Overview
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.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 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.
Indications
- 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 )
Common Doses
- Refer to label
Dosage
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 )
Contraindications
- 4 CONTRAINDICATIONS AZOPT is contraindicated in patients who are hypersensitive to any component of this product. Hypersensitivity to any component of this product. ( 4 )
Side Effects
- 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.
Interactions
- 7 DRUG INTERACTIONS • There is a potential additive effect of the known systemic effects of carbonic anhydrase inhibition in patients receiving both oral and topical carbonic anhydrase inhibitors. ( 7.1 ) • Rare instances of acid-base alterations have occurred with high-dose salicylate therapy. ( 7.2 ) 7.1 Oral Carbonic Anhydrase Inhibitors There is a potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and AZOPT.