Brimonidine

General information

Brimonidine is a highly selective potent α ₂ -adrenoceptor agonist, which is distinguished from clonidine by a chemical modification that reduces its ability to cross the blood–brain barrier. Like apraclonidine, brimonidine has been used to treat glaucoma. However, unlike apraclonidine, it both reduces aqueous humor production and increases aqueous outflow through the uveoscleral pathway.

The most common adverse reactions to brimonidine are dry mouth, fatigue/drowsiness, and blurring of vision, which occurred significantly more often with brimonidine 0.5% than 0.2% [ , ]. It can also cause allergic conjunctivitis and ocular pruritus [ ]. Brimonidine causes fewer adverse reactions than apraclonidine, and, because it is a highly selective α ₂ -adrenoceptor agonist, does not cause mydriasis, lid retraction, or conjunctival blanching/rebound hyperemia [ ]. It is less polar than apraclonidine and is therefore more likely to cross the blood–brain barrier. However, symptoms of fatigue can occur.

Organs and systems