Azopt 1% Ophth Susp 15ml
It is used to lower high eye pressure.
Drug Class
Antiglaucoma Agent
Pharmacologic Class
Carbonic Anhydrase Inhibitor
Pregnancy Category
C
FDA Approved
Apr 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Azopt 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. It's commonly used to treat glaucoma or ocular hypertension.
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 results, use this medication only in your eyes.
Preparation and Administration
1. Shake the container well before use.
2. Wash your hands thoroughly before and after handling the medication.
3. Remove your contact lenses before applying the medication. You can reinsert them 15 minutes after use, unless your eyes are irritated or infected.
4. 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.
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. This helps retain the medication in your eye.
Using Multiple Eye Medications
If you are using more than one medication in the same eye, allow at least 10 minutes to pass between applications.
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 disposal or potential drug take-back programs in your area.
Missed Dose
If you miss a dose, use 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 results, use this medication only in your eyes.
Preparation and Administration
1. Shake the container well before use.
2. Wash your hands thoroughly before and after handling the medication.
3. Remove your contact lenses before applying the medication. You can reinsert them 15 minutes after use, unless your eyes are irritated or infected.
4. 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.
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. This helps retain the medication in your eye.
Using Multiple Eye Medications
If you are using more than one medication in the same eye, allow at least 10 minutes to pass between applications.
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 disposal or potential drug take-back programs in your area.
Missed Dose
If you miss a dose, use 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
- Wash hands thoroughly before administering eye drops.
- Shake the bottle well before each use.
- Do not touch the dropper tip to any surface to avoid contamination.
- If using other eye drops, wait at least 5 minutes between applications.
- Remove contact lenses before applying drops and wait at least 15 minutes before reinserting them.
- Do not wear soft contact lenses if your eyes are irritated or inflamed.
- Store at room temperature, away from light and moisture.
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
Child:
Not established (Safety and efficacy not established in pediatric patients <18 years of age)
Adolescent:
Not established (Safety and efficacy not established in pediatric patients <18 years of age)
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
Use with caution; not studied in patients with severe renal impairment (CrCl <30 mL/min)
Dialysis:
Use with caution; not studied in patients on dialysis
Hepatic Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
No specific dosage adjustment recommendations; use with caution due to limited data
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:
Systemic absorption occurs after ocular administration, but is low. Plasma concentrations are generally low.
Tmax:
Approximately 1-2 hours (for systemic absorption after ocular dose)
FoodEffect:
Not applicable for ophthalmic suspension
Distribution:
Vd:
Not precisely quantified for ophthalmic use, but widely distributed in red blood cells due to high affinity for carbonic anhydrase.
ProteinBinding:
Approximately 60% (to plasma proteins)
CnssPenetration:
Limited (due to high binding to red blood cells and low systemic concentrations)
Elimination:
HalfLife:
Approximately 111 days (in red blood cells, due to strong binding to carbonic anhydrase); plasma half-life is much shorter.
Clearance:
Primarily renal excretion of unchanged drug and metabolites.
ExcretionRoute:
Renal (urine)
Unchanged:
Approximately 60% of the dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 2 hours
PeakEffect:
Approximately 2-3 hours
DurationOfAction:
Up to 24 hours
Safety & Warnings
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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in vision, eye pain, or severe eye irritation
Rare but potentially deadly 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 extremely tired or weak
- 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Blurred vision
* Bad taste in your mouth
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, don't hesitate to reach out to your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Changes in vision, eye pain, or severe eye irritation
Rare but potentially deadly 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 extremely tired or weak
- 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Blurred vision
* Bad taste in your mouth
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, don't hesitate to reach out to 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 eye infection (e.g., redness, swelling, discharge)
- Allergic reactions (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Unusual tiredness or weakness
- Numbness or tingling in hands or feet (rare, but possible systemic effect)
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 the medication's safety and efficacy.
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 with your other medications 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 the medication's safety and efficacy.
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 with your other medications 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:
- Electrolyte imbalance (e.g., acidosis)
- Development of a severe acidotic state
- Nervous system effects (e.g., drowsiness, confusion)
- Gastrointestinal upset (e.g., nausea, vomiting)
What to Do:
Overdose with ophthalmic administration is unlikely due to limited systemic absorption. If accidental ingestion occurs or systemic toxicity is suspected, treatment should be symptomatic and supportive. Monitor electrolyte levels and acid-base balance. Contact a poison control center immediately (e.g., 1-800-222-1222 in the US).
Drug Interactions
Moderate Interactions
- Oral Carbonic Anhydrase Inhibitors (e.g., acetazolamide, methazolamide)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess severity of glaucoma/ocular hypertension.
Timing: Prior to initiation of therapy
Visual Acuity
Rationale: To establish baseline visual function.
Timing: Prior to initiation of therapy
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by ophthalmologist (e.g., 2-4 weeks after initiation, then every 3-6 months)
Target: Individualized, typically <21 mmHg or target set by ophthalmologist
Action Threshold: IOP not adequately controlled, or significant increase from target
Ocular Examination (e.g., slit lamp, fundoscopy)
Frequency: Periodically, as determined by ophthalmologist
Target: Not applicable
Action Threshold: Signs of ocular irritation, inflammation, or other adverse effects
Symptom Monitoring
- Blurred vision
- Ocular discomfort (e.g., burning, stinging)
- Foreign body sensation
- Dry eye
- Headache
- Taste perversion (dysgeusia)
Special Patient Groups
Pregnancy
Brinzolamide is Pregnancy Category C. Studies in rabbits showed teratogenicity (fetal malformations) at doses 6 mg/kg/day (20 times the maximum recommended human ophthalmic dose). There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity based on animal studies; avoid if possible.
Second Trimester:
Limited human data; use with caution, weighing risks vs. benefits.
Third Trimester:
Limited human data; use with caution, weighing risks vs. benefits.
Lactation
It is not known whether brinzolamide is excreted in human milk. Systemic absorption occurs, and many drugs are excreted in human milk. Due to the potential for serious adverse reactions in nursing infants from brinzolamide, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Lactation risk is L3 (moderately safe).
Infant Risk:
Possible risk of systemic effects in infant, though unlikely with low systemic absorption from ophthalmic use. Monitor infant for drowsiness, poor feeding, or metabolic acidosis.
Pediatric Use
Safety and efficacy have not been established in pediatric patients younger than 18 years of age. Use is generally not recommended.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. No specific dosage adjustment is required.
Clinical Information
Clinical Pearls
- Shake the bottle well before each use to ensure uniform suspension.
- If patients experience blurred vision after instillation, advise them to wait until vision clears before driving or operating machinery.
- Patients with a history of sulfonamide allergy should be monitored closely, as brinzolamide is a sulfonamide. While systemic absorption is low, cross-reactivity is theoretically possible.
- Advise patients to avoid wearing soft contact lenses during treatment, or to remove them prior to instillation and wait 15 minutes before reinserting, due to the presence of benzalkonium chloride preservative.
- This medication is for ophthalmic use only; do not inject or swallow.
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)
- Combination products (e.g., Cosopt, Combigan)
Cost & Coverage
Average Cost:
Price varies, typically $100-$200 per 15ml bottle
Generic Available:
Yes
Insurance Coverage:
Often Tier 2 or Tier 3, may require prior authorization depending on plan.
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure 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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.