Esmolol information from DrugsUpdate  

Pharmacodynamics

Pharmacokinetics

Esmolol HCl is a cardioselective agent, which competitively blocks β1 adrenergic receptor. At higher doses, it inhibits β2 receptors located chiefly in the bronchial and vascular musculature.

Onset
2-10 minutes (IV).

Duration
10-30 minutes (IV).

Distribution
Protein-binding: 55%.

Metabolism
RBC: Metabolised by esterases.

Excretion
Via urine (as de-esterified metabolite); 9 minutes (elimination half-life).

Esmolol Indications / Esmolol Uses

Information Not Available

Esmolol Adverse Reactions / Esmolol Side Effects

Hypotension, bradycardia, heart failure, local irritation, diaphoresis, peripheral ischaemia, dizziness, somnolence, confusion, fatigue, paraesthesia, peripheral neuropathy, headache, weakness, irritability, dyspnoea, nausea, vomiting, blurred vision, urinary retention, fever, rigor, muscular pain.

Potentially Fatal: Profound bradycardia, AV block, cardiogenic shock, asystole, bronchospasm.

Precautions

Information Not Available

Special Precautions

Hypotension, tachycardia, PVD, uncompensated heart failure, haemodynamically compromised patients, depressed cardiac contractility, DM, bronchospastic disease, renal impairment. Lactation. Children.

Other Drug Interactions

Esmolol HCl may increase blood digoxin levels; it may prolong neuromuscular blockade of succinylcholine. Morphine and warfarin may increase steady-state blood esmolol levels. Bradycardia may occur when used concurrently with MAOIs. Esmolol may reduce elimination of theophylline.

Potentially Fatal: Increased risk of bradycardia, AV block, hypotension and CHF with IV calcium channel blockers. Increased hypertensive risk with inotropes, adrenaline or noradrenaline. Hypotension or marked bradycardia with catecholamine depletors.

Other Interactions

Information Not Available

Dosage

Intravenous
Rapid temporary control of ventricular rate in supraventricular arrhythmias
Adult: As HCl: Loading dose: 500 mcg/kg over 1 minute followed by a maintenance infusion of 50 mcg/kg/minute for 4 minutes. If response is satisfactory, continue maintenance infusion. If satisfactory response is not achieved within 5 minutes, a 2nd loading dose of 500 mcg/kg may be given over 1 minute followed by maintenance infusion at 100 mcg/kg/minute for 4 minutes. May repeat procedure once or twice more if needed; maintenance infusion can be further increased each time by 50 mcg/kg/minute to a max of 200 mcg/kg/min. Once response is satisfactory, maintain infusion for up to 48 hr, if necessary.

Intravenous
Perioperative hypertension and/or tachycardia
Adult: As HCl: During anaesthesia: loading dose of 80 mg over 15-30 sec, followed by an infusion of 150 mcg/kg/minute, may increase to 300 mcg/kg/minute if necessary. After anaesthesia: 500 mcg/kg/minute infused for 4 minutes followed by another infusion of 300 mcg/kg/minute as needed. Postoperatively: Loading dose: 500 mcg/kg; Maintenance: 50 mcg/kg/minute for 4 minutes. If response is satisfactory, continue maintenance infusion. If response is unsatisfactory w/in the 1st 5 mins, give 2nd loading dose of 500 mcg/kg, then infuse at 100 mcg/kg/min for 4 mins. May repeat procedure another 1-2 times, if needed. Maintenance infusion can be increased by 50 mcg/kg/min each time up to a max of 300 mcg/kg/min. Once response is satisfactory, maintain infusion for up to 48 hr if needed.

Food(before/after)

Information Not Available

Esmolol and Pregnancy

Contraindicated in pregnancy

Esmolol and Lactation

Caution when used during lactation

Esmolol and Children

Information Not Available

Esmolol and Geriatic

Information Not Available

Esmolol and Other Contraindications

Sinus bradycardia, 2nd and 3rd ° AV block, cardiogenic shock, CHF, concomitant IV calcium channel blockers. Pregnancy (2nd and 3rd trimester).

Storage

Intravenous
Store at 25°C.

Lab interference

Intravenous
Store at 25°C.