Brevibloc 2000mg/100ml Inj, 100ml
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.
Drug Class
Antiarrhythmic, Antihypertensive
Pharmacologic Class
Beta-1 Selective Adrenergic Blocker
Pregnancy Category
C
FDA Approved
Dec 1987
DEA Schedule
Not Controlled
Overview
What is this medicine?
Esmolol is a fast-acting medicine given through a vein (IV) 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.
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 adhere to all guidelines provided. This drug is administered via infusion into a vein over a specified period of time.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- This medication is given in a hospital or clinical setting, so lifestyle modifications are generally not applicable during its acute use.
- Patients should report any unusual symptoms immediately to their healthcare provider.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Loading dose: 500 mcg/kg over 1 minute, followed by maintenance infusion: 50 mcg/kg/min for 4 minutes. Titrate as needed.
Dose Range:
25 - 300 mg
Condition-Specific Dosing:
supraventricularTachycardia:
Loading dose: 500 mcg/kg over 1 minute, then 50 mcg/kg/min for 4 minutes. If inadequate response, repeat loading dose and increase maintenance to 100 mcg/kg/min. Max 200 mcg/kg/min.
perioperativeHypertensionTachycardia:
Initial: 500 mcg/kg over 1 minute, then 50 mcg/kg/min. Titrate up to 300 mcg/kg/min. Or, 250-500 mcg/kg bolus over 1 minute, then 50-100 mcg/kg/min infusion.
myocardialIschemia:
Loading dose: 500 mcg/kg over 1 minute, then 50 mcg/kg/min. Titrate up to 200 mcg/kg/min.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Limited data. Initial: 500 mcg/kg loading dose over 1 minute, then 50 mcg/kg/min maintenance. Titrate up to 200-300 mcg/kg/min based on response and tolerability.
Adolescent:
Similar to adult dosing, but use caution and titrate carefully.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
No adjustment needed for parent drug. However, the acid metabolite is renally excreted; accumulation may occur. Monitor for adverse effects.
Dialysis:
Esmolol is not significantly removed by hemodialysis. The acid metabolite is dialyzable. Monitor for adverse effects.
Hepatic Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
No adjustment needed.
Pharmacology
Mechanism of Action
Esmolol is a cardioselective beta-1 adrenergic receptor blocker. It competitively blocks beta-1 receptors, primarily in the heart, leading to decreased heart rate, myocardial contractility, and conduction velocity through the AV node. At higher doses, it can also block beta-2 receptors.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Not applicable (IV infusion)
FoodEffect:
Not applicable (IV infusion)
Distribution:
Vd:
3.4 L/kg
ProteinBinding:
55%
CnssPenetration:
Limited
Elimination:
HalfLife:
Distribution half-life: approximately 2 minutes; Elimination half-life: approximately 9 minutes
Clearance:
117 mL/kg/min
ExcretionRoute:
Renal (acid metabolite)
Unchanged:
<2%
Pharmacodynamics
OnsetOfAction:
Within 2-10 minutes
PeakEffect:
Within 6-10 minutes
DurationOfAction:
10-30 minutes after discontinuation of infusion
Safety & Warnings
BLACK BOX WARNING
Abrupt discontinuation of beta-blockers in patients with coronary artery disease (CAD) may exacerbate angina pectoris, myocardial infarction, and ventricular arrhythmias. When discontinuing chronically administered esmolol, particularly in patients with CAD, the dosage should be gradually reduced over 1 to 2 weeks. If angina worsens or acute coronary insufficiency develops, esmolol administration should be reinstituted promptly, at least temporarily, and other measures appropriate for the management of angina pectoris should be taken. Patients should be warned against interruption or discontinuation of therapy without the physician's advice.
Side Effects
Urgent 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 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
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 acidosis (too much acid in the blood), 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 you experience any of these symptoms, notify your healthcare provider immediately.
Additional 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 unusual symptoms, contact your doctor for advice:
* 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.
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 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
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 acidosis (too much acid in the blood), 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 you experience any of these symptoms, notify your healthcare provider immediately.
Additional 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 unusual symptoms, contact your doctor for advice:
* 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.
Seek Immediate Medical Attention If You Experience:
- Severe dizziness or fainting
- Very slow heart rate
- Difficulty breathing or wheezing
- Swelling in ankles or feet
- Unusual tiredness or weakness
- Coldness or numbness in hands or feet
- Injection site pain, redness, or swelling
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:
+ Breathing problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart conditions, including heart block, heart failure (weak heart), shock caused by heart problems, or slow heartbeat
Specific heart-related conditions, including:
+ A certain type of abnormal heartbeat (sick sinus syndrome)
+ A certain type of chest pain (Prinzmetal's angina)
High pressure in the lungs (pulmonary hypertension)
If you are taking any of the following medications: diltiazem or verapamil
Additionally, it is crucial to discuss all of your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
Vitamins
with your doctor and pharmacist to ensure safe use. Do not start, stop, or change the dose of any medication without first consulting your doctor. This will help determine if it is safe for you to take this medication with your existing health conditions and medications.
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:
+ Breathing problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart conditions, including heart block, heart failure (weak heart), shock caused by heart problems, or slow heartbeat
Specific heart-related conditions, including:
+ A certain type of abnormal heartbeat (sick sinus syndrome)
+ A certain type of chest pain (Prinzmetal's angina)
High pressure in the lungs (pulmonary hypertension)
If you are taking any of the following medications: diltiazem or verapamil
Additionally, it is crucial to discuss all of your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
Vitamins
with your doctor and pharmacist to ensure safe use. Do not start, stop, or change the dose of any medication without first consulting your doctor. This will help determine if it is safe for you to take this medication with your existing health conditions and medications.
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.
Regular blood tests, as directed by your doctor, are crucial to monitor your condition. Discuss any concerns or questions with your doctor. 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 low blood sugar. This risk is particularly higher in individuals with diabetes, children, and those who are fasting, undergoing surgery, have a poor appetite, or are experiencing vomiting. If you have any questions or concerns, consult your doctor.
If you have diabetes, it is vital to closely monitor your blood sugar levels while taking this medication.
This medication may also conceal signs 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 any concerns 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.
Do not abruptly stop taking this medication, as this may lead to increased chest pain and, in some cases, a heart attack. The risk is 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.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the benefits and risks of this medication to both 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.
Regular blood tests, as directed by your doctor, are crucial to monitor your condition. Discuss any concerns or questions with your doctor. 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 low blood sugar. This risk is particularly higher in individuals with diabetes, children, and those who are fasting, undergoing surgery, have a poor appetite, or are experiencing vomiting. If you have any questions or concerns, consult your doctor.
If you have diabetes, it is vital to closely monitor your blood sugar levels while taking this medication.
This medication may also conceal signs 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 any concerns 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.
Do not abruptly stop taking this medication, as this may lead to increased chest pain and, in some cases, a heart attack. The risk is 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.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe bradycardia (very slow heart rate)
- Severe hypotension (very low blood pressure)
- Cardiogenic shock
- Cardiac arrest
- Bronchospasm
- Hypoglycemia
- Congestive heart failure
What to Do:
Treatment is symptomatic and supportive. For severe bradycardia, atropine or isoproterenol may be given. For hypotension, IV fluids and vasopressors (e.g., dopamine, norepinephrine) may be used. Glucagon may be effective for refractory bradycardia or hypotension. Bronchospasm can be treated with beta-2 agonists. Heart failure may require diuretics and inotropes. Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem): Increased risk of myocardial depression, severe bradycardia, and AV block.
- Digoxin: Increased risk of bradycardia and AV block.
- Insulin/Oral Hypoglycemics: May mask symptoms of hypoglycemia (tachycardia, palpitations) and prolong hypoglycemic episodes.
- Clonidine: Potentiation of rebound hypertension upon clonidine withdrawal.
- Fingolimod: Increased risk of severe bradycardia and heart block.
Moderate Interactions
- NSAIDs: May reduce the hypotensive effects of beta-blockers.
- Sympathomimetics (e.g., epinephrine, norepinephrine): May antagonize beta-blocker effects, or lead to unopposed alpha-adrenergic stimulation (hypertension, bradycardia).
- Other antiarrhythmics (e.g., amiodarone, propafenone): Additive effects on heart rate and AV conduction.
- Neuromuscular blockers (e.g., succinylcholine, mivacurium): Esmolol may prolong the duration of action of succinylcholine and mivacurium due to inhibition of plasma cholinesterase.
Minor Interactions
- Alcohol: May enhance hypotensive effects.
Monitoring
Baseline Monitoring
Heart Rate (HR)
Rationale: To establish baseline and guide initial dosing, and to monitor for bradycardia.
Timing: Prior to initiation of therapy
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing, and to monitor for hypotension.
Timing: Prior to initiation of therapy
Electrocardiogram (ECG)
Rationale: To assess baseline cardiac rhythm, PR interval, and QRS duration, and to monitor for AV block or other arrhythmias.
Timing: Prior to initiation of therapy
Respiratory Status/Lung Sounds
Rationale: To assess for signs of bronchospasm, especially in patients with history of asthma/COPD.
Timing: Prior to initiation of therapy
Routine Monitoring
Heart Rate (HR)
Frequency: Continuously (during infusion) or frequently (every 5-15 minutes initially, then hourly once stable)
Target: Individualized based on therapeutic goal (e.g., 60-80 bpm for rate control)
Action Threshold: <50 bpm or symptomatic bradycardia; consider dose reduction or discontinuation
Blood Pressure (BP)
Frequency: Continuously (during infusion) or frequently (every 5-15 minutes initially, then hourly once stable)
Target: Individualized based on therapeutic goal
Action Threshold: Significant hypotension (e.g., SBP <90 mmHg or symptomatic hypotension); consider dose reduction or discontinuation
Electrocardiogram (ECG)
Frequency: Continuous cardiac monitoring
Target: Normal sinus rhythm or controlled arrhythmia
Action Threshold: Development of new arrhythmias, significant AV block (e.g., 2nd or 3rd degree), or QRS widening; consider discontinuation
Peripheral Perfusion/Skin Temperature
Frequency: Hourly or as clinically indicated
Target: Warm, well-perfused extremities
Action Threshold: Signs of peripheral hypoperfusion (e.g., cold extremities, mottling); consider dose reduction
Blood Glucose (in diabetics)
Frequency: Regularly (e.g., every 4-6 hours)
Target: Normal glycemic range
Action Threshold: Hypoglycemia; be aware of masked symptoms
Symptom Monitoring
- Bradycardia
- Hypotension
- Dizziness
- Lightheadedness
- Fatigue
- Dyspnea
- Wheezing
- Chest pain
- Signs of heart failure exacerbation (e.g., edema, crackles, weight gain)
- Injection site reactions (e.g., irritation, phlebitis)
Special Patient Groups
Pregnancy
Category C. Esmolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Beta-blockers can cause bradycardia, hypoglycemia, and respiratory depression in the neonate. Prolonged exposure may lead to intrauterine growth restriction.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Potential for fetal bradycardia and growth restriction.
Third Trimester:
Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate for 24-48 hours after birth.
Lactation
L3 (Moderately Safe). Esmolol is present in human milk in small amounts. Due to its very short half-life and low oral bioavailability, infant exposure is expected to be minimal. Monitor breastfed infants for signs of beta-blockade (e.g., bradycardia, lethargy, poor feeding).
Infant Risk:
Low risk of adverse effects due to minimal exposure and rapid elimination. Observe for bradycardia, hypotension, and hypoglycemia.
Pediatric Use
Safety and efficacy in pediatric patients (especially neonates and infants) have not been fully established. Use with caution, and titrate carefully. Dosing is typically weight-based. Monitor closely for adverse effects, particularly hypotension and bradycardia.
Geriatric Use
No specific dose adjustment is required based on age alone. However, elderly patients may be more sensitive to the hypotensive and bradycardic effects of esmolol due to age-related decreases in renal function and cardiac reserve. Start with lower doses and titrate slowly, monitoring closely for adverse effects.
Clinical Information
Clinical Pearls
- Esmolol is an ultra-short-acting beta-blocker, making it highly titratable and suitable for acute, critical care settings where rapid control of heart rate or blood pressure is needed.
- Its rapid onset and offset allow for quick adjustment of therapy and rapid recovery from adverse effects upon discontinuation.
- Due to its metabolism by esterases in red blood cells, its elimination is not dependent on renal or hepatic function, making it a preferred beta-blocker in patients with significant liver or kidney disease (though the acid metabolite accumulates in renal failure).
- Always administer via continuous IV infusion after an initial loading dose. Avoid abrupt discontinuation, especially in patients with coronary artery disease, due to the risk of rebound effects.
- Monitor for injection site reactions, as esmolol can be irritating to veins, especially at higher concentrations or with prolonged infusions. Consider central line administration for prolonged use or high concentrations.
Alternative Therapies
- Other IV beta-blockers (e.g., metoprolol, labetalol, propranolol) for acute rate/BP control, though with longer durations of action.
- Calcium channel blockers (e.g., diltiazem, verapamil) for rate control in supraventricular tachycardias.
- Adenosine for acute termination of supraventricular tachycardias.
- Other antihypertensives (e.g., nicardipine, clevidipine, nitroglycerin, sodium nitroprusside) for acute blood pressure control.
- Amiodarone for various arrhythmias.
Cost & Coverage
Average Cost:
Varies widely, typically several hundred to over a thousand USD per 2500mg/10ml vial or 2000mg/100ml bag
Generic Available:
Yes
Insurance Coverage:
Typically covered by most insurance plans, often as a Tier 1 or Tier 2 generic. Brand name may require prior authorization.
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 or take someone else's medication. 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; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Additionally, some medications may come with a separate patient information leaflet, which your pharmacist can provide. 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 information about the medication taken, the amount, and the time it occurred.