Timolol Maleate 0.5% Ophth Sol 10ml
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 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 medication is commonly used to treat glaucoma and 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. Use this medication as directed, even if your symptoms improve. Take it 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 avoid contamination, do not touch the container tip to your eye, eyelid, or surrounding skin, as this can lead to bacterial infection and potentially cause severe eye problems or vision loss.
Tilt your head back, drop the medication into your eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye. Gently blot any excess solution from your eyelid.
If you are using multiple medications in the same eye, wait at least 5 minutes between each application. Some products are designed for morning use if taken once daily, while others may not have specific timing requirements. Consult your pharmacist for guidance on using this medication.
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 resume your regular schedule. Do not use two doses at the same time or take extra doses.
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 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 avoid contamination, do not touch the container tip to your eye, eyelid, or surrounding skin, as this can lead to bacterial infection and potentially cause severe eye problems or vision loss.
Tilt your head back, drop the medication into your eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye. Gently blot any excess solution from your eyelid.
If you are using multiple medications in the same eye, wait at least 5 minutes between each application. Some products are designed for morning use if taken once daily, while others may not have specific timing requirements. Consult your pharmacist for guidance on using this medication.
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 resume your regular schedule. Do not use two doses at the same time or take extra doses.
Lifestyle & Tips
- Do not touch the dropper tip to your eye or any other surface to avoid contamination.
- Wash your hands before and after using eye drops.
- If you wear contact lenses, remove them before applying the drops and wait at least 15 minutes before reinserting them.
- If you are using other eye drops, wait at least 5-10 minutes between applications.
- Close your eye gently and apply pressure to the inner corner of your eye (near the nose) for 1-2 minutes after instilling the drop to minimize systemic absorption and maximize local effect.
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:
1 drop of 0.25% or 0.5% solution in the affected eye(s) twice daily.
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
ocularHypertension:
1 drop of 0.25% or 0.5% solution in the affected eye(s) twice daily.
openAngleGlaucoma:
1 drop of 0.25% or 0.5% solution in the affected eye(s) twice daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established, use with extreme caution due to potential for systemic effects (e.g., apnea, bradycardia). Lower concentrations (0.25%) may be considered if absolutely necessary.
Child:
Not established, use with extreme caution due to potential for systemic effects. Lower concentrations (0.25%) may be considered if absolutely necessary.
Adolescent:
Similar to adult dosing, but initiate with lower concentration (0.25%) and monitor closely for systemic effects.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
Moderate:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
Severe:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
Dialysis:
Considerations: Timolol is dialyzable, but systemic absorption from ophthalmic drops is usually minimal. Monitor for systemic effects.
Hepatic Impairment:
Mild:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
Moderate:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
Severe:
No specific adjustment recommended for ophthalmic use, but monitor for systemic effects if significant systemic absorption occurs.
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 for reducing aqueous humor production is not fully elucidated but is thought to involve blockade of beta-2 receptors on the ciliary epithelium.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (systemic absorption occurs after ocular administration)
Tmax:
Ocular hypotensive effect typically begins within 20-30 minutes, with peak effect occurring within 1-2 hours. Systemic peak plasma concentrations occur approximately 1-2 hours after oral administration.
FoodEffect:
Not applicable for ophthalmic solution.
Distribution:
Vd:
Not available (systemic Vd is approximately 1.7 L/kg)
ProteinBinding:
Approximately 10%
CnssPenetration:
Limited (can cross blood-brain barrier, but ophthalmic systemic absorption is usually low)
Elimination:
HalfLife:
Approximately 4-6 hours (systemic)
Clearance:
Not available (systemic clearance is approximately 500 mL/min)
ExcretionRoute:
Renal (primarily as metabolites, small amount unchanged drug)
Unchanged:
Approximately 20% (systemic)
Pharmacodynamics
OnsetOfAction:
20-30 minutes
PeakEffect:
1-2 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 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, including:
+ 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, including:
+ 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
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 report any concerns to your doctor. If you experience any of the following, contact your doctor or seek medical help:
Burning or stinging sensations
Eye irritation
Dry eyes
Feeling of something in the eye
Dizziness or headache
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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, including:
+ 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, including:
+ 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
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 report any concerns to your doctor. If you experience any of the following, contact your doctor or seek medical help:
Burning or stinging sensations
Eye irritation
Dry eyes
Feeling of something in the eye
Dizziness or headache
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe eye pain or sudden vision changes
- Signs of allergic reaction (rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Very slow heart rate (bradycardia)
- Dizziness or fainting (hypotension)
- Shortness of breath or wheezing (bronchospasm), especially if you have asthma or COPD
- Unusual tiredness 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 (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 with this medication. 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 all your other medications and health conditions.
* Never start, stop, or change the dose 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 (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 with this medication. 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 all your other medications and health conditions.
* Never start, stop, or change the dose 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, particularly in individuals with asthma. If you have any questions or concerns, discuss them with your doctor.
This medication may also mask symptoms of hyperthyroidism, such as a rapid heartbeat. If you have hyperthyroidism and suddenly stop taking this medication, your condition may worsen, potentially leading to life-threatening consequences. Consult your doctor for guidance.
If you have a history of severe allergic reactions, inform your doctor, as you may be at increased risk of a more severe reaction if you are re-exposed to the allergen. Furthermore, if you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential 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, 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, particularly in individuals with asthma. If you have any questions or concerns, discuss them with your doctor.
This medication may also mask symptoms of hyperthyroidism, such as a rapid heartbeat. If you have hyperthyroidism and suddenly stop taking this medication, your condition may worsen, potentially leading to life-threatening consequences. Consult your doctor for guidance.
If you have a history of severe allergic reactions, inform your doctor, as you may be at increased risk of a more severe reaction if you are re-exposed to the allergen. Furthermore, if you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
Overdose Information
Overdose Symptoms:
- Severe bradycardia (very slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm (difficulty breathing, wheezing)
- Acute cardiac failure
- Dizziness
- Fainting
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.
Drug Interactions
Major Interactions
- Oral beta-blockers (additive systemic effects, e.g., bradycardia, hypotension)
- Calcium channel blockers (e.g., verapamil, diltiazem - risk of AV conduction disturbances, bradycardia, hypotension)
- Catecholamine-depleting drugs (e.g., reserpine, guanethidine - risk of additive hypotensive and/or bradycardic effects)
- Digitalis (risk of additive bradycardia, AV block)
- Quinidine (can inhibit timolol metabolism via CYP2D6, leading to increased systemic timolol levels and enhanced beta-blockade)
- Clonidine (paradoxical hypertension upon clonidine withdrawal in patients on beta-blockers)
Moderate Interactions
- Adrenergic psychotropic drugs (e.g., MAOIs, tricyclic antidepressants - potential for exaggerated hypertensive response)
- Inhalation anesthetics (e.g., halothane, isoflurane - potential for exaggerated hypotension and myocardial depression)
- Insulin and oral hypoglycemic agents (beta-blockers can mask symptoms of hypoglycemia and prolong hypoglycemic response)
- NSAIDs (may reduce the hypotensive effect of beta-blockers)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Before initiation of therapy
Heart Rate and Blood Pressure
Rationale: To assess for potential systemic beta-blockade effects (bradycardia, hypotension).
Timing: Before initiation of therapy
Pulmonary Function (e.g., spirometry)
Rationale: To assess for underlying respiratory conditions (e.g., asthma, COPD) that may be exacerbated by beta-blockade.
Timing: Before initiation of therapy, especially in patients with respiratory history
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 based on disease severity and progression.
Action Threshold: IOP not at target, or signs of disease progression.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial therapy or dose adjustments.
Target: Normal range for patient, avoiding symptomatic bradycardia (<50 bpm) or hypotension.
Action Threshold: Symptomatic bradycardia, hypotension, or significant changes from baseline.
Visual Acuity and Visual Fields
Frequency: Annually or as clinically indicated to monitor glaucoma progression.
Target: Stable or improved.
Action Threshold: Worsening vision or visual field defects.
Symptom Monitoring
- Blurred vision
- Eye irritation (stinging, burning)
- Dry eyes
- Bradycardia (slow heart rate)
- Hypotension (dizziness, lightheadedness)
- Bronchospasm (wheezing, shortness of breath)
- Fatigue
- Depression
- Masking of hypoglycemia symptoms in diabetics
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Timolol has been shown to cause adverse effects in animal studies at doses higher than human therapeutic doses. Systemic absorption can occur.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, though human data are limited. Avoid if possible.
Second Trimester:
Limited data, but systemic absorption could lead to fetal bradycardia or growth restriction.
Third Trimester:
Potential for fetal bradycardia, hypotension, and respiratory depression, especially if used close to delivery. Neonatal hypoglycemia and respiratory distress have been reported with systemic beta-blocker use.
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.
Infant Risk:
L3 (Moderately safe, but caution advised). Potential for bradycardia, hypotension, and respiratory depression in the infant, especially in preterm or neonates. Monitor infant for signs of beta-blockade.
Pediatric Use
Use with extreme caution, especially in infants and young children, due to increased risk of systemic adverse effects (e.g., apnea, bradycardia, bronchospasm) from systemic absorption. Lower concentrations (0.25%) may be preferred if use is unavoidable. Close monitoring of heart rate, blood pressure, and respiratory status is essential.
Geriatric Use
Generally well-tolerated in elderly patients. However, elderly patients may be more susceptible to systemic adverse effects (e.g., bradycardia, hypotension, bronchospasm) due to age-related decreases in renal and hepatic function, and increased prevalence of comorbidities. Monitor closely for systemic effects.
Clinical Information
Clinical Pearls
- Timolol is a first-line agent for glaucoma due to its efficacy, once or twice daily dosing, and relatively low cost.
- Proper instillation technique (nasolacrimal occlusion) can minimize systemic absorption and reduce the risk of systemic side effects.
- Patients with a history of asthma, severe COPD, sinus bradycardia, second or third-degree AV block, or overt cardiac failure should generally avoid timolol due to the risk of exacerbating these conditions.
- Be aware of the potential for masking symptoms of hypoglycemia in diabetic patients.
- Patients may experience transient stinging or burning upon instillation.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Alpha-2 adrenergic agonists (e.g., brimonidine)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide)
- Miotics (e.g., pilocarpine)
- Rho kinase inhibitors (e.g., netarsudil)
- Laser trabeculoplasty
- Glaucoma filtration surgery
Cost & Coverage
Average Cost:
Varies widely, typically $15-$50 per 10ml bottle of 0.5% solution
Generic Available:
Yes
Insurance Coverage:
Tier 1 (Generic)
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 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 overdose, including the medication taken, the amount, and the time it occurred.