SUMMARY CMI

Azopt Eye Drops 1%^®

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

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.

More instructions can be found in Section 4. How do I use Azopt? in the full CMI.

5. What should I know while using Azopt?

For more information, see Section 5. What should I know while using Azopt? in the full CMI.

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.

FULL CMI

Azopt Eye Drops 1%^®

Active ingredient(s): brinzolamide

Consumer Medicine Information (CMI)

This leaflet provides important information about using Azopt. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using Azopt.

Where to find information in this leaflet:

1. Why am I using Azopt?
2. What should I know before I use Azopt?
3. What if I am taking other medicines?
4. How do I use Azopt?
5. What should I know while using Azopt?
6. Are there any side effects?
7. Product details

1. Why am I using Azopt?

Azopt contains the active ingredient brinzolamide. Azopt belongs to class of drugs called "Carbonic anhydrase inhibitors".

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). It is either used alone or in combination with other eye drops/medicines. Azopt helps to lower the eye pressure by reducing the production of fluid that the eye naturally produces.

2. What should I know before I use Azopt?

Warnings

Do not use Azopt if:

• you are allergic to brinzolamide, or any of the ingredients listed at the end of this leaflet.
• you have problems with your kidney's or hyperchloraemic acidosis (a condition in which there are high levels of chloride in your blood)
• you are allergic to sulfonamides medications.
  Symptoms of allergic reactions may include:
  Stevens-Johnson syndrome (SJS) [A skin disease having symptoms such as blisters and sores on skin, eyes, nose, genitals, mouth, skin pain, rash, fever]
  and toxic epidermal necrolysis (TEN) [severe form of SJS having symptoms such as peeling and blistering of skin, including mouth, eyes and genitals]
  If you think you may be allergic, ask your doctor for advice.

Always check the ingredients to make sure you can use this medicine.

Check with your doctor if you:

• have acute angle-closure glaucoma (eye disorder)
• have diabetes mellitus or problems with your cornea, corneal dystrophies (a group of rare hereditary eye disorders that affect cornea)
• have liver or kidney disease.

Do not put Azopt eye drops in your eyes if you are wearing contact lenses as it may cause irritation to your eyes and discolor soft contact lenses.

Remove your contact lenses before putting Azopt eye drops in and wait at least 15 minutes before you reinsert your contact lenses into your eyes.

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Check with your doctor if you are pregnant or intend to become pregnant.

Your doctor will advise you regarding the potential possible risks and benefits of using Azopt during pregnancy.

Talk to your doctor if you are breastfeeding or intend to breastfeed.

Your doctor will advise you regarding the potential possible risks and benefits of using Azopt during breast feeding.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may interfere with Azopt and affect how it works. They may include:

High doses of salicylate-containing medicines which act as pain killers.

Other medicines known as "oral carbonic anhydrase inhibitors"

Nonsteroidal anti-inflammatory drugs (NSAIDs)

If you are taking any of the above medications, consult your doctor for advice.

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect Azopt.

4. How do I use Azopt?

How much to use

• Put one drop of AZOPT eye drop in affected eye(s) twice daily.  
• Follow the instructions provided and use Azopt until your doctor tells you to stop.
• In case you are using other topical eye drop medications, administer Azopt with an interval of at least five minutes. If you are using any eye ointments, administer them last.
• If you do not understand how to use your eye drops, consult your doctor for advice.
• If you are being advised to change your eye drops to Azopt, follow your doctor's instructions carefully as to when to stop the old drops and when to start the new drops.

When to use Azopt

• Instill Azopt eye drops in the conjunctival sac of affected eye(s) twice daily.

How to use Azopt

• Sitting or lying down might make administration of your eye drops process simpler.
• Remove contact lenses if you are wearing them before instilling the eye drops.
• Shake the bottle well prior to use.

Follow below steps to use Azopt Eye Drops:

• Wash your hands thoroughly with soap and water.
• Before using a bottle for the first time, break the safety seal around the neck area and throw the loose plastic ring away.
• Mix the contents of the bottle by inverting 5 to 10 times.
• Remove the cap from the bottle.
• Hold the bottle upside down in one hand between your thumb and middle finger (see Diagram 1).

• Tilt your head back, gently pull down the lower eyelid of your eye to form a pouch/pocket.
• Place the tip of the bottle close to your eye. Do not touch the tip to your eye as this may cause injury to the eye
• Do not touch the dropper tip to any surface to avoid contamination.
• Release one drop into the pouch/pocket formed between your eye and eyelid by gently tapping or pressing the base of the bottle with your forefinger (see Diagrams 2 and 3).

• Close your eye. Do not blink or rub your eye.
• When your eye is closed, place your index finger against the inside corner of your eye and press against your nose for about two minutes. This may result in a decrease in systemic side effects and an increase in local activity.
• This will also help to reduce the unpleasant taste sensation that some people experience when using these drops.
• If necessary, repeat the above steps for the other eye.
• It is normal for a small amount of the eye drop to spill onto your cheek since your eyelids can only hold less than one drop at a time. Wipe away any spillage with a tissue.
• Replace the cap on the bottle, closing it tightly.
• Always keep the bottle tightly closed when not in use.
• Wash your hands again with soap and water to remove any residue.
• You may feel a slight burning sensation or discomfort in the eye shortly after using Azopt eye drops.
• Contact your doctor immediately if the discomfort persists for a long time.
• If you want to wear your contact lenses, wait 15 minutes after instillation of the dose before reinserting the contact lenses.
• Do not use the eye drops after 4 weeks from opening it.
• Discard any remaining solution after four weeks and open a new bottle every four weeks.

If you forget to use Azopt

Azopt should be used regularly at the same time each day. If you miss your dose at the usual time, use the eye drops as soon as you remember.

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Do not take a double dose to make up for the dose you missed as it may cause undesirable side effects.

If you use too much Azopt

If you think that you have used too much Azopt, you may need urgent medical attention.

Symptoms of overdose may include:

Electrolyte imbalance

Development of an acidotic state

Nervous system problems.

You should immediately:

• phone the Poisons Information Centre
  (by calling 13 11 26), or
• contact your doctor, or
• go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

If you accidentally instilled several drops in your eyes, immediately wash your eyes with warm tap water and consult your doctor.

5. What should I know while using Azopt?

Things you should do

Call your doctor straight away if you:

• feel any persisting discomfort in your eyes after putting eye drops in.
• become pregnant while using Azopt eye drops.
• notice any signs of allergic reactions such as skin rash, red skin, blistering of the lip's eyes or mouth, fever.
• develop an eye infection or have any eye injury or an eye surgery.

Remind any doctor, dentist or pharmacist you visit that you are using Azopt.

Keep the Azopt eye drops away from children.

Have your eye pressure checked regularly.

Things you should not do

• Do not stop using this medicine suddenly.
• Do not use Azopt eye drops to treat other problems unless your doctor or pharmacist tells you to.

Do not give Azopt eye drops to anyone else, even if they seem to have the same condition as you.

Driving or using machines

Be careful before you drive or use any machines or tools until you know how Azopt affects you.

Azopt may cause blurred vision or other visual disturbances in some people after putting eye drops in.

Wait until vision clears before driving or using machinery.

Azopt may also cause nervous system disorders. Precaution should be taken before driving and using any machinery.

Looking after your medicine

• Store below 25°C.
• Do not freeze the eye drops.
• Do not leave the top off the bottle for any time. Put the top back on the bottle immediately after use to avoid any contamination.

Follow the instructions in the carton on how to take care of your eye drops properly.

Store it in a cool dry place away from moisture, heat or sunlight; for example, do not store it:

• in the bathroom or near a sink, or
• in the car or on window sills.

Keep it where young children cannot reach it.

When to discard your medicine

Do not use the eye drops after 4 weeks from opening it. Discard any remaining solution after four weeks and open a new bottle every four weeks.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

Do not use this medicine after the expiry date.

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

Less serious side effects

Serious side effects

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Other side effects not listed here may occur in some people.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is only available with a doctor's prescription.

What Azopt contains

Do not take this medicine if you are allergic to any of these ingredients.

What Azopt looks like

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

AZOPT Eye Drops 1.0% is available in LDPE bottle dispenser. Pack sizes: 1 x 5 mL and 1 x 10 mL

Not all pack sizes may be marketed.

Australian registration number

AUST R 72750.

Who distributes Azopt

Azopt is supplied in Australia by:

Novartis Pharmaceuticals Australia Pty Limited
ABN 18 004 244 160
54 Waterloo Road
Macquarie Park NSW 2113
Telephone: 1-800-671-203.
Web site: www.novartis.com.au

This leaflet was prepared in February 2025.

Internal document code:
azo091123c_V2 based on PI azo091123i

Published by MIMS March 2025

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

4.1 Therapeutic Indications

Azopt Eye Drops 1.0% are indicated to decrease intraocular pressure in: ocular hypertension, open angle glaucoma.

4.2 Dose and Method of Administration

The recommended dosage is one drop of Azopt in the conjunctival sac of the affected eye(s) twice daily.
When substituting another ophthalmic antiglaucoma agent with Azopt, the other agent should be discontinued and Azopt should be started the following day.

Concomitant therapy.

Method of administration.

4.3 Contraindications

Azopt is contraindicated in patients with a known hypersensitivity to brinzolamide, sulfonamides or any of the excipients in the product (see Section 6.1 List of Excipients).
Azopt is also contraindicated in patients with severe renal impairment and in patients with hyperchloraemic acidosis.

4.4 Special Warnings and Precautions for Use

Not for injection or oral ingestion.
The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents. Azopt has not been studied in patients with acute angle-closure glaucoma.
Brinzolamide is a sulfonamide and, although administered topically, is absorbed systemically. The same types of adverse reactions or hypersensitivity that are attributable to sulfonamides may, therefore, occur with topical administration. Hypersensitivity reactions reported with sulfonamide derivatives, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), can occur in patients receiving Azopt. At the time of prescription, patients should be advised of the signs and symptoms and monitored closely for skin reactions. Azopt should be discontinued immediately if signs of serious reactions or hypersensitivity occur.
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. The concomitant administration of Azopt and oral carbonic anhydrase inhibitors has not been studied and is not recommended.
Acid-base disturbances have been reported with oral carbonic anhydrase inhibitors. Azopt should be used with caution in patients with risk of renal impairment because of the possible risk of metabolic acidosis.
The possible role of brinzolamide on corneal endothelial function has not been investigated in patients with compromised corneas (particularly in patients with low endothelial cell count). Carbonic anhydrase inhibitors may affect corneal hydration, which may lead to a corneal decompensation and oedema. Careful monitoring of patients with compromised corneas, such as patients with diabetes mellitus or corneal dystrophies, is recommended.
Azopt contains benzalkonium chloride which may cause eye irritation and is known to discolour soft contact lenses. Avoid contact with soft contact lenses. Patients must be instructed to remove contact lenses prior to application of Azopt and wait at least 15 minutes before reinsertion.

Contact lenses.

Use in hepatic impairment.

Use in renal impairment.

Use in the elderly.

Paediatric use.

Effects on laboratory tests.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Specific drug interaction studies have not been performed with Azopt. In clinical studies, however, Azopt were used concomitantly with the following medications without evidence of adverse interactions: timolol maleate eye drops, systemic medications including ACE inhibitors, calcium-channel blockers, diuretics, non-steroidal anti-inflammatory drugs including aspirin, and hormones (e.g. oestrogen, insulin, thyroxine).
Association between Azopt and miotics or adrenergic agonists has not been fully evaluated during adjunctive glaucoma therapy.
Brinzolamide is a carbonic anhydrase inhibitor and, although administered topically, is absorbed systemically. In clinical studies, brinzolamide was not associated with acid-base disturbances. These disturbances have, however, been reported with oral carbonic anhydrase inhibitors and have, in some instances, resulted in drug interactions (e.g. nonsteroidal anti-inflammatory drugs (NSAIDs) and toxicity associated with high-dose salicylate therapy). The potential for such drug interactions should, therefore, be considered in patients receiving Azopt.
There is potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and Azopt. The concomitant administration of Azopt and oral carbonic anhydrase inhibitors is not recommended.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

4.7 Effects on Ability to Drive and Use Machines

As with other ophthalmic medications, patients should be advised to exercise caution if they experience transient blurred vision or other visual disturbances following instillation of eye drops; patients should wait until their vision clears before driving or using machinery.
Additionally, nervous system disorders have been reported with the use of the product which may affect the ability to drive or use machines (see Section 4.8 Adverse Effects (Undesirable Effects)).

4.8 Adverse Effects (Undesirable Effects)

In well-controlled clinical studies, undesirable effects related to Azopt were nonserious, generally mild to moderate, and usually did not lead to discontinuation of therapy. Tabulated adverse reaction data (considered to be possibly, probably or definitely related to treatment), providing comparisons to placebo and other active comparators (to an incidence of 1% or greater), which have been generated from all clinical studies with Azopt, are provided in Table 1.
Uncommon ophthalmic events (incidence < 1% and ≥ 0.1%) not detailed in Table 1 included blepharitis, conjunctivitis, lid margin crusting, sticky sensation, eye fatigue, abnormal vision, keratopathy, keratoconjunctivitis, corneal staining, eye disorder, photophobia, diplopia, meibomitis, vision changes, irritation, glare and lid disorder.
Uncommon non-ocular events (incidence < 1% and ≥ 0.1%) not detailed in Table 1 included:

Body as a whole.

Digestive.

Nervous.

Respiratory.

Skin and appendages.

Special senses.

Urogenital.

Postmarketing experience.

Eye disorders.

Psychiatric disorders.

Nervous system disorders.

Cardiac disorders.

Respiratory, thoracic and mediastinal disorders.

Gastrointestinal disorders.

Skin and subcutaneous tissue disorders.

General disorders and administration site conditions.

Reporting suspected adverse effects.

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

5.1 Pharmacodynamic Properties

Mechanism of action.

Clinical trials.

Concomitant therapy.

5.2 Pharmacokinetic Properties

Following topical ocular administration, brinzolamide is absorbed into the systemic circulation. Due to its high affinity for carbonic anhydrase II (CA-II), brinzolamide distributes extensively into the red blood cells (RBCs) and exhibits a long half-life in whole blood (approximately 111 days). In humans, the metabolite N-desethyl brinzolamide is formed, which also binds to CA and accumulates in RBCs. This metabolite binds mainly to CA-I in the presence of brinzolamide. In plasma, both parent brinzolamide and N-desethyl brinzolamide concentrations are low and generally below assay quantitation limits (< 10 nanogram/mL). Binding to plasma proteins is not extensive (approximately 60%). Brinzolamide is eliminated predominantly in the urine as unchanged drug. N-Desethyl brinzolamide is also found in the urine along with lower concentrations of the N-desmethoxypropyl and O-desmethyl metabolites.
An oral pharmacokinetic study was conducted in which healthy volunteers received 1 mg capsules of brinzolamide twice daily for up to 32 weeks. This regimen provided a higher systemic exposure rate than topical ocular administration of Azopt dosed in both eyes three times daily, and simulated systemic drug and metabolite concentrations similar to those achieved with long-term topical dosing. RBC CA activity was measured to assess the degree of systemic CA inhibition.
Brinzolamide saturation of RBC CA-II was achieved within 4 weeks (RBC concentrations of approximately 20 microM). N-Desethyl brinzolamide accumulated in RBCs to steady state within 20-28 weeks reaching concentrations ranging from 6-30 microM. The inhibition of total RBC CA activity at steady state was approximately 70-75%, which is below that expected to adversely affect renal function or respiration in healthy subjects.
An oral pharmacokinetic study was conducted in which subjects with mild to moderate renal impairment (creatinine clearance of 30-60 mL/minute) received 1 mg capsules of brinzolamide twice daily for up to 54 weeks. By week 4 of treatment, parent drug RBC concentrations ranged from approximately 20 to 40 microM and showed little subsequent change. At steady state, parent drug and N-desethyl metabolite RBC concentrations ranged from 22.0 to 46.1 and 17.1 to 88.6 microM, respectively. Metabolite RBC concentrations, but not those of parent drug, showed a significant (p < 0.05) increase with decreasing creatinine clearance. Total RBC CA activity, but not CA-II activity, showed a significant decrease as creatinine clearance decreased. In spite of the greater inhibition of total CA activity in subjects showing the highest degree of renal impairment, all subjects showed < 90% total CA inhibition at steady-state. This is below the 99% or greater inhibition associated with systemic adverse effects.
In a topical ocular study, patients with open-angle glaucoma or ocular hypertension received Azopt either two or three times daily for up to 18 months. Steady-state concentrations of brinzolamide were reached for most subjects within 6-9 months, while steady-state for the N-desmethyl metabolite was reached within 12 to 18 months. At steady-state, brinzolamide RBC concentrations were similar to those found in the oral study, but levels of the N-desethyl metabolite were lower. Carbonic anhydrase activity was approximately 40-70% of predose levels, indicating a degree of inhibition that was substantially lower than that observed orally and unlikely to elicit systemic side effects.

5.3 Preclinical Safety Data

Genotoxicity.

Carcinogenicity.

6 Pharmaceutical Particulars

6.1 List of Excipients

Mannitol, carbomer 974P, sodium chloride, tyloxapol, disodium edetate, sodium hydroxide and/or hydrochloric acid (for pH adjustment), purified water and benzalkonium chloride.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

Discard container 4 weeks after opening.
In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 25°C.

6.5 Nature and Contents of Container

Azopt Eye Drops 1.0% is available in LDPE bottle dispenser. Pack sizes: 1 x 5 mL and 1 x 10 mL.
Not all pack sizes may be marketed.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

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.

CAS number.

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (Schedule 4).

Summary Table of Changes