Brimonidine
Brimonidine
Alphagan P (ophthalmic glaucoma), Mirvaso (topical rosacea)
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Summary
Common uses
Primary open-angle glaucoma0, Ocular hypertension0, Persistent erythema of rosacea (topical Mirvaso)0
Pharmacy
Starting dose
Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily
Preparations
0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza)
US FDA Max
TID per eye
Pharmacology
Routes
Topical ophthalmic, topical skin
Onset
IOP lowering at 1 hour; max at 2-3 hours
Duration
8-12 hours
Half-life
~3 hours[1]
Bioavailability
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children[1]
Pregnancy
Limited data.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Brimonidine is a selective α2 adrenergic receptor agonist; in the ciliary body it reduces aqueous humor production and increases uveoscleral outflow, lowering intraocular pressure by ~20-25%.0 Systemic absorption with α2-mediated CNS depression (somnolence, fatigue) limits dosing in children and can be clinically significant in adults using bilateral ophthalmic therapy. Allergic conjunctivitis (delayed-onset, after months of use) is a recognized class effect. The topical rosacea formulation exploits cutaneous α-mediated vasoconstriction for transient erythema reduction[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Alphagan P (brimonidine tartrate), Allergan, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021262s020lbl.pdf