Dosing and uses of Brevibloc (esmolol)
Adult dosage forms and strengths
infusion bags
- 2g/100mL
- 2.5g/250mL
injectable solution
- 10mg/mL
- 20mg/mL
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
Pediatric dosage forms and strengths
infusion bags
- 2g/100mL
- 2.5g/250mL
injectable solution
- 10mg/mL
- 20mg/mL
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)
Geriatric dosage forms and strengths
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
Brevibloc (esmolol) adverse (side) 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
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
Pregnancy and 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.
Pharmacology of Brevibloc (esmolol)
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
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
