncommon (< 1%) - allergic reactions, alopecia, conjunctivitis, diplopia, chest pain, diarrhea, dizziness, xerostomia, dyspnea, dyspepsia, eye fatigue, hypertonia, keratoconjunctivitis, keratopathy, kidney pain, nausea, pharyngitis, tearing, urticaria, eyelid margin crusting or sticky sensation 3) other - dysuria ?, hyperglycemia ? - acetazolamide, another carbonic anhydrase inhibitor, may be associated with dysuria, hyperglycemia Drug interactions: 1) concurrent use of other carbonic anhydrase inhibitors 2) high dose salicylates in combination may result in renal toxicity Mechanism of action: - carbonic anhydrase inhibitor - inhibition of carbonic anhydrase in the ciliary body of the eye decreases aqueous humor production, presumably by reducing formation of bicarbonate with reduction of Na+ & fluid transport, thus reducing intraocular pressure - intraocular pressure reduction of 4-5 mm Hg when used TID (similar to dorzolamide) [3]

Interactions

drug adverse effects of diuretics monitor with carbonic anhydrase inhibitors

General

carbonic anhydrase inhibitor ophthalmic agent (eyedrops)

Database Correlations

PUBCHEM cid=68844

References

  1. UpToDate 13.3 http://www.utdol.com LexiComp Drug Information
  2. MedlinePlus: Brinzolamide Ophthalmic http://www.nlm.nih.gov/medlineplus/druginfo/meds/a601233.html
  3. Highlights of Prescribing Information Azopt. (brinzolamide ophthalmic suspension 1%) Alcon. A Novartis Co.

Component-of

brimonidine/brinzolamide (Simbrinza)