Timolol Hemi 0.5% Ophth Soln 5ml

Manufacturer SOMERSET THERAPEUTICS 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.
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Drug Class
Antiglaucoma Agent
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Pharmacologic Class
Non-selective Beta-Adrenergic Blocker
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Pregnancy Category
Category C
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FDA Approved
Sep 1978
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Timolol eye drops are used to lower the pressure inside your eye. This helps treat glaucoma and can prevent further vision loss. It works by reducing the amount of fluid your eye makes.
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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 eyes only. Before using, remove your contact lenses. You can put them back in 15 minutes after administering the medication, unless your eyes are irritated or infected.

To avoid contamination and potential severe eye problems or vision loss, do not touch the container tip to your eye, eyelid, or surrounding skin. Tilt your head back, drop the medication into your eye, and then keep your eyes closed. Apply gentle pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye. Gently blot any excess solution from your eyelid.

If you are using multiple medications in the same eye, wait at least 5 minutes between each application. Some products are designed for morning use if taken once daily, while others may not have specific timing requirements. Consult your pharmacist for guidance on the best schedule for your particular 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 scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or use extra doses to make up for a missed one.
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Lifestyle & Tips

  • Wash your hands thoroughly before administering 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 eye.
  • Do not touch the dropper tip to your eye or any other surface to prevent contamination.
  • Close your eye gently and apply pressure to the inner corner of your eye (near the nose) for 1-2 minutes. This helps prevent the medicine from being absorbed into your bloodstream and increases its effect in the eye.
  • If using other eye drops, wait at least 5-10 minutes between applications.
  • Remove contact lenses before using the drops and wait at least 15 minutes before reinserting them.
  • Store at room temperature, away from light and moisture.

Dosing & Administration

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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:

initial_therapy: Start with 0.25% solution, if response is insufficient, increase to 0.5% solution.
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Pediatric Dosing

Neonatal: Not established; use with extreme caution due to potential for systemic adverse effects (e.g., apnea, bradycardia).
Infant: Not established; use with extreme caution due to potential for systemic adverse effects (e.g., apnea, bradycardia).
Child: Not established; use with extreme caution due to potential for systemic adverse effects.
Adolescent: Not established; use with caution, consider adult dosing with close monitoring.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment typically required for ophthalmic use.
Moderate: No specific adjustment typically required for ophthalmic use.
Severe: No specific adjustment typically required for ophthalmic use, but monitor for systemic effects if significant renal impairment is present.
Dialysis: No specific adjustment typically required for ophthalmic use.

Hepatic Impairment:

Mild: No specific adjustment typically required for ophthalmic use.
Moderate: No specific adjustment typically required for ophthalmic use.
Severe: No specific adjustment typically required for ophthalmic use, but monitor for systemic effects if significant hepatic impairment is present.

Pharmacology

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Mechanism of Action

Timolol is a non-selective beta-adrenergic receptor blocking agent that reduces elevated and normal intraocular pressure (IOP). It primarily acts by decreasing the production of aqueous humor. It does not significantly affect aqueous outflow.
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Pharmacokinetics

Absorption:

Bioavailability: Variable, systemic absorption occurs after ophthalmic administration.
Tmax: Approximately 1-2 hours (for systemic effects after ophthalmic administration).
FoodEffect: Not applicable for ophthalmic administration.

Distribution:

Vd: Not available (for ophthalmic specific).
ProteinBinding: Approximately 10% (systemic).
CnssPenetration: Limited (for ophthalmic use, but systemic absorption can lead to CNS effects).

Elimination:

HalfLife: Approximately 2.5-5 hours (systemic).
Clearance: Not available (for ophthalmic specific).
ExcretionRoute: Primarily renal excretion of metabolites and unchanged drug.
Unchanged: Approximately 20% (systemic).
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Pharmacodynamics

OnsetOfAction: Within 30 minutes.
PeakEffect: 1-2 hours.
DurationOfAction: Up to 24 hours.
Confidence: Medium

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Help 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 attention 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, 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, such as:
+ 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 fatal. 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 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.
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Seek Immediate Medical Attention If You Experience:

  • Slow or irregular heartbeat
  • Dizziness or lightheadedness
  • Shortness of breath or wheezing
  • Chest pain
  • Swelling of ankles or feet
  • Unusual fatigue or weakness
  • Depression or mood changes
  • Blurred vision or eye irritation that persists
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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. Describe the allergic reaction you experienced, including any symptoms.
Certain health conditions, including:
+ Respiratory problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart conditions, including heart block, heart failure (weak heart), or 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.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
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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, discuss them with your doctor.

This medication may also make it more challenging to recognize symptoms of hyperthyroidism, 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 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, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
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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 overdose is suspected, seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222 in the US). Management may include supportive care, atropine for bradycardia, beta-adrenergic stimulants for bronchospasm, or diuretics for cardiac failure.

Drug Interactions

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Contraindicated Interactions

  • Bronchial asthma
  • History of bronchial asthma
  • Severe chronic obstructive pulmonary disease (COPD)
  • Sinus bradycardia
  • Second or third degree atrioventricular block
  • Overt cardiac failure
  • Cardiogenic shock
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Major Interactions

  • Oral beta-adrenergic blocking agents (additive systemic effects)
  • Calcium channel blockers (e.g., verapamil, diltiazem - additive effects on AV conduction and myocardial contractility)
  • Digitalis (additive bradycardia)
  • Quinidine (increased timolol levels due to CYP2D6 inhibition)
  • Clonidine (potential for rebound hypertension upon clonidine withdrawal while on beta-blocker)
  • Catecholamine-depleting drugs (e.g., reserpine - additive hypotensive and/or bradycardic effects)
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Moderate Interactions

  • Adrenergic psychotropic drugs (e.g., MAOIs - potential for hypertensive crisis)
  • General anesthetics (potential for exaggerated hypotension)
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Minor Interactions

  • Not many specific minor interactions for ophthalmic use.

Monitoring

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Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline and assess efficacy.

Timing: Prior to initiation of therapy.

Heart Rate and Blood Pressure

Rationale: To assess for systemic beta-blocker effects, especially in patients with cardiac conditions.

Timing: Prior to initiation of therapy.

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

Rationale: To identify contraindications or high-risk patients.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly (e.g., 2-4 weeks after initiation, then every 3-6 months or as clinically indicated).

Target: Individualized, typically <21 mmHg or target set by ophthalmologist.

Action Threshold: IOP not adequately controlled, or significant increase from baseline.

Heart Rate and Blood Pressure

Frequency: Periodically, especially in patients with cardiac conditions or on other systemic medications.

Target: Normal physiological range for the patient.

Action Threshold: Significant bradycardia (<50 bpm), hypotension, or symptomatic changes.

Respiratory Symptoms

Frequency: Periodically, inquire about new or worsening shortness of breath, wheezing.

Target: Not applicable.

Action Threshold: Development or worsening of respiratory symptoms.

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Symptom Monitoring

  • Bradycardia (slow heart rate)
  • Hypotension (low blood pressure)
  • Bronchospasm (wheezing, shortness of breath)
  • Dizziness or lightheadedness
  • Fatigue or weakness
  • Depression or mood changes
  • Signs of cardiac failure (e.g., swelling of ankles/feet, unusual fatigue, shortness of breath)

Special Patient Groups

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Pregnancy

Timolol is classified as 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 can cause adverse effects in the fetus/neonate (e.g., bradycardia, hypoglycemia).

Trimester-Specific Risks:

First Trimester: Potential for fetal exposure, but data are limited. Risk generally considered low for ophthalmic use.
Second Trimester: Potential for fetal exposure, monitor for fetal bradycardia.
Third Trimester: Increased risk of adverse effects in the neonate (e.g., bradycardia, respiratory depression, hypoglycemia) if exposed close to delivery. Monitor neonate closely.
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Lactation

Timolol is excreted in human milk. While the amount transferred via ophthalmic use is likely small, caution is advised. Monitor breastfed infants for signs of beta-blockade (e.g., bradycardia, lethargy, poor feeding).

Infant Risk: L3 (Moderately Safe) - Detectable in breast milk, but adverse effects are not expected. However, some sources may classify as L4 (Possibly Hazardous) due to potential for systemic effects in sensitive infants.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use with extreme caution in infants and young children due to increased risk of systemic adverse effects (e.g., apnea, bradycardia, hypotension) due to higher systemic absorption relative to body weight. Close monitoring is essential if used.

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Geriatric Use

No specific dose adjustment is typically required. However, elderly patients may be more susceptible to systemic adverse effects (e.g., bradycardia, hypotension, CNS effects) due to age-related changes in organ function. Monitor closely for adverse reactions.

Clinical Information

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Clinical Pearls

  • Timolol ophthalmic solution can cause systemic beta-blocker effects due to systemic absorption. Always inquire about a patient's history of asthma, COPD, bradycardia, or heart failure before prescribing.
  • To minimize systemic absorption and maximize ocular bioavailability, instruct patients to occlude the nasolacrimal duct (apply gentle pressure to the inner corner of the eye) for 1-2 minutes after instillation.
  • Patients should be advised to remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
  • Regular monitoring of intraocular pressure, heart rate, and blood pressure is crucial, especially during the initial weeks of therapy.
  • Timolol is often a first-line agent for glaucoma due to its efficacy and once or twice-daily dosing, but contraindications must be carefully considered.
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Alternative Therapies

  • Prostaglandin analogs (e.g., Latanoprost, Travoprost, Bimatoprost)
  • Alpha-adrenergic agonists (e.g., Brimonidine)
  • Carbonic anhydrase inhibitors (e.g., Dorzolamide, Brinzolamide)
  • Miotics (e.g., Pilocarpine)
  • Rho kinase inhibitors (e.g., Netarsudil)
  • Laser trabeculoplasty
  • Surgical procedures (e.g., trabeculectomy)
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Cost & Coverage

Average Cost: Varies widely by pharmacy and formulation (e.g., 5ml bottle of 0.5% solution can range from $10-$50+). per 5ml bottle
Generic Available: Yes
Insurance Coverage: Typically Tier 1 or Tier 2 for generic formulations, Tier 3 or higher for brand names.
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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 this medication, don't hesitate to discuss them with 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, including the amount taken and the time it happened, to help healthcare professionals provide the best possible care.