Brinzolamide 1% Ophth Susp 10ml
It is used to lower high eye pressure.
Drug Class
Antiglaucoma Agent
Pharmacologic Class
Carbonic Anhydrase Inhibitor, Ophthalmic
Pregnancy Category
Category C
FDA Approved
Apr 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Brinzolamide is an eye drop used to lower high pressure inside the eye, which can be caused by glaucoma or other eye conditions. It works by reducing the amount of fluid produced in the eye.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. This medication is for ophthalmic use only.
Preparation and Administration
1. Shake the container well before use.
2. Wash your hands before and after handling the medication.
3. Remove contact lenses before administering the medication. You can reinsert your lenses 15 minutes after use, unless your eyes are irritated or infected.
4. Avoid touching the container tip to your eye, lid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
5. Tilt your head back and gently drop the medication into your eye.
6. After administration, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Using Multiple Eye Medications
If you are using more than one medication in the same eye, administer them at least 10 minutes apart.
Storage and Disposal
1. Store the medication at room temperature or in the refrigerator. Do not freeze.
2. Keep all medications in a safe and secure location, out of reach of children and pets.
3. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on proper disposal, and consider participating in local drug take-back programs.
Missed Dose Instructions
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not use two doses at once or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. This medication is for ophthalmic use only.
Preparation and Administration
1. Shake the container well before use.
2. Wash your hands before and after handling the medication.
3. Remove contact lenses before administering the medication. You can reinsert your lenses 15 minutes after use, unless your eyes are irritated or infected.
4. Avoid touching the container tip to your eye, lid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
5. Tilt your head back and gently drop the medication into your eye.
6. After administration, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Using Multiple Eye Medications
If you are using more than one medication in the same eye, administer them at least 10 minutes apart.
Storage and Disposal
1. Store the medication at room temperature or in the refrigerator. Do not freeze.
2. Keep all medications in a safe and secure location, out of reach of children and pets.
3. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on proper disposal, and consider participating in local drug take-back programs.
Missed Dose Instructions
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not use two doses at once or take extra doses.
Lifestyle & Tips
- Shake the bottle well before each use.
- Wash hands thoroughly before administering eye drops.
- Do not touch the dropper tip to the eye or any other surface to avoid contamination.
- If using other eye drops, wait at least 5 minutes between applications.
- Remove contact lenses before using this medication and wait at least 15 minutes after instilling the drops before reinserting contact lenses.
- Do not wear soft contact lenses if your eyes are irritated or inflamed.
- Follow your doctor's instructions regarding regular eye exams and IOP measurements.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
One drop in the affected eye(s) three times daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
Use with caution in patients with severe renal impairment (CrCl < 30 mL/min) due to potential for systemic accumulation of brinzolamide and its metabolite.
Dialysis:
Use with caution; systemic exposure may be increased. Monitoring for systemic effects is advised.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended; however, caution is advised as brinzolamide is metabolized in the liver.
Pharmacology
Mechanism of Action
Brinzolamide is a carbonic anhydrase inhibitor (CAI) that works by reversibly inhibiting the enzyme carbonic anhydrase (CA) in the ciliary body of the eye. This inhibition reduces the formation of bicarbonate ions and the subsequent transport of sodium and fluid, thereby decreasing the secretion of aqueous humor. The reduction in aqueous humor secretion leads to a decrease in intraocular pressure (IOP).
Pharmacokinetics
Absorption:
Bioavailability:
Not available (systemic absorption occurs after ocular administration)
Tmax:
Plasma concentrations are generally low and variable after ocular administration. Brinzolamide accumulates in red blood cells (RBCs).
FoodEffect:
Not applicable for ophthalmic administration.
Distribution:
Vd:
Not available (accumulates in RBCs)
ProteinBinding:
Approximately 60% bound to plasma proteins.
CnssPenetration:
Limited (low systemic concentrations, but some potential for CNS effects with systemic absorption).
Elimination:
HalfLife:
Approximately 111 days (in red blood cells, reflecting binding to CA-I); plasma half-life is shorter but not precisely defined due to low plasma levels.
Clearance:
Not precisely quantified for ophthalmic route.
ExcretionRoute:
Primarily renal (unchanged drug and metabolite).
Unchanged:
Approximately 60% of the dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 2 hours
PeakEffect:
Within 2-4 hours
DurationOfAction:
Approximately 8-12 hours (consistent with three times daily dosing)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in eyesight, eye pain, or severe eye irritation
Rare but serious effects associated with sulfa drugs, including:
+ Liver problems
+ Blood problems
+ Severe skin reactions (Stevens-Johnson syndrome/toxic epidermal necrolysis)
+ Symptoms may include:
- 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
- Signs of liver problems, such as:
- Dark urine
- Tiredness
- Decreased appetite
- Upset stomach or stomach pain
- Light-colored stools
- Vomiting
- Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Blurred eyesight
* Bad taste in your mouth
Reporting Side Effects
This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in eyesight, eye pain, or severe eye irritation
Rare but serious effects associated with sulfa drugs, including:
+ Liver problems
+ Blood problems
+ Severe skin reactions (Stevens-Johnson syndrome/toxic epidermal necrolysis)
+ Symptoms may include:
- 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
- Signs of liver problems, such as:
- Dark urine
- Tiredness
- Decreased appetite
- Upset stomach or stomach pain
- Light-colored stools
- Vomiting
- Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Blurred eyesight
* Bad taste in your mouth
Reporting Side Effects
This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe eye pain or discomfort
- Sudden vision changes
- Signs of an allergic reaction (e.g., rash, itching, swelling of the face, lips, or tongue, difficulty breathing)
- Persistent eye redness or irritation
- Signs of infection (e.g., discharge, swelling, increased pain)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have kidney disease, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: Acetazolamide, dichlorphenamide, methazolamide, or zonisamide, as these may interact with this drug.
To ensure safe treatment, it is crucial to disclose all of your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
Vitamins
Additionally, inform your doctor about any existing health problems. This information will help your doctor and pharmacist determine whether it is safe for you to take this medication in combination with your other drugs and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have kidney disease, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: Acetazolamide, dichlorphenamide, methazolamide, or zonisamide, as these may interact with this drug.
To ensure safe treatment, it is crucial to disclose all of your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
Vitamins
Additionally, inform your doctor about any existing health problems. This information will help your doctor and pharmacist determine whether it is safe for you to take this medication in combination with your other drugs and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. When performing tasks that require clear vision, such as driving, exercise caution to ensure your safety. If you have a known allergy to sulfa (sulfonamide) medications, consult with your doctor to discuss potential risks. Regularly schedule appointments with your doctor to monitor your eye pressure and vision, as advised. Notify your doctor if you experience an eye infection, suffer an eye injury, or are scheduled to undergo eye surgery. Additionally, if you are pregnant, planning to become pregnant, or are breastfeeding, consult with your doctor to weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- While systemic overdose from ophthalmic administration is unlikely due to low systemic absorption, potential symptoms could include electrolyte imbalance (e.g., acidosis), renal impairment, or central nervous system effects (e.g., drowsiness, fatigue).
What to Do:
In case of accidental ingestion or suspected overdose, contact a poison control center immediately (e.g., 1-800-222-1222) or seek emergency medical attention. Treatment is supportive and symptomatic.
Drug Interactions
Moderate Interactions
- Oral Carbonic Anhydrase Inhibitors (e.g., acetazolamide, methazolamide)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess the need for treatment.
Timing: Prior to initiation of therapy.
Ocular Examination
Rationale: To assess overall eye health and identify any pre-existing conditions.
Timing: Prior to initiation of therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by the treating physician (e.g., 2-4 weeks after initiation, then every 3-6 months).
Target: Individualized, typically aiming for a significant reduction from baseline IOP.
Action Threshold: If target IOP is not achieved or maintained, consider dose adjustment, addition of another agent, or alternative therapy.
Ocular Examination
Frequency: Periodically, as clinically indicated.
Target: Not applicable
Action Threshold: Any signs of ocular irritation, inflammation, or other adverse reactions.
Symptom Monitoring
- Blurred vision (transient)
- Eye discomfort/irritation
- Foreign body sensation
- Ocular hyperemia (redness)
- Dysgeusia (bitter, sour, or unusual taste)
- Dry eye
- Headache
- Signs of allergic reaction (e.g., rash, itching, swelling of face/lips/tongue)
- Signs of systemic carbonic anhydrase inhibition (rare, but possible with significant systemic absorption): fatigue, malaise, paresthesia, acid-base disturbances.
Special Patient Groups
Pregnancy
Brinzolamide is classified as Pregnancy Category C. Animal studies have shown adverse effects on fetal development at maternally toxic doses. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity based on animal data; human data lacking.
Second Trimester:
Potential for developmental toxicity based on animal data; human data lacking.
Third Trimester:
Potential for developmental toxicity based on animal data; human data lacking.
Lactation
It is not known whether brinzolamide is excreted in human milk. However, due to low systemic absorption after ocular administration, excretion into breast milk is expected to be minimal. Caution should be exercised when brinzolamide is administered to a nursing woman. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for brinzolamide and any potential adverse effects on the breastfed infant from brinzolamide or from the underlying maternal condition.
Infant Risk:
Low risk due to minimal systemic absorption and expected low levels in breast milk. Monitor infant for potential adverse effects, though unlikely.
Pediatric Use
Safety and effectiveness in pediatric patients under 18 years of age have not been established. Use is generally not recommended in this population.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger adult patients. Dosage adjustment is generally not required based on age alone.
Clinical Information
Clinical Pearls
- Instruct patients to shake the bottle well before each use, as it is a suspension.
- Transient blurred vision is a common side effect immediately after instillation; advise patients to wait until vision clears before driving or operating machinery.
- Some patients may experience a bitter, sour, or unusual taste (dysgeusia) after instillation due to nasolacrimal drainage; this is generally transient.
- Brinzolamide is a sulfonamide. Patients with a history of sulfonamide allergy should be monitored for hypersensitivity reactions, although topical administration generally carries a lower risk of systemic reactions compared to oral sulfonamides.
- If patients wear contact lenses, they should remove them before instilling the drops and wait at least 15 minutes before reinserting them.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Beta-blockers (e.g., timolol, betaxolol)
- Alpha-adrenergic agonists (e.g., brimonidine)
- Other carbonic anhydrase inhibitors (e.g., dorzolamide)
- Rho kinase inhibitors (e.g., netarsudil)
- Miotics (e.g., pilocarpine)
Cost & Coverage
Average Cost:
$50 - $150 per 10ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.