Timolol 0.25% GF Ophth 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 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 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 only in the eye.
2. Remove contact lenses before using the medication. You can put them back in 15 minutes after administration, 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, lid, or skin, as this can lead to bacterial infection and potentially cause severe eye problems or vision loss.
6. Tilt your head back and drop the medication into your eye.
7. After administration, keep your eyes closed and apply gentle 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, 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 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 only in the eye.
2. Remove contact lenses before using the medication. You can put them back in 15 minutes after administration, 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, lid, or skin, as this can lead to bacterial infection and potentially cause severe eye problems or vision loss.
6. Tilt your head back and drop the medication into your eye.
7. After administration, keep your eyes closed and apply gentle 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, 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 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 one drop. Close your eye gently for 1-2 minutes to allow the medication to be absorbed and reduce systemic absorption.
- If using other eye drops, wait at least 5-10 minutes between applications.
- Remove contact lenses before applying eye drops and wait at least 15 minutes before reinserting them.
- Inform your doctor about all other medications you are taking, especially oral beta-blockers, heart medications, or asthma medications.
- Do not stop using this medication without consulting your doctor, even if you feel well, as high eye pressure often has no 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:
1 drop of 0.25% solution in the affected eye(s) once daily (for gel-forming solution)
Dose Range:
0.25 - 0.5 mg
Condition-Specific Dosing:
ocularHypertension:
1 drop of 0.25% solution in the affected eye(s) once daily
openAngleGlaucoma:
1 drop of 0.25% solution in the affected eye(s) once daily
Pediatric Dosing
Neonatal:
Not established; generally not recommended due to risk of systemic absorption and adverse effects.
Infant:
Not established; generally not recommended due to risk of systemic absorption and adverse effects.
Child:
Not established; use with extreme caution and only if benefits outweigh risks, due to potential for systemic adverse effects.
Adolescent:
Dosing similar to adults may be considered, but caution is advised due to potential for systemic adverse effects.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
Moderate:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
Severe:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
Dialysis:
No specific adjustment needed for ophthalmic use.
Hepatic Impairment:
Mild:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
Moderate:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
Severe:
No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.
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 of aqueous humor production. Some studies suggest a slight increase in aqueous humor outflow facility may also contribute.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 70-80% (systemic absorption after ophthalmic administration, though variable)
Tmax:
Approximately 1-2 hours (systemic after ophthalmic administration)
FoodEffect:
Not applicable for ophthalmic administration.
Distribution:
Vd:
Not available (systemic Vd for oral timolol is approximately 1.7 L/kg)
ProteinBinding:
Approximately 10%
CnssPenetration:
Limited (can cross blood-brain barrier, but ophthalmic systemic levels are low)
Elimination:
HalfLife:
Approximately 4-6 hours (systemic after ophthalmic administration)
Clearance:
Not available
ExcretionRoute:
Renal (metabolites and unchanged drug)
Unchanged:
Approximately 20% (excreted unchanged in urine)
Pharmacodynamics
OnsetOfAction:
Approximately 30 minutes
PeakEffect:
Approximately 1-2 hours
DurationOfAction:
Up to 24 hours (especially for gel-forming solution)
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
+ Difficulty 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
+ Changes in balance
+ Drooping on one side of the face
+ Blurred vision
Eye problems, such as:
+ Changes in vision
+ Eye pain
+ Severe eye irritation
Cardiovascular symptoms, including:
+ Severe dizziness or fainting
+ 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, or if they persist or bother you, 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
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.
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
+ Difficulty 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
+ Changes in balance
+ Drooping on one side of the face
+ Blurred vision
Eye problems, such as:
+ Changes in vision
+ Eye pain
+ Severe eye irritation
Cardiovascular symptoms, including:
+ Severe dizziness or fainting
+ 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, or if they persist or bother you, 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
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 irritation, redness, or pain
- Changes in vision
- Slow heart rate (bradycardia)
- Dizziness or fainting
- Shortness of breath, wheezing, or difficulty breathing
- Swelling of the face, lips, tongue, or throat (signs of allergic reaction)
- 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:
+ 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 a similar medication. 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 existing medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ 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 a similar medication. 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 existing medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. When performing tasks that require clear vision, such as driving, exercise caution to ensure your safety.
This medication may mask certain symptoms of 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 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 obscure 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 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 increased risk of a more severe reaction if you are exposed to the allergen again. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may be less effective while taking this drug.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
This medication may mask certain symptoms of 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 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 obscure 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 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 increased risk of a more severe reaction if you are exposed to the allergen again. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may be less effective while taking this drug.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe bradycardia (very slow heart rate)
- Hypotension (very low blood pressure)
- Bronchospasm (severe difficulty breathing)
- Acute cardiac failure
- Dizziness
- Headache
What to Do:
If overdose is suspected, seek immediate medical attention or call a poison control center (1-800-222-1222). Management is supportive and symptomatic. Atropine for bradycardia, beta-adrenergic stimulants for bronchospasm, vasopressors for hypotension, and diuretics for cardiac 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)
- Quinidine (may inhibit CYP2D6, leading to increased systemic timolol levels and enhanced beta-blockade)
- Clonidine (risk of rebound hypertension upon clonidine withdrawal while on beta-blocker)
- Digitalis glycosides (increased risk of bradycardia, AV block)
Moderate Interactions
- Catecholamine-depleting drugs (e.g., reserpine - additive effects, hypotension, bradycardia)
- Adrenergic psychotropic drugs (e.g., MAOIs - potential for hypertensive crisis)
- Other topical beta-blockers (additive effects)
- Pilocarpine (may enhance IOP lowering)
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Prior to initiation of therapy.
Heart Rate and Blood Pressure
Rationale: To monitor for potential systemic beta-blockade effects (bradycardia, hypotension).
Timing: Prior to initiation of therapy.
Respiratory Function (e.g., spirometry)
Rationale: For patients with pre-existing respiratory conditions (asthma, COPD) due to risk of bronchospasm.
Timing: Prior to initiation of therapy, if indicated.
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 target IOP, typically <21 mmHg or a significant reduction from baseline.
Action Threshold: If IOP is not adequately controlled or increases, consider dose adjustment or alternative therapy.
Heart Rate and Blood Pressure
Frequency: Periodically, especially during initial treatment or dose changes.
Target: Maintain within normal limits for the patient.
Action Threshold: Significant bradycardia (<50 bpm), hypotension, or symptomatic cardiovascular effects warrant re-evaluation.
Ocular Examination (e.g., slit lamp, visual acuity)
Frequency: Regularly, as determined by ophthalmologist.
Target: Not applicable
Action Threshold: Any signs of ocular irritation, allergic reaction, or vision changes.
Symptom Monitoring
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Dizziness or lightheadedness
- Bronchospasm (difficulty breathing, wheezing)
- Fatigue
- Depression
- Ocular irritation (burning, stinging, itching)
- Blurred vision
- Dry eyes
Special Patient Groups
Pregnancy
Timolol is Pregnancy Category C. It should be used during pregnancy 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:
Limited data, but potential for fetal exposure. Use only if clearly needed.
Second Trimester:
Potential for fetal exposure and systemic effects. Monitor fetal heart rate.
Third Trimester:
Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate closely after birth.
Lactation
Timolol is excreted in human milk. The American Academy of Pediatrics considers timolol to be compatible with breastfeeding, but caution is advised. Monitor breastfed infants for signs of beta-blockade (e.g., bradycardia, somnolence, poor feeding).
Infant Risk:
L3 (Moderately Safe) - Monitor infant for bradycardia, somnolence, and other signs of beta-blockade. Consider using the lowest effective dose and applying nasolacrimal occlusion to minimize systemic absorption.
Pediatric Use
Use in pediatric patients, especially neonates and infants, is generally not recommended due to the potential for serious systemic adverse reactions (e.g., apnea, bradycardia, bronchospasm) from systemic absorption. If used, extreme caution and close monitoring are required. Dosing is not well-established.
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 gel-forming solution (GF) is typically dosed once daily, which can improve patient adherence compared to twice-daily solutions.
- Instruct patients on proper instillation technique, including nasolacrimal occlusion (closing the eye and gently pressing on the inner corner for 1-2 minutes) to minimize systemic absorption and potential side effects.
- Always inquire about a patient's history of asthma, COPD, bradycardia, heart block, or heart failure before prescribing timolol, as it is contraindicated or requires extreme caution in these conditions.
- Be aware of potential drug interactions, especially with oral beta-blockers, calcium channel blockers, and quinidine, which can lead to additive systemic effects.
- If a patient experiences significant ocular irritation or systemic side effects, consider switching to a different class of IOP-lowering medication or a lower concentration of timolol.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, bimatoprost, travoprost)
- Alpha-adrenergic agonists (e.g., brimonidine, apraclonidine)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide, acetazolamide)
- Rho kinase inhibitors (e.g., netarsudil)
- Cholinergic agonists (e.g., pilocarpine)
- Laser trabeculoplasty
- Surgical procedures (e.g., trabeculectomy)
Cost & Coverage
Average Cost:
$20 - $60 per 5ml 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 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.