Brimonid/timol 0.2/0.5% Op Sol 5ml
It is used to treat glaucoma.It is used to lower high eye pressure.
Drug Class
Antiglaucoma agent, Ophthalmic
Pharmacologic Class
Alpha-2 adrenergic agonist / Non-selective beta-adrenergic blocker (ophthalmic)
Pregnancy Category
Category C
FDA Approved
Oct 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
This eye drop contains two medicines, brimonidine and timolol, that work together to lower the pressure inside your eye. High eye pressure can damage your optic nerve and lead to vision loss (glaucoma). This medication helps reduce the amount of fluid your eye makes and helps fluid drain better, which lowers the pressure.
How to Use This Medicine
Proper Use of This Medication
To use this eye medication correctly, follow your doctor's instructions and read the information provided. For optimal results, use the medication as directed.
Apply the medication only to the eye.
Remove contact lenses before using the medication and wait 15 minutes before putting them back in. However, if your eyes are irritated or infected, do not put your contact lenses back in.
To prevent contamination and potential severe eye problems or vision loss, avoid touching the container tip to the eye, lid, or surrounding skin.
Wash your hands thoroughly before and after using the medication.
Tilt your head back, drop the medication into the eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of the eye for 1 to 2 minutes to help the medication stay in the eye. Gently blot any excess solution from the eyelid.
If you are using multiple medications in the same eye, allow at least a 5-minute interval between each application.
Continue using the medication as directed, even if your symptoms improve.
Do not use the medication if the solution has changed color, is cloudy, leaking, or contains particles.
Storage and Disposal
To maintain the medication's effectiveness and safety:
Store the medication at room temperature, protected from light and moisture. Avoid storing it in a bathroom.
Keep the medication out of the reach of children and pets.
* Dispose of unused or expired medication properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so. Consult your pharmacist for guidance on the best disposal method, and consider participating in local drug take-back programs.
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 the same time or take extra doses.
To use this eye medication correctly, follow your doctor's instructions and read the information provided. For optimal results, use the medication as directed.
Apply the medication only to the eye.
Remove contact lenses before using the medication and wait 15 minutes before putting them back in. However, if your eyes are irritated or infected, do not put your contact lenses back in.
To prevent contamination and potential severe eye problems or vision loss, avoid touching the container tip to the eye, lid, or surrounding skin.
Wash your hands thoroughly before and after using the medication.
Tilt your head back, drop the medication into the eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of the eye for 1 to 2 minutes to help the medication stay in the eye. Gently blot any excess solution from the eyelid.
If you are using multiple medications in the same eye, allow at least a 5-minute interval between each application.
Continue using the medication as directed, even if your symptoms improve.
Do not use the medication if the solution has changed color, is cloudy, leaking, or contains particles.
Storage and Disposal
To maintain the medication's effectiveness and safety:
Store the medication at room temperature, protected from light and moisture. Avoid storing it in a bathroom.
Keep the medication out of the reach of children and pets.
* Dispose of unused or expired medication properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so. Consult your pharmacist for guidance on the best disposal method, and consider participating in local drug take-back programs.
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 the same time or take extra doses.
Lifestyle & Tips
- Administer drops consistently, approximately 12 hours apart.
- 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.
- Wash hands thoroughly before and after use.
- Avoid touching the dropper tip to the eye or any other surface to prevent contamination.
- Apply gentle pressure to the tear duct (inner corner of the eye) for 1-2 minutes after instillation to minimize systemic absorption and potential side effects.
- Inform your doctor about all other medications you are taking, especially heart or blood pressure medications, or any history of asthma, COPD, or heart conditions.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
One drop in the affected eye(s) twice daily, approximately 12 hours apart.
Condition-Specific Dosing:
glaucoma:
One drop in the affected eye(s) twice daily, approximately 12 hours apart.
Pediatric Dosing
Neonatal:
Not established (contraindicated in infants <2 years due to risk of apnea and bradycardia with brimonidine)
Infant:
Not established (contraindicated in infants <2 years due to risk of apnea and bradycardia with brimonidine)
Child:
Not established (contraindicated in children <2 years; caution in children 2-12 years due to potential for systemic effects)
Adolescent:
One drop in the affected eye(s) twice daily, approximately 12 hours apart (use with caution, monitor for systemic effects)
Dose Adjustments
Renal Impairment:
Mild:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Moderate:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Severe:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Dialysis:
Use with caution; systemic exposure may be increased. Monitor for systemic adverse effects.
Hepatic Impairment:
Mild:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Moderate:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Severe:
No specific dosage adjustment recommended, but use with caution due to potential for increased systemic exposure.
Pharmacology
Mechanism of Action
Brimonidine is an alpha-2 adrenergic agonist that reduces aqueous humor production and increases uveoscleral outflow. Timolol is a non-selective beta-adrenergic receptor blocker that reduces aqueous humor production. The combination provides an additive effect in reducing elevated intraocular pressure (IOP).
Pharmacokinetics
Absorption:
Bioavailability:
Not available (ophthalmic, systemic absorption occurs)
Tmax:
Brimonidine: 1-4 hours (plasma); Timolol: 1-3 hours (plasma)
FoodEffect:
Not applicable (ophthalmic)
Distribution:
Vd:
Not available (ophthalmic)
ProteinBinding:
Brimonidine: Approximately 29%; Timolol: Approximately 60%
CnssPenetration:
Limited (both can cross blood-brain barrier to some extent, leading to CNS effects)
Pharmacodynamics
OnsetOfAction:
Within 30 minutes
PeakEffect:
Approximately 2-8 hours
DurationOfAction:
Up to 12 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Slow heartbeat
Abnormal heartbeat
Chest pain
Dizziness or fainting
Muscle weakness
Heart problems, which can be rare but potentially deadly. If you experience:
+ Shortness of breath
+ Sudden significant weight gain
+ Swelling in the arms or legs
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Eye irritation
Itching
* Burning or stinging
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Slow heartbeat
Abnormal heartbeat
Chest pain
Dizziness or fainting
Muscle weakness
Heart problems, which can be rare but potentially deadly. If you experience:
+ Shortness of breath
+ Sudden significant weight gain
+ Swelling in the arms or legs
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Eye irritation
Itching
* Burning or stinging
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 sudden vision changes
- Signs of an allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Very slow heart rate (bradycardia)
- Dizziness or fainting
- Shortness of breath or wheezing (especially if new or worsening)
- Chest pain
- Severe fatigue or depression
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. Be sure to describe the symptoms you experienced.
Certain health conditions, such as:
+ Breathing problems, including asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (weak heart)
+ Shock caused by heart problems
+ Slow heartbeat
* If you are currently using another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
Special Considerations for Children:
If the patient is under 2 years of age, do not administer this medication. It is not recommended for children younger than 2 years old.
Additional Precautions:
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. Verify that it is safe to take this medication with your existing medications and health conditions. Never start, stop, or modify the dosage of any medication without consulting 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. Be sure to describe the symptoms you experienced.
Certain health conditions, such as:
+ Breathing problems, including asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (weak heart)
+ Shock caused by heart problems
+ Slow heartbeat
* If you are currently using another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
Special Considerations for Children:
If the patient is under 2 years of age, do not administer this medication. It is not recommended for children younger than 2 years old.
Additional Precautions:
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. Verify that it is safe to take this medication with your existing medications and health conditions. Never start, stop, or modify the dosage of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness or clear vision, such as driving, wait until you understand how this drug affects you.
This medication may mask certain symptoms of low blood sugar, including a rapid heartbeat, which can increase the risk of severe or prolonged hypoglycemia. This risk is particularly elevated in individuals with diabetes, children, and those who are fasting, undergoing surgery, have a poor appetite, or are experiencing vomiting. If you have any questions or concerns, consult your doctor.
Regularly schedule appointments with your doctor to monitor your eye pressure and vision, as advised. Additionally, notify your doctor if you have an eye infection, eye injury, or are scheduled to undergo eye surgery.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, discuss the potential risks with your doctor.
Although rare, this medication has been associated with severe respiratory problems, which can be life-threatening, particularly in individuals with asthma. If you have any questions or concerns, consult your doctor.
If you have a history of severe allergic reactions, inform your doctor, as you may be at risk of an even more severe reaction if you are exposed to the allergen again. Furthermore, if you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
This drug may also make it more challenging to recognize symptoms of hyperthyroidism, such as a rapid heartbeat. If you have hyperthyroidism and suddenly stop taking this medication, your condition may worsen and become life-threatening. Consult your doctor for guidance.
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
This medication may mask certain symptoms of low blood sugar, including a rapid heartbeat, which can increase the risk of severe or prolonged hypoglycemia. This risk is particularly elevated in individuals with diabetes, children, and those who are fasting, undergoing surgery, have a poor appetite, or are experiencing vomiting. If you have any questions or concerns, consult your doctor.
Regularly schedule appointments with your doctor to monitor your eye pressure and vision, as advised. Additionally, notify your doctor if you have an eye infection, eye injury, or are scheduled to undergo eye surgery.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, discuss the potential risks with your doctor.
Although rare, this medication has been associated with severe respiratory problems, which can be life-threatening, particularly in individuals with asthma. If you have any questions or concerns, consult your doctor.
If you have a history of severe allergic reactions, inform your doctor, as you may be at risk of an even more severe reaction if you are exposed to the allergen again. Furthermore, if you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
This drug may also make it more challenging to recognize symptoms of hyperthyroidism, such as a rapid heartbeat. If you have hyperthyroidism and suddenly stop taking this medication, your condition may worsen and become life-threatening. Consult your doctor for guidance.
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
Overdose Information
Overdose Symptoms:
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm (difficulty breathing)
- Cardiac arrest
- CNS depression (drowsiness, lethargy, coma)
- Hypoglycemia (low blood sugar)
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For advice, call a poison control center at 1-800-222-1222. Treatment is supportive and symptomatic. Atropine for bradycardia, vasopressors for hypotension, bronchodilators for bronchospasm, glucagon for hypoglycemia.
Drug Interactions
Contraindicated Interactions
- Monoamine oxidase inhibitors (MAOIs)
- Antidepressants that affect noradrenergic transmission (e.g., tricyclic antidepressants, mianserin) - may potentiate hypotensive effect
- Patients with bronchial asthma or severe chronic obstructive pulmonary disease (COPD)
- Sinus bradycardia, sick sinus syndrome, sinoatrial block, second or third degree atrioventricular block (without a pacemaker), overt cardiac failure, cardiogenic shock
- Infants and children under 2 years of age
Major Interactions
- Systemic beta-blockers (additive systemic effects, e.g., bradycardia, hypotension)
- Oral calcium channel blockers (additive effects on AV conduction, heart rate, blood pressure)
- Cardiac glycosides (e.g., digoxin) (additive effects on AV conduction, heart rate)
- Clonidine (additive hypotensive effects)
- CNS depressants (e.g., alcohol, barbiturates, opiates, sedatives, anesthetics) (additive CNS depression)
- Adrenergic psychotropic drugs (e.g., chlorpromazine, methylphenidate, reserpine) (potential for additive or potentiated effects)
- Quinidine (increased plasma levels of timolol due to CYP2D6 inhibition)
Moderate Interactions
- Cimetidine (may increase timolol levels)
- Fluoxetine, paroxetine (CYP2D6 inhibitors, may increase timolol levels)
- Propafenone (CYP2D6 inhibitor, may increase timolol levels)
- Rifampin (may decrease timolol levels)
- Topical ophthalmic beta-blockers (additive IOP lowering and systemic effects)
- Pilocarpine (may reduce efficacy of timolol)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess treatment efficacy.
Timing: Prior to initiation of therapy
Heart Rate and Blood Pressure
Rationale: To monitor for systemic beta-blocker effects (bradycardia, hypotension).
Timing: Prior to initiation of therapy
Ophthalmic examination (e.g., slit lamp, fundoscopy)
Rationale: To assess ocular health and rule out other conditions.
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 pressure to prevent progression
Action Threshold: IOP not adequately controlled, or signs of progression
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial treatment or dose changes
Target: Within normal limits for the patient
Action Threshold: Significant bradycardia (<50 bpm), hypotension, or symptomatic changes
Ocular adverse effects (e.g., hyperemia, stinging, dry eye)
Frequency: At each follow-up visit
Target: Minimal to none
Action Threshold: Persistent or severe discomfort, allergic reactions
Systemic adverse effects (e.g., dizziness, fatigue, respiratory symptoms)
Frequency: At each follow-up visit
Target: Minimal to none
Action Threshold: New or worsening systemic symptoms
Symptom Monitoring
- Blurred vision
- Ocular discomfort (stinging, burning, itching)
- Ocular hyperemia (redness)
- Dry eye
- Dizziness
- Fatigue
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Respiratory symptoms (e.g., shortness of breath, wheezing, especially in patients with asthma/COPD history)
- Depression
- Insomnia
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Timolol is a Category C drug and has been associated with adverse effects in animal studies and potential for systemic effects in humans. Brimonidine is Category B. Systemic absorption of timolol can lead to fetal bradycardia and growth restriction.
Trimester-Specific Risks:
First Trimester:
Potential for fetal exposure, but organogenesis is most sensitive period. Risk of cardiovascular malformations with beta-blockers is low but not excluded.
Second Trimester:
Risk of fetal bradycardia, growth restriction, and other systemic effects from timolol.
Third Trimester:
Risk of neonatal bradycardia, hypotension, respiratory depression, and hypoglycemia if exposed near term.
Lactation
Both brimonidine and timolol are excreted in human milk. Due to the potential for serious adverse reactions in nursing infants (e.g., apnea, bradycardia, CNS depression from brimonidine; bradycardia, hypotension, respiratory depression from timolol), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. L3 (moderately safe) for timolol, L3 for brimonidine. Consider alternative or monitor infant closely.
Infant Risk:
Moderate risk (L3). Potential for bradycardia, hypotension, respiratory depression, CNS depression, and apnea in the infant.
Pediatric Use
Contraindicated in infants and children under 2 years of age due to the potential for severe systemic adverse reactions (e.g., apnea, bradycardia, somnolence, hypotension) associated with brimonidine. Use with caution in children 2-12 years of age due to potential for systemic absorption and associated adverse effects. Safety and efficacy in pediatric patients have not been fully established.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals to the systemic effects of timolol cannot be ruled out. Use with caution in patients with underlying cardiovascular or respiratory conditions. Monitor for systemic adverse effects.
Clinical Information
Clinical Pearls
- This combination ophthalmic solution is often used when monotherapy is insufficient to achieve target IOP.
- Patients should be instructed on proper instillation technique to minimize systemic absorption and maximize local effect.
- Advise patients to wait 5 minutes between instilling this product and any other ophthalmic medications.
- Due to the timolol component, caution is advised in patients with a history of asthma, COPD, or certain cardiac conditions. Systemic absorption, though minimal, can still cause significant adverse effects.
- Patients should be monitored for signs of systemic beta-blockade (e.g., bradycardia, hypotension, fatigue) and CNS depression (e.g., somnolence, lethargy).
- The brimonidine component can cause ocular hyperemia (redness) and allergic conjunctivitis in some patients.
Alternative Therapies
- Prostaglandin analogs (e.g., Latanoprost, Travoprost, Bimatoprost)
- Beta-blockers (e.g., Timolol, Betaxolol)
- Alpha-2 adrenergic agonists (e.g., Brimonidine)
- Carbonic anhydrase inhibitors (e.g., Dorzolamide, Brinzolamide, Acetazolamide)
- Rho kinase inhibitors (e.g., Netarsudil)
- Cholinergic agonists (e.g., Pilocarpine)
Cost & Coverage
Average Cost:
Varies, typically $100-$300 per 5ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (generic often Tier 1 or 2)
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 information about the medication taken, the amount, and the time it happened.