Esmolol

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 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 ) 1.1 Supraventricular 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.ICD-10: I10, I48.91

• 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 )].contraindicated

• 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 ) 2.1 Dosing 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.

• 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 ) 5.1 Hypotension 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. 5.2 Bradycardia 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 )].

Most common adverse reactions (incidence >10%) are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Gland Pharma at 864-879-9994 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical 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 )] .

8.1 Pregnancy 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. 8.2 Labor 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.

Metabolism

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 output; thus the metabolism of esmolol is not limited by the rate of blood flow to metabolizing tissues such as the liver or affected by hepatic or renal blood flow.

10.1 Signs 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 (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. 10.2 Treatment 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.

• Dec 31, 1986NDANDA019386Baxter Hlthcare
• May 2, 2005ANDAANDA076474Mylan Institutional
• May 2, 2005ANDAANDA076573Fresenius Kabi Usa
• Jul 23, 2015ANDAANDA205520Eugia Pharma
• Apr 7, 2016NDANDA205703Hq Spclt Pharma
• Jun 8, 2018ANDAANDA206608Mylan Labs Ltd
• Jun 8, 2018ANDAANDA207107Sagent Pharms Inc
• Aug 14, 2019ANDAANDA208538Gland

1. 1Drug Ineffective3614%
2. 2Cardiac Arrest218.0%
3. 3Hypotension197.3%
4. 4Bradycardia176.5%
5. 5Product Use Issue155.7%
6. 6Product Use In Unapproved Indication124.6%
7. 7Renal Failure114.2%
8. 8Hypertension93.4%
9. 9Ventricular Fibrillation93.4%
10. 10Atrial Fibrillation83.1%
11. 11Hepatotoxicity83.1%
12. 12Hyperbilirubinaemia83.1%
13. 13Pulmonary Oedema83.1%
14. 14Respiratory Failure83.1%
15. 15Condition Aggravated72.7%

The 10 most recently updated of 111 ClinicalTrials.gov registrations naming Esmolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Opioid-free Anesthesia and Postoperative Delirium
  Not yet recruiting · Phase 1 · Interventional · 174 enrolled · Qianfoshan Hospital
  NCT07603596updated 2026-05-22
• Esmolol Versus Sufentanil on the Quality of Post-cholecystectomy Recovery Laparoscopic Anaesthesia With Orotracheal Intubation on an Outpatient Basis
  Recruiting · Phase 4 · Interventional · 120 enrolled · University Hospital, Limoges
  NCT07019818updated 2026-04-13
• Opioid Free and Opioid Based Anesthesia in Elective Lumbar Spine Surgery
  Recruiting · Observational · 75 enrolled · Marmara University
  NCT07489001updated 2026-03-23
• POCUS-Guided Esmolol in Septic Shock: A Pilot RCT
  Not yet recruiting · Phase 1 · Phase 2 · Interventional · 100 enrolled · John Basmaji
  NCT07313605updated 2026-01-06
• Effect of MGRNOX-Guided General Anesthesia on Opioid Consumption in Patients
  Recruiting · Interventional · 112 enrolled · Peking University Shenzhen Hospital
  NCT07004686updated 2025-12-18
• Reduction of Edema With a Specialized Cocktail for Ultra-early Management in Intracerebral Hemorrhage
  Not yet recruiting · Phase 3 · Interventional · 58 enrolled · Second Affiliated Hospital, School of Medicine, Zhejiang University
  NCT06863558updated 2025-05-14
• Age Comparisons of Exercising Muscle O2 Supply in Healthy Adults: Effects of Esmolol Infusion
  Completed · Early phase 1 · Interventional · 30 enrolled · David N. Proctor, PhD
  NCT04181606updated 2025-05-13
• Effect of Opioid-free Anaesthesia on Postoperative Delirium in Elderly Patients Undergoing Gastrointestinal Surgery
  Not yet recruiting · Phase 4 · Interventional · 406 enrolled · Qianfoshan Hospital
  NCT06958393updated 2025-05-06
• Opioids Continue to Play a Primary Role in the Management of Perioperative Pain Due to Opioid-Free Anesthesia in Open Heart Surgery.
  Completed · Observational · 98 enrolled · Ankara City Hospital Bilkent
  NCT06683911updated 2025-05-06
• Reduction of Edema With a Specialized Cocktail for Ultra-early Management in Ischemic Stroke
  Recruiting · Phase 3 · Interventional · 68 enrolled · Second Affiliated Hospital, School of Medicine, Zhejiang University
  NCT06863571updated 2025-04-18

CPIC-curated drug–gene pairs for Esmolol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• ADRA2CCPIC C
  CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers
• ADRB1CPIC C
  CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers
• GRK4CPIC C
  CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers
• GRK5CPIC C
  CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers

Frequently asked questions

How does Esmolol work?

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.

What is Esmolol used for?

According to FDA labeling, Esmolol carries indications including: 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 ) 1.1 Supraventricular 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Esmolol?

Esmolol is classified as Beta blocking agents, selective, beta-Adrenergic Blocker, Adrenergic alpha1-Antagonists, Adrenergic beta-Antagonists, Calcium Channel Antagonists, Decreased Blood Pressure, Negative Chronotropy, Negative Inotropy.

What are the brand names for Esmolol?

Esmolol is marketed under brand names including Brevibloc.

What are the contraindications for Esmolol?

Esmolol labeling lists contraindications including: 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 )].. Always consult the full prescribing information and a clinician.