Comparative Pharmacology
Head-to-head clinical analysis: COREG CR versus LABETALOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COREG CR versus LABETALOL.
COREG CR vs Labetalol
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nonselective beta-1, beta-2, and alpha-1 adrenergic receptor antagonist; no intrinsic sympathomimetic activity; reduces myocardial oxygen demand, decreases peripheral vascular resistance, and suppresses renin-angiotensin-aldosterone system.
Labetalol is a racemic mixture of four stereoisomers, each with distinct activity. It is a non-selective beta-adrenergic antagonist (blocking beta1 and beta2 receptors) and a selective alpha1-adrenergic antagonist. The alpha1 blockade causes vasodilation and reduces peripheral vascular resistance, while beta blockade reduces heart rate and myocardial contractility, leading to decreased blood pressure without significant reflex tachycardia.
Initial dose 20 mg orally once daily for patients with heart failure; may increase at 2-week intervals to a target dose of 80 mg once daily.
Oral: 200-1200 mg/day in 2 divided doses; initial 100 mg twice daily. IV: 20 mg bolus over 2 minutes, may repeat 40 mg at 10-minute intervals. Max cumulative dose: 300 mg.
None Documented
None Documented
Clinical Note
moderateLabetalol + Digitoxin
"Labetalol may increase the bradycardic activities of Digitoxin."
Clinical Note
moderateLabetalol + Deslanoside
"Labetalol may increase the bradycardic activities of Deslanoside."
Clinical Note
moderateLabetalol + Acetyldigitoxin
"Labetalol may increase the bradycardic activities of Acetyldigitoxin."
Clinical Note
moderateLabetalol + Ouabain
"Labetalol may increase the bradycardic activities of Ouabain."
Terminal elimination half-life is 7-10 hours; due to controlled-release formulation, effective half-life is prolonged to support once-daily dosing
6-8 hours (terminal elimination half-life); may be prolonged in hepatic impairment, unchanged in renal impairment.
Renal (16% unchanged, 60% as glucuronide conjugates), biliary/fecal (20%)
Renal (55-60% as unchanged drug and metabolites); biliary/fecal (minor, approximately 5-10%); remainder metabolized in liver.
Category C
Category A/B
Beta-Blocker
Alpha/Beta-Blocker