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esmolol (Brevibloc)
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:
1) 5 g in 500 mL (10 mg/mL)
2) loading dose 500 ug/kg/min IV over 1 min
3) IV @ 50-200 ug/kg/min
4) 70 kg: 40 mL/hr = 100 ug/kg/min
Injection: 250 mg/mL (10 mL).
Pharmacokinetics:
1) rapidly hydrolyzed in the blood
2) plasma levels decline rapidly upon discontinuation
3) elimination 1/2life is about 9 minutes
4) clearance not altered in renal or hepatic insufficiency
Adverse effects:
1) common to less common (> 1%)
- hypotension with faster infusion rates
- diaphoresis which resolves with stopping infusion
- nausea/vomiting
- diarrhea, cramps*
- peripheral ischemia
- dizziness
- confusion
- headache
- agitation
- fatigue
- infusion site reactions
- phlebitis
- vesication
2) 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 interactions:
1) morphine results in a 50% increase in esmolol concentration
2) esmolol may prolong 1/2life of succinylcholine
Mechanism of action:
1) short-acting, selective beta-1 antagonist
2) beta-1 selectivity is diminished at high doses (> 300 ug/kg/min)
Interactions
drug interactions
drug adverse effects (more general classes)
General
beta-1 adrenergic receptor antagonist (beta-1 blocker)
Properties
MISC-INFO: elimination route PLASMA
1/2life 9 MINUTES
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
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
- Deprecated Reference