Comparative Pharmacology
Head-to-head clinical analysis: BRIMONIDINE TARTRATE AND TIMOLOL MALEATE versus COREG CR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BRIMONIDINE TARTRATE AND TIMOLOL MALEATE versus COREG CR.
BRIMONIDINE TARTRATE AND TIMOLOL MALEATE vs COREG CR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Brimonidine tartrate is a selective alpha-2 adrenergic receptor agonist that reduces aqueous humor production and increases uveoscleral outflow. Timolol maleate is a non-selective beta-adrenergic receptor antagonist that decreases aqueous humor production by blocking beta-2 receptors in the ciliary epithelium.
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.
One drop in the affected eye(s) twice daily (approximately 12 hours apart).
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
Brimonidine: ~2.9 hours (terminal) after ophthalmic administration. Timolol: ~4 hours (terminal); clinically, systemic exposure is low due to topical route.
Terminal elimination half-life is 7-10 hours; due to controlled-release formulation, effective half-life is prolonged to support once-daily dosing
Brimonidine: ~74% renal (unchanged and metabolites), ~22% fecal. Timolol: ~20% renal (unchanged), ~80% hepatic metabolism with biliary and fecal elimination.
Renal (16% unchanged, 60% as glucuronide conjugates), biliary/fecal (20%)
Category A/B
Category C
Beta-Blocker
Beta-Blocker