Timolol Maleate 5mg Tablets
WARNING: Do not stop taking this drug all of a sudden. If you do, chest pain that is worse and in some cases heart attack may occur. The risk may be greater if you have certain types of heart disease. To avoid side effects, you will want to slowly stop this drug as ordered by your doctor. Call your doctor right away if you have new or worse chest pain or if other heart problems occur. @ COMMON USES: It is used to treat high blood pressure.It is used after a heart attack to help prevent future heart attacks and lengthen life.It is used to prevent migraine headaches.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antihypertensive, Antianginal, Antimigraine
Pharmacologic Class
Non-selective Beta-Adrenergic Blocker
Pregnancy Category
C
FDA Approved
May 1978
DEA Schedule
Not Controlled
Overview
What is this medicine?
Timolol is a type of medicine called a beta-blocker. It works by slowing down your heart rate and relaxing blood vessels, which helps to lower high blood pressure, prevent chest pain (angina), and reduce the frequency of migraine headaches. It's important to take it regularly as prescribed and never stop it suddenly without talking to your doctor.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless specifically instructed to do so. Instead, consult with your pharmacist for guidance on the proper disposal method. You may also want to inquire about drug take-back programs available in your area.
What to Do If You Miss a 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 take extra doses to make up for the missed one.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless specifically instructed to do so. Instead, consult with your pharmacist for guidance on the proper disposal method. You may also want to inquire about drug take-back programs available in your area.
What to Do If You Miss a 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 take extra doses to make up for the missed one.
Lifestyle & Tips
- Continue to monitor your blood pressure and heart rate at home as advised by your doctor.
- Do not stop taking this medication suddenly, as it can worsen your condition.
- Avoid or limit alcohol consumption, as it can increase the blood pressure-lowering effect.
- Maintain a healthy diet low in sodium and saturated fats.
- Engage in regular physical activity as recommended by your doctor.
- Report any unusual symptoms, especially shortness of breath, slow heart rate, or dizziness.
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:
Hypertension: Initially 10 mg once daily or 5 mg twice daily. Maintenance 10-20 mg once daily. Angina: 15-45 mg per day in 2-3 divided doses. Migraine Prophylaxis: Initially 10 mg twice daily, maintenance 10-20 mg twice daily.
Dose Range:
5 - 60 mg
Condition-Specific Dosing:
hypertension:
Initial: 10 mg once daily or 5 mg twice daily. Maintenance: 10-20 mg once daily, max 60 mg/day.
anginaPectoris:
15-45 mg per day in 2-3 divided doses.
migraineProphylaxis:
Initial: 10 mg twice daily. Maintenance: 10-20 mg twice daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (limited data, generally not recommended)
Adolescent:
Not established (limited data, generally not recommended)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment usually needed.
Moderate:
Consider lower initial doses and careful titration.
Severe:
Reduce dose (e.g., by 50%) and monitor closely. Accumulation may occur.
Dialysis:
Timolol is not significantly removed by hemodialysis. Dose adjustment may be needed based on renal function.
Hepatic Impairment:
Mild:
No specific adjustment usually needed.
Moderate:
Consider lower initial doses and careful titration due to reduced metabolism.
Severe:
Reduce dose (e.g., by 50%) and monitor closely due to significantly impaired metabolism.
Pharmacology
Mechanism of Action
Timolol is a non-selective beta-adrenergic receptor blocking agent. It competitively blocks beta-1 (myocardial) and beta-2 (bronchial and vascular) adrenergic receptors. This results in decreased heart rate, decreased myocardial contractility, and reduced renin release from the kidneys, leading to a reduction in blood pressure. It also reduces intraocular pressure by decreasing aqueous humor production.
Pharmacokinetics
Absorption:
Bioavailability:
50-60%
Tmax:
1-2 hours
FoodEffect:
Food may slightly increase absorption but is not clinically significant.
Distribution:
Vd:
1.7 L/kg
ProteinBinding:
Approximately 10%
CnssPenetration:
Limited (can cross blood-brain barrier, leading to CNS effects)
Elimination:
HalfLife:
4-5 hours
Clearance:
Approximately 5-8 mL/min/kg
ExcretionRoute:
Renal (primarily as metabolites, small amount unchanged)
Unchanged:
Approximately 20% (renal)
Pharmacodynamics
OnsetOfAction:
Within 30 minutes
PeakEffect:
1-2 hours
DurationOfAction:
24 hours (with once-daily dosing due to sustained beta-blockade)
Safety & Warnings
BLACK BOX WARNING
Cardiac Ischemia After Abrupt Discontinuation: Following abrupt cessation of therapy with beta-adrenergic blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered timolol maleate, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 to 2 weeks and the patient should be carefully monitored. If angina worsens or acute coronary insufficiency develops, timolol maleate administration should be reinstituted promptly, at least temporarily, and other measures appropriate for the management of unstable angina pectoris should be taken. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue timolol maleate therapy abruptly even in patients treated only for hypertension. Bronchospastic Disease: Patients with bronchospastic diseases (e.g., bronchial asthma, chronic obstructive pulmonary disease) should not receive beta-blockers, including timolol maleate. If timolol maleate is the only available treatment option, it should be used with extreme caution and at the lowest effective dose.
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
Severe dizziness or fainting
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Chest pain or pressure
Slow heartbeat
Abnormal heartbeat
Muscle weakness
Changes in vision
Feeling cold
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although 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 unusual symptoms that bother you or persist, contact your doctor:
Dizziness
Fatigue
Weakness
* Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult 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
Severe dizziness or fainting
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Chest pain or pressure
Slow heartbeat
Abnormal heartbeat
Muscle weakness
Changes in vision
Feeling cold
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although 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 unusual symptoms that bother you or persist, contact your doctor:
Dizziness
Fatigue
Weakness
* Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult 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 dizziness or fainting
- Very slow heart rate (below 50 beats per minute)
- New or worsening shortness of breath or wheezing
- Swelling in your ankles or feet
- Unusual weight gain
- Chest pain or discomfort
- Symptoms of depression (e.g., persistent sadness, loss of interest)
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, 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
This list is not exhaustive, and it is crucial to discuss all your health problems with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription and over-the-counter (OTC) drugs
Natural products
* Vitamins
It is vital to verify that it is safe to take this medication with all your existing medications and health conditions. Never start, stop, or change the dose 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 allergic reaction you experienced, including any symptoms that occurred.
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
This list is not exhaustive, and it is crucial to discuss all your health problems with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription and over-the-counter (OTC) drugs
Natural products
* Vitamins
It is vital to verify that it is safe to take this medication with all your existing medications and health conditions. Never start, stop, or change the dose 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.
To ensure your safety, avoid driving and other activities that require alertness until you understand how this medication affects you. When changing positions, such as standing up from a sitting or lying down position, do so slowly to minimize the risk of dizziness or fainting. Be cautious when navigating stairs.
As directed by your doctor, regularly have your blood work and other laboratory tests checked. Additionally, monitor your blood pressure and heart rate as instructed by your healthcare provider.
Before consuming alcohol, discuss its potential effects with your doctor. This medication may mask certain symptoms of low blood sugar, such as 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, have a reduced appetite, or are experiencing vomiting. If you have concerns, consult your doctor.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. If you are taking this medication and have high blood pressure, consult your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.
This medication may also make it more challenging to recognize symptoms of an overactive thyroid, such as a rapid heartbeat. If you have an overactive thyroid and suddenly stop taking this medication, your condition may worsen and become life-threatening. Discuss this with your doctor.
If you have a history of severe allergic reactions, inform your doctor, as you may be at a higher risk of an even more severe reaction if you are exposed to the allergen again. If you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
Lastly, if you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
To ensure your safety, avoid driving and other activities that require alertness until you understand how this medication affects you. When changing positions, such as standing up from a sitting or lying down position, do so slowly to minimize the risk of dizziness or fainting. Be cautious when navigating stairs.
As directed by your doctor, regularly have your blood work and other laboratory tests checked. Additionally, monitor your blood pressure and heart rate as instructed by your healthcare provider.
Before consuming alcohol, discuss its potential effects with your doctor. This medication may mask certain symptoms of low blood sugar, such as 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, have a reduced appetite, or are experiencing vomiting. If you have concerns, consult your doctor.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. If you are taking this medication and have high blood pressure, consult your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.
This medication may also make it more challenging to recognize symptoms of an overactive thyroid, such as a rapid heartbeat. If you have an overactive thyroid and suddenly stop taking this medication, your condition may worsen and become life-threatening. Discuss this with your doctor.
If you have a history of severe allergic reactions, inform your doctor, as you may be at a higher risk of an even more severe reaction if you are exposed to the allergen again. If you use epinephrine to treat severe allergic reactions, consult your doctor, as this medication may reduce the effectiveness of epinephrine.
Lastly, if you are pregnant, plan to become pregnant, or are breastfeeding, discuss the 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
- Hypoglycemia (low blood sugar)
- Dizziness
- Fainting
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For advice, call a poison control center at 1-800-222-1222. Treatment may involve atropine for bradycardia, glucagon, vasopressors for hypotension, and bronchodilators for bronchospasm.
Drug Interactions
Contraindicated Interactions
- Non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem) in patients with impaired ventricular function or AV conduction abnormalities (risk of severe bradycardia, heart block, heart failure)
- MAO inhibitors (risk of hypertensive crisis after withdrawal of MAOI)
Major Interactions
- Other beta-blockers (additive effects, severe bradycardia, hypotension)
- Clonidine (risk of rebound hypertension upon clonidine withdrawal if beta-blocker is not tapered first)
- Digoxin (additive bradycardia)
- Insulin and oral hypoglycemics (masking of hypoglycemia symptoms, prolonged hypoglycemia)
- Amiodarone (increased risk of bradycardia, AV block, cardiac arrest)
- Propafenone, Quinidine, Fluoxetine, Paroxetine (CYP2D6 inhibitors, may increase timolol plasma concentrations)
Moderate Interactions
- NSAIDs (may reduce antihypertensive effect of timolol)
- Alpha-1 blockers (e.g., prazosin, doxazosin) (increased risk of first-dose hypotension)
- Sympathomimetics (e.g., epinephrine, norepinephrine) (reduced beta-agonist effect, potential for unopposed alpha-stimulation leading to hypertension and bradycardia)
- General anesthetics (additive myocardial depression, hypotension)
Minor Interactions
- Alcohol (may enhance hypotensive effect)
- Cimetidine (may increase timolol levels due to CYP inhibition, but generally not clinically significant)
Monitoring
Baseline Monitoring
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation
Heart Rate (HR)
Rationale: To establish baseline and assess for bradycardia risk.
Timing: Prior to initiation
Electrocardiogram (ECG)
Rationale: To assess for pre-existing conduction abnormalities (e.g., AV block).
Timing: Prior to initiation, especially in patients with cardiac history
Pulmonary Function Tests (PFTs)
Rationale: To assess for underlying bronchospastic disease (e.g., asthma, COPD) due to non-selective beta-blockade.
Timing: Prior to initiation in patients with respiratory symptoms or history
Blood Glucose
Rationale: To establish baseline in diabetic patients, as beta-blockers can mask hypoglycemia symptoms.
Timing: Prior to initiation in diabetic patients
Routine Monitoring
Blood Pressure (BP)
Frequency: Regularly (e.g., weekly during titration, then monthly or quarterly)
Target: <130/80 mmHg (individualized)
Action Threshold: Hypotension (<90/60 mmHg) or uncontrolled hypertension (>140/90 mmHg)
Heart Rate (HR)
Frequency: Regularly (e.g., weekly during titration, then monthly or quarterly)
Target: 50-70 bpm (resting)
Action Threshold: <50 bpm or symptomatic bradycardia
Blood Glucose
Frequency: More frequently in diabetic patients, especially during dose changes
Target: Individualized based on diabetes management
Action Threshold: Frequent or severe hypoglycemic episodes
Symptoms of Heart Failure
Frequency: At each visit
Target: N/A
Action Threshold: New or worsening dyspnea, edema, weight gain
Respiratory Symptoms
Frequency: At each visit
Target: N/A
Action Threshold: New or worsening wheezing, shortness of breath
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fatigue
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Shortness of breath
- Wheezing
- Cold extremities
- Depression
- Insomnia
- Masked symptoms of hypoglycemia (in diabetics)
Special Patient Groups
Pregnancy
Timolol is Pregnancy Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Beta-blockers can cause fetal bradycardia, hypoglycemia, and growth restriction. Neonates exposed to beta-blockers in utero may be at risk for hypoglycemia and bradycardia.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Potential for fetal bradycardia, growth restriction.
Third Trimester:
Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression at birth.
Lactation
Timolol is excreted into breast milk. The American Academy of Pediatrics considers timolol to be compatible with breastfeeding, but caution is advised. Monitor the infant for signs of beta-blockade (e.g., bradycardia, lethargy, hypoglycemia).
Infant Risk:
Low to Moderate (potential for bradycardia, hypoglycemia, lethargy in infant)
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is generally not recommended due to lack of data and potential for adverse effects.
Geriatric Use
Elderly patients may be more sensitive to the effects of beta-blockers, particularly bradycardia and hypotension. Start with lower doses and titrate slowly. Monitor renal and hepatic function closely.
Clinical Information
Clinical Pearls
- Timolol is a non-selective beta-blocker, meaning it blocks both beta-1 and beta-2 receptors. This makes it effective for hypertension and angina but requires caution in patients with bronchospastic diseases (e.g., asthma, COPD) due to the risk of bronchoconstriction.
- Abrupt discontinuation of timolol can lead to rebound hypertension, angina exacerbation, or myocardial infarction, especially in patients with ischemic heart disease. Always taper the dose gradually over 1-2 weeks.
- In diabetic patients, timolol can mask the symptoms of hypoglycemia (e.g., tremor, palpitations, tachycardia), making it harder to recognize low blood sugar. Patients should be educated to monitor blood glucose more closely.
- Timolol can cause central nervous system side effects like fatigue, dizziness, and depression. Patients should be advised about these potential effects.
- While primarily used for systemic conditions, be aware that ophthalmic timolol (for glaucoma) can also cause systemic absorption and effects, especially in susceptible individuals.
Alternative Therapies
- Other beta-blockers (e.g., atenolol, metoprolol, carvedilol, propranolol)
- ACE inhibitors (e.g., lisinopril, enalapril)
- Angiotensin Receptor Blockers (ARBs) (e.g., losartan, valsartan)
- Calcium Channel Blockers (e.g., amlodipine, nifedipine, diltiazem, verapamil)
- Diuretics (e.g., hydrochlorothiazide, furosemide)
- Alpha-blockers (e.g., prazosin, doxazosin)
- Central alpha-agonists (e.g., clonidine)
- For migraine prophylaxis: Topiramate, Valproic acid, CGRP inhibitors, Amitriptyline.
Cost & Coverage
Generic Available:
Yes
Insurance Coverage:
Tier 1 (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 overdose, including the medication taken, the amount, and the time it occurred.