Brevibloc

— THERAPEUTIC CATEGORIES —
  • CHF and arrhythmias

Brevibloc Generic Name & Formulations

General Description

Esmolol HCl 10mg/mL, 20mg/mL; soln for IV inj; preservative-free.

Pharmacological Class

Cardioselective beta-blocker.

How Supplied

Inj (10mL ready-to-use vials)—25; Premixed inj (250mL ready-to-use IntraVia Bags)—1; Premixed Double Strength Inj (100mL ready-to-use IntraVia Bags)—1

Manufacturer

Generic Availability

YES

Mechanism of Action

Esmolol HCl injection is a beta1-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. It inhibits the beta1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta2 receptors located chiefly in the bronchial and vascular musculature.

Brevibloc Indications

Indications

Rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Noncompensatory sinus tachycardia where, in the physician’s judgment, the rapid heart rate requires specific intervention. For the short-term treatment of tachycardia and hypertension that occur during induction and tracheal intubation, during surgery, on emergence from anesthesia, and in the postoperative period, when in the physician’s judgment such specific intervention is considered indicated.

Brevibloc Dosage and Administration

Adult

Supraventricular tachycardia or noncompensatory sinus tachycardia (Step-wise dosing): Initial loading dose: 500mcg/kg infused over 1min followed by maintenance infusion of 50mcg/kg/min for the next 4mins; if needed, may continue maintenance infusion at 50mcg/kg/min or increase step-wise (eg, 100mcg/kg/min, 150mcg/kg/min, to max 200mcg/kg/min) with each step being maintained for 4mins. Effective maintenance dose (continuous or step-wise): 50–200mcg/kg/min (although, doses as low as 25mcg/kg/min have been adequate); infusions may be continued for up to 48hrs. Intraoperative and postoperative tachycardia and hypertension (Immediate control): 1mg/kg bolus dose over 30secs followed by 150mcg/kg/min infusion, if necessary; (Gradual control):  500mcg/kg bolus dose over 1min followed by 4-min maintenance infusion of 50mcg/kg/min. May adjust infusion rate as required up to max 200mcg/kg/min for tachycardia or max 300mcg/kg/min for hypertension. Once adequate control of HR and a stable clinical status is achieved, may transition to alternative antiarrhythmic drugs. Transition to alternative drug: reduce Brevibloc dose by ½ after 30mins following the first dose of the alternative drug; discontinue Brevibloc if satisfactory control is maintained for the first hour after administering the second dose of the alternative drug.

Children

Not established.

Brevibloc Contraindications

Contraindications

Severe sinus bradycardia. Heart block >1st degree. Sick sinus syndrome. Decompensated heart failure. Cardiogenic shock. Concomitant IV calcium channel antagonists (eg, verapamil) in close proximity. Pulmonary hypertension. 

Brevibloc Boxed Warnings

Not Applicable

Brevibloc Warnings/Precautions

Warnings/Precautions

Hemodynamically compromised. Increased risk for bradycardia (in those with 1st degree AV block, sinus node dysfunction, or conduction disorders). Discontinue and initiate supportive care at the 1st sign/symptom of impending cardiac failure. Vasoconstriction associated with hypothermia. Reactive airways disease: not recommended. Discontinue immediately if bronchospasm occurs. Increased risk for hypoglycemia esp. in diabetics or those who are fasting (eg, surgery, not eating regularly, or vomiting). Avoid infusions into small veins or through a butterfly catheter. Avoid extravasation. Prinzmetal’s angina. Pheochromocytoma. Hypovolemic. Peripheral circulatory disorders (eg, Raynaud’s disease or syndrome, peripheral occlusive vascular disease). Metabolic acidosis. Hyperthyroidism. Hyperkalemia. Monitor serum electrolytes during therapy. Avoid abrupt cessation. Monitor for myocardial ischemia, thyrotoxicosis when discontinuing treatment. Renal impairment. Elderly. Labor & delivery. Pregnancy. Nursing mothers: not recommended.

Brevibloc Pharmacokinetics

Distribution

Plasma protein bound: 55%.

Metabolism

Hydrolysis.

Elimination

Renal (73–88%). Half-life: ~9 minutes.

Total body clearance: ~20 L/hr.

Brevibloc Interactions

Interactions

Increased risk of cardiac failure with concomitant drugs that decrease peripheral resistance, myocardial filling or contractility, or electrical impulse propagation in the myocardium. May be potentiated by catecholamine-depleting drugs (eg, reserpine). Caution with digoxin, succinylcholine, verapamil. Concomitant dopamine, epinephrine, norepinephrine: not recommended. Increased risk for withdrawal rebound hypertension with clonidine, guanfacine, or moxonidine. Antagonized by sympathomimetic drugs.

Brevibloc Adverse Reactions

Adverse Reactions

Symptomatic hypotension (hyperhidrosis, dizziness), asymptomatic hypotension, infusion site reactions (inflammation, induration), nausea, somnolence; hypersensitivity reactions. 

Brevibloc Clinical Trials

See Literature

Brevibloc Note

Not Applicable

Brevibloc Patient Counseling

See Literature