Consumer medicine information

1. Why am I using Azopt?

Azopt contains the active ingredient brinzolamide. Azopt is used to treat ocular hypertension (high pressure in eye) and open-angle glaucoma (an eye disorder that causes damage to the optic nerve of the eye).
For more information, see Section 1. Why am I using Azopt? in the full CMI.

2. What should I know before I use Azopt?

Do not use if you have ever had an allergic reaction to Azopt or any of the ingredients listed at the end of the CMI.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.
For more information, see Section 2. What should I know before I use Azopt? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with Azopt and affect how it works.
A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Azopt?

• Put one drop of AZOPT eye drop in affected eye or eyes twice daily.

• If you do not understand how to use your eye drops, consult your doctor for advice.

5. What should I know while using Azopt?

6. Are there any side effects?

Common side effects include blurred vision, double vision, dry or itchy eye(s), discomfort, discharge from eye(s), hives, headache, nervousness, keratitis (an eye disease of the cornea)
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

1 Name of Medicine

Brinzolamide.

2 Qualitative and Quantitative Composition

The eye drops suspension contains 10 mg/1 mL (1%) brinzolamide and also 0.1 mg/1 mL benzalkonium chloride as a preservative.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Eye drops.
Azopt is a white to off-white, uniform suspension.

4 Clinical Particulars

4.9 Overdose

No information on systemic overdosage is available in humans. Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic state and possible nervous system effects may occur. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored.
A topical overdose of Azopt may be flushed from the eyes with warm tap water.
Contact the Poisons Information Centre on 13 11 26 for advice on management.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Genotoxicity studies with brinzolamide did not demonstrate any mutagenic potential in one in vitro (Ames assay) or chromosomal damage in an in vivo assay (micronucleus formation). Brinzolamide did induce forward mutations in the mouse lymphoma assay in vitro, with, but not without metabolic activation. Brinzolamide was negative in a sister chromatid exchange assay in mice.
Carcinogenicity. A two year bioassay, in which rats were dosed by oral gavage at doses up to 8 mg/kg/day brinzolamide revealed no evidence of a carcinogenic effect. A similar study conducted in mice (0, 1, 3 and 10 mg/kg/day brinzolamide dosed by oral gavage) also showed that brinzolamide was non-carcinogenic. The mouse study did, however, reveal a statistically significant increase in urinary bladder tumours in female mice given 10 mg/kg/day orally for 24 months. Dose-related proliferative changes in the urinary bladder were observed in female mice at all dose levels and among males at 10 mg/kg/day. The elevated bladder tumour incidence was due to the increased incidence of a tumour considered to be unique to mice.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Brinzolamide is presented as white to off-white crystals or powder.
Brinzolamide is very slightly soluble in water at neutral pH.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSBRINZO.gif Molecular weight: 383.51.
Empirical formula: C₁₂H₂₁N₃O₅S₃.
Chemical name: (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide.
CAS number. 138890-62-7.

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (Schedule 4).

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/AZOPTEST.gif