Timolol Maleate 0.25% Opht Sol 5ml
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 if not treated. It works by reducing the amount of fluid your eye makes.
How to Use This Medicine
Proper Use of This Medication
To use this eye 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
1. Remove your contact lenses before using the medication. You can put them back in 15 minutes after administration, unless your eyes are irritated or infected.
2. Avoid touching the container tip to your eye, lid, or skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
3. Tilt your head back and gently drop the medication into your eye.
4. After administration, keep your eyes closed and apply 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.
Using Multiple Medications
If you are using more than one eye medication, administer each medication at least 5 minutes apart.
Special Instructions
Some products are designed for morning use if taken once daily, while others may not have specific timing requirements. Consult with your pharmacist to determine the best administration schedule for your medication.
Storage and Disposal
Store the medication in an upright position at room temperature, away from light and freezing temperatures.
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 dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or use extra doses.
To use this eye 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
1. Remove your contact lenses before using the medication. You can put them back in 15 minutes after administration, unless your eyes are irritated or infected.
2. Avoid touching the container tip to your eye, lid, or skin, as this can contaminate the medication and lead to severe eye problems or vision loss.
3. Tilt your head back and gently drop the medication into your eye.
4. After administration, keep your eyes closed and apply 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.
Using Multiple Medications
If you are using more than one eye medication, administer each medication at least 5 minutes apart.
Special Instructions
Some products are designed for morning use if taken once daily, while others may not have specific timing requirements. Consult with your pharmacist to determine the best administration schedule for your medication.
Storage and Disposal
Store the medication in an upright position at room temperature, away from light and freezing temperatures.
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 dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or use extra doses.
Lifestyle & Tips
- Wash hands thoroughly before and after using eye drops.
- Do not touch the dropper tip to your eye or any other surface to avoid contamination.
- Tilt your head back, pull down your lower eyelid to form a pocket, and instill the prescribed number of drops. Close your eye gently for 1-2 minutes and apply pressure to the inner corner of your eye (near the nose) 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 0.25% solution in the affected eye(s) twice daily.
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
initialTherapy:
Start with 0.25% solution. If clinical response is not adequate, dosage may be increased to one drop of 0.5% solution in the affected eye(s) twice daily.
maintenance:
Continue with the lowest effective concentration and frequency.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Use with caution; generally not recommended due to potential for systemic adverse effects (e.g., bradycardia, bronchospasm, apnea). Specific dosing for pediatric glaucoma may be determined by a specialist.
Adolescent:
Use with caution; generally not recommended due to potential for systemic adverse effects (e.g., bradycardia, bronchospasm, apnea). Specific dosing for pediatric glaucoma may be determined by a specialist.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (minimal systemic absorption from ophthalmic use).
Moderate:
No adjustment needed.
Severe:
No adjustment needed.
Dialysis:
No specific considerations for ophthalmic use.
Hepatic Impairment:
Mild:
No adjustment needed (minimal systemic absorption from ophthalmic use).
Moderate:
No adjustment needed.
Severe:
No adjustment needed.
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), whether or not accompanied by glaucoma. The precise mechanism of action in lowering IOP is not definitively established, but it is believed to be primarily due to a reduction in aqueous humor production. Some studies suggest a slight increase in aqueous humor outflow facility.
Pharmacokinetics
Absorption:
Bioavailability:
Systemic absorption occurs after ocular administration, but specific bioavailability percentage is not well-quantified for ophthalmic use. Peak plasma concentrations are typically low (ng/mL range).
Tmax:
Approximately 1-2 hours after ocular administration for peak plasma concentrations.
FoodEffect:
Not applicable for ophthalmic administration.
Distribution:
Vd:
Not well-quantified for ophthalmic use due to low systemic concentrations.
ProteinBinding:
Approximately 60% (for systemic timolol).
CnssPenetration:
Limited, but can occur, leading to CNS side effects in susceptible individuals.
Elimination:
HalfLife:
Approximately 4-6 hours (systemic half-life after oral administration, relevant for systemically absorbed ophthalmic drug).
Clearance:
Not well-quantified for ophthalmic use.
ExcretionRoute:
Primarily renal (metabolites and unchanged drug).
Unchanged:
Approximately 20% of an oral dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 30 minutes after single dose.
PeakEffect:
1-2 hours after single dose.
DurationOfAction:
Up to 24 hours (IOP lowering effect).
Safety & Warnings
BLACK BOX WARNING
Timolol maleate ophthalmic solution, like other topically applied beta-adrenergic blocking agents, can be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported.
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. Call your doctor immediately if you experience:
+ 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 or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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 is not an exhaustive list of 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
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. Call your doctor immediately if you experience:
+ 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 or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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 is not an exhaustive list of 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 or pain
- Vision changes
- Slow or irregular heartbeat
- Dizziness or fainting
- Shortness of breath, wheezing, or difficulty breathing
- Swelling of hands or feet
- 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 issues like asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weakened heart)
+ Shock caused by heart problems
+ A slow heartbeat
If you are currently using another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions between this medication and other substances or health conditions.
To ensure your safety, it is crucial to discuss the following with your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your overall health status
Before starting, stopping, or adjusting the dosage of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with 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.
Certain health conditions, including:
+ Respiratory issues like asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weakened heart)
+ Shock caused by heart problems
+ A slow heartbeat
If you are currently using another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
Please note that this is not an exhaustive list of all potential interactions between this medication and other substances or health conditions.
To ensure your safety, it is crucial to discuss the following with your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your overall health status
Before starting, stopping, or adjusting the dosage of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with 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 mask 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, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks of this medication 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 mask 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, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks of this medication to you and your baby.
Overdose Information
Overdose Symptoms:
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm (difficulty breathing)
- Acute cardiac failure
- Dizziness
- Headache
- Nausea
- Vomiting
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, digitalis and diuretics for cardiac failure, glucagon for refractory hypotension/bradycardia.
Drug Interactions
Contraindicated Interactions
- Patients with bronchial asthma, a history of bronchial asthma, or severe chronic obstructive pulmonary disease (COPD)
- Sinus bradycardia
- Second or third degree atrioventricular block
- Overt cardiac failure
- Cardiogenic shock
Major Interactions
- Oral beta-adrenergic blocking agents (additive systemic effects, e.g., bradycardia, hypotension)
- Calcium channel blockers (e.g., verapamil, diltiazem) (potential for AV conduction disturbances, left ventricular failure, hypotension)
- Catecholamine-depleting drugs (e.g., reserpine, guanethidine) (additive hypotensive and/or marked bradycardia)
- Digitalis (potential for AV conduction disturbances, bradycardia)
- Quinidine (can inhibit CYP2D6, leading to increased plasma levels of timolol and enhanced beta-blockade)
- Clonidine (potential for rebound hypertension upon withdrawal of clonidine while on beta-blocker)
Moderate Interactions
- Adrenergic psychotropic drugs (e.g., MAOIs, tricyclic antidepressants) (potential for exaggerated hypertensive response)
- Inhalation anesthetics (potential for exaggerated hypotension)
- Insulin and oral hypoglycemic agents (beta-blockers may mask signs of hypoglycemia, e.g., tachycardia)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Prior to initiation of therapy.
Visual Acuity
Rationale: To establish baseline and monitor for changes.
Timing: Prior to initiation of therapy.
Optic Nerve Head and Visual Fields
Rationale: To assess baseline glaucomatous damage and monitor progression.
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 contraindications or risk factors for bronchospasm.
Timing: Prior to initiation of therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, typically 2-4 weeks after initiation/change in therapy, then every 3-6 months or as clinically indicated.
Target: Individualized, typically <21 mmHg or target IOP set by ophthalmologist.
Action Threshold: IOP not adequately controlled, or significant fluctuations.
Optic Nerve Head and Visual Fields
Frequency: Annually or more frequently if progression is suspected.
Target: Stable, no progression of glaucomatous damage.
Action Threshold: Evidence of progression.
Heart Rate and Blood Pressure
Frequency: Periodically, especially in patients with cardiac risk factors or on concomitant medications.
Target: Within normal limits for the patient.
Action Threshold: Significant bradycardia (<50 bpm), hypotension, or new onset of cardiac symptoms.
Respiratory Symptoms (e.g., dyspnea, wheezing)
Frequency: At each visit, or as symptoms arise.
Target: Absence of respiratory distress.
Action Threshold: New or worsening respiratory symptoms.
Symptom Monitoring
- Blurred vision
- Ocular irritation (stinging, burning, dry eyes)
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm (difficulty breathing, wheezing)
- Dizziness or lightheadedness
- Fatigue
- Depression
- Headache
- Nausea
Special Patient Groups
Pregnancy
Timolol is Pregnancy Category C. Use only if the potential benefit justifies the potential risk to the fetus. Systemic absorption can occur, and beta-blockers have been associated with adverse effects in the fetus/neonate (e.g., bradycardia, hypoglycemia, respiratory depression).
Trimester-Specific Risks:
First Trimester:
Potential for fetal exposure; data limited.
Second Trimester:
Potential for fetal exposure; monitor for fetal bradycardia.
Third Trimester:
Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression if used close to delivery. Monitor neonate for several days after birth.
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 (Moderate risk). Potential for bradycardia, hypotension, and respiratory depression in the infant. Monitor infant for signs of beta-blockade.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in pediatric patients, especially infants and neonates, is generally not recommended due to increased risk of systemic adverse effects (e.g., apnea, bradycardia, bronchospasm) due to higher systemic absorption relative to body weight. If used, extreme caution and close monitoring are required.
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., cardiac or pulmonary effects) due to age-related decline in organ function or concomitant medical conditions. Use with caution and monitor closely.
Clinical Information
Clinical Pearls
- Timolol is a first-line agent for reducing intraocular pressure in many forms of glaucoma and ocular hypertension.
- Despite being an ophthalmic preparation, significant systemic absorption can occur, leading to systemic beta-blockade effects. Always inquire about patient's cardiac and respiratory history (asthma, COPD, heart block, heart failure).
- Patients should be instructed on proper instillation technique, including nasolacrimal occlusion (pressing on the inner corner of the eye for 1-2 minutes after instillation) to minimize systemic absorption and maximize local effect.
- Monitor for signs of systemic beta-blockade, especially bradycardia, hypotension, and bronchospasm.
- If a patient is already on an oral beta-blocker, consider the additive effects on heart rate and blood pressure.
- Timolol-induced depression or fatigue can occur; inquire about mood changes.
Alternative Therapies
- Prostaglandin analogs (e.g., Latanoprost, Travoprost, Bimatoprost)
- Alpha-2 adrenergic agonists (e.g., Brimonidine)
- Carbonic anhydrase inhibitors (e.g., Dorzolamide, Brinzolamide)
- Rho kinase inhibitors (e.g., Netarsudil)
- Cholinergic agonists (e.g., Pilocarpine) - less common first-line
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 5ml bottle
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 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.