Comparative Pharmacology
Head-to-head clinical analysis: BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER versus BRIMONIDINE TARTRATE AND TIMOLOL MALEATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER versus BRIMONIDINE TARTRATE AND TIMOLOL MALEATE.
BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER vs BRIMONIDINE TARTRATE AND TIMOLOL MALEATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective beta-1 adrenergic receptor antagonist; reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects at beta-1 receptors.
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.
Intravenous: For stable patients, an initial loading dose of 500 mcg/kg/min over 1 minute followed by a maintenance infusion of 50 mcg/kg/min for 4 minutes; if response is inadequate, increase maintenance infusion to 100 mcg/kg/min and repeat loading dose after 10 minutes. Titrate in 50 mcg/kg/min increments up to 200 mcg/kg/min. For intraoperative and postoperative use, see full prescribing information.
One drop in the affected eye(s) twice daily (approximately 12 hours apart).
None Documented
None Documented
Terminal elimination half-life is approximately 9 minutes (range 8–10 minutes). Clinically, the half-life is consistent with rapid offset of effect upon discontinuation; steady state is achieved within 30 minutes of continuous infusion.
Brimonidine: ~2.9 hours (terminal) after ophthalmic administration. Timolol: ~4 hours (terminal); clinically, systemic exposure is low due to topical route.
Primarily metabolized by red blood cell esterases; <1% excreted unchanged in urine. Elimination is not dependent on renal or hepatic function.
Brimonidine: ~74% renal (unchanged and metabolites), ~22% fecal. Timolol: ~20% renal (unchanged), ~80% hepatic metabolism with biliary and fecal elimination.
Category C
Category A/B
Beta-Blocker
Beta-Blocker