Esmolol HCl

Uses

Esmolol HCl Hydrochloride is a beta adrenergic blocker used for 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.

Esmolol HCl is also used to associated treatment for these conditions: Atrial Fibrillation, Tachycardia, Supraventricular, Intraoperative Hypertension, Intraoperative Tachycardia, Noncompensatory Sinus tachycardia, Postoperative Hypertension, Postoperative Tachycardia

How Esmolol HCl works

Similar to other beta-blockers, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites. Because it predominantly blocks the beta-1 receptors in cardiac tissue, it is said to be cardioselective. In general, so-called cardioselective beta-blockers are relatively cardioselective; at lower doses they block beta-1 receptors only but begin to block beta-2 receptors as the dose increases. At therapeutic dosages, esmolol does not have intrinsic sympathomimetic activity (ISA) or membrane-stabilizing (quinidine-like) activity. Antiarrhythmic activity is due to blockade of adrenergic stimulation of cardiac pacemaker potentials. In the Vaughan Williams classification of antiarrhythmics, beta-blockers are considered to be class II agents.

Dosage

Esmolol HCl dosage

Administer intravenously. Titrate using ventricular rate or blood pressure at ≥4 minute intervals. 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

• Loading dose: 500 mcg per kg over 1 minute for gradual control (1 mg per kg over 30 seconds for immediate control).
• Than 50 mcg per kg per minute 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 minute.

Side Effects

Most common adverse reactions (incidence> 10%) are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension.

Toxicity

Symptoms of overdose include cardiac arrest, bradycardia, hypotension, electromechanical dissociation and loss of consciousness.

Precaution

• Risk of hypotension, bradycardia, and cardiac failure: Reduce or discontinue use
• Risk of exacerbating reactive airway disease
• Diabetes mellitus: Increases the effect of hypoglycemic agents and masks hypoglycemic tachycardia
• Risk of unopposed alpha-agonism and severe hypertension in untreated pheochromocytoma
• Risk of myocardial ischemia when abruptly discontinued in patients with coronary artery disease

Interaction

• Digitalis glycosides: Risk of bradycardia
• Anticholinesterases: Prolongs neuromuscular blockade
• Antihypertensive agents: Risk of rebound hypertension
• Sympathomimetic drugs: Dose adjustment needed
• Vasoconstrictive and positive inotropic effect substances: Avoid concomitant use

Food Interaction

Esmolol HCl Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Esmolol HCl Drug Interaction

Moderate: epinephrine, epinephrine, meperidine, meperidine, midazolam, midazolamMinor: aspirin, aspirinUnknown: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, acetaminophen, acetaminophen, tramadol, tramadol, valproic acid, valproic acid, ascorbic acid, ascorbic acid, phytonadione, phytonadione

Esmolol HCl Disease Interaction

Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hypersensitivity, ischemic heart disease, PVDModerate: cerebrovascular insufficiency, glaucoma, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, asthma/COPD, renal dysfunction

Elimination Route

Rapidly absorbed, steady-state blood levels for dosages from 50-300 µg/kg/min (0.05-0.3 mg/kg/mm) are obtained within five minutes.

Half Life

Rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes. The acid metabolite has an elimination half-life of about 3.7 hours.

Clearance

• 20 L/kg/hr [Men]

Elimination Route

Consistent with the high rate of blood-based metabolism of esmolol hydrochloride, less than 2% of the drug is excreted unchanged in the urine. The acid metabolite has an elimination half-life of about 3.7 hours and is excreted in the urine with a clearance approximately equivalent to the glomerular filtration rate. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about ten-fold that of normals, and plasma levels considerably elevated.

Pregnancy & Breastfeeding use

Pregnancy Category C. Esmolol HCl hydrochloride has been shown to produce increased fetal resorptions with minimal maternal toxicity in rabbits when given in doses approximately 8 times the maximum human maintenance dose (300 mcg/kg/min). There are no adequate and well-controlled studies in pregnant women. Esmolol HCl Hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Esmolol HCl Hydrochloride, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

• Severe sinus bradycardia
• Heart block greater than first degree
• Sick sinus syndrome
• Decompensated heart failure
• Cardiogenic shock
• Coadministration of IV cardiodepressant calcium-channel antagonists (e.g. verapamil) in close proximity to Esmolol HCl hydrochloride
• Pulmonary hypertension
• Known hypersensitivity to esmolol

Storage Condition

Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.

Innovators Monograph

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