Timolol Maleate 0.25% Opht 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. It's a type of medicine called a beta-blocker.
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 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, 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. For once-daily use, some products should be administered in the morning, while others may not have specific timing requirements. Consult your pharmacist for guidance on the proper use of 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 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, 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. For once-daily use, some products should be administered in the morning, while others may not have specific timing requirements. Consult your pharmacist for guidance on the proper use of 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
- Always wash your hands thoroughly before and after using eye drops.
- Do not touch the dropper tip to your eye or any other surface to avoid contamination.
- 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.
- Follow your doctor's instructions carefully regarding dosage and frequency.
- Do not stop using the drops without consulting your doctor, even if your eye pressure is normal, as glaucoma is a chronic condition.
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% solution in the affected eye(s) twice daily
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
initial_therapy:
Start with 0.25% solution. If clinical response is not adequate, dosage may be increased to 0.5% solution.
maintenance:
Continue with the lowest effective concentration.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (use with caution, systemic absorption can lead to significant adverse effects)
Adolescent:
Not established (use with caution, systemic absorption can lead to significant adverse effects)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Moderate:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Severe:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption. However, monitor for systemic effects in patients with severe renal impairment if significant systemic absorption occurs.
Dialysis:
No specific adjustment needed for ophthalmic use. Timolol is dialyzable, but systemic exposure from ophthalmic drops is low.
Hepatic Impairment:
Mild:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Moderate:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Severe:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption. However, monitor for systemic effects in patients with severe hepatic impairment as timolol is metabolized in the liver.
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 reducing 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 in the ciliary body.
Pharmacokinetics
Absorption:
Bioavailability:
Low (variable systemic absorption after ophthalmic administration, approximately 50% of an oral dose is absorbed)
Tmax:
1-2 hours (for systemic plasma concentrations after ophthalmic administration)
FoodEffect:
Not applicable for ophthalmic solution
Distribution:
Vd:
Not precisely quantified for ophthalmic use, but distributes widely in tissues.
ProteinBinding:
Approximately 10%
CnssPenetration:
Limited (from ophthalmic administration, but can cross blood-brain barrier with systemic exposure)
Elimination:
HalfLife:
2-4 hours (systemic half-life)
Clearance:
Not precisely quantified for ophthalmic use, but primarily renal clearance of metabolites and unchanged drug.
ExcretionRoute:
Renal (primarily metabolites, some unchanged drug)
Unchanged:
Approximately 20% (of systemic dose)
Pharmacodynamics
OnsetOfAction:
Approximately 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, 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
Vision changes, 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
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 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
Vision changes, 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
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 pain or irritation
- Sudden changes in vision
- Signs of infection (redness, swelling, discharge)
- Slow or irregular heartbeat
- Dizziness or fainting
- Shortness of breath, wheezing, or difficulty breathing (especially if you have asthma or COPD)
- Unusual tiredness or weakness
- 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.
Certain health conditions, including:
+ Breathing problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block
+ 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.
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. They will help determine if it is safe to take this medication with 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:
+ Breathing problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block
+ 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.
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. They will help determine if it is safe to take this medication with 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, 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 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. 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 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 heartbeat)
- Hypotension (very low blood pressure)
- Bronchospasm (severe difficulty breathing)
- Acute cardiac failure
- Dizziness
- Headache
- Nausea
- Vomiting
What to Do:
If you suspect an overdose, seek immediate medical attention or call a poison control center. In the US, call 1-800-222-1222. Treatment is supportive and symptomatic. Atropine for bradycardia, bronchodilators for bronchospasm, vasopressors for hypotension, and diuretics for heart failure may be used.
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, heart failure)
- Catecholamine-Depleting Drugs (e.g., reserpine, guanethidine - additive hypotensive and bradycardic effects)
- Quinidine (can inhibit timolol metabolism via CYP2D6, leading to increased plasma levels of timolol and enhanced beta-blockade)
- Clonidine (potential for rebound hypertension if clonidine is withdrawn while patient is on timolol)
- Digitalis (increased risk of bradycardia and AV block)
Moderate Interactions
- Adrenergic Psychotropic Drugs (e.g., MAOIs, TCAs - potential for exaggerated pressor response)
- Inhalation Anesthetics (e.g., halothane, isoflurane - enhanced myocardial depression and hypotension)
- Insulin and Oral Hypoglycemics (beta-blockers can mask symptoms of hypoglycemia and prolong hypoglycemic episodes)
- NSAIDs (may reduce the hypotensive effect of beta-blockers)
Minor Interactions
- Topical Ophthalmic Alpha-Agonists (additive IOP lowering effect)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Prior to initiation of therapy
Visual Acuity and Ophthalmic Exam
Rationale: To assess baseline ocular health and identify any pre-existing conditions.
Timing: Prior to initiation of therapy
Heart Rate and Blood Pressure
Rationale: To assess for potential systemic beta-blockade effects, especially in patients with pre-existing cardiac conditions.
Timing: Prior to initiation of therapy
Respiratory Status (e.g., history of asthma/COPD)
Rationale: To identify patients at risk for bronchospasm due to non-selective beta-blockade.
Timing: Prior to initiation of therapy
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, typically <21 mmHg or target IOP set by ophthalmologist.
Action Threshold: If IOP remains elevated or continues to progress, consider dose increase or alternative therapy.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial therapy or dose adjustments, then as clinically indicated.
Target: Within normal limits for the patient.
Action Threshold: Significant bradycardia (<50 bpm) or hypotension, especially if symptomatic, warrants re-evaluation.
Ocular Adverse Effects (e.g., irritation, blurred vision)
Frequency: At each follow-up visit and as reported by patient.
Target: Absence of significant or intolerable symptoms.
Action Threshold: Persistent or severe symptoms may require discontinuation.
Systemic Adverse Effects (e.g., bronchospasm, dizziness, fatigue)
Frequency: At each follow-up visit and as reported by patient.
Target: Absence of significant or intolerable symptoms.
Action Threshold: Development of new or worsening systemic symptoms, especially respiratory or cardiovascular, requires immediate re-evaluation.
Symptom Monitoring
- Blurred vision
- Ocular irritation (stinging, burning, itching)
- Dry eyes
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Dizziness or lightheadedness
- Fatigue or weakness
- Bronchospasm (difficulty breathing, wheezing, shortness of breath)
- Depression
- Headache
- Nausea
Special Patient Groups
Pregnancy
Timolol maleate is Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Studies in animals have shown adverse effects on the fetus at doses higher than human therapeutic doses. Systemic absorption occurs after ophthalmic administration.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, though data is limited. Avoid if possible.
Second Trimester:
Potential for fetal harm, though data is limited.
Third Trimester:
Potential for fetal harm, including bradycardia, hypotension, and respiratory depression in the neonate, especially if used close to delivery. Beta-blockers can also mask signs of hypoglycemia in the infant.
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, respiratory depression).
Infant Risk:
L3 (Moderately safe; monitor infant for bradycardia, hypotension, respiratory depression, and hypoglycemia).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use with extreme caution due to potential for increased systemic absorption and higher risk of systemic adverse effects (e.g., bradycardia, respiratory depression, apnea), especially in infants and young children. Lower concentrations or alternative therapies may be preferred.
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 physiological changes. Monitor closely for systemic effects.
Clinical Information
Clinical Pearls
- Timolol is a first-line agent for glaucoma due to its efficacy and once or twice daily dosing.
- Proper instillation technique is crucial to minimize systemic absorption and maximize ocular effect. Advise patients to occlude the nasolacrimal duct (press finger on inner corner of eye) for 1-2 minutes after instillation to reduce systemic absorption.
- 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.
- Even with ophthalmic administration, systemic beta-blockade effects can occur. Always inquire about systemic beta-blocker use to avoid additive effects.
- Monitor for masking of hypoglycemia symptoms in diabetic patients and hyperthyroidism symptoms in patients with thyroid disorders.
- Long-term use may lead to a 'drift' in IOP lowering effect, requiring re-evaluation of therapy.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Alpha-adrenergic agonists (e.g., brimonidine, apraclonidine)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide, acetazolamide)
- Rho kinase inhibitors (e.g., netarsudil)
- Miotic agents (e.g., pilocarpine)
- Surgical interventions (e.g., laser trabeculoplasty, trabeculectomy)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 10ml bottle of 0.25% solution
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for 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 your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.