Overview:
Esmolol is a beta-blocker that aids in controlling the ventricular rate in patients suffering from atrial fibrillation (irregular heart rhythm). The Food and Drug Administration (FDA) approved the drug in September 2021. It is an intravenous beta-blocker primarily used in the short-term management of certain cardiac conditions. The drug is well known for its rapid onset of action, which aids in controlling blood pressure and heart rate. Overall, the drug is known to have excellent management of cardiovascular conditions. It is a beneficial drug for health professionals in the clinical setup to avoid emergencies.
How Does Esmolol Work?
The drug belongs to the drug classification called the beta blockers. It affects the response to nerve impulses in certain body parts, especially the heart. As a result, the heartbeat eventually slows down, decreasing blood pressure. As the blood pressure is lowered, the oxygen level increases in the heart. The drug can be availed only with a prescription.
Warnings:
It is always better to outweigh the side effects before administering any drug. The following is a list of warnings associated with the drug:
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Allergies - In case of any previous allergic reactions, it is better to inform the doctor. Also, informing allergies to other drugs or food items is equally important to help the doctor decide the medication dosage and prevent unwanted drug interactions.
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Pediatric - The drug safety and efficacy in the pediatric population is yet to be determined. So, Esmolol is currently not recommended for young children.
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Geriatric - The drug has to be carefully administered in elderly individuals, as they are more likely prone to a lot of comorbidities. So, dosage alteration is recommended to prevent any renal and hepatic problems.
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Breastfeeding - The drug's interaction with breast milk is not clearly understood. Hence, it is not advised to use the medication while breastfeeding to prevent any developmental conditions in children.
For Patients:
What Is Tachycardia?
Tachycardia refers to an increased heart rate. It is generally defined as the heart rate exceeding the average resting rate by over 100 beats per minute. The average resting heart rate is usually between 60 and 100 beats per minute. Tachycardia can initiate from different areas of the heart based on the underlying causes. Some common types are mentioned below:
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Sinus Tachycardia - It usually occurs when the electrical impulses controlling the heart rhythm get accelerated with sinus nodes, which is the natural pacemaker. It is a physiological response to stress, anxiety, pain, and fever.
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Ventricular Tachycardia - Ventricular tachycardia originates in the ventricles, which are the lower chambers of the heart. If the arrhythmia is severe, it could be life-threatening. The episodes usually last longer than 30 seconds and may cause dizziness, chest pain, and palpitations (pounding heart sensation). Immediate medical attention is recommended for patients with ventricular tachycardia.
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Atrial Fibrillation - It is a type of irregular heartbeat that originates in the atria. It is characterized by electric signals, which may result in fibrillating motion of the atria. It may lead to an increased risk of stroke and heart failure. The treatment aims to restore normal heart rhythm and manage the associated risks.
Learn More About Esmolol:-
When and How Often to Take Esmolol?
Esmolol can be injected in short terms by ensuring the dose infusion does not exceed 48 hours. Once the drug effects are not essential, they must be discontinued gradually to prevent any side effects. To treat tachycardia, 200 micrograms are provided intravenously to lower the heart rate.
How Effective Is Esmolol?
The drug has to be used safely and effectively for controlling blood pressure pre-operatively, as the drug has a short half-life. Half-life refers to the time the body requires to reduce the drug dosage to half the quantity. The drug is also indicated in sinus tachycardia, where there is an emergency to intervene at a rapid heart rate.
Things to Inform The Doctor Before They Prescribe Esmolol:
Before consuming the drug, informing the doctor about the medical history, family history, and history of any allergic reactions is better to ensure safety and prevent unwanted side effects or drug interactions.
Starting Esmolol:-
How to Take Esmolol?
The drug is administered intravenously in either of the below-mentioned methods:
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Administering 1000 mcg/ kg over a period of 30 seconds. Eventually, it is followed by 150 mcg/kg per minute with a maximum dose of 300 mcg/kg.
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Administer a 500 mcg/kg bolus in one minute, followed by a 50 mcg/ kg infusion over four minutes.
Things to Do After Starting Taking Esmolol:
Look Out for Side Effects:
The side effects of Esmolol are mentioned below:
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Feeling lightheaded.
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Slow heartbeats.
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Swelling in hand.
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Chest tightness.
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Feeling weak.
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Pain and irritation around the injection site.
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Shortness of breath.
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High potassium levels.
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Low blood sugar.
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Weakness.
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Unusual heart rate.
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Increased sweating.
Dietary Alterations:
No specific dietary alteration is recommended. Consuming a healthy and balanced diet could be very useful while taking medications.
What Should Be Done When a Dose Is Missed?
The drug is usually given in emergencies, especially in hospitals, under the supervision of health care professionals. Hence, there is rarely any chance of missing a dose.
What Should Be Done to Treat Esmolol Overdose?
Overdosing on Esmolol is very rare as the health professional in the hospital setup carefully administers it.
How to Store Esmolol?
The drug can be safely stored in controlled room temperatures and is stable for at least 24 hours.
How to Handle Esmolol?
The drug is an ultra-fast medication that quickly controls heart rate and blood pressure. Therefore, it has to be carefully handled in patients with tachycardia.
How to Dispose of Esmolol?
Disposing of the drug is essential to ensure the environment's safety. It is important to check the label for proper disposal of the drug. Some medications could have disposals provided by the manufacturer. Avoid flushing the medications down the toilet as it may contribute to water pollution. It is better to check for any local medication take-back program in the community. This allows for the safe disposal of unused or expired drugs.
Avoid Self-Medication:
It is better to avoid consuming or administering drugs without a prescription as it is unsafe. Self-medication can be an unknown self-threat. Hence, it is advised to consult a doctor before administering any medications after thoroughly examining the health conditions.
For Doctors:
Indication:
The drug is primarily used in managing cardiovascular events. Some of the common medical conditions are mentioned below:
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In acute supraventricular tachycardia, the drug is used for short-term treatment. It slows the heart rate and restores the normal sinus rhythm.
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In intraoperative and perioperative tachycardia, the drug is administered during surgical procedures to control abnormal heart rates and maintain hemodynamic stability.
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The drug is indicated in hypertensive emergencies for short-term treatment.
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The drug reduces oxygen demand in myocardial infarction by lowering the heart rate and blood pressure. It is considered to protect the heart muscle and limit any extensive damage.
Dosage:
The drug dosage may vary depending on the patient's age, weight, and specific medical conditions. Some of the dosage recommendations for each condition are listed below:
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In supraventricular tachycardia, the initial bolus is 0.5 mg/kg for one minute.
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In intraoperative and perioperative tachycardia, the initial infusion ranges from 25-300 mcg/kg/minute. The rate can be adjusted according to the individual needs.
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In hypertensive emergencies, the dosage is about 100 to 300 mcg/kg/minute. Understanding that the general dosage guidelines depend on the specific patient and clinical conditions is essential.
Pharmacology:
Mechanism of Action:
The drug is a beta-1 adrenergic receptor blocker that blocks the effects of adrenaline and noradrenaline. It reduces the response of the heart to sympathetic nervous system stimulation. This can result in several effects on the cardiovascular system. They include reducing the heart rate and decreasing heart contractility. It also aids with reducing blood pressure and has antiarrhythmic effects on the heart.
Pharmacodynamics:
Pharmacodynamics refers to the effects of the drug on the body, including interacting with the target receptors, resulting in physiological and biochemical changes. The pharmacodynamic properties of Esmolol are:
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Selective beta-1 adrenergic receptor.
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Negative inotropic effect.
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Negative chronotropic effect.
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Blood pressure reduction.
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Antiarrhythmic effects.
Ingredients:
Active Ingredient:
The active ingredient of the drug is Esmolol hydrochloride. It is a water-soluble beta-blocker that is available for intravenous administration. It is chemically derived from another beta-blocker called Propranolol. The selective blocking of the drug helps to reduce the effects of adrenaline and noradrenaline on the heart, leading to a decrease in the heart rate. Hydrochloride salt enhances the water solubility, facilitating intravenous administration.
Inactive Ingredients:
The inactive ingredients are:
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Sodium chloride.
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Water.
Absorption and Distribution:
As the drug is directly administered intravenously, it gets rapidly absorbed into the bloodstream and is distributed throughout the body. It reaches the target tissues, like the heart and blood vessels. The onset of the action is rapid. The intravenous route helps to achieve the required dosage for immediate therapeutic effects.
Metabolism and Elimination:
The drug primarily undergoes metabolism in the liver through enzymatic processes, and the pathway involves ester hydrolysis, which is mediated by esterases. The hydrolysis process converts the drug into an inactive metabolite. The drug has a short half-life of about nine minutes. Following the metabolism, the drug is eliminated from the body through renal excretion.
Toxicity:
The drug is well tolerated when used in appropriate dosage, as the healthcare professional suggests. However, a few potential side effects are mentioned below:
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Hypotension - The drug can cause a drop in blood pressure if administered rapidly into the body. It causes a few symptoms, like dizziness and fainting. So, close monitoring of the patients is required in patients with pre-existing cardiovascular conditions.
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Bradycardia - The drug can decrease the heart rate, leading to lightheadedness. Monitoring the heart rate is crucial, especially in patients with a previous history of heart block.
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Bronchospasm - The drug is known to cause bronchospasm in patients with underlying respiratory conditions. Hence, the drug is contraindicated in patients with severe bronchospastic conditions.
Warning and Precaution:
Certain considerations are to be taken into account before considering the drug. Some of the important warnings and precautions are:
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Bradycardia and heart block.
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Hypotension.
Administration of the Drug:
The drug is administered intravenously in a healthcare setting. The dosage and infusion rate depend on the individual and underlying medical condition.
Contraindications:
The drug is contraindicated in the following conditions:
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Hypersensitivity.
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Sinus bradycardia and heart block.
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Severe heart failure.
Clinical Studies for Esmolol:
Numerous studies evaluate the drug's safety and efficacy in various medical conditions. Some of them are listed below:
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A study published in the Journal of Medicine evaluated the use of the drug in treating supraventricular tachycardia and found the drug to be highly effective, with a reasonable success rate and minimal side effects.
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In cardiac surgery, studies have proved the drug can control the heart rate and blood pressure during cardiac surgery.
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Clinical trials have proved that the drug can effectively lower blood pressure and provide a safe environment for the patient.
Drug Interactions:
The drug can interact with other drugs, affecting efficacy or increasing the risk of adverse effects. Hence, collecting a detailed history from the patient before administering the drug is crucial to prevent any drug interactions. Some of the drug interactions caused by Esmolol are mentioned below:
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Calcium channel blockers can cause additive effects on heart rate and blood pressure.
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Combining the drug with beta-blockers can affect the effects of medication and increase the risk of adverse effects.
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The drug may interact with certain anesthetics and increase the risk of hypotension.
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The drug also interacts with certain antiarrhythmic medications like Amiodarone, leading to additive effects on the heart rate and rhythm. So, dose adjustments and monitoring may be required.
