Brinzolamide
- Atc Codes:S01EC04
- CAS Codes:138890-62-7
- PHARMGKB ID:138890-62-7
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Azopt; Belgium: Azopt; Czech Republic: Azopt; Denmark: Azopt; Estonia: Azopt; Finland: Azopt; France: Azopt; Germany: Azopt; Greece: Azopt; Hungary: Azopt; Ireland: Azopt; Italy: Azopt; Luxembourg: Azopt; Netherlands: Azopt; Poland: Azopt; Portugal: Azopt; Spain: Azopt; Sweden: Azopt; UK: Azopt.
North America
Canada: Azopt; USA: Azopt.
Latin America
Argentina: Azopt; Brazil: Azopt; Mexico: Azopt.
Asia
Japan: Azopt.
Drug combinations
Brinzolamide and Timolol
Chemistry
Brinzolamide: C~12~H~21~N~3~O~5~S~3~. Mw: 383.51. (1) 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)-; (2)(R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide. CAS-138890-62-7 (1997).
Pharmacologic Category
Antiglaucoma Agents; Carbonic Anhydrase Inhibitors. (ATC-Code: S01EC04).
Mechanism of action
Brinzolamide is a nonbacteriostatic sulfonamide derivative. Highly specific inhibitor of carbonic anhydrase type II isozyme (CA-II), resulting in a decrease in the rate of aqueous humor secretion and intraocular pressure (IOP) by slowing bicarbonate formation and reducing sodium and fluid transport. Due to some systemic absorption, following long-term topical administration to the eye, the drug and its metabolite accumulate in erythrocytes by CA-II binding (sufficient CA-II activity remains).
Therapeutic use
Reduction of IOP in open-angle glaucoma or ocular hypertension. Brinzolamide is as effective as dorzolamide, but less than timolol in reducing IOP.
Pregnancy and lactiation implications
Developmental toxicities observed in animal studies. There are no adequate studies in pregnant women. Use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus. Not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to brinzolamide, sulfonamides, or any component of the formulation.
Warnings and precautions
Systemic absorption may cause serious hypersensitivity reactions to recur. Use in sulfonamide allergy is specifically contraindicated (chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid); risk of cross-reaction). Not recommended if creatinine clearance less than 30 mL/minute. For topical use only.