Pharmacology Of Brimonidine

Indication For the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Pharmacodynamics Brimonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.
Mechanism of action Brimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.
Absorption Minimal systemic absorption occurs after ocular insertion.
Volume of distribution Not Available
Protein binding Not Available
Metabolism Metabolized primarily by the liver.
Route of elimination It is metabolized primarily by the liver. Urinary excretion is the major route of elimination of the drug and its metabolites.
Half life 2 hours
Clearance Not Available
Toxicity Oral LD50 is 50 mg/kg in mice and 100 mg/kg in rats.

Comments