Timolol Mal 0.5% Op Sol-Once Daily
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
Jan 1993
DEA Schedule
Not Controlled
Overview
What is this medicine?
Timolol eye drops are used to lower high pressure inside the eye, which can damage your vision. It works by reducing the amount of fluid your eye makes. This medicine is a beta-blocker, and even though it's an eye drop, some of it can be absorbed into your body, so it's important to tell your doctor about all your medical conditions and other medicines.
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 the medication as directed, even if your symptoms improve. Take the medication at the same time every day.
Administration
This medication is for use in the eye only. Before using, remove your contact lenses. You can put them back in 15 minutes after administering the medication, unless your eyes are irritated or infected.
To administer the medication:
1. Tilt your head back and gently drop the medication into your eye.
2. After use, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
3. Gently blot any excess solution from your eyelid.
Important Precautions
Do not touch the container tip to your eye, lid, or other skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
If you are using multiple medications in the same eye, wait at least 5 minutes between each application.
Storage and Disposal
Store the medication in an upright position at room temperature, away from light. Do not freeze the medication.
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 dose, skip the missed dose and continue with your regular schedule. Do not use two doses at the same time or take extra doses.
Additional Guidance
Some products are designed for morning use if taken once a day, while others may not have specific timing requirements. Consult with your pharmacist to determine the best usage schedule for your medication.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Use the medication as directed, even if your symptoms improve. Take the medication at the same time every day.
Administration
This medication is for use in the eye only. Before using, remove your contact lenses. You can put them back in 15 minutes after administering the medication, unless your eyes are irritated or infected.
To administer the medication:
1. Tilt your head back and gently drop the medication into your eye.
2. After use, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
3. Gently blot any excess solution from your eyelid.
Important Precautions
Do not touch the container tip to your eye, lid, or other skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
If you are using multiple medications in the same eye, wait at least 5 minutes between each application.
Storage and Disposal
Store the medication in an upright position at room temperature, away from light. Do not freeze the medication.
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 dose, skip the missed dose and continue with your regular schedule. Do not use two doses at the same time or take extra doses.
Additional Guidance
Some products are designed for morning use if taken once a day, while others may not have specific timing requirements. Consult with your pharmacist to determine the best usage schedule for your medication.
Lifestyle & Tips
- Wash hands thoroughly before and after administering eye drops.
- Do not touch the dropper tip to any surface (including the eye) to avoid contamination.
- Tilt head back, pull down the lower eyelid to form a pouch, and instill one drop. Close eye gently for 1-2 minutes, and apply pressure to the inner corner of the eye (punctal occlusion) to minimize systemic absorption.
- If using other eye drops, wait at least 5-10 minutes between applications.
- Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
- Store at room temperature, away from light and moisture.
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% gel-forming solution in the affected eye(s) once daily.
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
ocular_hypertension:
One drop of 0.5% gel-forming solution in the affected eye(s) once daily.
open_angle_glaucoma:
One drop of 0.5% gel-forming solution in the affected eye(s) once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (use with caution, lower concentrations may be considered if used off-label)
Adolescent:
Not established (use with caution, lower concentrations may be considered if used off-label)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment typically required for ophthalmic use.
Moderate:
No specific adjustment typically required for ophthalmic use; monitor for systemic effects.
Severe:
No specific adjustment typically required for ophthalmic use; monitor closely for systemic effects (e.g., bradycardia, hypotension) due to potential for increased systemic exposure.
Dialysis:
No specific adjustment for ophthalmic use; monitor for systemic effects.
Hepatic Impairment:
Mild:
No specific adjustment typically required for ophthalmic use.
Moderate:
No specific adjustment typically required for ophthalmic use; monitor for systemic effects.
Severe:
No specific adjustment typically required for ophthalmic use; monitor closely for systemic effects due to potential for increased systemic exposure.
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), primarily by decreasing the production of aqueous humor. The exact mechanism of action in reducing aqueous humor formation is not precisely established but is thought to involve blockade of beta-2 receptors on the ciliary epithelium.
Pharmacokinetics
Absorption:
Bioavailability:
Not directly quantifiable as a percentage for ophthalmic, but significant systemic absorption occurs.
Tmax:
Approximately 1-2 hours (for systemic plasma concentrations after ophthalmic administration).
FoodEffect:
Not applicable for ophthalmic solution.
Distribution:
Vd:
Not available (systemic Vd for oral timolol is 1.7 L/kg)
ProteinBinding:
Approximately 60% (systemic)
CnssPenetration:
Limited (for ophthalmic application, but systemic absorption can lead to CNS effects)
Elimination:
HalfLife:
Approximately 4-6 hours (systemic)
Clearance:
Not available (systemic clearance for oral timolol is 5-7 mL/min/kg)
ExcretionRoute:
Renal (primarily metabolites, some unchanged drug)
Unchanged:
Approximately 20% (systemic, excreted unchanged in urine)
Pharmacodynamics
OnsetOfAction:
Within 30 minutes
PeakEffect:
1-2 hours
DurationOfAction:
Up to 24 hours (for gel-forming solution)
Confidence:
Medium
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
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, including:
+ 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 immediately:
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
+ Bulging neck veins
Other Possible Side Effects
Most people taking this medication will not experience side effects, or they may be mild. However, if you notice any of the following side effects, or if they bother you or do not go away, contact your doctor or seek medical help:
Burning or stinging sensation
Eye irritation
Dry eyes
Feeling of something in the eye
Dizziness or headache
* Signs of a common cold
Reporting Side Effects
This is not a comprehensive list of all 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
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, including:
+ 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 immediately:
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
+ Bulging neck veins
Other Possible Side Effects
Most people taking this medication will not experience side effects, or they may be mild. However, if you notice any of the following side effects, or if they bother you or do not go away, contact your doctor or seek medical help:
Burning or stinging sensation
Eye irritation
Dry eyes
Feeling of something in the eye
Dizziness or headache
* Signs of a common cold
Reporting Side Effects
This is not a comprehensive list of all 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 irritation, pain, or vision changes
- Slow or irregular heartbeat
- Dizziness or lightheadedness
- Shortness of breath or wheezing
- Swelling of ankles or feet
- Unusual fatigue or weakness
- 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.
Certain health conditions, including:
+ Respiratory problems like asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weak heart)
+ Shock caused by heart problems
+ Slow heartbeat
If you are currently using a similar medication. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your 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 change the dosage of any medication without first 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, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Respiratory problems like asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weak heart)
+ Shock caused by heart problems
+ Slow heartbeat
If you are currently using a similar medication. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your 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 change the dosage of any medication without first 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. 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. Although rare, this medication has been associated with severe respiratory problems, which can be life-threatening, especially in individuals with asthma. If you have any questions, discuss them with your doctor.
This medication may also conceal 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 for an even more severe reaction if you are exposed to the allergen again. 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, plan to become pregnant, or are 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. Although rare, this medication has been associated with severe respiratory problems, which can be life-threatening, especially in individuals with asthma. If you have any questions, discuss them with your doctor.
This medication may also conceal 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 for an even more severe reaction if you are exposed to the allergen again. 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, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm (difficulty breathing, wheezing)
- Acute cardiac failure
- Dizziness
- Headache
What to Do:
If systemic overdose occurs, treatment should be symptomatic and supportive. Contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Oral beta-blockers (additive systemic effects)
- Calcium channel blockers (e.g., verapamil, diltiazem - increased risk of AV conduction disturbances, bradycardia, hypotension)
- Catecholamine-depleting drugs (e.g., reserpine, guanethidine - additive hypotensive and/or bradycardic effects)
- Digitalis (increased risk of bradycardia, AV block)
Moderate Interactions
- Quinidine (can inhibit timolol metabolism, leading to increased plasma levels and systemic beta-blockade)
- Clonidine (potential for paradoxical hypertension upon withdrawal of clonidine while on beta-blocker)
- Adrenergic psychotropic drugs (e.g., MAOIs - potential for hypertensive crisis)
- Inhalation anesthetics (e.g., halothane, isoflurane - enhanced myocardial depression)
Minor Interactions
- NSAIDs (may reduce hypotensive effect of beta-blockers)
- Cimetidine (may increase timolol levels)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess treatment efficacy.
Timing: Prior to initiation of therapy.
Visual Acuity and Visual Fields
Rationale: To assess baseline visual function and monitor for progression of glaucoma.
Timing: Prior to initiation of therapy.
Heart Rate and Blood Pressure
Rationale: To assess for systemic beta-blockade effects due to ophthalmic absorption.
Timing: Prior to initiation of therapy.
Respiratory Status (e.g., history of asthma, COPD)
Rationale: To identify contraindications or high-risk patients for bronchospasm.
Timing: Prior to initiation of therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, typically 2-4 weeks after initiation/change, then every 3-6 months or as clinically indicated.
Target: Individualized target IOP based on disease severity and progression.
Action Threshold: IOP above target, or signs of disease progression.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial therapy or dose changes.
Target: Normal physiological range for the patient.
Action Threshold: Significant bradycardia (<50 bpm), hypotension, or symptomatic changes.
Respiratory Symptoms (e.g., dyspnea, wheezing)
Frequency: At each follow-up visit.
Target: Absence of new or worsening respiratory symptoms.
Action Threshold: Onset or worsening of respiratory distress, especially in patients with pre-existing pulmonary conditions.
Ocular Examination (e.g., slit lamp, fundoscopy)
Frequency: Annually or as clinically indicated.
Target: Stable optic nerve and retinal health.
Action Threshold: Signs of optic nerve damage progression or other ocular pathology.
Symptom Monitoring
- Bradycardia
- Dizziness
- Fatigue
- Shortness of breath
- Wheezing
- Chest pain
- Syncope
- Eye irritation
- Blurred vision
- Dry eyes
- Headache
- Depression
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Timolol has been shown to cross the placenta. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown adverse effects at maternally toxic doses.
Trimester-Specific Risks:
First Trimester:
Potential for fetal growth restriction or other developmental effects based on animal data and systemic beta-blocker effects.
Second Trimester:
Potential for fetal growth restriction or other developmental effects.
Third Trimester:
Potential for adverse effects on the neonate (e.g., bradycardia, hypoglycemia, respiratory depression) if exposed near term due to systemic absorption.
Lactation
Timolol is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants from timolol, 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. Monitor breastfed infants for signs of beta-blockade (e.g., bradycardia, hypotension, respiratory distress).
Infant Risk:
Moderate risk (L3 on Hale's scale). Potential for bradycardia, hypotension, and respiratory depression in the infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in pediatric patients is generally not recommended due to potential for increased systemic absorption and higher risk of adverse effects (e.g., apnea, bradycardia, central nervous system depression), especially in infants and neonates. If used off-label, lower concentrations and careful monitoring are advised.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Monitor closely for systemic adverse effects (e.g., bradycardia, hypotension, respiratory issues) due to potential for age-related decreases in renal or hepatic function and increased sensitivity to beta-blockade.
Clinical Information
Clinical Pearls
- Timolol ophthalmic solution, especially the gel-forming formulation, is typically dosed once daily, often in the morning, for convenience and sustained IOP reduction.
- Despite being an eye drop, significant systemic absorption can occur, leading to systemic beta-blocker side effects. Always inquire about patient's cardiac and respiratory history (e.g., asthma, COPD, heart block, severe bradycardia).
- Punctal occlusion (pressing on the inner corner of the eye for 1-2 minutes after instillation) can help minimize systemic absorption and maximize ocular bioavailability.
- Patients should be educated on proper instillation technique to avoid contamination and ensure efficacy.
- Monitor IOP regularly to ensure the medication is effectively controlling the patient's glaucoma or ocular hypertension.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Alpha-adrenergic agonists (e.g., brimonidine)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide)
- Rho kinase inhibitors (e.g., netarsudil)
- Cholinergic agonists (e.g., pilocarpine)
- Laser trabeculoplasty
- Surgical interventions (e.g., trabeculectomy, glaucoma drainage devices)
Cost & Coverage
Average Cost:
Varies widely, typically $30-$100+ per 5mL bottle (0.5%)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 or higher (for brand)
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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.