Timolol 0.5% GF Opth Soln 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 the pressure inside your eye. High eye pressure can damage your optic nerve and lead to glaucoma, which can cause vision loss. These drops work by reducing the amount of fluid your eye produces.
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 Instructions
1. Use this medication for the eye only.
2. Remove contact lenses before using the medication. You can put them back in 15 minutes after application, unless your eyes are irritated or infected.
3. Before each use, turn the container upside down and shake it once.
4. If you use other eye medications, apply them 10 minutes before using this gel.
5. To avoid contamination, do not touch the container tip to your eye, eyelid, or skin.
6. Tilt your head back and gently drop the medication into your eye.
7. After application, 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.
8. Gently blot any excess solution from your eyelid.
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 the medication as directed, even if your symptoms improve. Take the medication at the same time every day.
Administration Instructions
1. Use this medication for the eye only.
2. Remove contact lenses before using the medication. You can put them back in 15 minutes after application, unless your eyes are irritated or infected.
3. Before each use, turn the container upside down and shake it once.
4. If you use other eye medications, apply them 10 minutes before using this gel.
5. To avoid contamination, do not touch the container tip to your eye, eyelid, or skin.
6. Tilt your head back and gently drop the medication into your eye.
7. After application, 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.
8. Gently blot any excess solution from your eyelid.
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
- Wash hands thoroughly before and after applying eye drops.
- Tilt your head back, pull down your lower eyelid to form a pocket, and look up. Gently squeeze the bottle to release one drop into the pocket. Do not touch the tip of the dropper to your eye or any other surface.
- Close your eye gently for 1-2 minutes and press a finger to the inner corner of your eye (near the nose) to prevent the medicine from draining into your tear duct and being absorbed systemically.
- If using other eye drops, wait at least 5-10 minutes between applications.
- Remove contact lenses before applying and wait at least 15 minutes before reinserting them.
- Store at room temperature, away from light and moisture. Do not freeze.
- Do not stop using this medication without consulting your doctor, even if you feel well, as eye pressure can increase without symptoms.
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% or 0.5% gel-forming solution in the affected eye(s) once daily.
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
open_angle_glaucoma:
One drop of 0.25% or 0.5% gel-forming solution in the affected eye(s) once daily.
ocular_hypertension:
One drop of 0.25% or 0.5% gel-forming solution in the affected eye(s) once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established, use with extreme caution due to potential for systemic adverse effects (e.g., apnea, bradycardia).
Child:
Not established, use with caution and lower concentrations/doses if used off-label. Systemic absorption can lead to significant adverse effects.
Adolescent:
Not established, use with caution and lower concentrations/doses if used off-label. 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.
Dialysis:
No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
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.
Pharmacology
Mechanism of Action
Timolol 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 through a reduction in aqueous humor production. Some studies suggest a slight increase in aqueous humor outflow facility.
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely quantified for ophthalmic, but systemic absorption occurs. Peak plasma concentrations are generally low (ng/mL range) after ophthalmic administration.
Tmax:
Approximately 1-2 hours after ophthalmic administration (for systemic absorption).
FoodEffect:
Not applicable for ophthalmic formulation.
Distribution:
Vd:
Not precisely quantified for ophthalmic, but distributes widely in tissues after systemic absorption.
ProteinBinding:
Approximately 60% (for systemic timolol).
CnssPenetration:
Limited, but can cross the blood-brain barrier to some extent, leading to CNS effects in susceptible individuals.
Elimination:
HalfLife:
Approximately 4 hours (systemic, after ophthalmic administration).
Clearance:
Not precisely quantified for ophthalmic.
ExcretionRoute:
Primarily renal (metabolites and unchanged drug).
Unchanged:
Approximately 20% of an oral dose is excreted unchanged in urine; proportion for ophthalmic is lower due to minimal absorption.
Pharmacodynamics
OnsetOfAction:
Within 30 minutes after single dose.
PeakEffect:
1-2 hours after single dose.
DurationOfAction:
Up to 24 hours (for gel-forming solution, allowing once-daily dosing).
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while 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
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with 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.
Although rare, some people may experience severe and potentially life-threatening side effects while 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
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with 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 irritation, redness, or pain
- Changes in vision
- Slow or irregular heartbeat
- Dizziness or lightheadedness
- Shortness of breath, wheezing, or difficulty breathing
- Swelling of the ankles 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 allergic reaction you experienced, including any symptoms that occurred.
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 taking another medication similar to this one. If you are unsure, consult your doctor or pharmacist to determine if there are any potential interactions.
Please note that this is not an exhaustive list of all possible interactions between this medication and other drugs or health conditions. Therefore, 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 complete medical history, including any health problems you have
To ensure your safety, always verify with your doctor before starting, stopping, or changing the dose of any medication.
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 allergic reaction you experienced, including any symptoms that occurred.
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 taking another medication similar to this one. If you are unsure, consult your doctor or pharmacist to determine if there are any potential interactions.
Please note that this is not an exhaustive list of all possible interactions between this medication and other drugs or health conditions. Therefore, 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 complete medical history, including any health problems you have
To ensure your safety, always verify with your doctor before starting, stopping, or changing the dose of any medication.
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 hypoglycemia (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 concerns or questions, 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 exams to check your intraocular pressure and vision.
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 or concerns, discuss them with your doctor.
This medication may also conceal symptoms of hyperthyroidism (an overactive thyroid), 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 exposed to the allergen again. 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 hypoglycemia (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 concerns or questions, 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 exams to check your intraocular pressure and vision.
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 or concerns, discuss them with your doctor.
This medication may also conceal symptoms of hyperthyroidism (an overactive thyroid), 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 exposed to the allergen again. 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 (very low blood pressure)
- Bronchospasm (difficulty breathing, wheezing)
- Acute cardiac failure
- Dizziness
- Fainting
What to Do:
If you suspect an overdose, seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222 in the US). Treatment is supportive and symptomatic. Atropine for bradycardia, beta-adrenergic stimulants for bronchospasm, 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)
- Calcium channel blockers (e.g., verapamil, diltiazem) (risk of AV conduction disturbances, left ventricular failure, hypotension)
- Catecholamine-depleting drugs (e.g., reserpine, guanethidine) (additive hypotensive and/or bradycardic effects)
- Digitalis (additive effects on AV conduction and heart rate)
- Quinidine (increased plasma levels of timolol due to CYP2D6 inhibition)
- Clonidine (potential for rebound hypertension upon clonidine withdrawal while on beta-blocker)
Moderate Interactions
- Adrenergic psychotropics (e.g., epinephrine, norepinephrine) (potential for exaggerated pressor response)
- NSAIDs (may reduce the hypotensive effect of beta-blockers)
- Insulin and oral hypoglycemic agents (beta-blockers may mask signs of hypoglycemia)
- General anesthetics (potential for exaggerated hypotension)
Minor Interactions
- Not specifically identified for ophthalmic timolol beyond systemic interactions.
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 monitor for systemic beta-blockade effects (bradycardia, hypotension).
Timing: Before initiation of therapy.
Respiratory Status (e.g., lung sounds, history of asthma/COPD)
Rationale: To assess risk of bronchospasm, especially in susceptible patients.
Timing: Before initiation of therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by ophthalmologist (e.g., 2-4 weeks after initiation, then every 3-6 months).
Target: Individualized, typically <21 mmHg or target pressure to prevent progression.
Action Threshold: If IOP remains elevated or increases, consider dose adjustment or alternative therapy.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial therapy or dose changes.
Target: Normal physiological range for the patient.
Action Threshold: Bradycardia (<50 bpm), significant hypotension, or symptomatic changes warrant evaluation and potential discontinuation.
Ocular Examination (e.g., visual acuity, optic nerve head, visual fields)
Frequency: Regularly, as part of glaucoma management.
Target: Stable or improved.
Action Threshold: Progression of glaucoma warrants re-evaluation of treatment.
Symptom Monitoring
- Blurred vision
- Ocular irritation (stinging, burning)
- Dry eyes
- Bradycardia (slow heart rate)
- Hypotension (dizziness, lightheadedness)
- Bronchospasm (shortness of breath, wheezing)
- Fatigue
- Depression
- Headache
- Insomnia
Special Patient Groups
Pregnancy
Timolol is Pregnancy Category C. Studies in animals have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal studies; systemic absorption, though minimal, can occur.
Second Trimester:
Similar considerations as first trimester.
Third Trimester:
Potential for systemic beta-blockade effects in the neonate (e.g., bradycardia, hypoglycemia, respiratory depression) if used close to delivery.
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). Potential for bradycardia, hypotension, and respiratory depression in the infant, especially with higher doses or in premature infants. Monitor infant for signs of beta-blockade.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in infants and children, especially neonates, is generally not recommended due to increased risk of systemic adverse effects (e.g., apnea, bradycardia, hypotension) due to higher systemic absorption relative to body weight. If used, extreme caution, lower concentrations, 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., bradycardia, hypotension) due to age-related physiological changes or concomitant cardiovascular/respiratory conditions. Monitor closely.
Clinical Information
Clinical Pearls
- Timolol gel-forming solution (e.g., Timoptic-XE) is designed for once-daily dosing, which can improve patient adherence compared to twice-daily solutions.
- Instruct patients 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 potential side effects.
- Patients with a history of asthma, COPD, or significant cardiac conditions (e.g., severe bradycardia, heart block, heart failure) should be carefully screened before initiating timolol ophthalmic due to the risk of systemic beta-blockade.
- Be aware of potential masking of hypoglycemia symptoms in diabetic patients and hyperthyroidism symptoms in patients with thyrotoxicosis.
- Regular monitoring of intraocular pressure is crucial to assess treatment efficacy.
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 by pharmacy and concentration/formulation (e.g., $20-$100+) 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. 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.