Ocular and systemic pharmacokinetics of brimonidine and brinzolamide after topical administration in rabbits: comparison between fixed-combination and single-drug formulations

Patient Factors Influencing Intraocular Penetration of Brimonidine-Related Eye Drops in Adults: A Post Hoc Pooled Analysis

“…In this study, although there were differences in the formulation compositions among Aiphagan, Aibeta and Ailamide, the brimonidine concentrations in the aqueous and vitreous humor were comparable among the three eye drops containing brimonidine. A similar tendency was observed in studies on rabbits [ 50 , 51 ]; we consider that there are no species differences in the effects of formulation properties on ocular pharmacokinetics.…”

Periocular allergic contact dermatitis caused by brinzolamide

“…Brinzolamide is a carbonic anhydrase inhibitor that decreases aqueous humor secretion 4 . This active ingredient may be found as the main ingredient (Brinzolamide Sandoz), or in combination with brimonidine (Simbrinza).…”

Chemical Insights into Topical Agents in Intraocular Pressure Management: From Glaucoma Etiopathology to Therapeutic Approaches

“…Research suggests that the corneal, conjunctival, and scleral pathways are the major routes for the intraocular absorption of brimonidine [ 229 ]. In a 2020 study, Suzuki et al comparatively investigated the pharmacokinetics of brimonidine as a monotherapy and adjunctive therapy with brinzolamide in vivo [ 230 ]. In this study using rabbits, aqueous humor concentrations of brimonidine reached C max (472 ± 359 ng/mL) at 1 h after topical administration (0.1%) and exhibited a rapid distribution in the retina/choroid [ 230 ].…”

“…In a 2020 study, Suzuki et al comparatively investigated the pharmacokinetics of brimonidine as a monotherapy and adjunctive therapy with brinzolamide in vivo [ 230 ]. In this study using rabbits, aqueous humor concentrations of brimonidine reached C max (472 ± 359 ng/mL) at 1 h after topical administration (0.1%) and exhibited a rapid distribution in the retina/choroid [ 230 ]. The Tmax for 0.1% brimonidine was 1.5 h, the first time point, in the anterior and posterior retina/choroid.…”

“…The fact that the first time point was determined to be the T max and no earlier time points were available suggests that the T max value here could be an overestimation; the actual pharmacokinetics of the compound could be more rapid than this quantitative data imply. The plasma concentration of brimonidine reached C max (1420 ± 160 pg/mL) in 0.5 h and quickly decreased afterward [ 230 ]. Binding to ocular melanin reportedly can increase brimonidine ’s absorption and retention based on its marked affinity for melanin-containing ocular tissues in vitro [ 231 ].…”