esmolol (Brevibloc)
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Introduction
Tradename: Brevibloc.
Indications
- supraventricular tachyarrhythmias
- pre, intra & immediately post-operative hypertension & tachycardia
- acute myocardial infarction
- unstable angina
- dissecting aortic aneurysm[4]
- pheochromocytoma[4] *Use with caution in patients with systolic dysfunction.
Dosage
- 5 g in 500 mL (10 mg/mL)
- loading dose 500 ug/kg/min IV over 1 min
- IV @ 50-200 ug/kg/min
- 70 kg: 40 mL/hr = 100 ug/kg/min
Pharmacokinetics
- rapidly hydrolyzed in the blood
- plasma levels decline rapidly upon discontinuation
- elimination 1/2life is about 9 minutes
- clearance not altered in renal or hepatic insufficiency
elimination via plasma
1/2life = 9 minutes
Adverse effects
- common to less common (> 1%)
- uncommon (< 1%)
- pallor, flushing, bradycardia, chest pain, syncope, pulmonary edema, heart block, paresthesias, asthenia, depression, somnolence, anxiety, anorexia, lightheadedness, seizures, bronchospasm, wheezing, dyspnea, nasal congestion, dyspepsia, constipation, dry mouth, abdominal discomfort, edema, erythema, skin discoloration, thrombophlebitis, urinary retention, speech disorder, abnormal vision, rigors, fever
- drug adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of beta-1 adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- morphine results in a 50% increase in esmolol concentration
- esmolol may prolong 1/2life of succinylcholine
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- short-acting, selective beta-1 antagonist
- beta-1 selectivity is diminished at high doses (> 300 ug/kg/min)
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 4.2 Deprecated Reference