Azopt - General Information
Azopt is a carbonic anhydrase inhibitor. Carbonic anhydrase (CA) 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 (CA-II). 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 intraocular pressure. Azopt is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Pharmacology of Azopt
Used in the treatment of glaucoma, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss.
Azopt for patients
AZOPT® (brinzolamide ophthalmic suspension) 1% is a sulfonamide and although administered topically, it is absorbed systemically; therefore, the same types of adverse reactions attributable to sulfonamides may occur with topical administration. Patients should be advised that if serious or unusual ocular or systemic reactions or signs of hypersensitivity occur, they should discontinue the use of the product and consult their physician.
Vision may be temporarily blurred following dosing with AZOPT® (brinzolamide ophthalmic suspension) 1%. Care should be exercised in operating machinery or driving a motor vehicle.
Patients should be instructed to 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.
Patients should also be advised that if they have ocular surgery or develop an intercurrent ocular condition (e.g., trauma or infection), they should immediately seek their physician's advice concerning the continued use of the present multidose container.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least ten minutes apart. The preservative in AZOPT® (brinzolamide ophthalmic suspension) 1%, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of AZOPT® (brinzolamide ophthalmic suspension) 1%, but may be reinserted 15 minutes after instillation.
AZOPT (brinzolamide ophthalmic suspension) 1% contains a carbonic anhydrase inhibitor. Acid-base and electrolyte alterations were not reported in the clinical trials with brinzolamide. However, in patients treated with oral carbonic anhydrase inhibitors, rare instances of drug interactions have occurred with high-dose salicylate therapy. Therefore, the potential for such drug interaction should be considered in patients receiving AZOPT (brinzolamide ophthalmic suspension) 1%.
Brinzolamide is contraindicated in patients who are hypersensitive to any component of this product.
Additional information about Azopt
Azopt Indication: For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Mechanism Of Action: Brinxolamide is both a sulfonamide and a carbonic anhydrase II inhibitor. Carbonic anhydrase catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. 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 intraocular pressure, and thereby a reduction in the risk of optic nerve damage and glaucomatous visual field loss.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Brinzolamide
Synonyms: Not Available
Drug Category: Antiglaucomic Agents; Ophthalmics; Carbonic Anhydrase Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Brinzolamide: Azopt;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Approximately 60%.
Half Life: 111 days
Dosage Forms of Azopt: Suspension Ophthalmic
Chemical IUPAC Name: (4R)-4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[4,5-e]thiazine-6-sulfonamide
Chemical Formula: C12H21N3O5S3
Brinzolamide on Wikipedia: http://en.wikipedia.org/wiki/Brinzolamide
Organisms Affected: Humans and other mammals