Comparative Pharmacology
Head-to-head clinical analysis: BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER versus BRIMONIDINE TARTRATE TIMOLOL MALEATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER versus BRIMONIDINE TARTRATE TIMOLOL MALEATE.
BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER vs BRIMONIDINE TARTRATE; 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 is a selective alpha-2 adrenergic receptor agonist that reduces aqueous humor production and increases uveoscleral outflow. Timolol is a non-selective beta-adrenergic receptor blocker that decreases aqueous humor production by inhibiting 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 of the fixed combination (0.2% brimonidine/0.5% timolol) 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: ~3 hours (terminal); timolol: ~4–6 hours (terminal). Clinical context: allows twice-daily dosing for brimonidine/timolol combination.
Primarily metabolized by red blood cell esterases; <1% excreted unchanged in urine. Elimination is not dependent on renal or hepatic function.
Brimonidine: primarily renal (74% as unchanged drug); timolol: renal (20% unchanged, remainder as metabolites) and fecal (small amount).
Category C
Category A/B
Beta-Blocker
Beta-Blocker