Azopt 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 damage your vision. It works by reducing the amount of fluid your eye makes.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. For optimal use:
Use this medication only in the eye.
Shake the container well before each use.
Wash your hands before and after handling the medication.
Remove contact lenses before applying the medication. You can reinsert your lenses 15 minutes after use, unless your eyes are irritated or infected.
Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
Administration Technique
1. Tilt your head back and gently drop the medication into your eye.
2. After application, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes. This helps retain the medication 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
Store this medication at room temperature or in the refrigerator. Do not freeze.
Keep all medications in a secure location, out of the reach of children and pets.
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 or potential drug take-back programs in your area.
Missed Dose
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 the information provided. For optimal use:
Use this medication only in the eye.
Shake the container well before each use.
Wash your hands before and after handling the medication.
Remove contact lenses before applying the medication. You can reinsert your lenses 15 minutes after use, unless your eyes are irritated or infected.
Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
Administration Technique
1. Tilt your head back and gently drop the medication into your eye.
2. After application, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes. This helps retain the medication 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
Store this medication at room temperature or in the refrigerator. Do not freeze.
Keep all medications in a secure location, out of the reach of children and pets.
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 or potential drug take-back programs in your area.
Missed Dose
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.
- 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.
- Avoid touching the dropper tip to your eye or any other surface to prevent contamination.
- If using other eye drops, wait at least 5 minutes between applications.
- Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
- Do not wear contact lenses if your eyes are red or irritated.
- Report any new or worsening eye symptoms, such as pain, redness, or vision changes, to your doctor immediately.
- Some people may experience a bitter or unusual taste in their mouth after using these drops; this is a common side effect and usually temporary.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
1 drop in the affected eye(s) 3 times daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants under 2 years of age
Child:
For patients 2 years of age and older: 1 drop in the affected eye(s) 3 times daily
Adolescent:
1 drop in the affected eye(s) 3 times daily
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
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.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No specific studies, but unlikely to require adjustment due to minimal systemic metabolism.
Pharmacology
Mechanism of Action
Brinzolamide is a carbonic anhydrase inhibitor (CAI) that works by inhibiting the enzyme carbonic anhydrase in the ciliary body of the eye. This inhibition reduces the formation of bicarbonate ions, which in turn reduces sodium and fluid transport, leading to a decrease in aqueous humor secretion. The net effect is a reduction in intraocular pressure (IOP).
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption after ocular administration. Peak plasma concentrations are very low (typically < 10 ng/mL).
Tmax:
Plasma Tmax: Approximately 1-2 hours after ocular administration. RBC Tmax: Longer, due to extensive binding to carbonic anhydrase in red blood cells.
FoodEffect:
Not applicable for ophthalmic administration.
Distribution:
Vd:
Not readily quantifiable due to extensive binding to carbonic anhydrase in red blood cells (RBCs). Brinzolamide distributes into RBCs, where it binds to carbonic anhydrase.
ProteinBinding:
Approximately 60% bound to plasma proteins.
CnssPenetration:
Limited systemic penetration; however, systemic CAI effects (e.g., taste disturbance) can occur.
Elimination:
HalfLife:
RBC half-life: Approximately 111 days (reflects systemic accumulation and binding). Plasma half-life: Shorter, but less clinically relevant due to RBC binding.
Clearance:
Primarily renal clearance of unchanged drug and metabolite.
ExcretionRoute:
Renal (urine)
Unchanged:
Approximately 60% of the dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 30 minutes
PeakEffect:
Approximately 2 hours
DurationOfAction:
Up to 24 hours (allows for TID 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 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 other unusual symptoms, contact your doctor or seek medical help if they bother you or do not go away:
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.
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 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 other unusual symptoms, contact your doctor or seek medical help if they bother you or do not go away:
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.
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/tongue/throat, severe dizziness, trouble breathing)
- New or worsening eye redness or irritation
- Signs of systemic carbonic anhydrase inhibition (e.g., unusual tiredness, muscle weakness, numbness/tingling, kidney stones, severe skin reactions, blood dyscrasias - though rare with ophthalmic use)
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 allergic reaction you experienced, including any symptoms that occurred.
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 medications and health conditions. Never 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 allergic reaction you experienced, including any symptoms that occurred.
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 medications and health conditions. Never 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 minimal absorption, theoretical symptoms could include electrolyte imbalance (acidosis), renal effects, and central nervous system effects (e.g., drowsiness, fatigue).
What to Do:
In case of accidental ingestion or suspected overdose, contact a poison control center (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): Concomitant use is not recommended due to potential for additive systemic effects of carbonic anhydrase inhibition.
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess the need for treatment.
Timing: Prior to initiating therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by the ophthalmologist (e.g., 2-4 weeks after initiation, then every 3-6 months).
Target: Individualized target IOP, typically < 21 mmHg or a significant reduction from baseline.
Action Threshold: If IOP is not adequately controlled or continues to rise, consider alternative or additional therapy.
Ocular Examination (e.g., slit lamp, fundoscopy)
Frequency: Periodically, as determined by the ophthalmologist.
Target: Not applicable
Action Threshold: Any signs of ocular irritation, inflammation, or other adverse reactions.
Symptom Monitoring
- Blurred vision
- Ocular discomfort (e.g., stinging, burning)
- Foreign body sensation
- Ocular discharge
- Dry eye
- Taste disturbance (bitter, sour, or unusual taste)
- Headache
- Dizziness
- Fatigue
- Hypersensitivity reactions (e.g., rash, itching, redness)
Special Patient Groups
Pregnancy
Brinzolamide is classified as Pregnancy Category C. Studies in rabbits showed teratogenicity (fetal malformations) at doses much higher than the maximum recommended human ophthalmic dose. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity observed in animal studies; use only if clearly needed.
Second Trimester:
Use with caution; systemic absorption is minimal but cannot be entirely ruled out.
Third Trimester:
Use with caution; potential for systemic effects on the fetus, though unlikely with ophthalmic use.
Lactation
It is unknown whether brinzolamide or its metabolites are excreted in human milk. Systemic absorption is minimal, but caution is advised. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Azopt and any potential adverse effects on the breastfed infant from Azopt or from the underlying maternal condition. L3 (Moderately Safe).
Infant Risk:
Low risk of adverse effects on the infant due to minimal systemic absorption, but potential for systemic carbonic anhydrase inhibitor effects cannot be entirely excluded. Monitor infant for drowsiness, poor feeding, or unusual symptoms.
Pediatric Use
Safety and efficacy have been established in pediatric patients 2 years of age and older. Use in pediatric patients younger than 2 years of age is not recommended due to insufficient data.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. No specific dose adjustment is required for geriatric patients.
Clinical Information
Clinical Pearls
- Instruct patients to shake the bottle well before each use, as it is a suspension.
- Advise patients about the potential for a bitter or unusual taste after instillation, which is a common and usually transient side effect.
- Remind patients to remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
- Brinzolamide is a sulfonamide. Patients with a history of sulfonamide hypersensitivity should be monitored for potential allergic reactions, although topical administration reduces systemic exposure.
- Consider the potential for additive systemic effects if the patient is also taking an oral carbonic anhydrase inhibitor.
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)
- Cholinergic Agonists (e.g., pilocarpine)
- Combination products (e.g., Cosopt, Combigan)
Cost & Coverage
Average Cost:
$150 - $250 per 10mL bottle (brand)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for brand); Tier 1 (for generic)
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 is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not 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 medication taken, the amount, and the time it occurred.