Esmolol

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Brevibloc, Esmolol; Belgium: Brevibloc; Cyprus: Brevibloc; Czech Republic: Brevibloc, Esmocard, Esmolol; Denmark: Brevibloc; Finland: Brevibloc; France: Brevibloc; Germany: Brevibloc, Esmocard; Greece: Brevibloc, Esmocard, Esmolol; Hungary: Brevibloc, Esmocard; Ireland: Brevibloc, Esmocard; Italy: Brevibloc; Latvia: Esmocard; Lithuania: Esmocard; Malta: Brevibloc; Netherlands: Brevibloc, Esmolol; Poland: Brevibloc, Esmocard; Portugal: Brevibloc, Esmocard; Slovakia: Esmocard; Spain: Brevibloc; Sweden: Brevibloc, Esmocard.

North America

Canada: Brevibloc; USA: Brevibloc, Esmolol.

Latin America

Argentina: Dublon, Esmolol; Brazil: Brevibloc.

Asia

Japan: Brevibloc.

Drug combinations

Chemistry

Esmolol Hydrochloride: C~16~H~25~NO~4~ HCl. Mw: 331.83. (1) Benzenepropanoic acid, 4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-, methyl ester, hydrochloride, (±)-; (2)(±)-Methyl p-[2-hydroxy-3-(isopropylamino)propoxy]hydrocinnamate hydrochloride. CAS-81161-17-3; CAS-103598-03-4 (esmolol)(1983).

Pharmacologic Category

β-Adrenergic Blocking Agents. Class II Antiarrhythmic Agent. β~1~-Selective β-Adrenergic Blocker. (ATC-Code: C07AB09).

Mechanism of action

A short-acting β~1~-selective adrenergic blocking agent. Competitively blocks response to β~1~-adrenergic stimulation with little or no effect on β~2~-receptors except at high doses, no intrinsic sympathomimetic activity, no membrane-stabilizing activity.

Therapeutic use

Used in management of supraventricular tachyarrhythmias (e.g. atrial flutter and/or fibrillation, sinus tachycardia). Used to prevent or treat increases in blood pressure associated with surgical events, including hypertensive crises (i.e. emergencies and urgencies). Treatment of noncompensatory sinus tachycardia.

Pregnancy and lactiation implications

Teratogenic effects were not noted in animal studies. Fetal bradycardia can occur when administered in the 3^rd^ trimester of pregnancy or at delivery. Use with caution during lactation.

Unlabeled use

In children, for supraventricular tachycardia and postoperative hypertension.

Contraindications

Hypersensitivity to esmolol or any component of the formulation. Sinus bradycardia. Heart block greater than first degree (except with functioning artificial pacemaker). Cardiogenic shock. Bronchial asthma (relative). Uncompensated cardiac failure. Hypotension. Pregnancy (2^nd^ and 3^rd^ trimesters).

Warnings and precautions

Use caution in history of severe anaphylaxis to allergens. Hypotension is common. Extravasation can lead to skin necrosis and sloughing. In general, patients with bronchospastic disease should not receive β-blockers (esmolol, with β~1~ selectivity, has been used cautiously). Consider pre-existing conditions such as sick sinus syndrome before initiating. Use with caution in the following cases: diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms), in compensated heart failure, in myasthenia gravis, in peripheral vascular disease (including Raynaud’s), in history of psychiatric illness (may cause or exacerbate CNS depression), or in renal impairment (active metabolite retained). Use with caution in patients on concurrent verapamil or diltiazem (bradycardia or heart block can occur). Adequate α-blockade is required prior to use of any β-blocker in untreated pheochromocytoma. Concentrations >10 mg/mL or infusion into small veins or through a butterfly catheter should be avoided (can cause thrombophlebitis). β-Blocker therapy should not be withdrawn abruptly (particularly in CAD). Do not use in treatment of hypertension associated with vasoconstriction related to hypothermia. Caution in history of severe anaphylaxis to allergens, diabetes mellitus, compensated heart failure, sick sinus syndrome, myasthenia gravis, peripheral vascular disease (Raynaud’s), history of psychiatric illness, renal impairment or with verapamil or diltiazem (avoid I.V.). Avoid in bronchospastic disease or in hypertension with vasoconstriction related to hypothermia. Adequate α-blockade prior to use. Do not withdraw abruptly (CAD).

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