Comparative Pharmacology
Head-to-head clinical analysis: COREG CR versus TIMOLOL MALEATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COREG CR versus TIMOLOL MALEATE.
COREG CR vs TIMOLOL MALEATE
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.
Non-selective beta-adrenergic receptor antagonist (beta-blocker). Competitively blocks beta1 and beta2 receptors, reducing heart rate, myocardial contractility, and cardiac output. Also decreases aqueous humor production in the eye by blocking beta2 receptors on ciliary epithelium.
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.
Systemic: 1 drop of 0.25% or 0.5% solution in affected eye(s) twice daily. Additional indication: 0.5% gel-forming solution once daily. Oral: 10 mg twice daily, may increase to 20 mg twice daily if needed.
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
2-3 hours (terminal); prolonged in hepatic impairment
Renal (16% unchanged, 60% as glucuronide conjugates), biliary/fecal (20%)
Renal: 20% unchanged; biliary/fecal: 80% as metabolites
Category C
Category A/B
Beta-Blocker
Beta-Blocker