Brinzolamide

Generic name: brinzolamide ophthalmic
Brand name: Azopt
Dosage form: ophthalmic suspension (1%)
Drug class: Ophthalmic glaucoma agents

Medically reviewed by A Ras MD.

What is brinzolamide?

Brinzolamide is a prescription medicine that is used to lower high eye pressure.

Description

Brinzolamide ophthalmic suspension USP, 1% contains a carbonic anhydrase inhibitor formulated for

multidose topical ophthalmic use. Brinzolamide, USP is described chemically as: (R)-(+)-4-Ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno [3,2-e]-1,2-thiazine-6-sulfonamide-1,1- dioxide. Its molecular formula is C12H21N3O5S3, and its structural formula is:

Brinzolamide, USP has a molecular weight of 383.5 g/mol and a melting point of about 131°C. It is a white powder, which is insoluble in water, very soluble in methanol and soluble in ethanol.

Brinzolamide ophthalmic suspension USP, 1% is supplied as a sterile, aqueous suspension of brinzolamide which has been formulated to be readily suspended and slow settling, following shaking. It has a pH of approximately 7.5 and an osmolality of 300 mOsm/kg.

Each mL of Brinzolamide ophthalmic suspension USP, 1% contains: Active ingredient: brinzolamide USP, 10 mg. Preservative: Benzalkonium chloride 0.1 mg. Inactives: Carbomer homopolymer type B (974P), edetate disodium dihydrate, mannitol, sodium chloride, tyloxapol, and Water for Injection, with hydrochloric acid and/or sodium hydroxide to adjust pH.

Mechanism of Action

Carbonic anhydrase is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II, found primarily in red blood cells (RBCs), but also in other tissues. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in IOP.

Brinzolamide ophthalmic suspension 1% contains brinzolamide, an inhibitor of carbonic anhydrase II. Following topical ocular administration, brinzolamide inhibits aqueous humor formation and reduces elevated IOP. Elevated IOP is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss.

Before taking brinzolamide, tell your doctor:

If you are allergic to brinzolamide; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
If you have kidney disease.
If you are taking any of these drugs: Acetazolamide, dichlorphenamide, methazolamide, or zonisamide.
If you are breast-feeding or plan to breast-feed.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take brinzolamide with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take brinzolamide?

Tell all of your health care providers that you take brinzolamide. This includes your doctors, nurses, pharmacists, and dentists.
Use care when driving or doing other tasks that call for clear eyesight.
If you have a sulfa (sulfonamide) allergy, talk with your doctor.
Have your eye pressure and eyesight checked as you have been told by the doctor.
Tell your doctor if you have an eye infection, eye injury, or will be having eye surgery.
Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using brinzolamide while you are pregnant.

How is brinzolamide best taken?

Use brinzolamide as ordered by your doctor. Read all information given to you. Follow all instructions closely.

For the eye only.
Shake well before use.
Wash hands before and after use.
Take out contact lenses before using brinzolamide. Lenses may be put back in 15 minutes after brinzolamide is given. Do not put contacts back in if your eyes are irritated or infected.
Do not touch the container tip to the eye, lid, or other skin.
Tilt your head back and drop drug into the eye.
After use, keep your eyes closed. Put pressure on the inside corner of the eye. Do this for 1 to 2 minutes. This keeps the drug in your eye.
If more than 1 drug is being used in the same eye, use the drugs at least 10 minutes apart.

What do I do if I miss a dose?

Use a missed dose as soon as you think about it.
If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
Do not use 2 doses at the same time or extra doses.

What are the side effects of brinzolamide that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Change in eyesight, eye pain, or very bad eye irritation.
Rarely, very bad effects have happened with sulfa drugs. Sometimes, these have been deadly. These effects have included liver problems, blood problems, and very bad skin reactions (Stevens-Johnson syndrome/toxic epidermal necrolysis). Call your doctor right away if you have a rash; red, swollen, blistered, or peeling skin; red or irritated eyes; sores in your mouth, throat, nose, or eyes; fever, chills, or sore throat; cough that is new or worse; feeling very tired or weak; any bruising or bleeding; or signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.

What are some other side effects of brinzolamide?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Blurred eyesight.
Bad taste in your mouth.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out brinzolamide?

Store at room temperature or in a refrigerator. Do not freeze.
Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Label

PRINCIPAL DISPLAY PANEL

NDC 0591-2127-79
Brinzolamide Ophthalmic Suspension, USP
1%
For Topical Ophthalmic Use Only
Rx only
10 mL

SRC: NLM .

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