Comparative Pharmacology
Head-to-head clinical analysis: COREG versus COREG CR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COREG versus COREG CR.
COREG vs COREG CR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Carvedilol is a nonselective beta-blocker with alpha1-blocking activity. It competitively blocks beta1, beta2, and alpha1 adrenergic receptors, leading to decreased cardiac output, reduced sympathetic tone, and vasodilation. It also has antioxidant and anti-proliferative properties.
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.
Heart failure: Start 3.125 mg orally twice daily; titrate up to target 25 mg twice daily as tolerated. Hypertension: Start 6.25 mg orally twice daily; increase to max 50 mg twice daily. Post-MI LV dysfunction: Start 3.125-6.25 mg orally twice daily; titrate to target 25 mg twice daily.
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.
None Documented
None Documented
Terminal elimination half-life is 7-10 hours in most patients, but may be prolonged in severe hepatic impairment (up to 14-18 hours). The half-life is not significantly altered in renal impairment.
Terminal elimination half-life is 7-10 hours; due to controlled-release formulation, effective half-life is prolonged to support once-daily dosing
Renal excretion of unchanged drug and metabolites accounts for approximately 16% of the dose; fecal excretion accounts for about 84% (mainly as metabolites). Less than 2% is excreted unchanged in urine.
Renal (16% unchanged, 60% as glucuronide conjugates), biliary/fecal (20%)
Category C
Category C
Beta-Blocker
Beta-Blocker