Brinzolamide 1% Ophth Susp 15ml

Manufacturer TEVA /ACTAVIS Active Ingredient Brinzolamide(brin ZOH la mide) Pronunciation brin-ZOH-la-mide
It is used to lower high eye pressure.
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Drug Class
Antiglaucoma Agent; Carbonic Anhydrase Inhibitor
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Pharmacologic Class
Carbonic Anhydrase Inhibitor
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Pregnancy Category
C
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FDA Approved
Apr 1998
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Brinzolamide is an eye drop used to lower high pressure inside the eye, which can be caused by conditions like glaucoma. It works by reducing the amount of fluid your eye produces.
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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 eye 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 using this medication. You can reinsert them 15 minutes after administration, 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 this medication at room temperature or in the refrigerator. Do not freeze.
2. Keep all medications in a safe location, out of the 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 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 take two doses at once or use extra doses to make up for a missed dose.
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Lifestyle & Tips

  • Shake the bottle well before each use.
  • Wash hands thoroughly before administering eye drops.
  • Do not touch the dropper tip to your eye or any other surface to prevent contamination.
  • If you wear contact lenses, remove them before instilling the drops and wait at least 15 minutes before reinserting them.
  • If using other eye drops, wait at least 5 minutes between applications.
  • Tilt your head back, pull down your lower eyelid to form a pocket, and instill one drop. Close your eye gently for 1-2 minutes to allow the medication to be absorbed.
  • Transient blurred vision may occur after instillation; avoid driving or operating machinery until vision clears.

Dosing & Administration

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Adult Dosing

Standard Dose: 1 drop in the affected eye(s) 3 times daily
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Pediatric Dosing

Neonatal: Not established
Infant: Not established (under 2 years)
Child: Not established (under 2 years); limited data for older children, consult specialist
Adolescent: Not established (under 2 years); limited data for older children, consult specialist
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended; monitor for systemic effects if severe impairment is present.
Moderate: No specific adjustment recommended; monitor for systemic effects if severe impairment is present.
Severe: Use with caution in patients with severe renal impairment (CrCl < 30 mL/min) due to potential for increased systemic exposure and acid-base disturbances. Not recommended by some sources.
Dialysis: Use with caution; monitor for systemic effects and acid-base balance.

Hepatic Impairment:

Mild: No specific adjustment recommended.
Moderate: No specific adjustment recommended.
Severe: No specific adjustment recommended; use with caution as systemic exposure is low but metabolism occurs in the liver.

Pharmacology

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Mechanism of Action

Brinzolamide is a carbonic anhydrase inhibitor (CAI). Carbonic anhydrase is found in the ciliary body of the eye, where it catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases the secretion of aqueous humor, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. This results in a reduction of intraocular pressure (IOP).
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Pharmacokinetics

Absorption:

Bioavailability: Not precisely quantified for ocular administration due to low systemic levels; systemic absorption occurs.
Tmax: Plasma concentrations are generally low and variable. Steady-state RBC concentrations are reached within 4 weeks.
FoodEffect: Not applicable for ophthalmic administration.

Distribution:

Vd: Not specifically reported for ophthalmic use; extensively bound to carbonic anhydrase in red blood cells (RBCs).
ProteinBinding: Approximately 60% in plasma.
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 111 days (in RBCs due to binding to carbonic anhydrase); plasma half-life is shorter but less clinically relevant.
Clearance: Primarily renal clearance of parent drug and metabolite.
ExcretionRoute: Renal (urine)
Unchanged: Significant portion excreted unchanged in urine.
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Pharmacodynamics

OnsetOfAction: Within 30 minutes
PeakEffect: 1-2 hours
DurationOfAction: Up to 12 hours

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while 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 severe effects associated with sulfa drugs, including:
+ Liver problems
+ Blood problems
+ Severe skin reactions (Stevens-Johnson syndrome/toxic epidermal necrolysis)
If you experience any of the following, call your doctor right away:
+ Rash
+ Red, swollen, blistered, or peeling skin
+ Red or irritated eyes
+ Sores in your mouth, throat, nose, or eyes
+ Fever, chills, or sore throat
+ New or worsening cough
+ 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 may cause side effects. Many people experience no side effects or only minor ones. If you notice any of the following side effects or any others that bother you or do not go away, contact your doctor or seek medical help:

Blurred vision
Bad taste in your mouth

Reporting Side Effects

This is not an exhaustive list of 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe eye pain or discomfort that worsens or does not resolve.
  • Sudden changes in vision.
  • Signs of an allergic reaction (e.g., rash, itching, swelling of the face/tongue/throat, severe dizziness, trouble breathing).
  • Persistent eye irritation, redness, or discharge.
  • Signs of systemic side effects (e.g., unusual tiredness, muscle weakness, irregular heartbeat, confusion, numbness/tingling in hands/feet - though rare with ophthalmic use).
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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 complications.
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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. Additionally, notify your doctor if you have an existing eye infection, have experienced an eye injury, or are scheduled to undergo eye surgery. 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.
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Overdose Information

Overdose Symptoms:

  • Systemic overdose from ophthalmic administration is unlikely due to low systemic absorption.
  • If significant systemic absorption occurs, symptoms could include electrolyte imbalance (e.g., acidosis), renal effects, and central nervous system effects (e.g., drowsiness, fatigue, headache).

What to Do:

In case of suspected overdose, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention. Treatment is supportive and symptomatic, focusing on correcting electrolyte imbalances and acidosis if present.

Drug Interactions

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Major Interactions

  • Oral carbonic anhydrase inhibitors (e.g., acetazolamide, methazolamide) - potential for additive systemic effects (acid-base disturbances, electrolyte imbalances).
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Moderate Interactions

  • High-dose salicylates - may increase systemic exposure of carbonic anhydrase inhibitors.

Monitoring

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Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline and assess treatment efficacy.

Timing: Prior to initiation of therapy.

Ocular Examination

Rationale: To assess ocular health and rule out other conditions.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly (e.g., 2-4 weeks after initiation, then periodically as determined by clinician)

Target: Individualized target IOP as determined by treating ophthalmologist.

Action Threshold: IOP not adequately controlled or increasing.

Ocular Examination

Frequency: Periodically, or as clinically indicated.

Target: Not applicable

Action Threshold: Development of new or worsening ocular symptoms or signs.

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Symptom Monitoring

  • Ocular discomfort (burning, stinging, itching)
  • Blurred vision (transient)
  • Taste disturbance (bitter, metallic, dysgeusia)
  • Dry eye
  • Foreign body sensation
  • Headache
  • Fatigue
  • Signs of systemic acidosis (rare with ophthalmic use, but possible with significant systemic absorption, especially in renal impairment)

Special Patient Groups

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Pregnancy

Pregnancy Category C. Use only if the potential benefit justifies the potential risk to the fetus. Studies in rabbits showed developmental toxicity at high systemic doses. While systemic absorption from ophthalmic use is low, caution is warranted.

Trimester-Specific Risks:

First Trimester: Potential risk based on animal studies; systemic exposure is low but caution advised.
Second Trimester: Potential risk based on animal studies; systemic exposure is low but caution advised.
Third Trimester: Potential risk based on animal studies; systemic exposure is low but caution advised.
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Lactation

It is unknown whether brinzolamide is excreted in human milk, although it is excreted in the milk of lactating rats. Caution should be exercised when brinzolamide is administered to a nursing woman. Weigh the developmental and health benefits of breastfeeding against 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 to moderate risk (L3 per Hale's), but manufacturer advises caution due to unknown excretion in human milk and potential for systemic effects in infant.
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Pediatric Use

Safety and effectiveness have not been established in pediatric patients younger than 2 years of age. Limited data exist for older pediatric patients; use should be under the guidance of a specialist.

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Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients. No specific dose adjustment is required based on age alone.

Clinical Information

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Clinical Pearls

  • Shake the bottle well before each use to ensure uniform suspension.
  • Brinzolamide is a sulfonamide; patients with a history of sulfonamide allergy should be monitored for hypersensitivity reactions, although topical administration reduces systemic exposure.
  • Can cause transient blurred vision immediately after instillation; advise patients to wait until vision clears before driving or operating machinery.
  • Some patients may experience a bitter or unusual taste (dysgeusia) after instillation due to nasolacrimal drainage.
  • Useful as monotherapy or adjunctive therapy for patients who cannot tolerate beta-blockers or for whom beta-blockers are contraindicated.
  • Monitor for signs of systemic carbonic anhydrase inhibition, such as acid-base imbalance or electrolyte disturbances, especially in patients with severe renal impairment or those receiving concomitant oral CAIs.
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Alternative Therapies

  • Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
  • Beta-adrenergic blockers (e.g., timolol, betaxolol)
  • Alpha-adrenergic agonists (e.g., brimonidine)
  • Other carbonic anhydrase inhibitors (e.g., dorzolamide ophthalmic solution)
  • Rho kinase inhibitors (e.g., netarsudil)
  • Miotics (e.g., pilocarpine)
  • Laser trabeculoplasty
  • Surgical interventions (e.g., trabeculectomy, glaucoma drainage devices)
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Cost & Coverage

Average Cost: Varies widely; typically $50-$150 for brand (Azopt), significantly less for generic. per 15ml bottle
Generic Available: Yes
Insurance Coverage: Tier 2 or 3 (generic often Tier 1 or 2, brand Tier 3 or higher)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, 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. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 detailed information about the overdose, including the substance taken, the amount, and the time it occurred.