Esmolol Hydrochloride 10 mg/mL Injection, Solution
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the beta-Adrenergic Blocker class.
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🏭 Manufacturer & labeler
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🩺 Clinical
- Esmolol is an IV medication specifically designed for situations where your heart rate or blood pressure needs to be brought under control very quickly — like during or after surge...
- Why am I getting esmolol instead of a pill for my heart rate?
- Esmolol is intended for short-term use only. Your care team will run the infusion only as long as needed to control your heart rate or blood pressure in the current situation. Once...
- Some people feel a drop in blood pressure, which can cause dizziness or sweating. Nausea or drowsiness can also occur. The most common issue is low blood pressure — your care team...
Patient education
Supplement & herbal interactions
Esmolol may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.
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Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII Q40Q9N063P
Acetic acid is a weak organic acid commonly used in medicines as a buffer and pH adjuster. It helps maintain the proper acidity level to ensure the drug remains stable and effective in its formulation.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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UNII NVG71ZZ7P0
A salt derived from acetic acid, sodium acetate anhydrous is used in medicines as a buffer to help maintain stable pH levels and sometimes as a preservative or bulking agent in solid formulations.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
5 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $15.33 | $1,533.01 / 100 ml |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
| Medicare Part B allowsASP · J1805 | $0.230 / J1805 unit | — |
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🧾 Billing & reimbursement
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Esmolol Hydrochloride 10 mg/mL 00404-9785-10 | Henry | 1 vial | — | AP | FDA listed | — |
| Brevibloc 10 mg/mL 00404-9825-10 | Henry | 1 vial | — | AP | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 00404-9858-10 | Henry | 1 vial | — | AP | FDA listed | — |
| Brevibloc 10 mg/mL 10019-0115-01 | Baxter | 25 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 10019-0120-01 | Baxter | 25 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 51662-1322-01 | HF | 10 ml | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 51662-1371-01 | HF | 10 ml | — | — | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 51662-1444-01 | HF | 10 ml | — | AP | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 55150-0194-10 | Eugia | 25 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 63323-0652-10 | Fresenius | 25 vials | — | — | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 63323-0661-14 | Fresenius | 25 vials | — | — | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mLthis 67457-0182-10 | Mylan | 10 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 68083-0211-25 | Gland | 25 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 70518-4410-00 | REMEDYREPACK | 25 vials | — | AP | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 71872-7049-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 71872-7136-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Esmolol Hydrochloride 100 mg/10mL 84549-0194-10 | ProPharma | 10 ml | — | AP | FDA listed | — |
| Brevibloc 10 mg/mL 10019-0670-10 | Baxter | 250 ml | — | AP | FDA listed | — |
| esmolol hydrochloride 10 mg/mL 25021-0308-84 | Sagent | 250 ml | — | AP | FDA listed | — |
| Esmolol Hydrochloride in Water 10 mg/mL 44567-0811-10 | WG | 250 ml | — | — | FDA listed | — |
| Brevibloc 10 mg/mL 10019-0055-61 | Baxter | 250 ml | — | AP | FDA listed | — |
| Brevibloc 10 mg/mL 10019-0672-10 | Baxter | 250 ml | — | AP | FDA listed | — |
| Esmolol Hydrochloride 10 mg/mL 51662-1427-01 | HF | 250 ml | — | AP | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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🗺️ Medicaid utilization & spend
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 67457-0182-10 You're viewing this | 10 VIAL in 1 CARTON (67457-182-10) / 10 mL in 1 VIAL (67457-182-00) | 2007-05-29 | Active |
🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Esmolol hydrochloride injection is a beta adrenergic blocker indicated 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 ( 1.1 ) • Control of perioperative tachycardia and hypertension ( 1.2 )
1.1Supraventricular Tachycardia or Noncompensatory Sinus Tachycardia Esmolol hydrochloride injection is indicated for the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Esmolol hydrochloride injection is also indicated in noncompensatory sinus tachycardia where, in the physician’s judgment, the rapid heart rate requires specific intervention.
Esmolol hydrochloride injection is intended for short-term use.
1.2Intraoperative and Postoperative Tachycardia and/or Hypertension Esmolol hydrochloride injection is indicated for the short-term treatment of tachycardia and hypertension that occur during induction and tracheal intubation, during surgery, on emergence from anesthesia and in the postoperative period, when in the physician’s judgment such specific intervention is considered indicated. Use of esmolol hydrochloride injection to prevent such events is not recommended.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION • Administer intravenously ( 2.1 , 2.2 ) • Titrate using ventricular rate or blood pressure at ≥ 4-minute intervals. ( 2.1 , 2.2 ) • Supraventricular tachycardia (SVT) or noncompensatory sinus tachycardia ( 2.1 ) • 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 and hypertension ( 2.2 ) • 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 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 ( 2.2 )
2.1Dosing for the Treatment of Supraventricular Tachycardia or Noncompensatory Sinus Tachycardia Esmolol hydrochloride injection is administered by continuous intravenous infusion with or without a loading dose. Additional loading doses and/or titration of the maintenance infusion (step-wise dosing) may be necessary based on desired ventricular response. Table 1: Step-Wise Dosing Step Action 1 Optional loading dose (500 mcg per kg over 1 minute), then 50 mcg per kg per min for 4 min 2 Optional loading dose if necessary, then 100 mcg per kg per min for 4 min 3 Optional loading dose if necessary, then 150 mcg per kg per min for 4 min 4 If necessary, increase dose to 200 mcg per kg per min In the absence of loading doses, continuous infusion of a single concentration of esmolol reaches pharmacokinetic and pharmacodynamic steady-state in about 30 minutes.
The effective maintenance dose for continuous and step-wise dosing is 50 to 200 mcg per kg per minute, although doses as low as 25 mcg per kg per minute have been adequate. Dosages greater than 200 mcg per kg per minute provide little added heart rate lowering effect, and the rate of adverse reactions increases. Maintenance infusions may be continued for up to 48 hours.
2.2Intraoperative and Postoperative Tachycardia and Hypertension In this setting it is not always advisable to slowly titrate to a therapeutic effect. Therefore two dosing options are presented: immediate control and gradual control. Immediate Control • Administer 1 mg per kg as a bolus dose over 30 seconds followed by an infusion of 150 mcg per kg per min if necessary. • Adjust the infusion rate as required to maintain desired heart rate and blood pressure.
Refer to Maximum Recommended Doses below. Gradual Control • Administer 500 mcg per kg as a bolus dose over 1 minute followed by a maintenance infusion of 50 mcg per kg per min for 4 minutes. • Depending on the response obtained, continue dosing as outlined for supraventricular tachycardia. Refer to Maximum Recommended Doses below.
Maximum Recommended Doses • For the treatment of tachycardia, maintenance infusion dosages greater than 200 mcg per kg per min are not recommended; dosages greater than 200 mcg per kg per min provide little additional heart rate-lowering effect, and the rate of adverse reactions increases. • For the treatment of hypertension, higher maintenance infusion dosages (250-300 mcg per kg per min) may be required. The safety of doses above 300 mcg per kg per minute has not been studied.
2.3Transition from Esmolol Hydrochloride Injection Therapy to Alternative Drugs After patients achieve adequate control of the heart rate and a stable clinical status, transition to alternative antiarrhythmic drugs may be accomplished. When transitioning from esmolol hydrochloride injection to alternative drugs, the physician should carefully consider the labeling instructions of the alternative drug selected and reduce the dosage of esmolol hydrochloride injection as follows: 1. Thirty minutes following the first dose of the alternative drug, reduce the esmolol hydrochloride infusion rate by one-half (50%).
2. After administration of th…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Table 2: Esmolol Hydrochloride Injection Presentation Product Name Esmolol Hydrochloride Injection Total Dose 100 mg/10 mL Esmolol Hydrochloride Concentration 10 mg/mL Packaging 10 mL Single-Dose Vial Injection: 100 mg/10 mL (10 mg/mL) in 10 mL single-dose vial ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Esmolol hydrochloride injection is contraindicated in patients with: • Severe sinus bradycardia: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2) ] . • Heart block greater than first degree: Second- or third-degree atrioventricular block may precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2) ] . • Sick sinus syndrome: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2) ] . • Decompensated heart failure: May worsen heart failure. • Cardiogenic shock: May precipitate further cardiovascular collapse and cause cardiac arrest. • IV administration of cardiodepressant calcium-channel antagonists (e.g., verapamil) and esmolol hydrochloride injection in close proximity (i.e., while cardiac effects from the other are still present); fatal cardiac arrests have occurred in patients receiving esmolol hydrochloride injection and intravenous verapamil. • Pulmonary hypertension: May precipitate cardiorespiratory compromise. • Hypersensitivity reactions, including anaphylaxis, to esmolol or any of the inactive ingredients of the product (cross-sensitivity between beta blockers is possible). • Severe sinus bradycardia ( 4 ) • Heart block greater than first degree ( 4 ) • Sick sinus syndrome ( 4 ) • Decompensated heart failure ( 4 ) • Cardiogenic shock ( 4 ) • Coadministration of IV cardiodepressant calcium-channel antagonists (e.g. verapamil) in close proximity to esmolol hydrochloride injection ( 4 , 7 ) • Pulmonary hypertension ( 4 ) • Known hypersensitivity to esmolol ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Risk of hypotension, bradycardia, and cardiac failure: Monitor for signs and symptoms of cardiovascular adverse effects. Reduce or discontinue use ( 5.1 , 5.2 , 5.3 , 5.10 ) • Risk of exacerbating reactive airway disease ( 5.5 ) • Diabetes: May mask symptoms of hypoglycemia and alter glucose levels; monitor ( 5.6 ) • Risk of unopposed alpha-agonism and severe hypertension in untreated pheochromocytoma ( 5.9 ) • Risk of myocardial ischemia when abruptly discontinued in patients with coronary artery disease ( 5.12 , 5.15 )
5.1Hypotension Hypotension can occur at any dose but is dose-related. Patients with hemodynamic compromise or on interacting medications are at particular risk. Severe reactions may include loss of consciousness, cardiac arrest, and death.
For control of ventricular heart rate, maintenance doses greater than 200 mcg per kg per min are not recommended. Monitor patients closely, especially if pretreatment blood pressure is low. In case of an unacceptable drop in blood pressure, reduce or stop esmolol hydrochloride injection.
Decrease of dose or termination of infusion reverses hypotension, usually within 30 minutes.
5.2Bradycardia Bradycardia, including sinus pause, heart block, severe bradycardia, and cardiac arrest have occurred with the use of esmolol hydrochloride injection. Patients with first-degree atrioventricular block, sinus node dysfunction, or conduction disorders may be at increased risk. Monitor heart rate and rhythm in patients receiving esmolol hydrochloride injection [see Contraindications (4) ] .
If severe bradycardia develops, reduce or stop esmolol hydrochloride injection.
5.3Cardiac Failure Beta blockers, like esmolol hydrochloride 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 esmolol hydrochloride injection and start supportive therapy [see Overdosage (10) ] .
5.4Intraoperative and Postoperative Tachycardia and/or Hypertension Monitor vital signs closely and titrate esmolol hydrochloride injection slowly in the treatment of patients whose blood pressure is primarily driven by vasoconstriction associated with hypothermia.
5.5Reactive Airways Disease Patients with reactive airways disease should, in general, not receive beta blockers. Because of its relative beta 1 selectivity and titratability, titrate esmolol hydrochloride injection to the lowest possible effective dose. In the event of bronchospasm, stop the infusion immediately; a beta 2 stimulating agent may be administered with appropriate monitoring of ventricular rates.
5.6Hypoglycemia Beta-blockers may prevent early warning signs of hypoglycemia, such as tachycardia, and increase the risk for severe or prolonged hypoglycemia at any time during treatment, especially in patients with diabetes mellitus or children and patients who are fasting (i.e., surgery, not eating regularly, or are vomiting). If severe hypoglycemia occurs, patients should be instructed to seek emergency treatment.
5.7Infusion Site Reactions Infusion site reactions have occurred with the use of esmolol hydrochloride injection. They include irritation, inflammation, and severe reactions (thrombophlebitis, necrosis, and blistering), in particular when associated with extravasation [see Adverse Reactions (6) ] . 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.
5.8Use in Patients with Prinzmetal’s Angina Beta blockers may exacerbate anginal attacks in patients with Prinzmetal’s angina because of unopposed alpha receptor–mediated coronary artery vasoconstriction. Do not use nonselective beta blockers.
5.9Use in Patients with Pheochromocytoma If esmolol hydrochloride injection is used in the setting of pheochromocytoma, give it in combination with an alpha-blocker, and only after the a…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Most common adverse reactions (incidence > 10%) are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Mylan at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The following adverse reaction rates are based on use of esmolol hydrochloride injection in clinical trials involving 369 patients with supraventricular tachycardia and over 600 intraoperative and postoperative patients enrolled in clinical trials.
Most adverse effects observed in controlled clinical trial settings have been mild and transient. The most important and common adverse effect has been hypotension [see Warnings and Precautions (5.1) ] . Deaths have been reported in post-marketing experience occurring during complex clinical states where esmolol hydrochloride injection was presumably being used simply to control ventricular rate [see Warnings and Precautions (5.5) ] .
Table 3: Clinical Trial Adverse Reactions (Frequency ≥ 3%) System Organ Class (SOC) Preferred MedDRA Term Frequency VASCULAR DISORDERS Hypotension Hypotension resolved during esmolol hydrochloride infusion in 63% of patients. In 80% of the remaining patients, hypotension resolved within 30 minutes following discontinuation of infusion. Asymptomatic hypotension Symptomatic hypotension (hyperhidrosis, dizziness) 25% 12% GENERAL DISORDERS AND ADMINISTRATION SITE CONDITIONS Infusion site reactions (inflammation and induration) 8% GASTROINTESTINAL DISORDERS Nausea 7% NERVOUS SYSTEM DISORDERS Dizziness 3% Somnolence 3% Clinical Trial Adverse Reactions (Frequency < 3%): Psychiatric Disorders: Confusional state and agitation (~2%) Anxiety, depression and abnormal thinking (< 1%) Nervous System Disorders: Headache (~2%) Paresthesia, syncope, speech disorder, and lightheadedness (< 1%) Convulsions (< 1%), with one death Vascular Disorders: Peripheral ischemia (~1%) Pallor and flushing (< 1%) Gastrointestinal Disorders: Vomiting (~1%) Dyspepsia, constipation, dry mouth, and abdominal discomfort (< 1%) Renal and Urinary Disorders: Urinary retention (< 1%)
6.2Post-Marketing Experience In addition to the adverse reactions reported in clinical trials, the following adverse reactions have been reported in the post-marketing experience. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate reliably their frequency or to establish a causal relationship to drug exposure. Cardiac Disorders: Cardiac arrest, Coronary arteriospasm Skin and Subcutaneous Tissue Disorders: Angioedema, Urticaria, Psoriasis
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Concomitant use of esmolol hydrochloride injection with other drugs that can lower blood pressure, reduce myocardial contractility, or interfere with sinus node function or electrical impulse propagation in the myocardium can exaggerate esmolol hydrochloride injection’s effects on blood pressure, contractility, and impulse propagation. Severe interactions with such drugs can result in, for example, severe hypotension, cardiac failure, severe bradycardia, sinus pause, sinoatrial block, atrioventricular block, and/or cardiac arrest.
In addition, with some drugs, beta blockade may precipitate increased withdrawal effects. (See clonidine, guanfacine, and moxonidine below.) Esmolol hydrochloride injection should therefore be used only after careful individual assessment of the risks and expected benefits in patients receiving drugs that can cause these types of pharmacodynamic interactions, including but not limited to: • Digitalis glycosides: Concomitant administration of digoxin and esmolol hydrochloride injection leads to an approximate 10% to 20% increase of digoxin blood levels at some time points.
Digoxin does not affect esmolol hydrochloride injection pharmacokinetics. Both digoxin and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use increases the risk of bradycardia. • Anticholinesterases: Esmolol hydrochloride injection prolonged the duration of succinylcholine-induced neuromuscular blockade and moderately prolonged clinical duration and recovery index of mivacurium. • Antihypertensive agents clonidine, guanfacine, or moxonidine: Beta blockers also increase the risk of clonidine-, guanfacine-, or moxonidine-withdrawal rebound hypertension.
If, during concomitant use of a beta blocker, antihypertensive therapy needs to be interrupted or discontinued, discontinue the beta blocker first, and the discontinuation should be gradual. • Calcium channel antagonists: In patients with depressed myocardial function, use of esmolol hydrochloride injection with cardiodepressant calcium channel antagonists (e.g., verapamil) can lead to fatal cardiac arrests. • Sympathomimetic drugs: Sympathomimetic drugs having beta-adrenergic agonist activity will counteract effects of esmolol hydrochloride injection. • Vasoconstrictive and positive inotropic agents: Because of the risk of reducing cardiac contractility in presence of high systemic vascular resistance, do not use esmolol hydrochloride injection to control tachycardia in patients receiving drugs that are vasoconstrictive and have positive inotropic effects, such as epinephrine, norepinephrine, and dopamine. • Digitalis glycosides: Risk of bradycardia ( 7 ) • Anticholinesterases: Prolongs neuromuscular blockade ( 7 ) • Antihypertensive agents: Risk of rebound hypertension ( 7 ) • Sympathomimetic drugs: Dose adjustment needed ( 7 ) • Vasoconstrictive and positive inotropic effect substances: Avoid concomitant use ( 7 )
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Esmolol 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 hydrochloride injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Teratogenicity studies in rats at intravenous dosages of esmolol hydrochloride up to 3000 mcg/kg/min (10 times the maximum human maintenance dosage) for 30 minutes daily produced no evidence of maternal toxicity, embryotoxicity or teratogenicity, while a dosage of 10,000 mcg/kg/min produced maternal toxicity and lethality. In rabbits, intravenous dosages up to 1000 mcg/kg/min for 30 minutes daily produced no evidence of maternal toxicity, embryotoxicity or teratogenicity, while 2500 mcg/kg/min produced minimal maternal toxicity and increased fetal resorptions.
8.2Labor and Delivery Although there are no adequate and well-controlled studies in pregnant women, use of esmolol in the last trimester of pregnancy or during labor or delivery has been reported to cause fetal bradycardia, which continued after termination of drug infusion. Esmolol hydrochloride injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
8.3Nursing Mothers 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 hydrochloride injection, 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.
8.4Pediatric Use The safety and effectiveness of esmolol hydrochloride injection in pediatric patients have not been established.
8.5Geriatric Use Clinical studies of esmolol hydrochloride injection did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should usually start at the low end of the dosing range, reflecting greater frequency of decreased renal or cardiac function and of concomitant disease or other drug therapy.
8.6Hepatic Impairment No special precautions are necessary in patients with hepatic impairment because esmolol hydrochloride injection is metabolized by red-blood cell esterases [see Clinical Pharmacology (12) ] .
8.7Renal Impairment No dosage adjustment is required for esmolol in patients with renal impairment receiving a maintenance infusion of esmolol 150 mcg/kg for 4 hours. There is no information on the tolerability of maintenance infusions of esmolol using rates in excess of 150 mcg/kg or maintained longer than 4 hours [see Clinical Pharmacology (12) ] .
🤰 Pregnancy ▾
8.1Pregnancy Esmolol 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 hydrochloride injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Teratogenicity studies in rats at intravenous dosages of esmolol hydrochloride up to 3000 mcg/kg/min (10 times the maximum human maintenance dosage) for 30 minutes daily produced no evidence of maternal toxicity, embryotoxicity or teratogenicity, while a dosage of 10,000 mcg/kg/min produced maternal toxicity and lethality. In rabbits, intravenous dosages up to 1000 mcg/kg/min for 30 minutes daily produced no evidence of maternal toxicity, embryotoxicity or teratogenicity, while 2500 mcg/kg/min produced minimal maternal toxicity and increased fetal resorptions.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of esmolol hydrochloride injection in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of esmolol hydrochloride injection did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should usually start at the low end of the dosing range, reflecting greater frequency of decreased renal or cardiac function and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE
10.1Signs and Symptoms of Overdose Overdoses of esmolol hydrochloride injection can cause cardiac and central nervous system effects. These effects may precipitate severe signs, symptoms, sequelae, and complications (for example, severe cardiac and respiratory failure, including shock and coma), and may be fatal. Continuous monitoring of the patient is required. • Cardiac effects include bradycardia, atrioventricular block (1 st -, 2 nd -, 3 rd 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.
10.2Treatment Recommendations Because of its approximately 9-minute elimination half-life, the first step in the management of toxicity should be to discontinue the esmolol hydrochloride infusion. Then, based on the observed clinical effects, 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 beta 2 stimulating agent or a theophylline derivative.
10.3Dilution Errors Massive accidental overdoses of esmolol hydrochloride injection have resulted from dilution errors. Some of these overdoses have been fatal while others resulted in permanent disability. Bolus doses in the range of 625 mg to 2.5 g (12.5-50 mg/kg) have been fatal.
Patients have recovered completely from overdoses as high as 1.75 g given over one minute or doses of 7.5 g given over one hour for cardiovascular surgery. The patients who survived appear to be those whose circulation could be supported until the effects of esmolol hydrochloride injection resolved.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Esmolol hydrochloride injection is a beta 1 -selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. Esmolol hydrochloride injection inhibits the beta 1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta 2 receptors located chiefly in the bronchial and vascular musculature.
12.2Pharmacodynamics Clinical pharmacology studies in normal volunteers have confirmed the beta blocking activity of esmolol hydrochloride injection, showing reduction in heart rate at rest and during exercise, and attenuation of isoproterenol-induced increases in heart rate. Blood levels of esmolol hydrochloride injection have been shown to correlate with extent of beta blockade. After termination of infusion, substantial recovery from beta blockade is observed in 10-20 minutes.
The acid metabolite of esmolol exhibits negligible pharmacological activity. In human electrophysiology studies, esmolol hydrochloride injection produced effects typical of a beta blocker: a decrease in the heart rate, increase in sinus cycle length, prolongation of the sinus node recovery time, prolongation of the AH interval during normal sinus rhythm and during atrial pacing, and an increase in antegrade Wenckebach cycle length. In patients undergoing radionuclide angiography, esmolol hydrochloride injection, at dosages of 200 mcg/kg/min, produced reductions in heart rate, systolic blood pressure, rate pressure product, left and right ventricular ejection fraction and cardiac index at rest, which were similar in magnitude to those produced by intravenous propranolol (4 mg).
During exercise, esmolol hydrochloride injection produced reductions in heart rate, rate pressure product and cardiac index which were also similar to those produced by propranolol, but esmolol hydrochloride injection produced a significantly larger fall in systolic blood pressure. In patients undergoing cardiac catheterization, the maximum therapeutic dose of 300 mcg/kg/min of esmolol hydrochloride injection produced similar effects and, in addition, there were small, clinically insignificant increases in the left ventricular end diastolic pressure and pulmonary capillary wedge pressure.
At 30 minutes after the discontinuation of esmolol hydrochloride infusion, all of the hemodynamic parameters had returned to pretreatment levels. The relative cardioselectivity of esmolol hydrochloride injection was demonstrated in 10 mildly asthmatic patients. Infusions of esmolol hydrochloride injection 100, 200 and 300 mcg/kg/min produced no significant increases in specific airway resistance compared to placebo.
At 300 mcg/kg/min, esmolol hydrochloride injection produced slightly enhanced bronchomotor sensitivity to dry air stimulus. These effects were not clinically significant, and esmolol hydrochloride injection was well tolerated by all patients. Six of the patients also received intravenous propranolol, and at a dosage of 1 mg, two experienced significant, symptomatic bronchospasm requiring bronchodilator treatment.
One other propranolol-treated patient also experienced dry air-induced bronchospasm. No adverse pulmonary effects were observed in patients with COPD who received therapeutic dosages of esmolol hydrochloride injection for treatment of supraventricular tachycardia (51 patients) or in perioperative settings (32 patients).
12.3Pharmacokinetics Esmolol is rapidly metabolized by hydrolysis of the ester linkage, chiefly by the esterases in the cytosol of red blood cells and not by plasma cholinesterases or red cell membrane acetylcholinesterase. Total body clearance in man was found to be about 20 L/kg/hr, which is greater than cardiac out…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Esmolol hydrochloride injection is a beta 1 -selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. Esmolol hydrochloride injection inhibits the beta 1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta 2 receptors located chiefly in the bronchial and vascular musculature.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.1How Supplied Esmolol Hydrochloride Injection, 100 mg/10 mL (10 mg/mL) is supplied as: NDC 67457-182-10 carton containing 10 x 10 mL single-dose vials
16.2Storage Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from freezing. Avoid excessive heat. Discard unused portion.
📋 Description ▾
11 DESCRIPTION Esmolol hydrochloride injection is a beta adrenergic receptor blocker with a very short duration of action (elimination half-life is approximately 9 minutes). Esmolol hydrochloride is: • (±)-Methyl p-[2-hydroxy-3-(isopropylamino) propoxy] hydrocinnamate hydrochloride and has the following structure: • Esmolol hydrochloride has the molecular formula C 16 H 26 NO 4 Cl and a molecular weight of 331.8. It has one asymmetric center and exists as an enantiomeric pair. • Esmolol hydrochloride, USP is a white to off-white crystalline powder.
It is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for propranolol.
11.1Esmolol Hydrochloride Injection Dosage Forms Esmolol hydrochloride injection is a clear, colorless to light yellow, sterile, nonpyrogenic solution of esmolol hydrochloride. The formulation for esmolol hydrochloride injection is described in the table below: Table 4: Esmolol Hydrochloride Injection Formulation Q.S. = Quantity sufficient Esmolol Hydrochloride Injection Esmolol Hydrochloride, USP 10 mg/mL Water for Injection, USP Q.S. to volume of 10 mL Sodium Acetate Anhydrous, USP 1.688 mg/mL (equivalent to 2.8 mg/mL Sodium Acetate Trihydrate) Glacial Acetic Acid, USP 0.546 mg/mL Sodium Hydroxide Q.S. to adjust pH to 4.5 to
5.5Hydrochloric Acid Q.S. to adjust pH to 4.5 to
5.5 Esmolol Hydrochloride Structural Formula
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Physicians should inform patients of the risks associated with esmolol hydrochloride injection: • The most common adverse reactions are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension. • Inform patients or caregivers that there is a risk of hypoglycemia when esmolol is given to patients who are fasting or who are vomiting. Monitor for symptoms of hypoglycemia [see Warnings and Precautions (5.6) ] . Manufactured for: Mylan Institutional LLC Morgantown, WV 26505 U.S.A.
Manufactured by: Mylan Institutional Galway, Ireland 50103382 Revised: 2/2025 MI:ESMOIJ:R6