Esmolol

What is Esmolol?

• Esmolol (Brevibloc) is a cardioselective beta adrenergic blocker used in the treatment of supraventricular tachycardia and severe hypertension.

Esmolol Structure

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Esmolol-Enantiomere

What are the uses of this medicine?

Esmolol (Brevibloc) is used or the short-term treatment of:

• Control of ventricular rate in supraventricular tachycardia including atrial fibrillation and atrial flutter and control of heart rate in noncompensatory sinus tachycardia.
• Control of perioperative tachycardia and hypertension.

How does this medicine work?

• Esmolol (es' moe lol) is considered a “selective” beta-adrenergic receptor blocker in that it has potent activity against beta-1 adrenergic receptors which are found in cardiac muscle, but has little or no activity against beta-2 adrenergic receptors found on bronchial and vascular smooth muscle.
• Esmolol has a rapid time of onset and short duration of action, which makes it useful for intravenous therapy of acute arrhythmias and severe hypertension or in patients with hypertension who are unable to take oral medications.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Severe sinus bradycardia
• Heart block greater than first degree
• Sick sinus syndrome
• Decompensated heart failure
• Cardiogenic shock
• Pulmonary hypertension
• Hypersensitivity reactions, including anaphylaxis

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention the following:

• digoxin
• Anticholinesterases
• Antihypertensive agents clonidine, guanfacine, or moxonidine
• calcium channel antagonists (e.g., verapamil)
• Sympathomimetic drugs
• epinephrine, norepinephrine, and dopamine

Is this medicine FDA approved?

• Esmolol was approved for use in the United States in 1986 and is currently used for the intravenous therapy of supraventricular tachycardias, hypertension in the perioperative period and during episodes of acute myocardial ischemia or infarction.

How should this medicine be used?

Recommended dosage: Supraventricular tachycardia (SVT) or noncompensatory sinus tachycardia:

• Optional loading dose: 500 mcg per kg infused over one minute
• Then 50 mcg per kg per minute for the next 4 minutes
• Adjust dose as needed to a maximum of 200 mcg per kg per minute.
• Additional loading doses may be administered

Perioperative tachycardia or hypertension:

• Loading dose: 500 mcg per kg over 1 minute for gradual control (1 mg per kg over 30 seconds for immediate control)
• Then 50 mcg per kg per min infusion for gradual control (150 mcg per kg per minute for immediate control) adjusted to a maximum of 200 (tachycardia) or 300 (hypertension) mcg per kg per min

Administration:

• Administer intravenously.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection

This medicine is available in fallowing brand namesː

• Brevibloc

What side effects can this medication cause?

The most common side effects of this medicine include:

• Hypotension
• Infusion site reactions
• Nausea
• Dizziness
• Somnolence
• Confusional state and agitation
• Anxiety, depression and abnormal thinking
• Headache
• Paresthesia, syncope, speech disorder, and lightheadedness
• Peripheral ischemia
• Pallor and flushing
• Urinary retention

• At high doses, esmolol is less cardioselective and can induce acute bronchospasm. As with all beta-blockers, sudden withdrawal can trigger rebound hypertension.

What special precautions should I follow?

• Hypotension can occur at any dose but is dose-related. Monitor patients closely, especially if pretreatment blood pressure is low. In case of an unacceptable drop in blood pressure, reduce or stop Brevibloc injection. Decrease of dose or termination of infusion reverses hypotension, usually within 30 minutes.
• Bradycardia, including sinus pause, heart block, severe bradycardia, and cardiac arrest have occurred with the use of Brevibloc injection. Monitor heart rate and rhythm in patients receiving Brevibloc injection. If severe bradycardia develops, reduce or stop Brevibloc injection.
• Beta blockers, like Brevibloc injection, can cause depression of myocardial contractility and may precipitate heart failure and cardiogenic shock. At the first sign or symptom of impending cardiac failure, stop Brevibloc injection and start supportive therapy
• Monitor vital signs closely and titrate Brevibloc injection slowly.
• Patients with reactive airways disease should, in general, not receive beta blockers.
• In patients with hypoglycemia, or diabetic patients (especially those with labile diabetes) who are receiving insulin or other hypoglycemic agents, beta blockers may mask tachycardia occurring with hypoglycemia. Concomitant use of beta blockers and antidiabetic agents can enhance the effect of antidiabetic agents.
• Infusion site reactions have occurred with the use of Brevibloc injection. Avoid infusions into small veins or through a butterfly catheter.If a local infusion site reaction develops, use an alternative infusion site and avoid extravasation.
• Beta blockers may exacerbate anginal attacks in patients with Prinzmetal’s angina. Do not use nonselective beta blockers.
• If Brevibloc injection is used in the setting of pheochromocytoma, give it in combination with an alpha-blocker, and only after the alpha-blocker has been initiated.
• In hypovolemic patients, Brevibloc injection can attenuate reflex tachycardia and increase the risk of hypotension.
• In patients with peripheral circulatory disorders, Brevibloc injection may aggravate peripheral circulatory disorders.
• Severe exacerbations of angina, myocardial infarction, and ventricular arrhythmias have been reported in patients with coronary artery disease upon abrupt discontinuation of beta blocker therapy.
• Beta blockers, including Brevibloc injection, have been associated with increases in serum potassium levels and hyperkalemia. Monitor serum electrolytes during therapy with Brevibloc injection.
• Beta blockers, including Brevibloc injection, have been reported to cause hyperkalemic renal tubular acidosis. Acidosis in general may be associated with reduced cardiac contractility.
• Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Abrupt withdrawal of beta blockade might precipitate a thyroid storm; therefore, monitor patients for signs of thyrotoxicosis when withdrawing beta blocking therapy.
• Patients using beta blockers may be unresponsive to the usual doses of epinephrine used to treat anaphylactic or anaphylactoid reactions.
• Esmolol has not been linked to instances of clinically apparent drug induced liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Cardiac effects include bradycardia, atrioventricular block (1st -, 2nd -, 3rd degree), junctional rhythms, intraventricular conduction delays, decreased cardiac contractility, hypotension, cardiac failure (including cardiogenic shock), cardiac arrest/asystole, and pulseless electrical activity.

• Central nervous system effects include respiratory depression, seizures, sleep and mood disturbances, fatigue, lethargy, and coma.

• In addition, bronchospasm, mesenteric ischemia, peripheral cyanosis, hyperkalemia, and hypoglycemia (especially in children) may occur.

Management of overdosage: Consider the following general measures:

Bradycardia:

• Consider intravenous administration of atropine or another anticholinergic drug or cardiac pacing.

Cardiac Failure:

• Consider intravenous administration of a diuretic or digitalis glycoside. In shock resulting from inadequate cardiac contractility, consider intravenous administration of dopamine, dobutamine, isoproterenol, or inamrinone. Glucagon has been reported to be useful.

Symptomatic hypotension:

• Consider intravenous administration of fluids or vasopressor agents such as dopamine or norepinephrine.

Bronchospasm:

• Consider intravenous administration of a beta2 stimulating agent or a theophylline derivative.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• Brevibloc injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The safety and effectiveness of Brevibloc injection in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• ESMOLOL HYDROCHLORIDE

Inactive ingredients:

• SODIUM ACETATE
• SODIUM CHLORIDE
• ACETIC ACID
• WATER
• SODIUM HYDROXIDE
• HYDROCHLORIC ACID

Who manufactures and distributes this medicine?

Manufactured for:

• Baxter Healthcare Corporation
• Deerfield, IL USA

What should I know about storage and disposal of this medication?

• Store at 25˚C (77˚F). Excursions permitted to 15˚-30˚C (59˚-86˚F).
• Protect from freezing.
• Avoid excessive heat.

Antihypertensive agents

• Dailymed label info on Esmolol
• FDA Esmolol

Esmolol Resources
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