Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Brimonidine
Drug ID BADD_D00294
Description Brimonidine is an alpha-adrenergic agonist and 2-imidazoline derivative that was first introduced in 1996.[A178951] It is considered to be a third generation alpha-2 aadrenergic receptor agonist, since it displays preferential binding at alpha-2 adrenoceptors over alpha-1 receptors.[A179002] Brimonidine displays a higher selectivity toward the alpha-2 adrenergic receptors than [clonidine] or [apraclonidine], which are also alpha-2 adrenergic agonists.[A178969] Alpha-2 adrenergic agonists are members of the ocular hypotensive agent drug class that are used in the chronic treatment of glaucoma. Early treatment and management of glaucoma, which predominantly involves the lowering of intraocular pressure, is critical since glaucoma is considered to be a common cause of blindness worldwide.[A178948,A178969] Ophthalmically, brimonidine is used to lower intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow. Because it is oxidately stable, brimonidine is associated with fewer reports of ocular allergic reactions compared to other alpha-2 adrenergic agonists.[A178969] The ophthalmic solution of brimonidine was first approved by the FDA in 1996 as Alphagan [label] and brimonidine is the only selective alpha-adrenergic receptor agonist approved for chronic treatment in glaucoma.[A36674] Brimonidine is also found in ophthalmic solutions in combination with [brinzolamide] under the market name Simbrinza for the reduction in intraocular pressure. Unlike nonselective beta-blockers used in ocular hypertension, brimonidine is not associated with significantly adverse cardiopulmonary side effects.[A178945] Thus brimonidine is an effective and safe alternative to beta-blockers, in patients with, or at high risk for, cardiopulmonary disease.[A178948] The topical form of brimonidine was approved by the FDA in August 2013 for the symptomatic treatment of persistent facial erythema of rosacea in adults. It is marketed under the brand name Mirvaso.[L6535] Brimonidine is the first topical treatment approved for facial erythema of rosacea.[A178978]
Indications and Usage 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.
Marketing Status Prescription; OTC; Discontinued
ATC Code D11AX21; S01EA05; S01GA07
DrugBank ID DB00484
KEGG ID D07540
MeSH ID D000068438
PubChem ID 2435
NDC Product Code Not Available
Synonyms Brimonidine Tartrate | 5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline D-tartrate | Brimonidine Tartrate (1:1), (S-(R*,R*))-Isomer | Brimonidine Purite | AGN 190342 | AGN-190342 | AGN190342 | Sanrosa | Alphagan | Brimonidine | 5-bromo-6-(imidazolidinylideneamino)quinoxaline | 5-bromo-6-(imidazolin-2-ylamino)quinoxaline | Bromoxidine | Alphagan P | UK 14,304 | UK-14304 | UK14304 | UK 14304 | Ratio-Brimonidine | Ratio Brimonidine | UK 14,304-18 | UK 14,304 18 | UK 14,30418 | UK-14,304-18 | UK14,30418 | UK 14308 | UK-14,308 | UK 14,308 | UK14,308 | Brimonidine Tartrate, (R-(R*,R*))-Isomer | Brimonidine Tartrate (1:1) | Mirvaso
Chemical Information
Molecular Formula C11H10BrN5
CAS Registry Number 59803-98-4
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Platelet aggregationAlpha-2A adrenergic receptorP08913T11448Not Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.001--Not Available
Abnormal sensation in eye06.01.01.0010.001079%Not Available
Acne23.02.01.001--Not Available
Anaphylactoid reaction24.06.03.007; Available
Arrhythmia02.03.02.001--Not Available
Arthropathy15.01.01.003--Not Available
Asthenia08.01.01.001--Not Available
Asthma22.03.01.002; Available
Blepharitis23.03.04.012; Available
Blindness06.02.02.001; Available
Blindness transient17.17.01.004; Available
Blindness unilateral17.17.01.016; Available
Blood pressure decreased13.14.03.0020.001438%Not Available
Blood pressure fluctuation24.06.01.0020.000719%Not Available
Blood pressure increased13.14.03.0050.001079%Not Available
Body temperature decreased13.15.01.010--Not Available
Bradycardia02.03.02.0020.002158%Not Available
Burning sensation17.02.06.001; Available
Cerebrovascular accident24.03.05.001;
Chest discomfort22.02.08.001;; Available
Chest pain22.02.08.003;; Available
Coma17.02.09.0010.001079%Not Available
Confusional state19.13.01.001;
Conjunctival follicles06.06.02.002--Not Available
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