Timolol Mal 0.5% Ophth Sol 60s
It is used to treat glaucoma.It is used to lower high eye pressure.
Drug Class
Antiglaucoma agent
Pharmacologic Class
Non-selective beta-adrenergic blocker
Pregnancy Category
Category C
FDA Approved
Sep 1978
DEA Schedule
Not Controlled
Overview
What is this medicine?
Timolol 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 important to use it regularly as prescribed, even if you don't feel any symptoms.
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. Use this medication as directed, even if your symptoms improve. Take it at the same time every day.
Administration
This medication is for eye use only. Remove your contact lenses before using it, and wait 15 minutes after administration before putting them back in. However, do not reinsert your contacts if your eyes are irritated or infected.
To avoid contamination and potential severe eye problems or vision loss, do not touch the container tip to your eye, lid, or surrounding skin. Tilt your head back, and gently drop the medication into your eye. 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. Use a tissue to blot any excess solution from your eyelid.
If you are using multiple medications in the same eye, administer them at least 5 minutes apart. Some products are designed for morning use if taken once daily, while others do not have specific timing requirements. Consult your pharmacist for guidance on the proper administration schedule.
Disposal
After use, discard any remaining medication. Do not save it for later use.
Storage and Handling
Store the foil pouch at room temperature. Once opened, discard any unused portion after 30 days. Keep unused containers in their original foil pouch until use. Do not freeze this medication.
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 take two doses at once or use extra doses to make up for a missed dose.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Use this medication as directed, even if your symptoms improve. Take it at the same time every day.
Administration
This medication is for eye use only. Remove your contact lenses before using it, and wait 15 minutes after administration before putting them back in. However, do not reinsert your contacts if your eyes are irritated or infected.
To avoid contamination and potential severe eye problems or vision loss, do not touch the container tip to your eye, lid, or surrounding skin. Tilt your head back, and gently drop the medication into your eye. 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. Use a tissue to blot any excess solution from your eyelid.
If you are using multiple medications in the same eye, administer them at least 5 minutes apart. Some products are designed for morning use if taken once daily, while others do not have specific timing requirements. Consult your pharmacist for guidance on the proper administration schedule.
Disposal
After use, discard any remaining medication. Do not save it for later use.
Storage and Handling
Store the foil pouch at room temperature. Once opened, discard any unused portion after 30 days. Keep unused containers in their original foil pouch until use. Do not freeze this medication.
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 take two doses at once or use extra doses to make up for a missed dose.
Lifestyle & Tips
- Administer eye drops correctly: Wash hands, tilt head back, pull down lower eyelid, create a pocket, instill one drop without touching the eye with the dropper tip. Close eye gently for 1-2 minutes, apply pressure to the inner corner of the eye (punctal occlusion) to minimize systemic absorption.
- Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting.
- Do not discontinue use without consulting your doctor, as eye pressure may increase.
- Inform your doctor about all other medications you are taking, especially other eye drops, oral beta-blockers, or heart medications.
Available Forms & Alternatives
Available Strengths:
- Timolol Maleate 10mg Tablets
- Timolol Maleate 20mg Tablets
- Timolol Maleate 0.25% Opht Sol 5ml
- Timolol Maleate 0.25% Opht Sol 10ml
- Timolol Maleate 0.25% Opht Sol 15ml
- Timolol Maleate 0.5% Ophth Soln 5ml
- Timolol Maleate 0.5% Ophth Sol 10ml
- Timolol Maleate 0.5% Ophth Sol 15ml
- Timolol Maleate 5mg Tablets
- Timolol 0.25% GF Ophth Soln 5ml
- Timolol 0.5% GF Opth Soln 5ml
- Timolol Mal 0.5% Op Sol-Once Daily
- Timolol Mal 0.5% Op Sol-Once Daily
- Timolol Mal 0.5% Ophth Sol 60s
- Timolol 0.25% Pf-Oph Sol 60's
- Timolol Hemi 0.5% Ophth Soln 5ml
- Timolol Hemi 0.5% Ophth Soln 10ml
- Timolol Hemi 0.5% Ophth Soln 15ml
Dosing & Administration
Adult Dosing
Standard Dose:
One drop of 0.5% solution in the affected eye(s) once daily.
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
open_angle_glaucoma:
One drop of 0.5% solution in the affected eye(s) once daily. If IOP is not adequately controlled, 0.25% solution may be used twice daily, or 0.5% solution may be used twice daily if needed, though once daily is often sufficient for 0.5%.
Pediatric Dosing
Neonatal:
Not established (use with extreme caution due to potential for systemic effects, especially in premature infants and neonates)
Infant:
Not established (use with extreme caution due to potential for systemic effects)
Child:
Not established (use with caution, lower concentrations may be considered, monitor closely for systemic effects)
Adolescent:
Similar to adult dosing, but monitor for systemic effects.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed for ophthalmic use.
Moderate:
No specific adjustment needed for ophthalmic use.
Severe:
No specific adjustment needed for ophthalmic use, but caution if systemic absorption is significant in patients with severe renal impairment and co-morbidities.
Dialysis:
No specific adjustment needed for ophthalmic use.
Hepatic Impairment:
Mild:
No specific adjustment needed for ophthalmic use.
Moderate:
No specific adjustment needed for ophthalmic use.
Severe:
No specific adjustment needed for ophthalmic use, but caution if systemic absorption is significant in patients with severe hepatic impairment and co-morbidities.
Pharmacology
Mechanism of Action
Timolol maleate is a non-selective beta-adrenergic receptor blocking agent. When applied topically to the eye, it reduces elevated and normal intraocular pressure (IOP) by decreasing the production of aqueous humor. The exact mechanism of action for reducing aqueous humor production is not definitively established but is thought to involve blockade of beta-2 receptors on the ciliary epithelium.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (variable, typically <10% of administered dose reaches systemic circulation, but can be higher)
Tmax:
Peak IOP reduction typically occurs within 1 to 2 hours after administration.
FoodEffect:
Not applicable for ophthalmic solution.
Distribution:
Vd:
Not specifically quantified for ophthalmic use; widely distributed if systemically absorbed.
ProteinBinding:
Approximately 60% (for systemic timolol)
CnssPenetration:
Limited (can cross blood-brain barrier if systemically absorbed, leading to CNS effects)
Elimination:
HalfLife:
Approximately 2.5 to 5 hours (systemic)
Clearance:
Not specifically quantified for ophthalmic use.
ExcretionRoute:
Renal (metabolites and unchanged drug)
Unchanged:
Approximately 20% (systemic)
Pharmacodynamics
OnsetOfAction:
Within 30 minutes
PeakEffect:
1 to 2 hours
DurationOfAction:
Up to 24 hours
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 medical attention immediately:
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
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Eye problems, such as:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Cardiovascular symptoms, such as:
+ Very bad dizziness or passing out
+ Slow heartbeat
+ Abnormal heartbeat
+ Chest pain
+ Muscle weakness
Heart failure, which can be life-threatening. If you experience any of the following, seek medical help right away:
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
+ Bulging neck veins
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, contact your doctor or seek medical help if they bother you or do not go away:
Burning or stinging
Eye irritation
Dry eyes
Feeling that something is in the eye
Dizziness or headache
* Signs of a common cold
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. 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 medical attention immediately:
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
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Eye problems, such as:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Cardiovascular symptoms, such as:
+ Very bad dizziness or passing out
+ Slow heartbeat
+ Abnormal heartbeat
+ Chest pain
+ Muscle weakness
Heart failure, which can be life-threatening. If you experience any of the following, seek medical help right away:
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
+ Bulging neck veins
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, contact your doctor or seek medical help if they bother you or do not go away:
Burning or stinging
Eye irritation
Dry eyes
Feeling that something is in the eye
Dizziness or headache
* Signs of a common cold
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. 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 irritation, redness, or pain
- Changes in vision
- Slow or irregular heartbeat
- Dizziness or lightheadedness
- Unusual tiredness or weakness
- Difficulty breathing, wheezing, or shortness of breath
- Swelling of ankles or feet
- Depression or mood changes
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 as a result of the allergy.
Certain health conditions, including:
+ Breathing problems, such as 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 taking another medication similar to this one. If you are unsure, consult your doctor or pharmacist to determine if the medications are similar.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult your doctor to ensure your safety. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
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 as a result of the allergy.
Certain health conditions, including:
+ Breathing problems, such as 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 taking another medication similar to this one. If you are unsure, consult your doctor or pharmacist to determine if the medications are similar.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult your doctor to ensure your safety. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
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.
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, or experiencing nausea and vomiting. If you have any questions or concerns, consult your doctor.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. Additionally, follow your doctor's recommendations for regular eye pressure and vision checks.
Notify your doctor if you have an eye infection, eye injury, or are scheduled to undergo eye surgery. In rare cases, this medication has been associated with severe respiratory problems, which can be life-threatening, especially in individuals with asthma. If you have any questions or concerns, discuss them with your doctor.
This medication 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 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 re-exposed to the allergen. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may be less effective while taking this drug.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to 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, or experiencing nausea and vomiting. If you have any questions or concerns, consult your doctor.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. Additionally, follow your doctor's recommendations for regular eye pressure and vision checks.
Notify your doctor if you have an eye infection, eye injury, or are scheduled to undergo eye surgery. In rare cases, this medication has been associated with severe respiratory problems, which can be life-threatening, especially in individuals with asthma. If you have any questions or concerns, discuss them with your doctor.
This medication 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 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 re-exposed to the allergen. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may be less effective while taking this drug.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe bradycardia (very slow heart rate)
- Hypotension (very low blood pressure)
- Bronchospasm (difficulty breathing)
- Acute cardiac failure
- Dizziness
- Headache
What to Do:
If overdose is suspected, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Treatment is symptomatic and supportive. Atropine for bradycardia, isoproterenol for bronchospasm, diuretics for cardiac failure, glucagon for refractory hypotension.
Drug Interactions
Major Interactions
- Oral beta-blockers (additive systemic effects, e.g., bradycardia, hypotension)
- Calcium channel blockers (e.g., verapamil, diltiazem - increased risk of AV conduction disturbances, bradycardia, hypotension)
- Catecholamine-depleting drugs (e.g., reserpine - additive hypotensive and/or bradycardic effects)
- Quinidine (can inhibit timolol metabolism via CYP2D6, leading to increased systemic timolol levels and enhanced beta-blockade)
Moderate Interactions
- Digitalis (increased risk of bradycardia, AV block)
- Clonidine (potential for rebound hypertension upon withdrawal of clonidine while on timolol)
- Adrenergic psychotropic drugs (e.g., MAOIs - theoretical risk of hypertensive crisis, though less likely with ophthalmic use)
- Inhalation anesthetics (potential for exaggerated hypotension)
Minor Interactions
- NSAIDs (may reduce hypotensive effect of beta-blockers, though less significant with ophthalmic use)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Before initiating therapy
Ophthalmic Examination
Rationale: To assess ocular health and rule out other causes of elevated IOP.
Timing: Before initiating therapy
Heart Rate and Blood Pressure
Rationale: To assess for potential systemic beta-blockade effects, especially in patients with pre-existing cardiac conditions.
Timing: Before initiating therapy
Respiratory Function (e.g., spirometry)
Rationale: To assess for potential bronchospasm, especially in patients with asthma or COPD.
Timing: Before initiating therapy in at-risk patients
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, typically 2-4 weeks after initiation/dose change, then every 3-6 months or as clinically indicated.
Target: Individualized target IOP, typically <21 mmHg or a significant reduction from baseline.
Action Threshold: IOP not adequately controlled, or significant fluctuations.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial therapy or dose adjustments, then as clinically indicated.
Target: Maintain within normal limits, avoid symptomatic bradycardia or hypotension.
Action Threshold: Symptomatic bradycardia (<50 bpm), significant hypotension, or worsening of cardiac symptoms.
Respiratory Symptoms (e.g., dyspnea, wheezing)
Frequency: Ongoing patient inquiry at follow-up visits.
Target: Absence of new or worsening respiratory symptoms.
Action Threshold: Onset or worsening of asthma/COPD symptoms, bronchospasm.
Symptom Monitoring
- Blurred vision
- Ocular irritation (stinging, burning, itching)
- Dry eyes
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Dizziness
- Fatigue
- Bronchospasm (difficulty breathing, wheezing)
- Congestive heart failure symptoms (e.g., swelling, shortness of breath)
- Depression
- Insomnia
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Timolol is classified as Pregnancy Category C.
Trimester-Specific Risks:
First Trimester:
Limited human data. Animal studies show adverse effects at high doses. Potential for fetal bradycardia and growth restriction.
Second Trimester:
Potential for fetal bradycardia and growth restriction.
Third Trimester:
Potential for fetal bradycardia, hypotension, respiratory depression, and hypoglycemia in the neonate due to systemic absorption and beta-blockade effects. Discontinuation several days before delivery may be considered if clinically feasible.
Lactation
Timolol is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants (e.g., bradycardia, respiratory depression), 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.
Infant Risk:
Risk L3 (Moderately Safe) - Potential for bradycardia, hypotension, respiratory depression, and hypoglycemia in the infant, especially in premature or compromised infants. Monitor infant for signs of beta-blockade.
Pediatric Use
Use with caution in pediatric patients, especially infants and neonates, due to increased systemic absorption and potential for severe systemic adverse reactions (e.g., bradycardia, respiratory depression, apnea). Lower concentrations (0.25%) or alternative therapies may be preferred. Close monitoring of heart rate and respiratory status is essential.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, elderly patients may be more susceptible to systemic adverse effects (e.g., bradycardia, hypotension) due to age-related decline in renal or hepatic function, or concomitant medications. Monitor closely for systemic effects.
Clinical Information
Clinical Pearls
- Timolol is a first-line agent for glaucoma due to its efficacy and once-daily dosing for the 0.5% concentration.
- Punctal occlusion (applying pressure to the inner corner of the eye for 1-2 minutes after instillation) can significantly reduce systemic absorption and minimize systemic side effects.
- Patients with a history of asthma, COPD, severe bradycardia, second- or third-degree AV block, or overt cardiac failure should generally avoid timolol due to the risk of exacerbating these conditions.
- Monitor for signs of systemic beta-blockade, even with ophthalmic use, especially in patients with pre-existing cardiovascular or respiratory conditions.
- If switching from another anti-glaucoma medication, continue the previous medication for one day while starting timolol, then discontinue the previous medication.
Alternative Therapies
- Prostaglandin analogs (e.g., Latanoprost, Travoprost, Bimatoprost)
- Carbonic anhydrase inhibitors (e.g., Dorzolamide, Brinzolamide)
- Alpha-adrenergic agonists (e.g., Brimonidine)
- Rho kinase inhibitors (e.g., Netarsudil)
- Cholinergic agonists (e.g., Pilocarpine)
Cost & Coverage
Average Cost:
Varies, typically $15-$50 per 60 unit-dose vials (0.5%)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (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's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this 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, including the amount taken and the time it happened, to help healthcare professionals provide the best possible care.