Brevibloc 10mg/ml Inj, 250ml

Manufacturer BAXTER HEALTHCARE CORPORATION Active Ingredient Esmolol(ES moe lol) Pronunciation ES-moe-lol
It is used to treat a fast heartbeat. 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
Antiarrhythmic; Antihypertensive
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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
Dec 1987
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Esmolol is a fast-acting medicine given through a vein (intravenously) to quickly slow down your heart rate or lower your blood pressure. It's often used in emergencies or during surgery because its effects wear off very quickly once the infusion is stopped.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and be sure to follow all instructions provided. This drug is administered as an intravenous infusion, which means it is given through a vein over a specified period of time.

If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.

If you miss a dose, contact your doctor immediately to receive guidance on what to do next.
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Lifestyle & Tips

  • This medication is given in a hospital setting under close medical supervision.
  • Report any discomfort at the injection site immediately.
  • Inform your healthcare provider if you feel dizzy, lightheaded, or have difficulty breathing.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial loading dose of 500 mcg/kg over 1 minute, followed by a maintenance infusion of 50 mcg/kg/min for 4 minutes. If inadequate response, repeat loading dose and increase maintenance infusion to 100 mcg/kg/min. Titrate by 50 mcg/kg/min increments every 5-10 minutes to a maximum of 200 mcg/kg/min (occasionally up to 300 mcg/kg/min for acute situations).
Dose Range: 50 - 300 mg

Condition-Specific Dosing:

supraventricularTachycardia: Loading: 500 mcg/kg over 1 min. Maintenance: 50-200 mcg/kg/min (max 300 mcg/kg/min).
perioperativeHypertensionTachycardia: Loading: 500 mcg/kg over 1 min. Maintenance: 50-200 mcg/kg/min.
myocardialIschemia: Loading: 500 mcg/kg over 1 min. Maintenance: 50-200 mcg/kg/min.
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Pediatric Dosing

Neonatal: Not established
Infant: Loading: 500 mcg/kg over 1 minute. Maintenance: 50-200 mcg/kg/min. Titrate to effect.
Child: Loading: 500 mcg/kg over 1 minute. Maintenance: 50-200 mcg/kg/min. Titrate to effect.
Adolescent: Loading: 500 mcg/kg over 1 minute. Maintenance: 50-200 mcg/kg/min. Titrate to effect.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed for parent drug. Monitor for accumulation of acid metabolite.
Moderate: No adjustment needed for parent drug. Monitor for accumulation of acid metabolite.
Severe: No adjustment needed for parent drug. Monitor for accumulation of acid metabolite. Use with caution.
Dialysis: Esmolol is not significantly dialyzable. Monitor for accumulation of acid metabolite.

Hepatic Impairment:

Mild: No adjustment
Moderate: No adjustment
Severe: No adjustment

Pharmacology

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Mechanism of Action

Esmolol is a beta-1 selective (cardioselective) adrenergic receptor blocking agent. It competitively blocks beta-1 adrenergic receptors, primarily in the heart, leading to decreased heart rate, myocardial contractility, and cardiac output. At higher doses, it can also block beta-2 receptors. Its ultra-short duration of action is due to rapid hydrolysis by esterases in red blood cells.
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Pharmacokinetics

Absorption:

Bioavailability: 100%
Tmax: Not applicable (IV administration)
FoodEffect: Not applicable

Distribution:

Vd: 3.4 L/kg
ProteinBinding: 55%
CnssPenetration: Limited

Elimination:

HalfLife: 9 minutes (elimination), 2 minutes (distribution)
Clearance: 117 mL/kg/min
ExcretionRoute: Renal (metabolites)
Unchanged: <2%
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Pharmacodynamics

OnsetOfAction: 2-10 minutes
PeakEffect: 5-10 minutes
DurationOfAction: 10-30 minutes after discontinuation of infusion

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Help Right Away

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 immediately:

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 high potassium levels, including:
+ Abnormal heartbeat
+ Confusion
+ Weakness, lightheadedness, or dizziness
+ Feeling like passing out
+ Numbness or tingling
+ Shortness of breath
Signs of too much acid in the blood (acidosis), such as:
+ Confusion
+ Rapid breathing
+ Rapid heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Dizziness or fainting
Excessive sweating
Shortness of breath, significant weight gain, or swelling in the arms or legs
Slow heartbeat
Abnormal heartbeat

If the medication leaks from the vein, it may cause tissue damage. Inform your nurse immediately if you experience any of the following symptoms at the injection site:
Redness
Burning
Pain
Swelling
Blisters
Skin sores
Fluid leakage

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 persist, contact your doctor or seek medical attention:
Upset stomach

This is not an exhaustive list of possible 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe dizziness or fainting
  • Very slow heart rate
  • Difficulty breathing or wheezing
  • Chest pain
  • Swelling in your ankles or feet
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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 and its symptoms.
Certain health conditions, including:
+ Respiratory problems like asthma or chronic obstructive pulmonary disease (COPD)
+ Heart conditions, such as heart block, heart failure (weak heart), or shock caused by heart problems
+ Abnormally slow heartbeat
Specific heart-related conditions, including:
+ Sick sinus syndrome, a type of abnormal heartbeat
+ Prinzmetal's angina, a particular type of chest pain
High blood pressure in the lungs (pulmonary hypertension)
If you are taking certain medications, such as diltiazem or verapamil

To ensure your safety, it is crucial to disclose all of your:

Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems

Your doctor and pharmacist need this information to determine if it is safe for you to take this medication with your existing health conditions and medications. 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. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.

To minimize the risk of dizziness or fainting, stand up slowly after sitting or lying down, and exercise caution when climbing stairs. Regular blood tests, as directed by your doctor, are crucial to monitor your condition. Additionally, check your blood pressure and heart rate as instructed by 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 higher in individuals with diabetes, children, and those who are fasting, undergoing surgery, or experiencing nausea and vomiting. If you have concerns, consult your doctor. If you have diabetes, it is vital to closely monitor your blood sugar levels.

This drug may also make it more challenging to recognize signs of an overactive thyroid, such as a rapid heartbeat. If you have hyperthyroidism 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, consult 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, inform your doctor, as this medication may reduce the effectiveness of epinephrine.

Do not abruptly stop taking this medication, as this can lead to increased chest pain and, in some cases, heart attack, particularly if you have certain types of heart disease. To avoid adverse effects, your doctor will guide you on how to gradually discontinue the medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.

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)
  • Cardiogenic shock
  • Asystole (cardiac arrest)
  • Bronchospasm
  • Hypoglycemia

What to Do:

Immediately discontinue esmolol infusion. Treatment is supportive and symptomatic. May include IV fluids, vasopressors (e.g., norepinephrine, dopamine), atropine for bradycardia, glucagon for severe bradycardia/hypotension, and bronchodilators for bronchospasm. Call 1-800-222-1222 (Poison Control) for further guidance.

Drug Interactions

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Major Interactions

  • Non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem): Risk of severe bradycardia, heart block, and hypotension.
  • Digoxin: Increased risk of bradycardia and AV block.
  • Insulin and oral hypoglycemics: May mask symptoms of hypoglycemia (e.g., tachycardia).
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Moderate Interactions

  • Other antihypertensives (e.g., ACE inhibitors, diuretics): Additive hypotensive effects.
  • Clonidine: Risk of rebound hypertension upon clonidine withdrawal if beta-blocker is not tapered.
  • NSAIDs: May reduce the hypotensive effects of beta-blockers.
  • Sympathomimetics (e.g., epinephrine, norepinephrine): May cause unopposed alpha-adrenergic stimulation leading to severe hypertension and bradycardia.

Monitoring

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Baseline Monitoring

Heart Rate (HR)

Rationale: To establish baseline and guide titration, as esmolol reduces HR.

Timing: Prior to initiation

Blood Pressure (BP)

Rationale: To establish baseline and guide titration, as esmolol reduces BP.

Timing: Prior to initiation

Electrocardiogram (ECG)

Rationale: To assess baseline cardiac rhythm and conduction.

Timing: Prior to initiation

Fluid Status

Rationale: To assess for signs of heart failure or hypovolemia.

Timing: Prior to initiation

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Routine Monitoring

Heart Rate (HR)

Frequency: Continuously (cardiac monitor)

Target: Individualized, typically 60-100 bpm or target for condition

Action Threshold: <50 bpm or symptomatic bradycardia (e.g., dizziness, syncope)

Blood Pressure (BP)

Frequency: Continuously (arterial line) or frequently (non-invasive cuff) every 5-15 minutes during titration, then every 15-30 minutes

Target: Individualized, typically SBP >90 mmHg or target for condition

Action Threshold: Significant hypotension (e.g., SBP <90 mmHg or symptomatic hypotension)

Electrocardiogram (ECG)

Frequency: Continuously (cardiac monitor)

Target: Normal sinus rhythm or controlled arrhythmia

Action Threshold: New onset arrhythmia, heart block, or significant QT prolongation

Infusion Site

Frequency: Every 1-2 hours

Target: No redness, swelling, or pain

Action Threshold: Signs of extravasation or phlebitis

Respiratory Status

Frequency: Continuously (pulse oximetry) and clinically

Target: SpO2 >92%

Action Threshold: Wheezing, dyspnea, or SpO2 <90%

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Symptom Monitoring

  • Bradycardia (slow heart rate)
  • Hypotension (low blood pressure)
  • Dizziness or lightheadedness
  • Fatigue or weakness
  • Dyspnea (shortness of breath)
  • Wheezing or bronchospasm
  • Signs of heart failure exacerbation (e.g., peripheral edema, crackles, jugular venous distension)
  • Cold extremities
  • Confusion or altered mental status

Special Patient Groups

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Pregnancy

Category C. Use only if the potential benefit justifies the potential risk to the fetus. Beta-blockers may cause bradycardia, hypoglycemia, and respiratory depression in the neonate. Prolonged exposure may lead to intrauterine growth restriction.

Trimester-Specific Risks:

First Trimester: Limited data, theoretical risk of developmental abnormalities.
Second Trimester: Potential for fetal bradycardia and growth restriction.
Third Trimester: Risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate for 24-48 hours after birth.
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Lactation

L3 (Moderately safe). Esmolol is rapidly metabolized and has a very short half-life, making infant exposure low. However, caution is advised, and monitoring the infant for signs of beta-blockade (e.g., bradycardia, lethargy) is recommended.

Infant Risk: Low risk of adverse effects due to rapid maternal metabolism and short half-life. Monitor for bradycardia, hypotension, and hypoglycemia.
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Pediatric Use

Esmolol has been used in pediatric patients for supraventricular tachycardia and hypertension. Dosing is weight-based and requires careful titration and monitoring due to potential for profound bradycardia and hypotension. Safety and efficacy in neonates are not fully established.

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Geriatric Use

Use with caution in elderly patients, as they may be more sensitive to the hypotensive and bradycardic effects of beta-blockers. Start with lower doses and titrate slowly. Monitor closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Esmolol is an ultra-short-acting beta-blocker, making it highly titratable and suitable for acute, critical care settings where rapid control and reversibility are desired.
  • Due to its rapid metabolism by esterases, its effects quickly dissipate upon discontinuation of the infusion, allowing for precise control of heart rate and blood pressure.
  • It is cardioselective (beta-1 selective) at lower doses, but this selectivity diminishes at higher doses, increasing the risk of beta-2 mediated side effects like bronchospasm.
  • Always administer via continuous intravenous infusion after an initial loading dose. Avoid abrupt discontinuation to prevent rebound effects, especially in patients with underlying coronary artery disease.
  • Monitor infusion site closely for signs of irritation or extravasation, as esmolol can be irritating to veins.
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Alternative Therapies

  • Metoprolol (IV)
  • Labetalol (IV)
  • Diltiazem (IV)
  • Verapamil (IV)
  • Adenosine (for SVT)
  • Nicardipine (IV)
  • Fenoldopam (IV)
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Cost & Coverage

Average Cost: Variable, check current pricing per 250ml vial
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (generic), Tier 3 (brand) - typically covered in hospital settings
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed otherwise, avoid flushing medications down the toilet or pouring them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for guidance. Many communities offer drug take-back programs, which your pharmacist can help you locate. Some medications may come with an additional patient information leaflet; check with your pharmacist for more information. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide details about the medication taken, the amount, and the time it occurred.