Consumer medicine information

What is in this leaflet

Read this leaflet carefully before you start to use Azopt Eye Drops.

This leaflet answers some common questions about Azopt. It does not contain all of the available information. It does not take the place of talking to your doctor or pharmacist.

The information in this leaflet was last updated on the date listed on the final page. More recent information on the medicine may be available.

You should ensure that you speak to your pharmacist or doctor to obtain the most up to date information on the medicine.

You can also download the most up to date leaflet from www.novartis.com.au

The updates may contain important information about the medicine and its use of which you should be aware.

All medicines have risks and benefits. Your doctor has weighed the expected benefits of you using Azopt against the risks this medicine could have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may need to read it again.

What Azopt is used for

Azopt Eye Drops contain the active ingredient brinzolamide, which belongs to a class of medicines known as "carbonic anhydrase inhibitors".

Azopt Eye Drops are used, either alone or in combination with other eye drops/medicines, to lower high pressure inside the eye(s) and to treat open-angle glaucoma or hypertension (high pressure) in the eye.

Glaucoma is a condition in which the pressure of fluid in the eye may be high. However, some people with glaucoma may have normal eye pressure.

Glaucoma is usually caused by a build up of the fluid which flows through the eye. This build up occurs because the fluid drains out of the eye more slowly than it is being pumped in. Since new fluid continues to enter the eye, joining the fluid already there, the pressure continues to rise. This raised pressure may damage the back of the eye resulting in gradual loss of sight. Damage can progress so slowly that the person is not aware of this gradual loss of sight. Sometimes even normal eye pressure is associated with damage to the back of the eye.

There are usually no symptoms of glaucoma. The only way of knowing that you have glaucoma is to have your eye pressure, optic nerve and visual field checked by an eye specialist or optometrist. If glaucoma is not treated, it can lead to serious problems, including total blindness. In fact, untreated glaucoma is one of the most common causes of blindness.

Azopt Eye Drops lower the pressure within the eye by reducing the production of fluid.

Although Azopt Eye Drops help to control your glaucoma, they do not cure it.

For more information about glaucoma, contact Glaucoma Australia Inc. (PO BOX 420, Crows Nest 1585 telephone 1800 500 880).

Ask your doctor if you have any questions about why Azopt has been prescribed for you. Your doctor may have prescribed it for another reason.

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

Azopt Eye Drops are not addictive.

Use in Children

Azopt Eye Drops are not recommended for use in children. The safety and effectiveness of Azopt Eye Drops in children has not been established.

Before you use Azopt

When you must not use it

Do not use Azopt if:

• You have an allergy to AZOPT Eye Drops or other medicines containing brinzolamide, other carbonic anhydrase inhibitors or any ingredients in Azopt Eye Drops that are listed at the end of this leaflet.
  If you think you may be allergic, ask your doctor or healthcare provider for advice.
  Some of the symptoms of an allergic reaction may include
  - shortness of breath
  - wheezing or difficulty breathing
  - swelling of the face, lips, tongue or other parts of the body
  - rash, itching or hives on the skin.
• You have severe kidney disease
• You have high levels of chloride in your blood (hyperchloraemia).

Do not take this medicine if the expiry date has passed, the packaging is torn or the safety seal around the closure and neck area is broken. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start using Azopt, talk to your doctor.

Before you start to take it

Tell your doctor if:

• You have an allergy to sulfonamide medicines
  The active ingredient of Azopt Eye Drops, brinzolamide, is a sulfur-containing medicine (a sulfonamide). If you are allergic to sulfur medicines, such as some antibiotics, medicines used to treat diabetes and also diuretics (water tablets), you may be allergic to Azopt Eye Drops. Check with your doctor or pharmacist if you are not sure whether you are allergic to sulfonamides.
• You are pregnant, or intend to become pregnant
  Your doctor will discuss the possible risks and benefits of using Azopt during pregnancy.
• You are breast-feeding or intend to breast-feed
  Your doctor will discuss the possible risks and benefits of using Azopt when you are breast-feeding.
• You have or have had any medical conditions such as problems with your liver or kidneys.
• You have impaired corneas which can occur in diabetes mellitus, low endothelial cell counts or in a condition called corneal dystrophies
  If you are unsure if you have any of these conditions ask your doctor.
• You have an allergy to any other medicines or any other substances, such as foods, preservatives or dyes.
• If you have or have had any severe skin reactions like skin rash, skin peeling, blistering of the lips, eyes or mouth.

If you have not told your doctor about any of the above, tell them before you use Azopt Eye Drops.

• Do not put Azopt Eye Drops into your eye(s) while you are wearing contact lenses.
  The preservative in Azopt Eye Drops, benzalkonium chloride, may cause eye irritation and is also known to discolour soft contact lenses.
  You can put your contact lenses back into your eyes 15 minutes after you have used Azopt Eye Drops.

Taking other medicines

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

Some medicines and Azopt Eye Drops may interfere with each other.

These include:

• Aspirin, in high doses
• High dose of salicylate-containing medicines which are used to relieve pain
• Other medicines known as "carbonic anhydrase inhibitors" that you take to treat glaucoma.

These medicines may be affected by Azopt Eye Drops or may affect how well it works. You may need different amounts of your medicines or you may need to take different medicines.

If you are taking another carbonic anhydrase inhibitor (acetazolamide or dorzolamide) or medicines that are nonsteroidal anti-inflammatory drugs (NSAIDs) or salicylates, talk to your doctor or healthcare provider.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

How to take Azopt

Use Azopt Eye Drops only as prescribed by your doctor.

Follow all directions given to you by your doctor or healthcare provider carefully. They may differ from the information contained in this leaflet.

Use Azopt Eye Drops only when prescribed by your doctor.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to use

The usual dose of Azopt Eye Drops is ONE DROP in the affected eye(s) TWICE A DAY. This will normally be in the morning and at night. Your doctor will tell you how many drops you need to use each day.

After using Azopt Eye Drops wait at least 5 minutes before putting any other eye drops in your eye(s). Eye ointment should be administered last.

If you are being changed from one eye drop to another, follow your doctor's instructions carefully as to when to stop the old drops and when to start the new drops.

If you are unsure about when, or how, to stop using Azopt Eye Drops you should talk to your doctor.

How to use Azopt

You may find it easier to use your eye drops if you are sitting or lying down.

If you are wearing contact lenses, remove them before putting the drops in your eye.

Follow these steps to use AZOPT Eye Drops:

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

6. While tilting your head back, gently pull down the lower eyelid of your eye to form a pouch/pocket.
7. Place the tip of the bottle close to your eye. Do not let it touch your eye.
8. 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).

9. Close your eye. Do not blink or rub your eye.
10. While 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 will help to stop the medicine from draining through the tear duct to the nose and throat, from where it can be absorbed into other parts of your body. This will also reduce the unpleasant taste sensation that some people experience when using these drops.
11. If necessary, repeat the above steps for the other eye.
12. Your eyelids can only hold less than one drop at a time, so it is normal for a small amount of the eye drop to spill onto your cheek. You should wipe away any spillage with a tissue.
13. Replace the cap on the bottle, closing it tightly.
14. Wash your hands again with soap and water to remove any residue.

You may feel a slight burning sensation in the eye shortly after using Azopt Eye Drops.

If this persists, or is very uncomfortable, contact your doctor or pharmacist.

Be careful not to touch the dropper tip against your eye, eyelid or anything else. This will help prevent the drops becoming dirty or contaminated.

After using Azopt Eye Drops, wait at least 5 minutes before putting any other eye drops in your eye(s).

Wait 15 minutes before replacing your contact lenses.

When to use it

Use Azopt Eye Drops at about the same time every day unless your doctor tells you otherwise.

Using your eye drops at the same time each day will have the best effect on your eye pressure. It will also help you remember when to use the eye drops.

How long to use it

Azopt Eye Drops help control your condition but will not cure it. Therefore Azopt Eye Drops must be used every day.

Continue using Azopt Eye Drops for as long as your doctor prescribes.

If you forget to take it

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

Otherwise, use the drops as soon as you remember, and then go back to the medicines as you would normally.

If you are not sure whether to skip the dose, talk to your doctor or pharmacist.

Do not use double the amount to make up for the dose that you missed. Using multiple doses may cause unwanted side effects.

If you use too much (overdose)

If you accidentally put several drops in your eye(s), immediately rinse your eye(s) with warm water.

If you think that you or anyone else may have swallowed any or all of the contents of a bottle of Azopt Eye Drops, immediately telephone your doctor or Poisons Information Centre on 131126 or go to Accident and Emergency at your nearest hospital.

Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention.

While you are using Azopt

Things you must do

To make sure that Azopt is working properly, have your eye pressure checked regularly.

Keep all your doctor’s appointments so that your progress can be checked.

If you develop an eye infection, receive an eye injury or have eye surgery tell your doctor.

If you notice signs of serious reactions or hypersensitivity including severe skin reaction such as skin rash, red skin, blistering of the lips, eyes or mouth, skin peeling and fever (signs of Stevens-Johnson syndrome or toxic epidermal necrolysis) discontinue the use of this medication and seek medical attention immediately.

Your doctor may tell you to use a new container of Azopt Eye Drops because of possible contamination of the old one, or may advise you to stop your treatment with Azopt Eye Drops.

If you become pregnant while using Azopt Eye Drops tell your doctor immediately.

If you are about to be started on any new medicine tell your doctor and pharmacist that you are using Azopt Eye Drops.

Tell all your doctors and pharmacists that you are using Azopt.

Things you must not do

Do not use Azopt Eye Drops to treat other complaints unless your doctor or pharmacist tells you to.

Do not give Azopt Eye Drops to anyone else, even if they appear to have the same condition as you.

Do not stop using Azopt Eye Drops without first talking to your doctor. If you stop using your eye drops, your eye pressure may rise again and damage to your eye may occur.

Do not let children handle Azopt Eye Drops. If a child accidentally swallows any of the drops read the instructions under "If you use too much (overdose)"

Things to be careful of

Be careful of driving or operating machinery until you know how Azopt Eye Drops affect you and your vision. As with any eye medicines, temporary blurred vision or other visual disturbances may affect the ability to drive and use machinery in some people. If blurred vision occurs when you use your drops, wait until your vision is clear before driving or operating machinery.

Side effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are using Azopt Eye Drops.

Azopt Eye Drops help most people with high eye pressure and glaucoma, but it may have unwanted side effects in a few people. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor or pharmacist if you notice any of the following effects in the eye(s) and the eye area and they worry you:

• Blurred or abnormal vision
• Discomfort, irritation or feeling of something in the eye(s)
• Redness of the eye(s)
• Dry eye(s)
• Eye pain
• Discharge from the eye(s)
• Itchy eye(s)
• Watering of the eye(s).

Additional side effects that can occur rarely include:

• Swelling of the clear front part of the eye(s)
• Red, itchy, irritated, crusty, swollen eyelid(s)
• Swelling of the skin around the eye(s)
• Crusty eyelashes
• Sticky sensation in the eye(s)
• Tired eye(s)
• Sensitivity to bright lights
• Double vision
• Seeing flashes or sparks of light
• Eye numbness.

Occasionally some people notice unwanted effects in the rest of their body as a result of using Azopt Eye Drops. These effects may include:

• Headache
• Chest pain, shortness of breath
• Unusual tiredness or weakness
• Dry mouth and/or nose
• Blocked or running nose
• Bleeding nose
• Sore throat, irritation and/or coughing
• Mucous in the chest
• Nausea, indigestion, diarrhoea and/or upset stomach
• Tingling, numbness and/or dizziness
• Depression
• Abnormal dreams
• Muscle stiffness
• Agitation
• Change in sensation of taste
• Loss of memory
• Nervousness
• Rash, itchy skin
• Hair loss
• Persistent noises in the ear(s)
• Impotence
• Kidney pain.

Tell your doctor immediately or go to Accident and Emergency at your nearest hospital if any of the following happen:

• Generalised itchiness
• Chest pain
• Shortness of breath
• Severe and sudden onset of pinkish, itchy swellings on the skin, also called hives or nettle rash.
• Skin rash, red skin, skin peeling, blistering of the lips, eyes or mouth, fever or any combination of these (Stevens-Johnson syndrome / toxic epidermal necrolysis)

These are hypersensitivity reactions and can be very serious side effects. You may need urgent medical attention or hospitalisation. These side effects are very rare.

Tell your doctor if you notice any other effects.

Other side effects not listed above may also occur in some patients.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using Azopt

Storage

Keep your eye drops in a cool place where the temperature stays below 25°C. Do not freeze the eye drops.

Do not store Azopt Eye Drops or any other medicine in the car, in the bathroom or in other warm, damp places. Heat and dampness can destroy some medicines.

A locked cupboard at least one and a half meters above the ground is a good place to store medicines.

Keep it where children cannot reach it.

Put the top back on the bottle right away after use to avoid contaminating the eye drops. Do not leave the top off the bottle for any length of time.

Disposal

Write the date on the bottle when you open the eye drops and throw out any remaining solution after four weeks.

Open a new bottle every four weeks. Eye drops contain a preservative which helps prevent germs growing in the solution for the first four weeks after opening the bottle. After this time there is a greater risk that the drops may become contaminated and cause an eye infection.

If your doctor tells you to stop using the eye drops or they have passed their expiry date, ask your pharmacist what to do with any remaining solution.

Product description

What it looks like

Azopt Eye Drops is a sterile suspension that comes in a 5mL dropper bottle with screw cap.

The safety seal must be removed before use.

Ingredients

The active ingredient in Azopt is brinzolamide 10 mg/mL (1.0%).

It also contains the inactive ingredients:

• mannitol
• carbomer 974P
• sodium chloride
• tyloxapol
• disodium edetate
• sodium hydroxide and/or hydrochloric acid (to adjust pH)
• purified water
• benzalkonium chloride 0.1 mg/mL (as a preservative),

Supplier

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

Australian registration number
AUST R 72750.

Date of preparation

This leaflet was prepared in November 2023.

® Registered Trademark

© Novartis Pharmaceuticals Australia Pty Limited 2022.

Internal document code

(azo091123c) based on PI (azo091123i)

Published by MIMS December 2023

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