Product Name

Brimonidine Tartrate

CAS Number

79570-19-7

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Product Name:
Brimonidine Tartrate
CAS Number:
79570-19-7
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.
Mode 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. The topical gel reduces erythema through direct vasocontriction.

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.

Metabolism:

Metabolized primarily by the liver.

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.

IUPAC:
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine
ATC:
D11AX21 — Brimonidine, S01EA05 — Brimonidine
PubChem:
2435
DrugBank:
DB00484 (APRD00034)
Formula:
C11H10BrN5
Molecular Mass:
292.135
Synonyms:
5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline, Brimonidina, Brimonidine, Brimonidinum, Bromoxidine
SMILES:
BrC1=C(NC2=NCCN2)C=CC2=NC=CN=C12
AHFS Code:
52:40.04 — Alpha-adrenergic Agonists, 84:92.00 — Misc. Skin and Mucous Membrane Agents
InChi:
InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17)
Date Modified:
03-12-19

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