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esmolol (Rx)Brand and Other Names:Brevibloc

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

infusion bags

  • 2g/100mL
  • 2.5g/250mL

injectable solution

  • 10mg/mL
  • 20mg/mL
more...

Intraoperative Tachycardia/Hypertension

Immediate control

  • Initial bolus: 80 mg (~1 mg/kg) IVP over 30 sec, THEN
  • 0.15-0.3 mg/kg/min IV infusion PRN 

Postoperative/gradual control

  • Load 0.5 mg/kg IV over 1 min, THEN
  • 0.05 mg/kg/min IV for 4 min
  • If inadequate response in 5 min
  • 2nd loading dose of 0.5 mg/kg/min for 1 min, THEN
  • 0.1 mg/kg/min IV 

Supraventricular Tachycardia

Load: 0.5 mg/kg IV over 1 min, THEN

Maintenance: Start 0.05 mg/kg/min IV for 4 min, may increase by 0.05 mg/kg up to 0.2 mg/kg/min 

If HR/BP not controlled after 5 min, repeat bolus (ie, 500 mcg/kg/min for 1 min), then initiate infusion of 0.1 mg/kg/min IV

May administer a 3rd bolus if needed, then a maintenance infusion of 0.15 mg/kg/min IV

Higher maintenance doses may be required, up to 0.25-0.3 mg/kg/min

Hypertensive Emergency

Load 0.25-0.5 mg/kg IVP over 1 min, THEN 

0.05-0.1 mg/kg/min IV for 4 min

May repeat loading dose or increase infusion up to 0.3 mg/kg/min if necessary

Renal Impairment

Not necessary to supplement dose; not dialyzable

Additional Information

Less effective than thiazide diuretics in black and geriatric patients

Shown to decrease mortality in hypertension and post-myocardial infarction

Other Indications & Uses

Paroxysmal Atrial Tachycardia, PSVT, ST

Off-label: Acute MI, angina, NSTEMI

Dosage Forms & Strengths

infusion bags

  • 2g/100mL
  • 2.5g/250mL

injectable solution

  • 10mg/mL
  • 20mg/mL
more...

Supraventricular Tachycardia (Off-label)

Load with 500-600 mcg/kg IV over 2 min, THEN 200 mcg/kg/min IV infusion (range 50-250 mcg/kg/min) 

Postoperative Hypertension (Off-label)

Load with 500-600 mcg/kg IV over 2 min, THEN 200 mcg/kg/min IV infusion (range 50-250 mcg/kg/min) 

Hypertension

2.5 mg PO qDay; increase dose gradually

Supraventricular tachycardia

Load: 0.5 mg/kg/IV over 1 min, THEN

Maintenance: Start 0.05 mg/kg/min IV for 4 min, may increase by 0.05 mg/kg up to 0.2 mg/kg/min 

If HR/BP not controlled after 5 min, repeat bolus (ie, 0.5 mg/kg/min for 1 min), then initiate infusion of 0.1 mg/kg/min IV

May administer a 3rd bolus if needed, then a maintenance infusion of 0.15 mg/kg/min IV

Higher maintenance doses may be required, up to 0.25-0.3 mg/kg/min

Hypertensive emergency

Load 0.25-0.5 mg/kg IVP over 1 min, THEN

0.05-0.1 mg/kg/min IV for 4 min

May repeat loading dose or increase infusion up to 0.3 mg/kg/min if necessary

Intraoperative tachycardia/hypertension

Immediate control

- Initial bolus: 80 mg (~1 mg/kg) IVP over 30 sec, THEN

- 0.15-0.3 mg/kg/min IV infusion PRN

Postoperative/gradual control

- Load 0.5 mg/kg over 1 min, THEN

- 0.05 mg/kg/min IV for 4 min

- If inadequate response in 5 min

- 2nd loading dose of 0.5 mg/kg/min for 1 min, THEN

- 0.1 mg/kg/min

Next

Interactions

Interaction Checker

esmolol and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Hypotension, asymptomatic (25-38%)

            Hypotension, symptomatic (12%)

            1-10%

            Injection site pain (8%)

            Nausea (7%)

            Dizziness (3%)

            Somnolence (3%)

            Agitation (2%)

            Confusion(2%)

            Headache (2%)

            Fatigue (1%)

            Vomiting (1%)

            <1%

            Bradycardia

            Chest pain

            Anxiety

            Anorexia

            Depression

            Abdominal discomfort

            Constipation

            Dry mouth

            Dyspepsia

            Taste perversion

            Bronchospasm

            Dyspnea

            Nasal congestion

            Wheezing

            Frequency Not Defined

            Decreased exercise tolerance

            Raynaud's phenomenon

            May increase triglyceride levels and insulin resistance, and decrease HDL levels

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            Warnings

            Contraindications

            Hypersensitivity

            Sinus bradycardia, 2°/3° heart block, cardiogenic shock, overt cardiac failure

            Asthma/COPD

            Sick sinus syndrome without permanent pacemaker

            Cautions

            Anesthesia/surgery (myocardial depression), bronchospastic disease, cerebrovascular insufficiency, CHF, DM, hyperthyroidism/thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease, myasthenic conditions

            Sudden discontinuation can exacerbate angina and lead to myocardial infarction

            Increased risk of stroke after surgery

            Use in pheochromocytoma

            Avoid abrupt withdrawal

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            Pregnancy & Lactation

            Pregnancy Category: C; D in 2nd and 3rd trimesters (expert analysis)

            Lactation: excretion in milk unknown; use with caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Class II antiarrhythmic; selective beta1-blocker with little or no effect on beta2 receptors except at high doses. It does not have intrinsic sympathomimetic activity

            Pharmacokinetics

            Onset of action: 2-10 min (IV)

            Duration: 10-30 min

            Protein Bound: 55%

            Vd: 3.4 L/kg

            Metabolism: Extensively metabolized by esterase in cytosol of red blood cells

            Metabolites: Major acid metabolite (ASL-8123), methanol (inactive)

            Excretion: Urine (73-88%)

            Half-Life

            • Parent drug (esmolol): 9 min
            • Acid metabolite: 3.7 hr
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            Administration

            IV Compatibilities

            Solution: compatible with common solvents

            Additive: aminophylline, atracurium, bretylium, heparin

            Y-site: (partial list): aminophylline, amiodarone, ampicillin, butorphanol, calcium chloride, cefazolin, cimetidine, clindamycin, diltiazem, dopamine, enalaprilat, erythromycin, famotidine, fentanyl, gentamicin, heparin, hydrocortisone, labetalol, linezolid, magnesium sulfate, metronidazole, midazolam, morphine, nitroglycerin, norepinephrine, KCl, ranitidine, sodium nitroprusside, trimethoprim/sulfamethoxazole, vancomycin

            IV Incompatibilities

            Solution: NaHCO3 (5%)

            Additive: Procainamide

            Y-site: Amphocetrin B cholesteryl sulfate, furosemide, lansoprazole, pantoprazole, warfarin

            IV Preparation

            Solution: 5 g in 500 mL or 2.5 g in 250 mL NS (10 mg/mL)

            IV Administration

            Do NOT infuse into small veins or through butterfly catheter

            Infuse at concentration 10 mg/mL, usually with infusion control device

            If local reaction develops, change infusion site

            Do not stop abruptly; possibility of withdrawal effects

            Intended for short-term use, no longer than 48 hr

            Watch for irritation & infiltration

            • Extravasation may cause tissue damage or necrosis

            Storage

            Store at room temp; protect from elevated temp

            Freezing does not affect product adversely

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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