Comparative Pharmacology
Head-to-head clinical analysis: LABETALOL versus LEVATOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LABETALOL versus LEVATOL.
Labetalol vs LEVATOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Labetalol is a nonselective beta-adrenergic antagonist with additional alpha1-adrenergic blocking activity. It competitively blocks beta1 and beta2 receptors and alpha1 receptors, leading to decreased heart rate, myocardial contractility, and systemic vascular resistance.
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.
50 mg orally once daily, increasing to 100 mg once daily after 2 weeks if tolerated; maximum 200 mg once daily.
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."
6-8 hours (terminal elimination half-life); may be prolonged in hepatic impairment, unchanged in renal impairment.
Terminal elimination half-life is 6-8 hours; prolonged to 10-16 hours in severe renal impairment (CrCl <30 mL/min).
Renal (55-60% as unchanged drug and metabolites); biliary/fecal (minor, approximately 5-10%); remainder metabolized in liver.
Renal excretion accounts for 55-60% as unchanged drug; biliary/fecal elimination accounts for 40-45% as metabolites and unchanged drug.
Category A/B
Category C
Alpha/Beta-Blocker
Beta-Blocker