Comparative Pharmacology
Head-to-head clinical analysis: COREG CR versus LABETALOL HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COREG CR versus LABETALOL HYDROCHLORIDE.
COREG CR vs LABETALOL HYDROCHLORIDE
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 non-selective beta-adrenoceptor blocker and selective alpha-1 adrenoceptor blocker. It reduces myocardial contractility, heart rate, and peripheral vascular resistance.
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: Initial 100 mg twice daily, titrate up to 200-400 mg twice daily; maximum 2400 mg/day. IV: 20 mg slow IV over 2 minutes, then 40-80 mg every 10 minutes as needed up to 300 mg total; or continuous IV infusion at 0.5-2 mg/min.
None Documented
None Documented
Terminal elimination half-life is 7-10 hours; due to controlled-release formulation, effective half-life is prolonged to support once-daily dosing
Terminal elimination half-life: 6-8 hours. In renal impairment, half-life may be slightly prolonged but not clinically significant; in hepatic impairment, half-life may be significantly prolonged.
Renal (16% unchanged, 60% as glucuronide conjugates), biliary/fecal (20%)
Primarily hepatic metabolism; ~5% excreted unchanged in urine; ~55-60% as glucuronide conjugates in urine; fecal excretion <5%.
Category C
Category A/B
Beta-Blocker
Alpha/Beta-Blocker