Timolol Maleate 0.5% Ophth Soln 5ml

Manufacturer SANDOZ Active Ingredient Timolol Eye Drops (Bottle)(TIM oh lol) Pronunciation TIM oh lol
It is used to treat glaucoma.It is used to lower high eye pressure.
đŸˇī¸
Drug Class
Antiglaucoma Agent
đŸ§Ŧ
Pharmacologic Class
Non-selective Beta-Adrenergic Blocker
🤰
Pregnancy Category
Category C
✅
FDA Approved
Sep 1978
âš–ī¸
DEA Schedule
Not Controlled

Overview

â„šī¸

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 important to use it regularly as prescribed, even if you don't feel any symptoms, to protect your eyesight.
📋

How to Use This Medicine

Proper Use of This Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. Use this medication as directed, even if your symptoms improve. Take it at the same time every day.

Administration

This medication is for use in the eye only. Before using, remove your contact lenses. You can put them back in 15 minutes after administering the medication, unless your eyes are irritated or infected.

To avoid contamination, do not touch the container tip to your eye, lid, or other skin, as this can lead to bacterial infection and potentially cause severe eye problems or vision loss.

Tilt your head back, drop the medication into your eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye. Gently blot any excess solution from your eyelid.

If you are using multiple medications in the same eye, wait at least 5 minutes between each application. Some products are designed for morning use if taken once daily, while others have no specific timing requirements. Consult your pharmacist for guidance on using this medication.

Storage and Disposal

Store the medication in an upright position at room temperature, away from light. Do not freeze the medication.

Missed Dose

If you miss a dose, use it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not use two doses at the same time or take extra doses.
💡

Lifestyle & Tips

  • Wash hands thoroughly before and after use.
  • Do not touch the dropper tip to any surface, including the eye, to avoid contamination.
  • Tilt head back, pull down lower eyelid, and look up. Gently squeeze the bottle to instill one drop into the eye. Close eye gently for 1-2 minutes to allow absorption and minimize systemic effects.
  • 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.
  • Inform your doctor about all other medications you are taking, especially oral beta-blockers or heart medications.
  • Do not stop using the drops suddenly without consulting your doctor.

Dosing & Administration

đŸ‘¨â€âš•ī¸

Adult Dosing

Standard Dose: 1 drop of 0.25% or 0.5% solution in the affected eye(s) twice daily.
Dose Range: 0.25 - 0.5 mg

Condition-Specific Dosing:

initialTherapy: 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.
đŸ‘ļ

Pediatric Dosing

Neonatal: Not established (use with extreme caution due to potential for systemic effects)
Infant: Not established (use with extreme caution due to potential for systemic effects)
Child: Not established (use with extreme caution due to potential for systemic effects, particularly in younger children and infants due to higher systemic absorption and potential for apnea, bradycardia, and hypotension). Limited data suggest 0.25% once or twice daily may be used in some cases under strict medical supervision.
Adolescent: Similar to adult dosing, but with caution and monitoring for systemic effects.
âš•ī¸

Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed for ophthalmic use.
Moderate: No specific adjustment needed for ophthalmic use.
Severe: No specific adjustment needed for ophthalmic use.
Dialysis: No specific adjustment needed for ophthalmic use, as systemic absorption is minimal.

Hepatic Impairment:

Mild: No specific adjustment needed for ophthalmic use.
Moderate: No specific adjustment needed for ophthalmic use.
Severe: No specific adjustment needed for ophthalmic use.

Pharmacology

đŸ”Ŧ

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 of aqueous humor production. Some studies suggest a slight increase in aqueous outflow facility may also contribute.
📊

Pharmacokinetics

Absorption:

Bioavailability: Systemic absorption occurs after ophthalmic administration, but is variable and generally low (e.g., 5-10% of topical dose can be absorbed systemically).
Tmax: Plasma concentrations peak approximately 1-2 hours after ophthalmic administration.
FoodEffect: Not applicable for ophthalmic solution.

Distribution:

Vd: Approximately 1.7 L/kg (systemic)
ProteinBinding: Approximately 10%
CnssPenetration: Limited (systemic absorption can lead to CNS effects, but direct penetration from ophthalmic application is low).

Elimination:

HalfLife: Approximately 2-4 hours (systemic, after ophthalmic administration)
Clearance: Approximately 5-8 mL/min/kg (systemic)
ExcretionRoute: Primarily renal (metabolites and some unchanged drug).
Unchanged: Approximately 20% (systemic, excreted unchanged in urine).
âąī¸

Pharmacodynamics

OnsetOfAction: Within 30 minutes after single dose.
PeakEffect: 1-2 hours after single dose.
DurationOfAction: 24 hours (IOP lowering effect).

Safety & Warnings

âš ī¸

Side Effects

Urgent Side Effects: Seek Medical Attention Immediately

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 medical help right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Neurological symptoms, including:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Eye problems, such as:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Cardiovascular symptoms, including:
+ Very bad dizziness or passing out
+ Slow heartbeat
+ Abnormal heartbeat
+ Chest pain
+ Muscle weakness
Heart failure, which can be fatal. Seek immediate medical attention 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 list is not exhaustive, and you may experience other 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
  • Changes in vision
  • Slow or irregular heartbeat
  • Dizziness or lightheadedness
  • Shortness of breath or wheezing
  • Swelling of hands or feet
  • Unusual fatigue 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
+ Slow heartbeat
If you are currently using a similar medication. If you are unsure, consult your doctor or pharmacist.

Please note that this is not an exhaustive list of all potential interactions with this medication. To ensure your safety, it is crucial to:

Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor and pharmacist.
Verify that it is safe to take this medication with your existing medications and health conditions.
* Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
âš ī¸

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.
🆘

Overdose Information

Overdose Symptoms:

  • Severe bradycardia (very slow heart rate)
  • Hypotension (low blood pressure)
  • Bronchospasm (difficulty breathing, wheezing)
  • Acute cardiac failure
  • Dizziness
  • Headache

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic, potentially including atropine for bradycardia, vasopressors for hypotension, and bronchodilators for bronchospasm.

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).
  • Catecholamine-depleting drugs (e.g., reserpine, guanethidine) (additive hypotensive and/or bradycardic effects).
  • Digitalis (increased risk of bradycardia and AV block).
🟡

Moderate Interactions

  • Quinidine (inhibits CYP2D6, potentially increasing systemic timolol levels and enhancing beta-blockade).
  • Clonidine (paradoxical hypertension upon clonidine withdrawal if beta-blocker is not also withdrawn gradually).
  • Adrenergic psychotropic drugs (e.g., MAOIs, TCAs) (potential for enhanced pressor response or hypotension).
đŸŸĸ

Minor Interactions

  • Not available

Monitoring

đŸ”Ŧ

Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline and assess efficacy of treatment.

Timing: Before initiating therapy.

Heart Rate and Blood Pressure

Rationale: To assess for potential systemic beta-blockade effects (bradycardia, hypotension).

Timing: Before initiating therapy.

Respiratory Status (e.g., lung sounds, history of asthma/COPD)

Rationale: To identify risk of bronchospasm, especially in patients with reactive airway disease.

Timing: Before initiating 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 target IOP to prevent optic nerve damage.

Action Threshold: IOP above target range or signs of glaucoma progression.

Heart Rate and Blood Pressure

Frequency: Periodically, especially during initial therapy or dose changes.

Target: Maintain within patient's normal limits, avoid symptomatic bradycardia (<50 bpm) or hypotension.

Action Threshold: Symptomatic bradycardia, hypotension, or significant changes from baseline.

Respiratory Symptoms (e.g., shortness of breath, wheezing)

Frequency: Ongoing patient inquiry.

Target: Absence of new or worsening respiratory symptoms.

Action Threshold: Development of new or worsening respiratory symptoms, especially in patients with pre-existing respiratory conditions.

đŸ‘ī¸

Symptom Monitoring

  • Blurred vision
  • Eye irritation (stinging, burning)
  • Bradycardia (slow heart rate)
  • Hypotension (dizziness, lightheadedness)
  • Bronchospasm (shortness of breath, wheezing, difficulty breathing)
  • Fatigue
  • Depression
  • Headache

Special Patient Groups

🤰

Pregnancy

Category C. Use only if the potential benefit justifies the potential risk to the fetus. Systemic absorption occurs, and beta-blockers can cause adverse effects in the fetus/neonate (e.g., bradycardia, hypoglycemia, respiratory depression).

Trimester-Specific Risks:

First Trimester: Potential for fetal exposure, but data on teratogenicity are limited and generally reassuring for beta-blockers.
Second Trimester: Risk of fetal growth restriction and other beta-blocker effects.
Third Trimester: Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression, especially if used close to delivery. Monitor neonate for these effects.
🤱

Lactation

Excreted in human milk. Caution should be exercised when timolol maleate is administered to a nursing mother. Potential for serious adverse reactions in the infant (e.g., bradycardia, respiratory depression). Consider discontinuing nursing or the drug, weighing the importance of the drug to the mother.

Infant Risk: Low to moderate risk. Monitor infant for bradycardia, lethargy, and poor feeding.
đŸ‘ļ

Pediatric Use

Use with extreme caution, especially in infants and young children, due to increased systemic absorption and potential for severe systemic adverse reactions (e.g., apnea, bradycardia, hypotension, hypothermia). Close monitoring is essential. Not recommended for routine use in neonates and infants.

👴

Geriatric Use

Generally well-tolerated, but elderly patients may be more susceptible to systemic adverse effects (e.g., bradycardia, hypotension, bronchospasm) due to decreased renal/hepatic function or concomitant medications. Start with lower concentrations and monitor closely.

Clinical Information

💎

Clinical Pearls

  • Timolol is often a first-line agent for glaucoma due to its efficacy and once or twice daily dosing.
  • 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.
  • Patients with asthma, COPD, severe bradycardia, or heart block should generally avoid timolol. If used, monitor closely.
  • Occluding the nasolacrimal duct (pressing on the inner corner of the eye for 1-2 minutes after instillation) can help minimize systemic absorption and maximize ocular bioavailability.
  • Inform patients about the potential for transient stinging or burning upon instillation.
  • Regular IOP monitoring is crucial to ensure therapeutic 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)
  • Laser trabeculoplasty
  • Glaucoma filtration surgery
💰

Cost & Coverage

Average Cost: Varies widely, typically $15-$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'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 ensure you receive the best possible care.