Metoprolol Tartrate 100mg Tablets

Manufacturer SUN Active Ingredient Metoprolol Tablets(me toe PROE lole) Pronunciation me toe PROE lole TAR trate
It is used to treat high blood pressure.It is used to treat some types of chest pain (angina).It is used after a heart attack to help prevent future heart attacks and lengthen life. It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihypertensive, Antianginal, Antiarrhythmic
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Pharmacologic Class
Beta-1 Selective Adrenergic Blocker
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Pregnancy Category
C
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FDA Approved
Jun 1978
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Metoprolol 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 your blood pressure and reduce the strain on your heart. It's used to treat high blood pressure, chest pain (angina), and to help prevent future heart problems after a heart attack.
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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. It's recommended to take this medication with or immediately after a meal. 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 in a dry location. Avoid storing it in a bathroom, as the moisture can affect the medication. Additionally, protect your medication from heat sources.

What to Do If You Miss a Dose

If you miss a dose, skip it 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.
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Lifestyle & Tips

  • Take metoprolol exactly as prescribed, usually with or immediately after a meal to increase absorption and reduce stomach upset.
  • Do not stop taking this medication suddenly, especially if you have heart disease, as it can worsen your condition. Your doctor will tell you how to gradually reduce the dose.
  • Monitor your blood pressure and heart rate regularly at home if advised by your doctor.
  • Maintain a healthy lifestyle, including a balanced diet (low in sodium and saturated fats), regular exercise (as advised by your doctor), and limiting alcohol intake.
  • Avoid activities that require alertness until you know how the medication affects you, as it can cause dizziness or fatigue.
  • Inform your doctor or dentist that you are taking metoprolol before any surgery or dental procedures.

Dosing & Administration

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Adult Dosing

Standard Dose: Hypertension: 100 mg daily in single or divided doses. Angina Pectoris: 100 mg daily in single or divided doses. Myocardial Infarction (early treatment): 50 mg every 6 hours for 48 hours, then 100 mg twice daily. Myocardial Infarction (late treatment): 100 mg twice daily.
Dose Range: 50 - 450 mg

Condition-Specific Dosing:

hypertension: Initial 50-100 mg daily, maintenance 100-450 mg daily.
anginaPectoris: Initial 100 mg daily, maintenance 100-400 mg daily.
myocardialInfarction: Acute: 50 mg q6h for 48h, then 100 mg BID. Long-term: 100 mg BID.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Hypertension (off-label): Initial 0.5-1 mg/kg/day divided BID, max 2 mg/kg/day or 200 mg/day.
Adolescent: Hypertension (off-label): Initial 0.5-1 mg/kg/day divided BID, max 2 mg/kg/day or 200 mg/day.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: No adjustment needed
Dialysis: Not significantly removed by hemodialysis; no supplemental dose needed.

Hepatic Impairment:

Mild: Consider lower initial dose and careful titration.
Moderate: Reduce dose significantly (e.g., by 50%) and monitor closely.
Severe: Reduce dose significantly (e.g., by 75%) and monitor closely due to extensive hepatic metabolism.

Pharmacology

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Mechanism of Action

Metoprolol is a cardioselective beta-1 adrenergic receptor blocker. It competitively blocks beta-1 adrenergic receptors, primarily located in the heart, reducing heart rate, myocardial contractility, and cardiac output. This leads to a decrease in blood pressure. It also reduces renin release from the kidneys. At higher doses, it can also block beta-2 adrenergic receptors.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 50% (highly variable, 30-70%) due to significant first-pass metabolism.
Tmax: 1.5-2 hours
FoodEffect: Food increases bioavailability by 20-40%.

Distribution:

Vd: 3.2-5.6 L/kg
ProteinBinding: Approximately 10-12%
CnssPenetration: Limited (lipophilic enough to cross BBB, but less than propranolol)

Elimination:

HalfLife: 3-7 hours (average 3-4 hours)
Clearance: Approximately 1 L/min
ExcretionRoute: Renal (primarily metabolites)
Unchanged: Approximately 3-10% (up to 30-40% in poor metabolizers)
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Pharmacodynamics

OnsetOfAction: Within 1 hour
PeakEffect: 2-4 hours
DurationOfAction: 10-20 hours (dose-dependent, allows once or twice daily dosing)

Safety & Warnings

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BLACK BOX WARNING

Ischemic Heart Disease: Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered metoprolol, 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 markedly worsens or acute coronary insufficiency develops, metoprolol 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 metoprolol therapy abruptly even in patients treated only for hypertension.
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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Signs of low blood sugar, including:
+ Dizziness
+ Headache
+ Feeling sleepy
+ Feeling weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Depression
Severe dizziness or fainting
New or worsening chest pain
New or worsening abnormal heartbeat
Slow heartbeat
Shortness of breath, significant weight gain, or swelling in the arms or legs

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:

Feeling dizzy, tired, or weak
Diarrhea
Upset stomach
Vomiting

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.
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Seek Immediate Medical Attention If You Experience:

  • Severe dizziness or fainting
  • Very slow heart rate (e.g., less than 50 beats per minute)
  • Difficulty breathing or wheezing
  • Swelling in your ankles or feet
  • Unusual weight gain
  • New or worsening chest pain
  • Symptoms of depression (mood changes, loss of interest)
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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. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain heart conditions, including:
+ Abnormal heart rhythms (heart block or sick-sinus syndrome)
+ Heart failure (a weakened heart)
+ Low blood pressure
+ Poor blood circulation to your arms or legs
+ Shock caused by heart problems
+ A slow heartbeat
Respiratory issues, such as:
+ Asthma
+ Chronic obstructive pulmonary disease (COPD) or other breathing problems

This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.

To ensure your safety, inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
All your health problems

Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
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Precautions & Cautions

Important Warnings and Cautions

It is crucial that you inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Caution with Daily Activities
Until you understand how this medication affects you, avoid driving and engaging in other activities that require alertness. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution when climbing stairs.

Monitoring Your Condition
Follow your doctor's instructions for checking your blood pressure and heart rate. Additionally, have your blood work and other laboratory tests performed as directed by your doctor.

Interference with Lab Tests
This medication may affect the results of certain laboratory tests. Be sure to inform all of your healthcare providers and laboratory personnel that you are taking this medication.

Risk of Low Blood Sugar
This medication may mask symptoms of low blood sugar, such as rapid heartbeat, which can increase the risk of severe or prolonged low blood sugar. 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 questions or concerns, consult your doctor.

Management of High Blood Sugar
If you have diabetes, it is essential to closely monitor your blood sugar levels while taking this medication.

Interactions with Other Medications
If you have high blood pressure and are taking this medication, consult your doctor before using over-the-counter products that may increase blood pressure, such as cough and cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.

Discontinuing the Medication
Do not stop taking this medication abruptly, as this may lead to worsened chest pain or even heart attack, particularly in individuals with certain types of heart disease. To minimize the risk of side effects, your doctor will instruct you on how to gradually discontinue the medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.

Thyroid Conditions
This medication may make it more challenging to recognize symptoms of an overactive thyroid, such as rapid heartbeat. If you have an overactive thyroid and stop taking this medication suddenly, your condition may worsen and become life-threatening. Consult your doctor for guidance.

Allergic Reactions
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, consult your doctor, as this medication may reduce the effectiveness of epinephrine.

Alcohol Consumption
Before consuming alcohol, discuss the potential risks with your doctor.

Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the benefits and risks of this medication to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe bradycardia (very slow heart rate)
  • Severe hypotension (very low blood pressure)
  • Cardiogenic shock
  • Bronchospasm (difficulty breathing)
  • Heart failure
  • Hypoglycemia
  • Seizures
  • Cardiac arrest

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment may involve atropine for bradycardia, glucagon, vasopressors, and intravenous fluids.

Drug Interactions

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Contraindicated Interactions

  • Severe bradycardia (<45 bpm)
  • Second- or third-degree AV block
  • Sick sinus syndrome (unless permanent pacemaker in place)
  • Cardiogenic shock
  • Decompensated heart failure
  • Peripheral arterial occlusive disease (severe, untreated)
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Major Interactions

  • Non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem): Increased risk of bradycardia, AV block, and hypotension.
  • Clonidine: Potentiation of rebound hypertension upon clonidine withdrawal.
  • Digoxin: Increased risk of bradycardia.
  • Fingolimod: Additive bradycardic effects.
  • MAO inhibitors: Increased risk of hypotension and bradycardia.
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Moderate Interactions

  • CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, propafenone, bupropion, ritonavir): May increase metoprolol plasma concentrations, leading to enhanced beta-blocking effects.
  • NSAIDs (e.g., ibuprofen, naproxen): May reduce the antihypertensive effect of metoprolol.
  • Insulin and oral hypoglycemics: May mask symptoms of hypoglycemia (e.g., tachycardia) and prolong hypoglycemic episodes.
  • Sympathomimetics (e.g., epinephrine, norepinephrine): May cause paradoxical hypertension and bradycardia.
  • Other antihypertensives: Additive hypotensive effects.
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Minor Interactions

  • Alcohol: May increase metoprolol levels.
  • Rifampin: May decrease metoprolol levels.

Monitoring

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Baseline Monitoring

Blood Pressure (BP)

Rationale: To establish baseline and assess efficacy.

Timing: Before initiation

Heart Rate (HR)

Rationale: To establish baseline and assess risk of bradycardia.

Timing: Before initiation

Electrocardiogram (ECG)

Rationale: To assess for pre-existing conduction abnormalities (e.g., AV block).

Timing: Before initiation, especially in patients with cardiac history

Renal Function (SCr, BUN)

Rationale: To assess kidney health, though metoprolol is primarily hepatically metabolized, renal function is important for overall patient assessment.

Timing: Before initiation

Liver Function Tests (ALT, AST, bilirubin)

Rationale: To assess hepatic function, as metoprolol is extensively metabolized by the liver.

Timing: Before initiation, especially in patients with suspected hepatic impairment

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly, e.g., weekly initially, then monthly or quarterly once stable.

Target: <130/80 mmHg (individualized based on guidelines and comorbidities)

Action Threshold: If persistently high, consider dose adjustment; if too low (<90/60 mmHg or symptomatic), consider dose reduction.

Heart Rate (HR)

Frequency: Regularly, e.g., weekly initially, then monthly or quarterly once stable.

Target: 50-60 bpm (resting, unless otherwise specified for condition)

Action Threshold: If <50 bpm or symptomatic bradycardia, consider dose reduction or discontinuation.

Symptoms of Heart Failure

Frequency: At each visit

Target: Absence of worsening symptoms (e.g., dyspnea, edema, weight gain)

Action Threshold: Worsening symptoms require immediate medical evaluation and potential dose adjustment or discontinuation.

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Fatigue
  • Bradycardia (slow heart rate)
  • Hypotension (low blood pressure)
  • Shortness of breath
  • Wheezing (especially in patients with asthma/COPD)
  • Cold extremities
  • Masked symptoms of hypoglycemia (in diabetics)

Special Patient Groups

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Pregnancy

Metoprolol is Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Beta-blockers can cause fetal growth restriction, bradycardia, and hypoglycemia. 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 growth restriction, bradycardia.
Third Trimester: Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate for 48-72 hours after birth.
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Lactation

Metoprolol is excreted into breast milk in small amounts. The American Academy of Pediatrics considers metoprolol to be compatible with breastfeeding. Monitor breastfed infants for signs of beta-blockade (e.g., bradycardia, drowsiness, hypoglycemia).

Infant Risk: Low risk. L3 (Moderately Safe).
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Pediatric Use

Safety and efficacy not established for routine pediatric use, especially in infants and neonates. Used off-label for hypertension in children, with careful dose titration based on weight and response. Close monitoring for adverse effects is crucial.

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Geriatric Use

Elderly patients may be more sensitive to the effects of beta-blockers and may require lower initial doses and slower titration. Increased risk of bradycardia, hypotension, and central nervous system effects (e.g., dizziness, fatigue). Monitor renal and hepatic function.

Clinical Information

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Clinical Pearls

  • Metoprolol tartrate is an immediate-release formulation, typically dosed twice daily. Metoprolol succinate is an extended-release formulation, dosed once daily.
  • Always taper metoprolol dose gradually over 1-2 weeks to avoid rebound hypertension, angina exacerbation, or myocardial infarction, especially in patients with ischemic heart disease.
  • Use with caution in patients with asthma or COPD, as beta-1 selectivity is dose-dependent and higher doses can cause bronchospasm.
  • Can mask symptoms of hypoglycemia in diabetic patients (e.g., tachycardia, tremors), but sweating may still occur.
  • May worsen symptoms of peripheral artery disease (e.g., claudication) in some patients.
  • Take with food to enhance absorption and reduce GI upset.
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Alternative Therapies

  • Other beta-blockers (e.g., atenolol, carvedilol, bisoprolol, propranolol)
  • ACE inhibitors (e.g., lisinopril, enalapril)
  • Angiotensin Receptor Blockers (ARBs) (e.g., losartan, valsartan)
  • Calcium Channel Blockers (e.g., amlodipine, nifedipine, verapamil, diltiazem)
  • Thiazide diuretics (e.g., hydrochlorothiazide)
  • Alpha-blockers (e.g., prazosin, doxazosin)
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (generic 100mg)
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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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. 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 medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.