Bisoprolol Fumarate 2.5mg Tablets

Manufacturer TRUPHARMA Active Ingredient Bisoprolol(bis OH proe lol) Pronunciation bis-OH-proe-lol
It is used to treat high blood pressure.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihypertensive, Antianginal
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Pharmacologic Class
Beta-1 selective adrenergic blocker
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Pregnancy Category
Category C
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FDA Approved
Jul 1992
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Bisoprolol is a medication that belongs to a class of drugs called beta-blockers. It works by slowing down your heart rate and relaxing your blood vessels, which helps to lower your blood pressure and improve blood flow. It's used to treat high blood pressure, chest pain (angina), and certain heart conditions like chronic heart failure.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food, and continue taking it even if you start feeling well. It's essential to follow your doctor's or healthcare provider's advice on dosage and duration of treatment.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding bathrooms and areas where children and pets can access it. Keep all medications in a safe location and out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult your pharmacist for guidance on proper disposal methods, which may include drug take-back programs in your area.

Missing a Dose

If you miss a dose, take it as soon as you remember. However, if it's 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 a missed one.
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Lifestyle & Tips

  • Take medication exactly as prescribed, do not stop abruptly.
  • Monitor your blood pressure and heart rate regularly at home if advised by your doctor.
  • Maintain a healthy diet, low in sodium and saturated fats.
  • Engage in regular physical activity as recommended by your doctor.
  • Avoid smoking and limit alcohol consumption.
  • Report any new or worsening symptoms to your healthcare provider.

Dosing & Administration

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Adult Dosing

Standard Dose: Hypertension/Angina: Initial 2.5-5 mg once daily; maintenance 2.5-20 mg once daily. Chronic Stable Heart Failure: Initial 1.25 mg once daily, titrated slowly over weeks to target 10 mg once daily.
Dose Range: 1.25 - 20 mg

Condition-Specific Dosing:

hypertension: Initial 2.5-5 mg once daily, maintenance 2.5-20 mg once daily.
angina: Initial 2.5-5 mg once daily, maintenance 2.5-20 mg once daily.
chronic_stable_heart_failure: Initial 1.25 mg once daily, doubled every 2 weeks as tolerated to a maximum of 10 mg once daily.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established (limited data, generally not recommended for routine use in hypertension/angina)
Adolescent: Not established (limited data, generally not recommended for routine use in hypertension/angina)
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed (CrCl > 50 mL/min)
Moderate: No adjustment needed (CrCl 20-50 mL/min)
Severe: Maximum 10 mg once daily (CrCl < 20 mL/min)
Dialysis: No additional dose needed after dialysis

Hepatic Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: Maximum 10 mg once daily

Pharmacology

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Mechanism of Action

Bisoprolol is a highly selective beta-1 adrenergic receptor blocking agent. It decreases heart rate, myocardial contractility, and cardiac output, leading to a reduction in blood pressure. It also reduces renin release from the kidneys.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 80%
Tmax: 2-4 hours
FoodEffect: Not significantly affected by food

Distribution:

Vd: Approximately 226 L
ProteinBinding: Approximately 30%
CnssPenetration: Limited

Elimination:

HalfLife: 9-12 hours
Clearance: Approximately 15 L/hour
ExcretionRoute: Renal (approximately 50% unchanged) and hepatic (approximately 50% metabolized)
Unchanged: Approximately 50%
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Pharmacodynamics

OnsetOfAction: Within 2 hours
PeakEffect: 2-4 hours
DurationOfAction: At least 24 hours

Safety & Warnings

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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 significant weight gain
Swelling in the arms or legs
Slow heartbeat
Feeling cold in the arms or legs

Other Possible Side Effects

Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor:

Headache
Feeling tired or weak
Symptoms 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 for medical advice. 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 heartbeat (e.g., less than 50 beats per minute)
  • Difficulty breathing or wheezing
  • Swelling in your ankles, feet, or legs
  • Unusual weight gain
  • Chest pain or discomfort that worsens after stopping the medication
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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 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 for clarification.

Please note that this is not an exhaustive list of all potential interactions between this medication and other drugs or health conditions. Therefore, it is crucial to discuss the following with your doctor and pharmacist:

All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems you have

To ensure your safety, do not start, stop, or change the dosage of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication in combination with all your other medications and health conditions.
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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.

Do not abruptly stop taking this medication, as this can lead to worsened chest pain and, in some cases, heart attack. This risk is particularly higher if you have certain types of heart disease. To minimize side effects, your doctor will instruct you on how to gradually stop taking this medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.

Until you understand how this medication affects you, avoid driving and other activities that require alertness. To reduce the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution when navigating stairs.

Regularly monitor your blood pressure and heart rate as directed by your doctor. Be aware that this medication may affect certain laboratory tests, so inform all your healthcare providers and laboratory personnel that you are taking this medication.

This medication may mask symptoms of low blood sugar, such as rapid heartbeat, which can increase the risk of severe or prolonged hypoglycemia, especially in individuals with diabetes, children, and those who are fasting or undergoing surgery. If you have questions or concerns, discuss them with your doctor.

If you have diabetes, it is crucial to closely monitor your blood sugar levels. Before using over-the-counter 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, or certain natural products, consult with your doctor.

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 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 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 with your doctor, as this medication may reduce the effectiveness of epinephrine.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.

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.
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Overdose Information

Overdose Symptoms:

  • Severe bradycardia (very slow heart rate)
  • Profound hypotension (very low blood pressure)
  • Bronchospasm (difficulty breathing, wheezing)
  • Acute heart failure
  • Hypoglycemia (low blood sugar)
  • Cardiogenic shock

What to Do:

Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive and may include atropine for bradycardia, glucagon, vasopressors, and bronchodilators.

Drug Interactions

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Contraindicated Interactions

  • Acute decompensated heart failure
  • Severe bradycardia (< 45-50 bpm)
  • Second- or third-degree AV block (without a pacemaker)
  • Cardiogenic shock
  • Sick sinus syndrome (without a pacemaker)
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Major Interactions

  • Non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem) - risk of severe bradycardia, AV block, heart failure
  • Clonidine (risk of rebound hypertension upon clonidine withdrawal)
  • Other beta-blockers (additive effects)
  • Fingolimod (risk of severe bradycardia)
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Moderate Interactions

  • NSAIDs (may reduce antihypertensive effect)
  • Alpha-1 blockers (e.g., prazosin, doxazosin) - additive hypotensive effects
  • Insulin and oral hypoglycemics (may mask symptoms of hypoglycemia)
  • Rifampin (may decrease bisoprolol levels)
  • CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine) - minor increase in bisoprolol levels
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Minor Interactions

  • Alcohol (additive hypotensive effect)
  • Antacids (minor effect on absorption)

Monitoring

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Baseline Monitoring

Blood Pressure (BP)

Rationale: To establish baseline and guide dosing

Timing: Prior to initiation

Heart Rate (HR)

Rationale: To establish baseline and assess for bradycardia

Timing: Prior to initiation

Electrocardiogram (ECG)

Rationale: To assess for pre-existing conduction abnormalities

Timing: Prior to initiation (especially in patients with cardiac history)

Renal Function (Cr, GFR)

Rationale: To assess kidney function and guide dose adjustments in severe impairment

Timing: Prior to initiation

Hepatic Function (LFTs)

Rationale: To assess liver function and guide dose adjustments in severe impairment

Timing: Prior to initiation

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly (e.g., weekly during titration, then monthly or as clinically indicated)

Target: <130/80 mmHg (or individualized target)

Action Threshold: Systolic >140 mmHg or Diastolic >90 mmHg (consider dose increase); Systolic <90 mmHg or symptomatic hypotension (consider dose decrease)

Heart Rate (HR)

Frequency: Regularly (e.g., weekly during titration, then monthly or as clinically indicated)

Target: 50-70 bpm (or individualized target)

Action Threshold: <50 bpm or symptomatic bradycardia (consider dose decrease/discontinuation)

Symptoms of Heart Failure

Frequency: Regularly

Target: Absence of worsening symptoms

Action Threshold: Worsening dyspnea, edema, weight gain (evaluate for heart failure exacerbation)

Symptoms of Bronchospasm

Frequency: Regularly (especially in patients with reactive airway disease)

Target: Absence of wheezing, shortness of breath

Action Threshold: New or worsening respiratory symptoms (consider discontinuation)

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Symptom Monitoring

  • Dizziness
  • Lightheadedness
  • Fatigue
  • Shortness of breath
  • Wheezing
  • Swelling in ankles/feet
  • Unusual weight gain
  • Slow or irregular heartbeat
  • Cold hands/feet

Special Patient Groups

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Pregnancy

Bisoprolol 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/neonatal bradycardia, hypoglycemia, and growth restriction. Monitor neonates for signs of beta-blockade for several days after birth.

Trimester-Specific Risks:

First Trimester: Limited data, but generally avoided unless clearly needed.
Second Trimester: Potential for fetal growth restriction, bradycardia, and hypoglycemia.
Third Trimester: Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate closely.
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Lactation

Bisoprolol is excreted in breast milk in small amounts. The risk to the infant is generally considered low, but monitor the infant for signs of beta-blockade (e.g., bradycardia, lethargy, hypoglycemia). Use with caution, especially in preterm or unstable infants.

Infant Risk: Low (L3 - Moderately safe)
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Pediatric Use

Safety and efficacy have not been established in pediatric patients for hypertension or angina. Use in pediatric heart failure is off-label and requires specialized care and monitoring.

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Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Start with lower doses (e.g., 2.5 mg) and titrate slowly due to potential for increased sensitivity to effects and adverse reactions.

Clinical Information

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Clinical Pearls

  • Do not abruptly discontinue bisoprolol, especially in patients with ischemic heart disease, as it can exacerbate angina, lead to myocardial infarction, or cause arrhythmias. Taper the dose gradually over 1-2 weeks.
  • Use with caution in patients with reactive airway disease (e.g., asthma, COPD), as even beta-1 selective agents can cause bronchospasm at higher doses or in susceptible individuals.
  • Bisoprolol can mask the signs and symptoms of hypoglycemia (e.g., tachycardia) in diabetic patients.
  • May worsen symptoms of peripheral artery disease due to reduced peripheral blood flow.
  • Effective for both hypertension and chronic stable heart failure, but dosing strategies differ significantly for these indications.
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Alternative Therapies

  • Other beta-blockers (e.g., metoprolol, carvedilol, atenolol)
  • ACE inhibitors (e.g., lisinopril, enalapril)
  • Angiotensin Receptor Blockers (ARBs) (e.g., valsartan, losartan)
  • Calcium Channel Blockers (e.g., amlodipine, nifedipine)
  • Thiazide diuretics (e.g., hydrochlorothiazide)
  • Loop diuretics (e.g., furosemide) for heart failure
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Cost & Coverage

Average Cost: $10 - $30 per 30 tablets (2.5mg generic)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (preferred generic)
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General Drug Facts

If your symptoms or health condition do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist for more information. If you have any questions or concerns about your medication, do not 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 detailed information about the overdose, including the name of the medication taken, the amount, and the time it occurred.