Rx00048 - Brimonidine


Name:
Brimonidine
Rx ID:
Rx00048
Validation Level:
Phenomic Similarity:
0.574
Reference ID:
DB00484
Primary Indications:
Anterior ischemic optic neuropathy
Orphan Indications:
No annotated orphan indications.
Rare Indications:
No annotated rare indications.
Common Indications:
Open-angle glaucoma; ocular hypertension
Pathways:
Monoamine GPCRs; Adrenaline signalling through Alpha-2 adrenergic receptor
Drug Interactions:
Aliskiren; Droperidol; Isocarboxazid; Linezolid; Methotrimeprazine; Moclobemide; Phenelzine; Procarbazine; Rasagiline; Selegiline; ...
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Food Interactions:
No annotated food interactions in DrugBank.

Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00048
Primary Indication
Secondary Indication

Visualize Chemical Properties

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
anterior ischemic optic neuropathy open-angle glaucoma 17 187 3365 109.008 1.06E-28 3.39e-25

Chemical, Pharmacological and Biological Annotations


ATC Code:
S01EA05
Brand:
Alphagan
Categories:
Antihypertensive Agents; Adrenergic alpha-2 Receptor Agonists; EENT Preparations
ChEBI ID:
3175
PubChem ID:
2435
KEGG Drug ID:
D02076
SMILE:
BrC1=C(NC2=NCCN2)C=CC2=NC=CN=C12
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)
Classification:
Kingdom:
Organic Compounds
Superclass:
Heterocyclic Compounds
Class:
Naphthyridines
Subclass:
Quinoxalines
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 adult...
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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.
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.
Mechanism:
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 mechani...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
+
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Non-inhibitor
P-glycoprotein inhibitor II:
Inhibitor
Renal organic cation transporter:
Inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
3.0196 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org