DESCRIPTION
Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. [Wikipedia] A topical gel formulation, marketed under the name Mirvaso, was FDA approved on August 2013 for the treatment of rosacea.
CHEMICAL FORMULA
C11H10BrN5
COMPOSITION
Brimonidine – 2mg
INDICATION
The ophthalmic solution is indicated for patients with open-angle glaucoma or ocular hypertension to lower intraocular pressure. The topical gel is indicated for the treatment of persistent (nontransient) facial erythema of rosacea in adults 18 years or older.
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.
No Information
ABSORPTION
Minimal systemic absorption occurs after ocular insertion. When the topical gel was applied to adult patients with facial erythema associated with rosacea, the plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) were 46 ± 62 pg/mL and 417 ± 264 pg.hr/mL, respectively. These values were reached on Day 15 of treatment.
METABOLISM
Metabolized primarily by the liver.
ELIMINATION
Urinary excretion is the major route of elimination of the drug and its metabolites.
HALF LIFE
2 hours [ophthalmic solution]
TOXICITY
Oral LD50 is 50 mg/kg in mice and 100 mg/kg in rats. Common adverse reactions of the topical gel formulation include erythema, flushing, skin burning sensation, and contact dermatitis.