Intravenous Rapid temporary control of ventricular rate in supraventricular arrhythmias
Adult: For cases including atrial fibrillation or flutter in perioperative, postoperative, or other emergent circumstances where short-term control of ventricular rate is necessary, and for non-compensatory sinus tachycardia wherein the rapid heart rate requires a specific intervention: 500 mcg/kg loading dose given over 1 minute, followed by a maintenance infusion of 50 mcg/kg/min for 4 minutes. If response is satisfactory, continue the maintenance infusion. If response is inadequate within 5 minutes, titrate the maintenance infusion in increments of 50 mcg/kg/min for 4 minutes up to Max of 200 mcg/kg/min until the desired response is achieved; an optional loading dose of 500 mcg/kg over 1 minute may be given prior to each increase in the maintenance infusion rate. If needed, the interval between dose titration may be increased from 5 minutes to 10 minutes. Once satisfactory response is achieved, maintenance infusions may be continued for up to 48 hours. Doses must be adjusted based on individual response and tolerance. Dosage regimen and treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Adult: During anaesthesia (immediate control): Loading dose of 1,000 mcg/kg (approx 80 mg) over 15-30 seconds via bolus inj, followed by an infusion of 150 mcg/kg/min if necessary. Adjust infusion rate as needed up to 300 mcg/kg/min. After waking from anaesthesia: 500 mcg/kg/min infused for 4 minutes, followed by an infusion of 300 mcg/kg/min as needed. Post-operative situations (when time for titration is available): 500 mcg/kg loading dose given over 1 minute, followed by a maintenance infusion of 50 mcg/kg/min for 4 minutes. If response is satisfactory, continue the maintenance infusion. If response is inadequate within 5 minutes, titrate the maintenance infusion in increments of 50 mcg/kg/min for 4 minutes up to Max of 300 mcg/kg/min until the desired response is achieved; an optional loading dose of 500 mcg/kg over 1 minute may be given prior to each increase in the maintenance infusion rate. Dosage regimen and treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Incompatibility
Incompatible with 5% Na bicarbonate solution. May cause precipitation with furosemide.
Contraindications
Decompensated heart failure, severe sinus bradycardia (<50 bpm), 2nd- or 3rd-degree AV block, severe AV-nodal conductance disorders (without pacemaker), sick sinus syndrome, cardiogenic shock, severe hypotension, pulmonary hypertension, asthma, untreated phaeochromocytoma, metabolic acidosis. Esmolol should not be used to control supraventricular tachycardia in patients receiving agents that have vasoconstrictive and positive inotropic effects (e.g. epinephrine, norepinephrine, dopamine). Concomitant use or recent (within 48 hours) administration of IV Ca channel blocker (e.g. verapamil).
Special Precautions
Patient with compensated heart failure, 1st-degree AV block, low pre-treatment heart rates, Prinzmetal’s angina, haemodynamic compromise, hypertension associated with hypothermia; bronchospastic disease, hypovolaemia, diabetes mellitus, myasthenia gravis, peripheral vascular disease (PVD), Raynaud’s disease; personal or family history of psoriasis; history of severe anaphylaxis to allergens. May mask the signs and symptoms of hypoglycaemia and hyperthyroidism (e.g. tachycardia). Avoid extravasation. Not intended to be used in a chronic setting. Avoid abrupt withdrawal. Elderly. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypotension; bradycardia, including sinus pause, heart block, and severe bradycardia; increased incidence and duration of anginal attacks; hyperkalaemia (particularly in patients with renal impairment), hyperkalaemic renal tubular acidosis; anaphylactic reactions, development or aggravation of psoriasis, may precipitate or aggravate symptoms of arterial insufficiency; infusion site irritation and inflammation, including severe reactions particularly associated with extravasation (e.g. thrombophlebitis, necrosis, blistering). Eye disorders: Visual impairment. Gastrointestinal disorders: Nausea, vomiting, dry mouth, abdominal pain, dysgeusia, dyspepsia, constipation. General disorders and administration site conditions: Asthenia, fatigue, chills, pyrexia, oedema, pain; infusion site induration. Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Musculoskeletal pain. Nervous system disorders: Headache, dizziness, somnolence, paraesthesia, attention disturbance, syncope, convulsion, speech disorder. Psychiatric disorders: Anxiety, depression, abnormal thinking, confusional state, agitation. Renal and urinary disorders: Urinary retention. Respiratory, thoracic and mediastinal disorders: Dyspnoea, bronchospasm, pulmonary oedema, wheezing, rhonchi, rales, nasal congestion. Skin and subcutaneous tissue disorders: Diaphoresis, erythema, skin discolouration. Vascular disorders: Peripheral ischaemia, pallor, flushing. Potentially Fatal: Severe cardiac reactions (e.g. precipitation of heart failure and cardiogenic shock, cardiac arrest).
Closely monitor blood pressure, mean arterial pressure, heart rate, continuous ECG, respiratory rate, serum K (particularly in patients with renal impairment), serum glucose (in diabetic patients), and IV site.
Overdosage
Symptoms: Severe hypotension, nausea, vomiting, hypoglycaemia, hyperkalaemia, heart and respiratory insufficiency, bronchospasm, sinus bradycardia, AV block, cardiogenic shock, convulsions, loss of consciousness leading to coma, and cardiac arrest. Management: Symptomatic treatment. Give IV atropine or another anticholinergic drug to treat bradycardia; if treatment is insufficient, a pacemaker may be necessary. To treat bronchospasm, administer β2-sympathomimetics via nebulisation or consider IV aminophylline or IV β2-sympathomimetic administration if nebulisation is insufficient. Administer fluids and/or pressor agents for hypotension. Treat cardiac failure with IV diuretics or digitalis glycosides. For shock resulting from inadequate contractility, consider the administration of IV dobutamine, dopamine, or isoprenaline.
Drug Interactions
Enhanced blood glucose lowering effect with insulin or oral antidiabetic agents. Increased effect or increased risk of adverse reactions with other antihypertensive agents or drugs that may cause hypotension or bradycardia. Increased risk of hypotension with dihydropyridine Ca channel antagonists (e.g. nifedipine), inhalation anaesthetics, and ganglion-blocking agents. May enhance the effect on atrial conduction time and induce negative inotropic effect with class I antiarrhythmic agents (e.g. disopyramide, quinidine) and amiodarone. Hypotensive effect may be decreased with NSAIDs. May cause additive blood pressure-lowering effect with TCAs (e.g. imipramine, amitriptyline), barbiturates, phenothiazines (e.g. chlorpromazine), and other antipsychotic agents (e.g. clozapine). Additive effect with catecholamine-depleting drugs (e.g. reserpine). May increase the rebound hypertensive effect of α2-agonist (e.g. clonidine, moxonidine) when it is abruptly withdrawn. May cause severe peripheral vasoconstriction and hypertension with ergot derivatives. AV conduction time may be increased with digitalis glycosides. May prolong the duration of the neuromuscular blockade of suxamethonium chloride. May moderately prolong the clinical duration and recovery index of mivacurium. Potentially Fatal: Increased risk of cardiac arrest with IV Ca channel blockers (e.g. verapamil). Increased risk of reduced cardiac contractility in the presence of high systemic vascular resistance with vasoconstrictive or inotropic drugs (e.g. epinephrine, dopamine, norepinephrine).
Action
Description: Mechanism of Action: Esmolol, a β1-selective (cardioselective) adrenergic receptor blocking agent, is a class II antiarrhythmic. It competitively inhibits response to β1-adrenergic stimulation in cardiac muscle with minimal or no effect on β2-receptors in bronchial and vascular muscles except at high doses. It possesses no significant intrinsic sympathomimetic activity or membrane stabilising activity at therapeutic doses. Onset: β-blockade: 2-10 minutes (IV). Duration: Haemodynamic effects: 10-30 minutes. Pharmacokinetics: Distribution: Volume of distribution: Approx 3.4 L/kg (esmolol); approx 0.4 L/kg (acid metabolite). Plasma protein binding: 55% (esmolol); 10% (acid metabolite). Metabolism: Rapidly metabolised in the blood via hydrolysis by RBC esterases into an acid metabolite and methanol (does not reach levels associated with methanol toxicity). Excretion: Via urine (approx 73-88% as acid metabolite, <2% as unchanged drug). Elimination half-life: 9 minutes (esmolol); 3.7 hours (acid metabolite).
Chemical Structure
Esmolol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 59768, Esmolol. https://pubchem.ncbi.nlm.nih.gov/compound/Esmolol. Accessed Feb. 23, 2023.
Storage
Store below 25°C. Do not freeze. Protect from light and excessive heat.
C07AB09 - esmolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
References
Anon. Esmolol. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 21/12/2022.Anon. Esmolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/12/2022.Buckingham R (ed). Esmolol Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/12/2022.Escord Injection 10 mg/mL (Zulat Pharmacy Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/11/2022.Esmolol Hydrochloride 10 mg/mL Solution for Infusion (Noridem Enterprises Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/11/2022.Esmolol Hydrochloride in Sodium Chloride Injection (AuroMedics Pharma LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/11/2022.Joint Formulary Committee. Esmolol Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/11/2022.
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