Esmolol Hydrochloride

Esmolol Hydrochloride is a beta adrenergic blocker indicated for the short-term
treatment of:

• Control of ventricular rate in supraventricular tachycardia including atrial fibrillation and atrial flutter and control of heart rate in noncompensatory sinus tachycardia.
• Control of perioperative tachycardia and hypertension.

Esmolol Hydrochloride is a beta-1 selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. Esmolol Hydrochloride inhibits the beta 1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta 2 receptors located chiefly in the bronchial and vascular musculature.

Administer intravenously. Titrate using ventricular rate or blood pressure at ≥4 minute intervals. Supraventricular tachycardia (SVT) or noncompensatory sinus tachycardia-

• Optional loading dose: 500 mcg per kg infused over one minute
• Then 50 mcg per kg per minute for the next 4 minutes
• Adjust dose as needed to a maximum of 200 mcg per kg per minute
• Additional loading doses may be administered

Perioperative tachycardia and hypertension-

• Loading dose: 500 mcg per kg over 1 minute for gradual control (1 mg per kg over 30 seconds for immediate control).
• Than 50 mcg per kg per minute for gradual control (150 mcg per kg per minute for immediate control) adjusted to a maximum of 200 (tachycardia) or 300 (hypertension) mcg per kg per minute.

• Digitalis glycosides: Risk of bradycardia
• Anticholinesterases: Prolongs neuromuscular blockade
• Antihypertensive agents: Risk of rebound hypertension
• Sympathomimetic drugs: Dose adjustment needed
• Vasoconstrictive and positive inotropic effect substances: Avoid concomitant use

• Severe sinus bradycardia
• Heart block greater than first degree
• Sick sinus syndrome
• Decompensated heart failure
• Cardiogenic shock
• Coadministration of IV cardiodepressant calcium-channel antagonists (e.g. verapamil) in close proximity to Esmolol hydrochloride
• Pulmonary hypertension
• Known hypersensitivity to esmolol

Most common adverse reactions (incidence> 10%) are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension.

Pregnancy Category C. Esmolol hydrochloride has been shown to produce increased fetal resorptions with minimal maternal toxicity in rabbits when given in doses approximately 8 times the maximum human maintenance dose (300 mcg/kg/min). There are no adequate and well-controlled studies in pregnant women. Esmolol Hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Esmolol Hydrochloride, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

• Risk of hypotension, bradycardia, and cardiac failure: Reduce or discontinue use
• Risk of exacerbating reactive airway disease
• Diabetes mellitus: Increases the effect of hypoglycemic agents and masks hypoglycemic tachycardia
• Risk of unopposed alpha-agonism and severe hypertension in untreated pheochromocytoma
• Risk of myocardial ischemia when abruptly discontinued in patients with coronary artery disease

Pediatric Use: The safety and effectiveness of Esmolol Hydrochloride in pediatric patients have not been established.

Geriatric Use: Clinical studies of Esmolol Hydrochloride did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects.

Hepatic Impairment: No special precautions are necessary in patients with hepatic impairment because Esmolol Hydrochloride is metabolized by red-blood cell esterases.

Renal Impairment: No dosage adjustment is required for esmolol in patients with renal impairment receiving a maintenance infusion of esmolol 150 mcg/kg for 4 hours.

Anti adrenergic agent (Beta blockers)

Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.