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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Brinzolamide
Generic Name
Brinzolamide
Active Ingredient
BrinzolamideCategory
Carbonic Anhydrase Inhibitor [EPC]
Variants
5
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Brinzolamide, you must consult a qualified healthcare professional.
| 10 mg/mL | SUSPENSION/ DROPS | OPHTHALMIC | 72162-2201 |
| 10 mg/mL | SUSPENSION/ DROPS | OPHTHALMIC | 24208-464 |
Detailed information about Brinzolamide
Brinzolamide is a highly specific carbonic anhydrase inhibitor [EPC] primarily used to reduce intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It works by decreasing aqueous humor secretion within the ciliary processes of the eye.
For the treatment of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension, the standard adult dosage of Brinzolamide 1% ophthalmic suspension is:
Clinical trials have demonstrated that dosing three times daily provides a consistent reduction in intraocular pressure throughout a 24-hour period. If Brinzolamide is being used as part of a multi-drug regimen, it is crucial to space the administration of different eye drops by at least 5 to 10 minutes to prevent the second drop from washing out the first.
The safety and effectiveness of Brinzolamide in pediatric patients have not been extensively established. While some studies have looked at its use in children with congenital or juvenile glaucoma, it is not currently FDA-approved for use in the pediatric population. Healthcare providers may use it off-label in specific cases, but this must be done under strict specialist supervision. Dosage for children, if prescribed, would be determined on a case-by-case basis by a pediatric ophthalmologist.
Brinzolamide has not been studied in patients with severe renal impairment (creatinine clearance < 30 mL/min). Because Brinzolamide and its metabolites are excreted primarily by the kidneys, its use is not recommended in patients with severe renal impairment. For patients with mild to moderate renal impairment, no specific dosage adjustment is typically required, but close monitoring is advised.
Brinzolamide has not been specifically studied in patients with hepatic impairment. While systemic levels are low, the drug is metabolized by liver enzymes. Caution should be exercised when prescribing Brinzolamide to patients with significant liver disease.
No overall differences in safety or effectiveness have been observed between elderly and younger patients. Standard adult dosing is generally appropriate for geriatric populations, provided renal function is adequate.
Proper administration technique is vital to ensure the medication reaches the target tissue and to minimize systemic absorption:
If you miss a dose of Brinzolamide, apply it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and return to your regular dosing schedule. Do not apply a double dose to make up for a missed one.
An ocular overdose is unlikely as the eye can only hold a limited amount of fluid. If the suspension is accidentally swallowed, symptoms of systemic carbonic anhydrase inhibition may occur, such as electrolyte imbalance, development of an acidotic state, and possible central nervous system effects.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop using the medication without medical guidance, as this could lead to a dangerous increase in eye pressure.
Brinzolamide is generally well-tolerated, but some patients may experience side effects. The most common side effect reported in clinical trials is:
These effects may occur in some patients and should be discussed with a doctor if they become bothersome:
Brinzolamide is a sulfonamide (a 'sulfa' drug). Even though it is administered as an eye drop, it is absorbed systemically. This means that the same types of adverse reactions attributable to systemic sulfonamides may occur with topical administration. Patients must be aware of the signs of serious allergic reactions. If any signs of serious reactions or hypersensitivity occur, discontinue use of this preparation immediately and consult a physician.
No FDA black box warnings for Brinzolamide.
Because Brinzolamide is a sulfonamide, it carries a risk of cross-reactivity. Patients with a known allergy to sulfa medications (such as Sulfamethoxazole/Trimethoprim) should not use Brinzolamide. Reactions can range from mild rashes to life-threatening anaphylaxis or severe dermatological conditions like Stevens-Johnson Syndrome.
Brinzolamide must NEVER be used in the following circumstances:
There are no adequate and well-controlled studies of Brinzolamide in pregnant women. Animal studies have shown that Brinzolamide can cause fetal toxicity (such as decreased fetal body weight and skeletal variations) when administered orally at doses much higher than the human ophthalmic dose.
It is not known whether Brinzolamide is excreted in human milk following topical ocular administration. However, many drugs are excreted in human milk, and systemic absorption does occur with Brinzolamide.
Brinzolamide is a highly potent inhibitor of Carbonic Anhydrase II (CA-II), the main intracellular enzyme involved in the transport of bicarbonate in the ciliary processes of the eye. By binding to the zinc-containing active site of the CA-II enzyme, Brinzolamide prevents the hydration of carbon dioxide. This results in a significant reduction in the production of bicarbonate ions. Since bicarbonate secretion is a primary driver of aqueous humor formation, its reduction leads to a decrease in fluid production and a subsequent lowering of intraocular pressure (IOP).
Common questions about Brinzolamide
Brinzolamide is primarily used to treat elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. By lowering the pressure inside the eye, it helps prevent damage to the optic nerve, which is essential for maintaining vision. It belongs to a class of drugs called carbonic anhydrase inhibitors, which work by reducing the production of fluid (aqueous humor) within the eye. Your doctor may prescribe it as a standalone treatment or in combination with other eye drops. It is specifically formulated as an ophthalmic suspension for topical use.
The most frequently reported side effect of Brinzolamide is temporary blurred vision immediately after applying the drops, which usually clears within a few minutes. Many patients also experience a bitter or unusual taste in their mouth, known as dysgeusia, caused by the medication draining into the throat. Other common effects include eye irritation, redness, or a feeling like something is in the eye. Some patients may also experience mild headaches or dry eyes. Most of these effects are mild, but you should inform your doctor if they persist or become severe.
There is no known direct interaction between Brinzolamide eye drops and alcohol consumption. Because Brinzolamide is applied topically to the eye, the amount that enters the bloodstream is very small. However, alcohol can sometimes affect eye pressure and overall hydration, which might influence your condition. Additionally, if you experience dizziness as a side effect of the medication, alcohol could potentially worsen this feeling. It is always best to consume alcohol in moderation and discuss your habits with your healthcare provider.
Brinzolamide is classified as FDA Pregnancy Category C, meaning there are no adequate studies in humans, but animal studies have shown potential risks at high doses. It should only be used during pregnancy if the potential benefit to the mother outweighs the potential risk to the fetus. If you are pregnant or planning to become pregnant, your doctor will carefully evaluate whether this is the best treatment for you. To minimize any risk, patients are advised to use nasolacrimal occlusion (pressing the corner of the eye) to reduce the amount of drug entering the systemic circulation. Always consult your obstetrician and ophthalmologist before use.
Brinzolamide begins to lower intraocular pressure relatively quickly, with the onset of action typically occurring within 1 to 2 hours after the first application. The peak effect, or the maximum reduction in eye pressure, is usually reached within 3 to 4 hours. However, it may take several days of consistent use to achieve a stable, long-term therapeutic effect on your eye pressure. It is important to use the medication exactly as prescribed, usually three times a day, to maintain consistent control over your glaucoma. Your doctor will schedule follow-up appointments to measure the drug's effectiveness.
You should never stop taking Brinzolamide suddenly without first consulting your ophthalmologist. Glaucoma is a 'silent' condition, meaning you often cannot feel the high pressure in your eye. If you stop the medication, your intraocular pressure may rise rapidly and significantly, which can cause irreversible damage to the optic nerve and lead to vision loss. If you are experiencing side effects that make you want to stop, contact your doctor immediately. They can help you transition to a different medication safely or adjust your current treatment plan.
If you miss a dose of Brinzolamide, apply the missed drop as soon as you remember. However, if it is almost time for your next scheduled dose, you should skip the missed dose and simply continue with your regular schedule. Do not apply two drops at once or use the medication more frequently to make up for the missed dose. Consistency is key in managing eye pressure, so try to use your drops at the same times each day. Setting an alarm on your phone can be a helpful way to remember your dosing schedule.
Weight gain is not a recognized or common side effect of Brinzolamide ophthalmic suspension. Because the medication is applied topically to the eye and systemic absorption is very low, it does not typically affect metabolism or appetite in a way that would lead to weight changes. If you experience unexplained weight gain while taking this medication, it is likely due to another cause or medication. You should discuss any significant changes in your weight or overall health with your primary care physician to determine the underlying cause.
Brinzolamide can interact with certain other medications, particularly oral carbonic anhydrase inhibitors like acetazolamide, which can increase the risk of systemic side effects. It may also have theoretical interactions with high-dose aspirin. If you are using other eye drops, you must wait at least 5 to 10 minutes between different medications to ensure they are both absorbed correctly. Always provide your doctor with a full list of all prescription drugs, over-the-counter medicines, and herbal supplements you are taking to avoid potential complications. Proper administration technique can help minimize the risk of interactions.
Yes, Brinzolamide 1% ophthalmic suspension is available as a generic medication. The generic version is bioequivalent to the brand-name drug (Azopt), meaning it contains the same active ingredient and works in the same way. Generic versions are typically more cost-effective for patients and are widely available at most pharmacies. When filling your prescription, you can ask your pharmacist if a generic version is available. Regardless of whether you use the brand or generic, the instructions for use and the safety precautions remain the same.
Other drugs with the same active ingredient (Brinzolamide)
Rare but documented side effects include:
While rare, serious reactions can occur. You must stop using Brinzolamide and contact your healthcare provider immediately if you experience:
> Warning: Stop taking Brinzolamide and call your doctor immediately if you experience any of these.
With prolonged use, some patients may develop chronic conjunctivitis or eyelid reactions. There is also a theoretical risk of systemic accumulation in red blood cells over months or years, although clinical complications from this sequestration are rarely observed in patients with healthy renal function. Long-term use requires regular monitoring of the corneal endothelium, especially in older adults or those with pre-existing corneal disease.
There are currently no FDA black box warnings for Brinzolamide. However, the labeling contains significant warnings regarding its nature as a sulfonamide and the potential for serious systemic reactions identical to those of oral sulfonamides.
Report any unusual symptoms to your healthcare provider. Even mild side effects can sometimes indicate a need for a change in treatment or administration technique.
The management of patients with acute angle-closure glaucoma requires immediate medical intervention to open the drainage angle. Brinzolamide has not been specifically studied in patients with acute angle-closure glaucoma and should not be used as the sole treatment for this emergency condition.
There have been reports of bacterial keratitis (infection of the cornea) associated with the use of multiple-dose containers of topical ophthalmic products. This is almost always due to the accidental contamination of the container by the patient. Always keep the dropper tip away from any surface.
Patients using Brinzolamide should undergo regular ophthalmic evaluations, including:
Brinzolamide may cause temporary blurred vision immediately after application. Do not drive, operate heavy machinery, or engage in hazardous activities until your vision has cleared. This usually takes only a few minutes.
There are no direct contraindications regarding alcohol use and Brinzolamide. However, alcohol can sometimes affect intraocular pressure and may exacerbate dizziness if you experience it as a side effect. It is best to discuss your alcohol consumption with your doctor.
Do not stop using Brinzolamide suddenly without consulting your ophthalmologist. Stopping the medication can cause a rapid rebound increase in intraocular pressure, which can damage the optic nerve. If you need to switch medications, your doctor will provide a specific tapering or transition schedule.
> Important: Discuss all your medical conditions, especially kidney disease, liver disease, and allergies, with your healthcare provider before starting Brinzolamide.
There are no known significant food interactions with Brinzolamide ophthalmic suspension, as the drug is applied topically and systemic levels remain very low. Unlike oral medications, its absorption is not affected by meals.
Brinzolamide is not known to interfere significantly with common laboratory tests. However, because it is a sulfonamide, it could theoretically interfere with certain urine tests for protein or sugar, although this is generally associated with oral sulfonamide administration.
For each major interaction, explain:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including those you only use occasionally.
Conditions requiring careful risk-benefit analysis include:
As mentioned, cross-sensitivity with other sulfonamides is the primary concern. This includes:
> Important: Your healthcare provider will evaluate your complete medical history, including all past allergic reactions, before prescribing Brinzolamide.
Brinzolamide is not approved for use in children. The safety and efficacy in patients under the age of 18 have not been established. In some clinical settings, it has been used off-label for congenital glaucoma, but this requires specialized pediatric ophthalmic care. There is a concern that systemic absorption in very small children could lead to metabolic acidosis due to their smaller blood volume and developing renal systems.
No overall differences in safety or effectiveness have been observed between elderly (65 and older) and younger patients. However, elderly patients are more likely to have reduced renal function and may be more susceptible to the effects of systemic absorption. They are also more likely to have compromised corneal endothelium, requiring closer monitoring for corneal edema.
As noted in the contraindications, Brinzolamide is not recommended for patients with a creatinine clearance less than 30 mL/min. For patients with CrCl between 30 and 60 mL/min, the drug should be used with caution, and electrolyte levels should be monitored if systemic symptoms appear.
There is no specific data for Brinzolamide in patients with hepatic impairment (Child-Pugh scores). While systemic levels are low, the liver is the site of metabolism. Use with caution in patients with moderate to severe hepatic disease.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you are pregnant, planning to become pregnant, or breastfeeding.
| Parameter | Value |
|---|---|
| Bioavailability | Low (Topical); High (Oral, but not used) |
| Protein Binding | ~60% in plasma; High affinity for RBC CA-II |
| Half-life | ~111 days (due to RBC binding) |
| Tmax | ~2 hours (in ocular tissues) |
| Metabolism | Hepatic via CYP3A4, 2A6, 2B6, 2C8, 2C9 |
| Excretion | Renal (primarily as unchanged drug) |
Brinzolamide is classified as a Carbonic Anhydrase Inhibitor [EPC]. It is part of a therapeutic class that includes other medications like Dorzolamide (topical) and Acetazolamide (oral). Within the glaucoma treatment hierarchy, it is often used as a second-line agent or as adjunctive therapy when prostaglandin analogs or beta-blockers are insufficient or contraindicated.