In the absence of loading doses, continuous infusion of a single concentration of esmolol reaches a pharmacokinetic and pharmacodynamic steady-state in about 30 minutes. Effective maintenance dose for continuous and stepwise dosing is 50 to 200 mcg/kg/min, although doses as low as 25 mcg/kg/min have been adequate. Doses greater than 200 mcg/kg/min provide little additional lowering of heart rate, and the rate of adverse reactions increases. Maintenance infusions may be continued for up to 48 hours. See Precautions/Monitor.
Intraoperative and postoperative tachycardia and/or hypertension:
Immediate control:
1 mg/kg over 30 seconds. Follow with an infusion of 150 mcg/kg/min (0.15 mg/kg/min) if necessary. Adjust as required to maintain desired HR and/or BP.
Gradual control:
Use procedure listed for SVT.
Immediate and gradual control:
Higher doses (250 to 300 mcg/kg/min [0.25 to 0.3 mg/kg/min]) may be required to control hypertension. Maintenance infusion doses greater than 200 mcg/kg/min are not recommended for the treatment of tachycardia. They provide little additional lowering of heart rate, and the rate of adverse reactions increases.
Transition to alternative drugs:
After control of HR and BP is achieved and clinical status is stable,
1. Administer the first dose of the alternative drug. In 30 minutes, reduce the esmolol infusion rate by one half (50%).
2. After administration of the second dose of the alternative drug, monitor patient response carefully. If control is satisfactory and is maintained for 1 hour, discontinue the esmolol infusion.
Pediatric dose
See Maternal/Child.
Antiarrhythmic (unlabeled):
Pediatric patients 1 to 12 years of age:
A loading dose of 100 to 500 mcg/kg (0.1 to 0.5 mg/kg) administered over 1 minute. Follow with a maintenance infusion of 25 to 100 mcg/kg/min (0.025 to 0.1 mg/kg/min). Titrate doses upward to response by 50 to 100 mcg/kg/min (0.05 to 0.1 mg/kg/min) at 5- to 10-minute intervals as needed. Dose requirements may be higher than in adults. Doses as high as 1,000 mcg/kg/min have been administered to pediatric patients 1 to 12 years of age.
Antihypertensive (postoperative [unlabeled]):
Pediatric patients 1 to 12 years of age:
A loading dose of 500 mcg/kg (0.5 mg/kg) administered over 1 minute. Follow with a maintenance infusion of 50 to 250 mcg/kg/min (0.05 to 0.25 mg/kg/min). Titrate doses upward 50 to 100 mcg/kg/min (0.05 to 0.1 mg/kg/min) as needed. Titrate to individual desired response. Dose requirements may be higher than in adults. Doses as high as 1,000 mcg/kg/min have been administered to pediatric patients 1 to 12 years of age.
Dose adjustments
Reduced dose may be required in impaired renal function. No dose adjustment required if the maintenance infusion does not exceed 150 mcg/kg/min for more than 4 hours; no data available for higher doses or longer duration. ■ No dose adjustment indicated in impaired hepatic function. ■ Reduction required with transfer to alternate agent; see Monitor. ■ See Drug/Lab Interactions.
Dilution
Available premixed as 10 mg/mL in 100 mL NS or as 20 mg/mL in 100 mL NS (double strength). Single-dose vials are available as 100 mg/10 mL and may be given by IV injection without further dilution or may be further diluted in D5W, D5R, D5LR, D5NS, D5/1/2NS, NS, LR, 1/2NS, or D5W with KCl 40 mEq/L. Premixed solutions have a delivery port and a medication port (for withdrawing the initial bolus only). Ready-to-use vials may be used to administer initial and subsequent boluses.
Storage:
Store vials and premix at CRT; protect from freezing and avoid excessive heat. Diluted solution stable at room temperature for 24 hours. If a bolus has been removed from the premixed bag, the bag should be used within 24 hours.
Compatibility (underline indicates conflicting compatibility information)
Consider any drug NOT listed as compatible to be INCOMPATIBLE until consulting a pharmacist; specific conditions may apply.
Manufacturer lists as incompatible with sodium bicarbonate and furosemide and states, “Do not add any additional medications to the bag” (premixed injection).
One source suggests the following compatibilities:
Additive:
Not recommended by manufacturer. Aminophylline, atracurium (Tracrium), heparin, sodium bicarbonate.
Y-site:
Amikacin, aminophylline, amiodarone (Nexterone), ampicillin, atracurium (Tracrium), bivalirudin (Angiomax), butorphanol (Stadol), calcium chloride, cefazolin (Ancef), ceftazidime (Fortaz), chloramphenicol (Chloromycetin), cisatracurium (Nimbex), clindamycin (Cleocin), dexmedetomidine (Precedex), diltiazem (Cardizem), dopamine, doripenem (Doribax), enalaprilat (Vasotec IV), erythromycin (Erythrocin), famotidine (Pepcid IV), fenoldopam (Corlopam), fentanyl, gentamicin, heparin, hetastarch in electrolytes (Hextend), hydrocortisone sodium succinate (Solu-Cortef), 6% hydroxyethyl starch (Voluven), insulin (regular), labetalol, linezolid (Zyvox), magnesium sulfate, methyldopate, metronidazole (Flagyl IV), micafungin (Mycamine), midazolam (Versed), morphine, nafcillin (Nallpen), nicardipine (Cardene IV), nitroglycerin IV, nitroprusside sodium, norepinephrine (Levophed), pancuronium, penicillin G potassium, phenytoin (Dilantin), potassium chloride (KCl), potassium phosphates, propofol (Diprivan), ranitidine (Zantac), remifentanil (Ultiva), sodium acetate, streptomycin, sulfamethoxazole/trimethoprim, tacrolimus (Prograf), tobramycin, vancomycin, vecuronium.
Rate of administration
IV injection:
See Usual Dose.
Infusion:
Titrate infusion according to procedure outlined in Usual Dose.
Actions
A short-acting, B1-selective adrenergic blocking agent with antiarrhythmic effects. Decreases HR and BP in a dose-related titratable manner. Hemodynamically similar to propranolol, but vascular resistance is not increased. Onset of action occurs within 1 to 2 minutes. Half-life is approximately 9 minutes, and the effects last about 20 to 30 minutes. Metabolized via esterases in RBCs and excreted in urine.
Indications and uses
Management of supraventricular tachycardia (atrial fibrillation or atrial flutter) in situations requiring short-term control of ventricular rate with a short-acting agent (perioperative, postoperative, or other emergent circumstances). ■ Management of noncompensatory tachycardia when HR requires specific intervention. ■ Management of intraoperative and postoperative tachycardia and/or hypertension.
Limitation of use:
Intended only for short-term use.
Contraindications
Cardiogenic shock. ■ Decompensated heart failure. ■ Heart block greater than first degree. ■ Hypersensitivity reactions, including anaphylaxis, to esmolol or any of its inactive ingredients (cross-sensitivity between beta-blockers is possible). ■ IV administration of cardiodepressant calcium-channel antagonists (e.g., verapamil) and esmolol in close proximity (i.e., while the cardiac effects of the other drug are still present). ■ Pulmonary hypertension. ■ Severe sinus bradycardia. ■ Sick sinus syndrome.
Precautions
For IV use only. ■ May cause hypotension at any dose but is dose related; risk is increased in patients with hemodynamic compromise, in patients receiving interacting medications, and with doses above 200 mcg/kg/min. Severe reactions may include loss of consciousness, cardiac arrest, and death. ■ Use caution in patients with first-degree AV block, sinus node dysfunction, or conduction disorders. May be at increased risk for bradycardia. Sinus pause, heart block, severe bradycardia, and cardiac arrest have occurred. ■ May further depress cardiac contractility and precipitate heart failure and cardiogenic shock. ■ Use caution in patients whose BP is primarily driven by vasoconstriction associated with hypothermia (e.g., intraoperative and postoperative tachycardia and hypertension). ■ Use with extreme caution in patients with reactive airway disease (e.g., asthma), diabetes mellitus and/or hypoglycemia, Prinzmetal’s angina, pheochromocytoma, hypovolemia, peripheral circulatory disorders (Raynaud’s disease, peripheral occlusive vascular disease), coronary artery disease, impaired renal function, metabolic acidosis, and hyperthyroidism. ■ In general, patients with reactive airway disease (e.g., asthma) should not receive beta-blockers. Titrate to the lowest possible effective dose. ■ In patients with hypoglycemia or diabetes who are receiving insulin or hypoglycemic agents, beta-blockers may mask tachycardia of hypoglycemia, but other manifestations of hypoglycemia such as dizziness and sweating may still be observed. ■ May exacerbate angina attacks in patients with Prinzmetal’s angina; do not use nonselective beta-blockers (e.g., propranolol). ■ A paradoxical increase in BP may occur if beta-blockers are administered to patients with pheochromocytoma. If use is necessary, administer an alpha-blocker (e.g., phentolamine) before the beta-blocker. ■ Can worsen reflex tachycardia and increase the risk of hypotension in hypovolemic patients. ■ May increase serum potassium levels, causing hyperkalemia. Risk is increased in patients with renal impairment and is potentially life threatening in hemodialysis patients. ■ Use caution in patients with metabolic acidosis; hyperkalemic renal tubular acidosis has been reported. ■ Beta-adrenergic blockade may mask the clinical signs of hyperthyroidism (e.g., tachycardia). Abrupt withdrawal may precipitate thyroid storm. ■ Patients at risk for hypersensitivity reactions may be more reactive to allergen exposure when receiving beta-blockers and may be unresponsive to the usual doses of epinephrine used to treat anaphylactic or anaphylactoid reactions; see Drug/Lab Interactions. ■ Infusion site reactions, including irritation, inflammation, and severe reactions (e.g., thrombophlebitis, necrosis, and blistering), have occurred; avoid infusion into small veins or through a butterfly catheter. ■ Although it has not been a problem with esmolol, it is recommended that the dose of beta-adrenergic blockers be reduced gradually to avoid rebound angina, MI, or ventricular arrhythmias. Use caution, especially in patients with coronary artery disease. ■ Intended for short-term use only. Transfer to an alternative antiarrhythmic agent (e.g., digoxin [Lanoxin], verapamil) is required after stable clinical status and HR control are obtained; see Usual Dose. ■ See Drug/Lab Interactions, Monitor, and Antidote.
Monitor:
Continuous observation of the patient and ECG and BP monitoring are mandatory during administration. Hypotension should reverse within 30 minutes after decreasing the infusion rate or discontinuing the drug. ■ Avoid infusion into small veins or through a butterfly catheter. Well tolerated if administered through a central vein. Monitor for infusion site reaction and prevent extravasation. Restart at an alternate infusion site. ■ Titrate BP slowly in patients whose BP is primarily driven by vasoconstriction associated with hypothermia (e.g., intraoperative and postoperative tachycardia and hypertension). ■ May mask symptoms of hypoglycemia; monitor blood glucose in patients with diabetes. ■ Monitor electrolyes as indicated. Monitor patients with increased risk factors very closely; see Precautions. ■ See Drug/Lab Interactions and Contraindications.
Maternal/child:
Category C: safety for use in pregnancy not established. Use only when clearly indicated. ■ Discontinue breast-feeding. ■ Safety and effectiveness for use in pediatric patients not established.
Elderly:
Numbers in clinical studies are insufficient to determine if the elderly respond differently from younger subjects. Consider age-related organ impairment (e.g., bone marrow reserve, renal, hepatic); monitor and reduce dose if indicated.
Drug/lab interactions
The effects of esmolol on BP, contractility, and impulse propagation can be increased with concomitant use of other drugs that can lower BP, reduce myocardial contractility, or interfere with sinus node function or electrical impulse propagation in the myocardium. May result in severe hypotension, cardiac failure, severe bradycardia, sinus pause, sinoatrial block, atrioventricular block, and/or cardiac arrest. ■ Sympathomimetic drugs having beta-adrenergic agonist activity (e.g., epinephrine [Adrenalin], norepinephrine [Levophed]) will counteract the effects of esmolol. ■ Use with calcium channel blockers (e.g., verapamil) may potentiate both drugs and result in severe depression of myocardium and AV conduction, severe hypotension, and fatal cardiac arrest. ■ Increases digoxin blood levels, synergistic with digoxin; both drugs slow AV conduction. Concomitant use increases the risk of bradycardia. ■ Esmolol should not be used in patients receiving vasoconstrictive or inotropic drugs (e.g., norepinephrine [Levophed], digoxin) because of the potential for reduced cardiac contractility when the systemic vascular resistance is high. ■ Concomitant use with certain antihypertensive agents (e.g., clonidine [Catapres], guanfacine [Intuniv]) may precipitate increased withdrawal effects (withdrawal rebound hypertension). If antihypertensive therapy is to be interrupted or discontinued, discontinue the beta-blocker first and then gradually discontinue the antihypertensive agent. ■ Concomitant use with catecholamine-depleting drugs (e.g., reserpine) may produce additive effects. Monitor for hypotension and bradycardia. ■ May prolong neuromuscular blockade produced by succinylcholine and moderately prolong neuromuscular blockade producd by mivacurium (Mivacron). ■ May mask S/S of developing hypoglycemia in patients on insulin or oral antidiabetic agents. ■ Concurrent use with xanthines (e.g., aminophylline, theophyllines) may result in mutual inhibition of therapeutic effects. ■ Patients taking beta-blockers who are exposed to a potential allergen may be unresponsive to the usual dose of epinephrine used to treat a hypersensitivity reaction.
Side effects
Symptomatic hypotension (dizziness, excessive sweating) and asymptomatic hypotension are most common. Inflammation or induration of the infusion site, nausea, and somnolence are also fairly common. Abdominal discomfort, abnormal thinking, agitation, anxiety, confusional state, constipation, convulsions (with one death), depression, dry mouth, dyspepsia, flushing, headache, light-headedness, pallor, paresthesia, peripheral ischemia, speech disorders, syncope, urinary retention, and vomiting have occurred.
Overdose:
Cardiac effects (e.g., atrioventricular block [first-, second-, third-degree], bradycardia, cardiac failure [including cardiogenic shock], decreased cardiac contractility, hypotension, intraventricular conduction delays, junctional rhythms, cardiac arrest/asystole, and pulseless electrical activity); CNS effects (e.g., fatigue, lethargy, respiratory depression, seizures, sleep and mood disturbances, and coma). In addition, bronchospasm, hyperkalemia, hypoglycemia (especially in children), mesenteric ischemia, and peripheral cyanosis may occur.
Post-marketing:
Angioedema, cardiac arrest, coronary arteriospasm, psoriasis, urticaria.
Antidote
Notify the physician of all side effects. Decrease rate or discontinue drug if hypotension occurs. Hypotension should reverse within 30 minutes. Trendelenburg position may be appropriate. May require treatment with IV fluids or vasopressors (e.g., dopamine, norepinephrine [Levophed]), but protracted severe hypotension may result. Unresponsive hypotension and bradycardia may be reversed by glucagon 5 to 10 mg over 30 seconds followed by a continuous infusion of 5 mg/hr. Reduce rate as condition improves. Decrease rate of or discontinue esmolol if severe bradycardia develops. Treat with an anticholinergic drug (e.g., atropine) or cardiac pacing. Discontinue esmolol at the first S/S of cardiac failure and start supportive treatment (e.g., digoxin and diuretics). In shock resulting from inadequate cardiac contractility, consider IV dobutamine or dopamine. Glucagon may be useful. Discontinue the infusion if bronchospasm occurs. Administer a beta2-stimulating agent (e.g., epinephrine, albuterol) and/or a theophylline derivative and monitor ventricular rate. Treat other side effects symptomatically and resuscitate as necessary.
Esomeprazole sodium
(es-oh-MEP-rah-zohl SO-dee-um)
Nexium IV
Proton pump inhibitor (gastric acid inhibitor) (PPI)
pH 9 to 11
Usual dose
GERD with erosive esophagitis:
Given as an alternative to oral therapy. Resume oral therapy as soon as practical. Safety and efficacy of IV use for more than 10 days not established. Dose and serum levels similar by IV or oral route.
Adults:
20 or 40 mg as an IV injection or infusion once daily for up to 10 days.
Risk reduction for rebleeding of gastric or duodenal ulcers following therapeutic endoscopy in adults:
80 mg as an IV infusion over 30 minutes followed by a continuous infusion of 8 mg/hr for 71.5 hours (a total treatment duration of 72 hours). Therapy is for management of the acute initial bleeding of gastric or duodenal ulcers and does not constitute full treatment. Follow with oral acid-suppressive therapy.
Pediatric dose
GERD with erosive esophagitis:
Administered as an infusion over 10 to 30 minutes. See comments under Usual Dose.
1 to 17 years of age:
Weight less than 55 kg: 10 mg. Weight 55 kg or more: 20 mg.
1 month to less than 1 year of age:
0.5 mg/kg.
Dose adjustments
GERD with erosive esophagitis:
No dose adjustment is required based on age or gender, in the elderly, in patients with renal insufficiency, or in patients with mild to moderate liver impairment (Child-Pugh Classes A and B). ■ Do not exceed a dose of 20 mg in patients with severe liver impairment (Child-Pugh Class C [10 or over]).
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