Products
Brinzolamide is form of eye drops commercially available (Azopt) and approved in many countries since 1991. Generic versions were released in 2015. Brinzolamide has also been available in a fixed combination with timolol since 2009 (Azarga). In 2015, a fixed combination with brimonidine was approved; see brinzolamide brimonidine (Simbrinza).
Structure and properties
Brinzolamide (C12H21N3O5S3, 383.51 g/mol) is a thienothiazine sulfonamide and a pure -(+)-enantiomer. It exists as a white powder that is insoluble in water and is therefore formulated as a suspension in pharmaceuticals.
Effects
Brinzolamide (ATC S01EC04) lowers intraocular pressure by selectively inhibiting carbonic anhydrase II to reduce aqueous humor formation. Brinzolamide is not antibacterial like other sulfonamides.
Indication
For the treatment of elevated intraocular pressure (ocular hypertension, open-angle glaucoma).
Dosage
According to the drug label. The eye drops are usually placed in the affected eyes in the morning and evening (twice daily). The vial must be shaken well before each use because it is a suspension. See also under Administering eye drops.
Contraindications
- Hypersensitivity, including to other sulfonamides.
- Severe renal dysfunction
- Hyperchloremic acidosis
For complete precautions, see the drug label.
Interactions
There is a possibility that brinzolamide may be absorbed systemically and have an effect on acid-base balance. Brinzolamide is metabolized by CYP450 isoenzymes and, according to the SmPC, should be used with caution in conjunction with CYP3A4 inhibitors. Other eye drops should be administered at least 10 minutes apart.
Adverse effects
The most common possible adverse effects include local reactions to the eye, taste disturbance, headache, and dry mouth.
