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Brevibloc

Generic Name: Esmolol Hydrochloride
Class: beta-Adrenergic Blocking Agents
VA Class: CV100
Chemical Name: 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzenepropanoic acid methyl ester hydrochloride
Molecular Formula: C16H25NO4•ClH
CAS Number: 81161-17-3

Introduction

Short-acting β1-selective adrenergic blocking agent.1 2 17 18 113 167

Uses for Brevibloc

Supraventricular Tachyarrhythmias (SVT)

Rapid, temporary control of ventricular rate in patients with atrial flutter and/or fibrillation associated with surgical or other manipulative procedures (e.g., cardiac catheterization), or other emergent situations requiring short-term control of ventricular rate.1 2 5 51 52 53 54 55 56 57 58 59 68 87 88 100 113 143 152 167

β-Adrenergic blocking agents, including esmolol, are one of several preferred antiarrhythmic agents for the treatment of stable, narrow-complex supraventricular tachycardias (e.g., paroxysmal supraventricular tachycardia [reentry supraventricular tachycardia], ectopic or multifocal atrial tachycardia, junctional tachycardia) if the rhythm is not controlled by vagal maneuvers or adenosine in patients with preserved left ventricular function and for rate control in atrial fibrillation or flutter in patients with preserved left ventricular function.167

Slideshow: Atrial Fibrillation - Stroke Prevention Guidelines & Treatment Options

May be useful in patients with noncompensatory sinus tachycardia for short-term control of rapid heart rate requiring intervention.1 2 37 59 60 61 62 63 64 65 66 67 68

Not intended for chronic use when other more appropriate antiarrhythmic agents would be preferred.1 2

Hypertension

Treatment of intraoperative and postoperative hypertension and/or tachycardia.a Has been used effectively for prevention or treatment of increases in BP associated with surgical events,63 64 71 72 73 74 75 109 113 125 142 including hypertensive crises (i.e., emergencies and urgencies).142 However, use for prevention of such events is not recommended by the manufacturer.a

Management of hypertensive urgencies or emergencies in adults.142

Rapid reduction of BP in the management of hypertensive urgencies or emergencies in pediatric patients 1–17 years of age.154

Treatment to produce controlled hypotension during anesthesia in order to reduce bleeding resulting from surgical procedures (e.g., orthopedic surgery, neurosurgery).75 114 124

AMI

Has been used for the management of acute tachyarrhythmias complicating AMI15 24 25 167 and to minimize myocardial ischemia following AMI.13 15 24 25 58 113 167

Unstable Angina and Non-ST-Segment Elevation MI

A β-blocker is used as part of standard therapeutic measures, including aspirin and/or clopidogrel, low-molecular weight or unfractionated heparin, and nitrates followed by either conservative medical management or early aggressive management (e.g., angiographic evaluation and revascularization procedures) as required.144 149 150 167

ACC and AHA recommend an IV β-blocker followed by oral β-blocker therapy for patients with unstable angina at high risk of death or nonfatal MI who do not have contraindications to these drugs.149 β-Blockers without intrinsic sympathomimetic activity (e.g., metoprolol, atenolol, propranolol, esmolol) are preferred to manage unstable angina.149 Oral β-blocker therapy is recommended for lower-risk patients.149

Brevibloc Dosage and Administration

Administration

Administer by IV infusion.1

May administer by direct IV injection for immediate control of intraoperative tachyarrhythmia and/or hypertension.a

Constant infusion is preferred for rapid BP reduction in children due to short duration of action.154

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

IV infusion usually administered via controlled infusion device to facilitate dosage titration.52 53 54 61 114 126

Esmolol hydrochloride concentrate (250 mg/mL) is not for direct IV injection and must be diluted prior to administration.1 2 3 Alternatively, use esmolol hydrochloride for injection (10 or 20 mg/mL) in ready-to-use vials or premixed injection (10 or 20 mg/mL) in ready-to-use bags for direct IV injection and infusion.a

Some clinicians state that an auxiliary label with the indication esmolol hydrochloride concentrate is not for direct injection and must be diluted before administration should be affixed to the ampul containing the concentrate.137 138

Take care to avoid extravasation.a Avoid using butterfly needles and very small veins for infusion.1 114 Use alternate infusion site if local reaction occurs at infusion site.1 Infusion concentration of 20 mg/mL associated with more serious venous irritation (e.g., thrombophlebitis) than 10-mg/mL solution.a Extravasation of 20-mg/mL solution may cause serious local reaction and possibly skin necrosis.1 2 3

Do not introduce additives into premixed solutions in ready-to-use bags.1 a

Do not use the premixed injection in series connections with other plastic containers since such use could result in air embolism.1

Infusion bag for premixed solution contains 2 outlet ports.1 Use medication port on the bag only for withdrawing an initial loading dose for direct IV injection.a Sterility cannot be guaranteed with repeated withdrawals; once drug has been withdrawn from the bag, use the solution within 24 hours.a

Dilution

For IV infusion, dilute esmolol hydrochloride concentrate (250 mg/mL) to a final concentration of 10 mg/mL by adding 5 g of esmolol hydrochloride to a 500-mL container of compatible IV infusion solution (see Compatibility under Stability);1 2 3 alternatively, dilute 2.5 g in 250 mL of a compatible IV infusion solution.a Prior to dilution, remove an appropriate amount of solution (according to overfill) from the diluent container.1

Use of the concentrate (with propylene glycol in formulation) diluted to a concentration >10 mg/mL has caused a higher incidence of venous irritation with continued infusion;a however, use of the concentrate diluted to a concentration >10 mg/mL has been well tolerated when administered via central vein.a

Rate of Administration

Administer 500-mcg/kg loading doses over 1 minute, followed by IV infusion of the drug.a Rate of IV infusion determined by patient response and tolerance.1 51 52 53 54 55 58 59 60 61 64 65 66 67 68

For immediate control of intraoperative hypertension and/or tachycardia, administer initial 80-mg bolus dose by IV injection over 30 seconds, followed by IV infusion, if necessary.a

Dosage

Available as esmolol hydrochloride; dosage expressed in terms of the salt.a

Pediatric Patients

Hypertension
Rapid Reduction of BP in Hypertensive Urgencies or Emergencies
IV

Children and adolescents 1–17 years of age: 100–500 mcg/kg per minute as constant infusion.154

Adults

SVT
IV

Loading dose of 500 mcg/kg per minute for 1 minute,1 51 52 53 54 55 58 167 followed by maintenance infusion of 50 mcg/kg per minute for 4 minutes.1 2 3 51 52 53 54 167

If desired response is not attained within first 5 minutes, may increase infusion rate in 50-mcg/kg per minute increments (i.e., to 100 mcg/kg per minute, then to 150 mcg/kg per minute) up to a maximum of 200 mcg/kg per minute; maintain each new rate for 4 or more minutes.1 Alternatively, some experts recommend a second loading dose of 500 mcg/kg per minute for 1 minute, followed by maintenance infusion of 100 mcg/kg per minute (maximum infusion rate is 300 mcg/kg per minute).167

Adjust rate and duration of infusion carefully according to patient’s tolerance and response (as indicated by ventricular rate and BP).1 51 52 53 54 55 58 143 150

Average maintenance dosage: 100 mcg/kg per minute (range: 50–200 mcg/kg per minute).1 2 3 51 52 53 54 55 58 Adequate heart rate control may occur with dosage as low as 25 mcg/kg per minute.1 55

Transfer to alternative antiarrhythmic therapy (e.g., longer-acting β-blocker, digoxin, verapamil) when adequate control of heart rate has been achieved and patient is stabilized.1

Rapid Dosage Titration (if rapid slowing of ventricular response is required)
IV

Loading dose of 500 mcg/kg per minute for 1 minute,1 51 52 53 54 55 58 143 167 followed by maintenance infusion of 50 mcg/kg per minute for 4 minutes.1 2 3 51 52 53 54 143 167

Administer second loading dose of 500 mcg/kg per minute for 1 minute,1 2 3 51 52 53 54 143 167 followed by maintenance infusion of 100 mcg/kg per minute for 4 minutes.1 2 3 51 52 53 54 143 167

If necessary, administer a third and final loading dose of 500 mcg/kg per minute for 1 minute, followed by 150 mcg/kg per minute for 4 minutes.1 52 55 57 58

If needed (without a fourth loading dose), increase maintenance dosage to maximum of 200 mcg/kg per minute.1 52 55 57 58

Once the desired ventricular rate1 or a patient tolerance end point (e.g., reduction in BP)52 53 54 has been nearly achieved,1 114 omit loading doses and titrate maintenance infusion rate upward (to 200 mcg/kg per minute) or downward as appropriate; may increase interval between dosage increments.1

Transfer to Alternative Antiarrhythmics
IV

Decrease esmolol infusion rate by 50% 30 minutes after the first dose of the alternative drug; if adequate response is maintained for ≥1 hour after the second dose of the alternative drug, discontinue esmolol.1

Consider dosing guidelines for the alternative drug when determining the appropriateness of this guideline for transferring therapy.1

Hypertension
Immediate Control of Intraoperative Hypertension and/or Tachycardia
IV

80 mg (approximately 1 mg/kg) by direct IV injection over 30 seconds; if necessary, follow with IV infusion of 150 mcg/kg per minute.1

Adjust as required to maintain desired heart rate and/or BP (maximum 300 mcg/kg per minute).1

Gradual Control of Intraoperative and Postoperative Hypertension and/or Tachycardia
IV

Loading dose of 500 mcg/kg per minute for 1 minute followed by maintenance infusion of 50 mcg/kg per minute for 4 minutes.a If desired response is not attained within first 5 minutes, administer second loading dose of 500 mcg/kg per minute for 1 minute followed by maintenance infusion of 100 mcg/kg per minute.a

Adjust dosage using titration schedule recommended for treatment of SVT;1 however, higher dosages (e.g., 250–300 mcg/kg per minute) may be required for adequate control of BP.1

Hypertensive Emergency
IV

Loading dose of 250–500 mcg/kg over 1 minute, followed by 50–100 mcg/kg per minute for 4 minutes;142 may repeat loading dose or increase infusion rate to 300 mcg/kg per minute as tolerated.153

Initial goal is ≤25% reduction of mean arterial BP within minutes to 1 hour, followed by further reduction (if stable) toward 160/100–110 mm Hg within next 2–6 hours.142

Implement further gradual reductions toward normal over next 24–48 hours if this BP is well tolerated and patient is clinically stable.153

Avoid excessive declines in pressure that could precipitate renal, cerebral, or coronary ischemia.142

In patients with aortic dissection, reduce SBP to <100 mm Hg if tolerated.153

Production of Controlled Hypotension during Anesthesia
IV

Dosage has been titrated upward to a level necessary to maintain the required reduction in BP (e.g., a 15% reduction in mean arterial pressure) or until maximum rate of 300 mcg/kg per minute is reached.75 124 126

AMI
IV

Loading dose of 500 mcg/kg per minute for 1 minute, followed by maintenance infusion of 50 mcg/kg per minute for 4 minutes.24

If necessary, gradually titrate upward (using titration regimen similar to that for SVT) until desired response or maximum dosage of 300 mcg/kg per minute is reached or SBP is decreased to <90 mm Hg.24

Unstable Angina or Non-ST-segment Elevation MI
IV

Initially, 100 mcg/kg per minute followed by increments of 50 mcg/kg per minute every 10–15 minutes as tolerated (by effect on BP) until desired response occurs, limiting symptoms develop, or dosage of 300 mcg/kg per minute is achieved.149

May administer loading dose of 500 mcg/kg over 2–5 minutes for more rapid onset.149

Target resting heart rate in unstable angina is 50–60 bpm in the absence of dose-limiting adverse effects.149

Prescribing Limits

Adults

SVT
IV

Manufacturer recommends maximum maintenance dosage of 200 mcg/kg per minute.a Maintenance dosages as high as 300 mcg/kg per minute have been used1 2 3 51 52 53 54 55 58 167 but provide little added benefit and increase the incidence of adverse effects.1 2 51 53 58 114 Safety of maintenance dosages >300 mcg/kg per minute not established.1 3

Administered for ≤24 hours in most patients;1 2 55 limited data indicate that infusions may be well tolerated for up to 48 hours.1 143

Hypertension
Intraoperative and Postoperative Hypertension and/or Tachycardia
IV

Maximum 300 mcg/kg per minute.1

Special Populations

Renal Impairment

Administer with caution, especially in patients with severe renal impairment.1 2

Cautions for Brevibloc

Contraindications

  • Cardiogenic shock.1

  • Overt cardiac failure.1 150

  • Second- or third-degree AV block.1 150

  • Sinus bradycardia.1

Warnings/Precautions

Warnings

Hypotension

Risk of hypotension,1 2 24 50 51 54 55 56 57 58 59 63 100 113 114 122 167 occasionally symptomatic (e.g., manifested as diaphoresis or dizziness).1 2 50 51 54 55 58 Can occur at any dose level but usually is dose related.1 2 51 53 58 Doses >200 mcg/kg per minute not recommended by manufacturer for SVT management.1 2 114

Dosage reduction or discontinuance of drug usually results in reversal of hypotension within 30 minutes.1

Monitor BP closely, especially in patients with low pretreatment BP (e.g., SBP <105 mm Hg).1 2 55 58 114 143 150

Intraoperative or Postoperative Hypertension

Do not use when hypertension is principally due to hypothermia-associated vasoconstriction.1

Cardiac Failure

Possible precipitation of CHF in patients with inadequate cardiac function; use with caution in such patients.1 2 Prolonged β-adrenergic blockade may lead to cardiac failure in patients with latent cardiac insufficiency.104

Avoid use in patients with overt CHF.1 Use cautiously, if necessary, in patients with compensated heart failure (e.g., those controlled with cardiac glycosides and/or diuretics).1

Discontinue at first sign or symptom of impending cardiac failure;1 if necessary, initiate specific therapy (e.g., a cardiac glycoside and/or diuretic).1 2 If continued esmolol therapy is necessary, may restart esmolol infusion at a slower rate once manifestations of cardiac failure have subsided.114

Bronchospastic Disease

In general, do not use β-blockers in patients with bronchospastic disease;1 2 105 106 107 116 117 143 150 167 however, may use esmolol with caution due to its relative β1-selective adrenergic blocking activity and short duration of action.1 2 Administer lowest effective dose since β1-selectivity is not absolute.1 2

Discontinue immediately if bronchospasm occurs.1 May administer a β2-adrenergic agonist (bronchodilator), but use extreme caution since the patient may have a preexisting rapid ventricular rate.1 2

Diabetes and Hypoglycemia

Possible decreased signs and symptoms of hypoglycemia (e.g., tachycardia, palpitation, BP changes, tremor, feelings of anxiety, but not sweating or dizziness) and increased insulin-induced hypoglycemia.1 2 108

Use with caution in patients with diabetes mellitus or hypoglycemia.1 2

General Precautions

Adverse effects generally resolve more rapidly than with other β-blockers because of esmolol’s short duration of action.1 2 3 4 5 113

Cardiovascular Precautions

Use with caution in patients with SVT who are compromised hemodynamically or are taking drugs that reduce peripheral resistance, myocardial filling, myocardial contractility, and/or electrical impulse propagation in the myocardium.1

Do not use in patients with acute atrial fibrillation who have severe left ventricular dysfunction,150 167 hypotension,143 150 167 or an accessory pathway.143 152 167

Deaths have been reported in patients with complex clinical states receiving esmolol (presumably to control ventricular rate).1

History of Anaphylactic Reactions

Patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated, accidental, diagnostic, or therapeutic challenge with such allergens and less responsive to usual doses of epinephrine.1

Abrupt Withdrawal of Therapy

Abrupt discontinuance has not produced the withdrawal effects (e.g., exacerbation of angina symptoms, precipitation of MI) associated with abrupt discontinuance of other β-adrenergic blocking agents used chronically.1 However, consider the possibility that such effects could occur with esmolol in patients with coronary artery disease; use caution when esmolol infusions are stopped abruptly in such patients.1

Extravasation

Avoid extravasation; skin necrosis may occur.1 (See IV Administration under Dosage and Administration.)

Specific Populations

Pregnancy

Category C.a

Lactation

Not known whether esmolol is distributed into milk.1 Use with caution in nursing women.1

Pediatric Use

Safety and efficacy not established in children <18 years of age.1 114

Use with caution for rapid reduction of BP in pediatric patients 1–17 years of age; may cause profound bradycardia, and reductions in BP may be modest.154

Renal Impairment

Use with caution in patients with renal impairment, especially severe impairment; de-esterified metabolite (ASL 8123) is eliminated mainly by the kidneys.1 2 47

Common Adverse Effects

Hypotension,1 2 24 50 51 53 54 55 56 57 58 59 63 100 113 114 122 dizziness,1 2 51 54 55 58 113 122 diaphoresis,1 2 50 51 54 55 58 113 122 headache,1 2 51 55 58 59 113 somnolence,1 2 50 55 58 113 confusion,1 2 55 58 113 agitation,1 2 55 58 63 113 nausea,1 2 51 55 56 58 59 113 infusion site reactions1 2 (e.g., inflammation,1 2 54 55 58 induration).1 2 55 58 59

Interactions for Brevibloc

Specific Drugs

Drug

Interaction

Comments

Digoxin

Possible increase in serum digoxin concentrations;1 2 49 113 esmolol pharmacokinetics unaffected1 2 49 113

Used safely and effectively; combined therapy apparently somewhat more effective than esmolol alone in lowering heart rate59 113

Verapamil

Rare but serious adverse reactions (including fatal cardiac arrest) with concomitant IV β-blocker and IV verapamil, especially in patients with severe cardiomyopathy, CHF, or recent MI1 141

Mibefradil (no longer commercially available in US)

Slowing or complete suppression of SA node activity, with slow ventricular rates139 140

Vasoconstrictors or inotropes (e.g., dopamine, epinephrine, norepinephrine)

Potential for blocked cardiac contractility when systemic vascular resistance is high1

Do not use esmolol to control SVT in patients receiving vasoconstrictive or inotropic drugs1

Catecholamine-depleting drugs (e.g., reserpine)

Possible additive effects1

Monitor closely for marked bradycardia or hypotension1

Morphine

Increased esmolol concentrations; morphine pharmacokinetics not affected1 2 49 113

Titrate esmolol dosage carefully1 2 49

Neuromuscular blocking agents (succinylcholine)

Possible prolonged duration of neuromuscular blockade1 2 113

Apparently not clinically important1 2 86 114

Warfarin

Slight increase in esmolol concentrations;1 2 49 113 warfarin concentrations not affected1 2 49 113

Titrate esmolol dosage carefully1

Brevibloc Pharmacokinetics

Absorption

Onset

Following rapid IV injection, 13–18% decrease in heart rate within 1 minute, 11–18% decrease in SBP within 2 minutes, and 13–22% prolongation of PR interval within 4 minutes after IV injection.41

In patients with SVT, 15–20% reduction in heart rate apparent within 5–22 minutes after initiation of IV infusion.59 68

Duration

Following discontinuance of IV infusion, β-blockade dissipates within about 1–2 minutes, substantial recovery occurs within about 10–20 minutes, and complete reversal occurs within about 20–30 minutes.1 2 5 27 34 39 113

Distribution

Extent

Distributed into liver and kidneys, but only minimally into CSF, spleen, or testes of rats.2 28 Rapidly and widely distributed in humans.2 39 99 113

Not known whether esmolol and/or ASL 8123 crosses the placenta in humans, 126 but the drug crosses the placenta in animals.114 115

Not known whether esmolol and/or ASL 8123 are distributed into milk.1

Plasma Protein Binding

Esmolol: 55%1 2 28 113 (albumin and α1-acid glycoprotein).28

Metabolite (ASL 8123): Approximately 10%.1 2 113

Elimination

Metabolism

Hydrolyzed rapidly, principally by esterases (probably arylesterase) in erythrocytic cytosol,1 2 39 40 45 46 99 113 to de-esterified (acid) metabolite (ASL 8123) and methanol.1 2 39 40 45 46 113 Acid metabolite has no appreciable β-blocking activity in humans.1 2 40

Elimination Route

Excreted principally in urine as the acid metabolite (73–88%); less than 2% excreted unchanged in urine.1 2 5 39 47 113 Small amounts (<5%) may be eliminated in feces.28 114

Half-life

Biphasic;1 2 39 99 113 distribution half-life of esmolol is about 2 minutes; 1 2 39 99 terminal elimination half-life is about 9 minutes (range: 5–23 minutes).1 2 39 40 99 114

Special Populations

In patients with renal impairment, elimination half-life of the metabolite may be increased up to 10-fold, but accumulation is not clinically important since ASL 8123 has only minimal β-blocking activity.2 43

About 24% (as metabolite) is removed by hemodialysis,114 and 21% by peritoneal dialysis;114 amount removed depends on several factors (e.g., dialysis flow-rate, dwell time).131 132 133 134

Stability

Storage

Parenteral

Injection

25°C (may be exposed to 15–30°C).1 a Do not freeze; protect from excessive heat.1 a

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Compatible

Dextrose 5% in Ringer’s injection

Dextrose 5% in Ringer’s injection, lactated

Dextrose 5% in sodium chloride 0.45 or 0.9%

Dextrose 5% in water

Dextrose 5% in water with potassium chloride 40 mEq/L

Ringer’s injection, lactated

Sodium chloride 0.45 or 0.9%

Drug Compatibility

Admix a compatible drug with esmolol hydrochloride only after diluting the concentrate for injection to a concentration of 10 mg/mL in a compatible IV infusion solution.1 2 Manufacturer states that additives should not be introduced into premixed solutions in ready-to-use bags.a

Admixture CompatibilityHID

Compatible

Aminophylline

Atracurium besylate

Heparin sodium

Incompatible

Diazepam2

Furosemide2 119

Procainamide HCl

Variable

Sodium bicarbonate1 2 3 HID

Y-Site CompatibilityHID

Compatible

Amikacin sulfate

Aminophylline

Amiodarone HCl

Ampicillin sodium

Atracurium besylate

Bivalirudin

Butorphanol tartrate

Calcium chloride

Cefazolin sodium

Ceftazidime

Chloramphenicol sodium succinate

Clindamycin phosphate

Co-trimoxazole

Dexmedetomidine HCl

Diltiazem HCl

Dopamine HCl

Doripenem

Enalaprilat

Erythromycin lactobionate

Famotidine

Fenoldopam mesylate

Fentanyl citrate

Gentamicin sulfate

Heparin sodium

Hetastarch in lactated electrolyte injection (Hextend)

Hydrocortisone sodium succinate

Hydroxyethyl starch 130/0.4 in sodium chloride 0.9%

Insulin, regular

Labetalol HCl

Linezolid

Magnesium sulfate

Methyldopate HCl

Metronidazole

Micafungin sodium

Midazolam HCl

Morphine sulfate

Nafcillin sodium

Nicardipine HCl

Nitroglycerin

Norepinephrine bitartrate

Pancuronium bromide

Penicillin G potassium

Phenytoin sodium

Polymyxin B sulfate

Potassium chloride

Potassium phosphates

Propofol

Ranitidine HCl

Remifentanil HCl

Sodium acetate

Sodium nitroprusside

Streptomycin sulfate

Tacrolimus

Tobramycin sulfate

Vancomycin HCl

Vecuronium bromide

Incompatible

Amphotericin B cholesteryl sulfate complex

Furosemide

Pantoprazole sodium

Warfarin sodium

Actions

  • Selectively blocks cardiac β1-adrenergic receptors with little effect on2-adrenergic receptors of bronchial and vascular smooth muscle.1 2 3 4 5 17 35 113 At high doses (e.g., >300 mcg/kg per minute), selectivity usually diminishes and competitive inhibition of β1- and β2-adrenergic receptors occurs.1 2 5 29 35 114

  • Does not exhibit appreciable intrinsic sympathomimetic2 5 9 17 18 113 or membrane-stabilizing activity2 5 17 113 at usual clinical doses.

  • Produces negative chronotropic and inotropic activity.2 17 18 19 20 22 23 24 26 36 113 123 Decreases resting1 2 17 18 19 20 22 23 24 26 27 36 113 123 and exercise-induced heart rate,1 2 22 23 27 113 reflex orthostatic tachycardia,1 2 17 18 19 myocardial contractility,2 18 rate of left ventricular pressure rise (dp/dt),2 18 20 36 right ventricular contractility,9 18 and cardiac index.1 2 22 23 36

  • Decreases SBP1 2 20 22 23 24 26 27 109 and DBP26 27 109 at rest1 2 20 22 23 24 26 27 and during exercise.1 2 22 23 May reduce BP by decreasing cardiac output, decreasing sympathetic outflow from the CNS, and/or suppressing renin release.30 31 32

  • Class II antiarrhythmic agent.33 Increases sinus cycle length, prolongs sinus node recovery time, and slows conduction in the AV node;1 2 3 5 29 34 apparently does not substantially affect sinoatrial conduction time, corrected sinus node recovery time, AV node refractoriness, retrograde AV nodal conduction time, or atrial, His-Purkinje, or ventricular conduction.2 5 29

Advice to Patients

  • Importance of informing clinicians of existing therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patient of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Esmolol Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For injection, concentrate, for IV infusion

250 mg/mL

Brevibloc

Baxter

Injection, for IV use

10 mg/mL

Brevibloc

Baxter

Injection, for IV use

20 mg/mL

Brevibloc Double Strength

Baxter

Esmolol Hydrochloride in Sodium Chloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for IV use

10 mg/mL (2.5 g) in 0.59% Sodium Chloride Injection

Brevibloc

Premixed (Intra Via)

Baxter

Injection, for IV use

20 mg/mL (2 g) in 0.41% Sodium Chloride Injection

BreviblocDouble Strength

Premixed (Intra Via)

Baxter

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 9, 2013. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Baxter. Brevibloc injection (esmolol hydrochloride) prescribing information. (dated 1998 Jun). In: Physicians’ desk reference. 54th ed. Montvale NJ: Medical Economics Company Inc; 2000:655-7.

2. Du Pont Critical Care. Brevibloc (esmolol HCL) the ultrashort-acting intravenous beta blocker: technical monograph and formulary information. Waukegan, IL; 1987 Feb.

3. Angaran DM, Schultz NJ, Tschida VH. Esmolol hydrochloride: an ultrashort-acting, β-adrenergic blocking agent. Clin Pharm. 1986; 5:288-303. [IDIS 213788] [PubMed 2871961]

4. Covinsky JO. Esmolol: a novel cardioselective, titratable, intravenous beta-blocker with ultrashort half-life. Drug Intell Clin Pharm. 1987; 21:316-21. [IDIS 228570] [PubMed 2882993]

5. Benfield P, Sorkin EM. Esmolol: a preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs. 1987; 33:392-412. [IDIS 236763] [PubMed 2885168]

6. Erhardt PW, Woo CM, Gorczynski RJ et al. Ultra-short-acting β-adrenergic receptor blocking agents. Part 1: (aryloxy)propanolamines containing esters in the nitrogen substituent. J Med Chem. 1982; 25:1402-7. [PubMed 6130153]

7. Erhardt PW, Woo CM, Anderson WG et al. Ultra-short-acting β-adrenergic receptor blocking agents. Part 2: (aryloxy)propanolamines containing esters on the aryl function. J Med Chem. 1982; 25:1408-12. [PubMed 6130154]

8. Sum CY, Yacobi A. Gas chromatographic-mass spectrometric assay for the ultra-short-acting β-blocker esmolol. J Pharm Sci. 1984; 73:1177-9. [IDIS 188872] [PubMed 6149299]

9. Lee YC, Baaske DM, Alam AS. High-performance liquid chromatographic method for the determination of esmolol hydrochloride. J Pharm Sci. 1984; 73:1660-1. [IDIS 193272] [PubMed 6520778]

10. Mimnaugh MN, Gearien JE. Adrenergic drugs. In: Foye WO, ed. Principles of medicinal chemistry. 2nd ed. Philadelphia: Lea & Febiger; 1981:377-93.

11. Machin PJ, Hurst DN, Bradshaw RN et al. β1-Selective adrenoceptor antagonists. Part 2: 4-ether-linked phenoxypropanolamines. J Med Chem. 1983; 26:1570-6. [IDIS 177952] [PubMed 6138435]

12. Woods PB, Robinson ML. An investigation of the comparative liposolubilities of β-adrenoceptor blocking agents. J Pharm Pharmacol. 1981; 33:172-3. [IDIS 134754] [PubMed 6116760]

13. Zaroslinski J, Borgman RJ, O’Donnell JP et al. Ultra-short acting beta-blockers: a proposal for the treatment of the critically ill patient. Life Sci. 1982; 31:899-907. [PubMed 6129559]

14. Schultz NJ, Angaran DM. Esmolol hydrochloride: an ultra-short acting / blocker. Clin Pharm. 1984; 3:447,50.

15. Keefe DL, Somberg JC. Esmolol: a novel ultra-short-acting beta-blocking agent. J Clin Pharmacol. 1986; 26(Suppl A):A1-2.

16. Sonnenblick EH. A symposium: esmolol—an ultra-short-acting intravenous beta blocker. Introduction. Am J Cardiol. 1985; 56(Suppl):1-2F. [IDIS 208206] [PubMed 4014012]

17. Gorczynski RJ, Shaffer JE, Lee RJ. Pharmacology of ASL-8052, a novel β-adrenergic receptor antagonist with an ultrashort duration of action. J Cardiovasc Pharmacol. 1983; 5:668-77. [PubMed 6193366]

18. Gorczynski RJ, Murthy VS, Hwang TF. β-blocking and hemodynamic effects of ASL-8052. J Cardiovasc Pharmacol. 1984; 6:1048-59.

19. Murthy VS, Hwang TF, Zagar ME et al. Cardiovascular pharmacology of ASL-8052, an ultra-short acting β blocker. Eur J Pharmacol. 1983; 94:43-51. [PubMed 6140172]

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