Adrenergic agonist brimonidine

Two a-adrenergic agonists are available on the market. Apraclonidine 0.5% is indicated when a patient on maximum tolerated medical therapy requires short-term additional lOP lowering. Before the introduction of brimonidine, apraclonidine was the only available a-adrenergic agonist and was FDA approved for short-term use. Approximately one-third of patients using apraclonidine showed little or no treatment effect. For another third the treatment effect (3 to 5 mm Hg) was short in duration (3 to 6 months) for the remainder the effect was more lasting. Consequently, this medication... 

Brimonidine and the less lipid-soluble and less receptor-selective apraclonidine are 2-adrenergic agonists structurally similar to cloni-dine. Apraclonidine is indicated and brimonidine is effective for prevention or control of postoperative or postlaser treatment increases in lOP and both are indicated in the treatment of open-angle glaucoma. Brimonidine is considered a first-line or adjunctive agent in the therapy of POAG, and apraclonidine is seen as a second-line or adjunctive therapy. 

Karamanos, N.K. Lamari, F. Katsimpris, J. Gartaganis, S. Development of an HPLC method for determining the alpha2-adrenergic receptor agonist brimonidine in blood serum and aqueous humor of the eye, Biomed.Chromatogr., 1999,13, 86-88. 

Brimonidine tartrate is an alph -adrenergic receptor agonist used to lower IOP in patients with open-angle glaucoma or ocular hypertension. This drug acts to reduce aqueous humor production and increase the outflow of aqueous humor. 

Pharmacology Brimonidine is an alpha-2 adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at 2 hours postdose. Brimonidine has a dual mechanism of action it reduces aqueous humor production and increases uveoscleral outflow. 

---